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ti Lu DRonate Di So Dium/ti Lu DRonic aci D 885 overdosage/acute t oxicity The cardiovascular system is apparently the target of toxicity in ani-mals. In cattle, doses up to 50 mg/kg IM did not cause death, but SC doses of 150 mg/kg did cause fatalities, as well as IV doses of 5 mg/kg. Doses as low as 10 mg/kg in swine caused increased respiration, emesis and seizures; 20 mg/kg IM caused deaths in most animals tested. In monkeys, 10 mg/kg administered once caused no signs of toxicity, but 20 mg/kg caused vomiting; 30 mg/kg caused death. In cases of human injection, contact physician immediately. The manufacturer has emergency telephone numbers to assist in deal-ing with exposure: 1-800-722-0987 or 1-317-276-2000. Drug interactions In swine, epinephrine increased the mortality associated with tilmi-cosin. No other specific information was noted; refer to the eryth-romycin monograph for potential interactions. Doses catt Le: T! For susceptible infections (subcutaneous injection under the skin in the neck, or if not accessible, behind the shoulders and over the ribs is suggested). a) For treatment of pneumonic pasteurellosis: 10 mg/kg SC ev-ery 72 hours (Shewen and Bateman 1993) b) Package insert (Micotil® 300—Elanco): 10 mg/kg SC (not more than 15 m L per injection site) SHee P: T! For susceptible infections:a) 10 mg/kg SC (not more than 15 m L per injection site). Sub-cutaneous injection under the skin in the neck, or if not ac-cessible, behind the shoulders and over the ribs is suggested. Do not use in lambs less than 15 kg of body weight. (Package insert; Micotil® 300—Elanco) Rabbit S, Ro Dent S, Sma LL mamma LS:T! Rabbits: Two regimens: 1) 25 mg/kg SC once; repeat in 3 days if necessary. 2) 5 mg/kg SC on day 0, if no reaction, give 10 mg/kg SC on days 7 and 14. Can cause weakness, pallor, tachypnea and sudden death. May cause acute death if given IV. SC injections can cause local swelling and necrosis. (Ivey and Morrisey 2000) monitoring Efficacy T! Withdrawal times T! client information If clients are administering the drug, they should be warned T! about the potential toxicity to humans, swine, and horses if ac-cidentally injected Carefully instruct in proper injection techniques T! Avoid contact with eyes T! chemistry/Synonyms A semi-synthetic macrolide antibiotic, tilmicosin phosphate is commercially available in a 300 mg/m L (of tilmicosin base) injec-tion with 25% propylene glycol. Tilmicosin may also be known as EL-870, LY-177370, Micotil® or Pulmotil®. Storage/Stability/compatibility Store the injection at or below room temperature. Avoid exposure to direct sunlight. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: Tilmicosin for Subcutaneous Injection: 300 mg/m L in 50 m L, 100 m L and 250 m L multi-dose vials; Micotil® 300 Injection (Elanco); (Rx). Approved for use in cattle and sheep. Not approved for use in female dairy cattle 20 months or older. Do not use in lactating ewes if milk is to be used for human consumption. Do not use in veal calves. Slaugh-ter withdrawal (at labeled doses) = 28 days. Tilmicosin Feed Medication: 90. 7 g/lb. Pulmotil® 90 (Elanco); (OTC). Approved for veterinary use in swine only. Slaughter withdrawal (at labeled doses) = 7 days. Human-Labe Le D PRo Duct S: None tiludronate di Sodiu M tiludronic acid (til-yoo-droe-nate) Tildren®, Skelid® bi SPho SPhonate b one re Sor Ption inhibitor Prescriber Highlights Bisphosphonate bone resorption inhibitor available in T T some countries for the intravenous treatment of navicu-lar disease in horses Adverse effects: Signs of colic, muscle tremor (hypocal-T T cemia), fatigue/lassitude, sweating, injection site effects, salivation, tail hypertonia Must be legally imported into the USAT T uses/indications Tiludronate disodium (tiludronic acid) is a bisphosphonate bone resorption inhibitor that is available in some countries for the in-travenous treatment of navicular disease in horses. Treatment earli-er in the course of the disease apparently results in greater efficacy. For humans, there is an orally administered FDA-approved product for treating Paget's disease (osteitis deformans). Pharmacology/actions Tiludronate, like other bisphosphonates, inhibit osteoclastic bone resorption by inhibiting osteoclast function after binding to bone hydroxyapatite thereby helping to regulate bone remodeling. Pharmacokinetics After intravenous injection in horses the drug is rapidly distributed to bone. Binding is greater to cancellous bone than cortical bone. Plasma protein binding is reported to be approximately 85% and elimination half-life is approximately 4. 5 hours. Repeated daily doses do not result in accumulation in plasma. Unbound drug is eliminated unchanged in the urine. Approximately 25-50% of a single IV dose is eliminated in the urine over 96 hours. contraindications/Precautions/Warnings The labeling for Tildren® states that the drug should not be used in horses with renal dysfunction or those producing milk for human consumption. Because there is an absence of data on the effects the drug may have on the skeleton of young animals, the manufacturer states to not administer to horses less than 3 years old. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
886 ti Lu DRonate Di So Dium/ti Lu DRonic aci D Since the safety of tiludronate has not been studied in pregnant or lactating mares, the manufacturer recommends not using it dur-ing pregnancy or lactation. Use with caution in horses with hypocalcemia or cardiac dys-function. If used in these patients, slow the rate of injection and watch these patients carefully for the first few hours post-injection. adverse effects Acute adverse effects reported in horses include colic (reduced ap-petite, abdominal discomfort, pawing/scratching at ground, rest-lessness), muscle tremor, fatigue/lassitude and sweating. The inci-dences of these effects are reported at 5% or less and are postulated to be due to a mild hypoglycemic effect. The onset of colic signs appear within a few hours of treatment and generally resolve with-out treatment. Should they persist, conventional colic treatments are recommended. Muscle tremors may be treated with intravenous calcium if required. Up to 9% of patients develop local reactions at the injection site (e. g., phlebitis), particularly after the 4th injection. Other adverse effects reported include salivation and tail hypertonia. Reproductive/nursing Safety Studies performed in male and female rats at dosages as high as 75mg/kg/day demonstrated no effects on fertility. Studies in pregnant rabbits given 2X-5X human dosages showed no skeletal abnormalities. Pregnant mice given 7X human dosages showed some adverse effects (decreased litter size, malformed paws in 6 fetuses from one litter). Rat studies have shown decreased litter sizes, but no teratogenic effects. In humans, the FDA categorizes tiludronate as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) As the safety of tiludronate has not been studied in pregnant or lactating mares, the manufacturer recommends not using it during pregnancy or lactation. overdosage/acute t oxicity Limited information is available. The manufacturer reports that doses of 3X in horses caused an increased frequency of adverse ef-fects, particularly signs of colic and muscle tremor. Intravenous cal-cium administration may be considered for signs associated with hypocalcemia. Drug interactions ca Lcium-T! or ma Gne Sium-containin G int Ra Venou S FLui DS : May complex with tiludronate and reduce its availability; do not mix with fluids or administer with fluids such as Lactated Ringer's, Ringer's, Plasma-Lyte®, normasol®, etc. Laboratory considerations No specific concerns were noted. Doses Ho RSe S:T! For navicular disease:a) 0. 1 mg/kg tiludronic acid slow IV (over 20-30 seconds per 10 m L given) once daily for 10 days. Alternate injection sites from day to day. (Label information; Tildren®—Ceva/ Sanofi)monitoring Clinical Efficacy T! Serum Calcium T! Adverse Effects (particularly within first 4 hours after dosing) T! client information This medication should be administered by a veterinary T! professional Patient should be observed for up to 4 hours post-administration T! for signs of hypocalcemia (muscle tremors, etc. ) or colic chemistry/Synonyms Tiludronate disodium is a bisphosphonate that occurs as a white powder having a molecular weight of 380. 6. Commercially avail-able products contain the disodium salt of tiludronic acid. 120 mg of tiludronate disodium is equivalent to 100 mg of tiludronic acid. Tiludronate disodium or tiludronic acid may also be known as ME-3737, SR-41319, acidum tiludronicum, Tildren® or Skelid®. Storage/Stability/compatibility Unless otherwise indicated, store the unreconstituted powder and diluent at room temperature (15-30°C) in the outer carton. Shelf life of properly stored unreconstituted product is generally 3 years. Reconstitute the powder by aseptically adding 10 m L of the provided diluent and mix gently. The resulting solution contains 5 mg/m L of tiludronic acid. After reconstitution, use immediately. Any remaining product should be discarded. Do not mix or administer with intravenous fluids containing calcium or magnesium (e. g., LRS, Ringer's, etc. ). Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None in the USA; it is available in France, Spain, The Netherlands, and Italy as: Tiludronic Acid: 50 mg (as tiludronate disodium) per vial, with one 10 m L vial of sterile water for reconstitution; Tildren® (Sanofi/Ceva). Labeled for use in horses. Not permitted for use in lactating animals producing milk for hu-man consumption. Labeled meat and offal withdrawal = 0 days. Refer to individual product labels for more information. The FDA may allow legal importation of this medication for com-passionate use in animals; for more information, see the Instructions for Legally Importing Drugs for Compassionate Use in the USA found in the appendix. One source recommended for obtaining Tildren® via this process is: manorveterinaryexports. com Human-Labe Le D PRo Duct S: Tiludronate Disodium Tablets: 240 mg (equiv. to 200 mg tiludronic acid); Skelid® (Sanofi-Synthelabo); (Rx) note : The information presented in this monograph pertains to the veterinary-labeled intravenous product only. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
tini Dazo Le 887 tinidazole (tye-ni-dah-zole) Tindamax® nitroimidazole anti Protozoal/ antibiotic Prescriber Highlights Drug similar to metronidazole, potentially useful for T T treating anaerobic infections (especially in the mouth), trichomoniasis, amebiasis and balantidiasis Little experience in veterinary medicine T T Adverse effects most likely GI-related, like metronidazole T T and ronidazole could cause neurotoxicity Many potential drug interactions T T uses/indications Little information is presently available on the use of tinidazole in dogs, cats, or horses. It potentially could be useful for treating an-aerobic infections, particularly associated with dental infections in small animals. Because of its antiprotozoal effects, it has been used as an alternative for treating giardiasis in small animals, and it could have efficacy against amebiasis, trichomoniasis or balantidiasis in veterinary species, but documentation of efficacy is not available. Tinidazole has a longer duration of action in dogs and cats than does metronidazole. In humans, oral tinidazole is FDA-approved for treating extraint-estinal and intestinal amebiasis, (Entamoeba histolytica), giardiasis (Giardia duodenalis/lamblia), and trichomoniasis (T. vaginalis). Pharmacology/actions Tinidazole is a 5-nitroimidazole similar to metronidazole. It is bac-tericidal against susceptible bacteria. Its exact mechanism of action is not completely understood, but it is taken-up by anaerobic or-ganisms where it is reduced to an unidentified polar compound. It is believed that this compound is responsible for the drug's antimi-crobial activity by disrupting DNA and nucleic acid synthesis in the bacteria. Tinidazole has activity against many obligate anaerobes and H. pylori. It has excellent activity against Porphyromonas spp. found in canine gingiva. Tinidazole is also trichomonacidal and amebicidal. Its mecha-nism of action for its antiprotozoal activity is not well under-stood. It has therapeutic activity against Entamoeba histolytica, Trichomonas, and Giardia. Pharmacokinetics In dogs and cats, tinidazole is practically completely absorbed after oral administration. Apparent volumes of distribution are 0. 66 L/kg in dogs and 0. 54 L/kg in cats. Dogs clear the drug about twice as fast as cats; elimination half-lives are about 4. 4 hours in dogs, 8. 4 hours in cats. In horses, tinidazole is practically completely absorbed after oral administration. Apparent volume of distribution is 0. 66 L/kg an elimination half-life of about 5. 2 hours. contraindications/Precautions/Warnings Tinidazole should not be used in patients documented to be hyper-sensitive to it or other 5-nitroimidazoles (e. g., metronidazole). Tinidazole is metabolized by the liver; use with caution in pa-tients with hepatic dysfunction. As other 5-nitroimidazoles (metronidazole, ronidazole) have been associated with neurotoxic signs in dogs and cats and seizures have been reported rarely with tinidazole use in humans, use with caution in animals susceptible to seizures. The human labeling for tinidazole carries a “black box warn-ing” stating: “Carcinogenicity has been seen in mice and rats treated chronically with another agent in the nitroimidazole class (metron-idazole). Although such data have not been reported for tinidazole, avoid unnecessary use of tinidazole. Reserve its use for the condi-tions for which it is indicated. ” adverse effects The adverse effect profiles for dogs, cats or horses are not well described since clinical use of this medication has been limited. Gastrointestinal effects including vomiting, inappetance, and diar-rhea are most likely. Giving the medication with food may help alle-viate these effects. Other 5-nitroimidazoles (metronidazole, ronida-zole) have been associated with neurotoxic signs in dogs and cats; seizures have been reported rarely with tinidazole use in humans. Tinidazole reportedly is very bitter tasting. If using compounded products, consider using capsules or having a flavored suspension prepared. Reproductive/nursing Safety In studies performed on male rats tinidazole decreased fertility and caused testicular histopathology. Tinidazole crosses the placenta. While studies in mice and rats have not demonstrated significant fetal effects, because of its muta-genic potential, it is stated that it should not be used in women dur-ing the first trimester of pregnancy. In humans, the FDA categorizes tinidazole as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) If considering use of this product in a pregnant animal, weigh the potential benefits of treatment versus the risks. Tinidazole is distributed into maternal milk at levels approxi-mating those found in serum. It is suggested that milk replacer be used if tinidazole is necessary for treating a nursing dam. overdosage/acute t oxicity Very limited information is available. In studies done in rats and mice, the oral LD 50 was >3. 6 g/kg for mice and >2 g/kg for rats. Treatment of acute overdoses of tinidazole is symptomatic and supportive. Gastric lavage or induction of emesis may be helpful. Hemodialysis can remove approximately 43% of the amount in the body (human) in a 6 hour session. Drug interactions In humans, the following drug interactions with metronidazole have been reported or are theoretical and may be of significance in veterinary patients receiving tinidazole: a Lco Ho LT! : May induce a disulfiram-like (nausea, vomiting, cramps, etc. ) reaction cimeti Dine, ketoconazo Le T! : May decrease the metabolism of ti-nidazole and increase the likelihood of dose-re lated side effects occurring cyc Lo SPo Rine, tac Ro Limu S T! (systemic ): Tinidazole may increase the serum levels of cyclosporine or tacrolimus FLuo Rou Raci LT! (systemic ): Tinidazole may increase the serum lev-els of fluorouracil and increase the risk of toxicity Lit Hium T! : Tinidazole may increase lithium serum levels and in-crease the risk for lithium toxicity | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
888 tio PRonin oxytet Racyc Line T! : Reportedly, may antagonize the therapeutic ef-fects of metronidazole (and presumably tinidazole) PHenoba Rbita L, Ri F am Pin T! or PHenytoin : May increase the metabo-lism of tinidazole thereby decreasing blood levels Wa RF a Rin T! : Metronidazole (and potentially tinidazole) may pro-long the prothrombin time (PT) in patients taking warfarin or other coumarin anticoagulants. Avoid concurrent use if possible; otherwise, intensify monitoring. Laboratory considerations a St, a Lt, LDH, triglycerides, Hexokinase glucose T! : Tinidazole, like metronidazole may interfere with enzymatic coupling of the as-say to oxidation-reduction of nicotinamide adenine. Falsely low values, including zero, may result. Doses Do GS:T! a) For stomatitis, anaerobic infections: 15-25 mg/kg PO q12h for 7 days. (Greene, Hartmannn et al. 2006) b) For giardiasis: 44 mg/kg PO q24h for 6 days. Potentially may be useful for treating trichomoniasis, amebiasis and balan-tidiasis, but efficacy data lacking for animals. (Barr 2006a) cat S:T! a) For stomatitis, anaerobic infections: 15 mg/kg PO q24h for 7 days. (Greene, Hartmannn et al. 2006) Ho RSe S:T! a) For susceptible anaerobic infections: 10-15 mg/kg PO q12h (Pvorala, Kotilainen et al. 1990) monitoring Clinical efficacy in treating the infection T! client information Give this medication with food T! Animals should not have access to alcohol when receiving this T! medication If gastrointestinal signs (vomiting, lack of appetite, diarrhea) are T! severe or persist, contact veterinarian Contact veterinarian immediately if animal shows signs of be-T! havior changes, eyes moving back and forth (nystagmus), con-vulsions, or if patient has difficulty walking, climbing stairs, etc. (ataxia); these could be signs that drug toxicity is occurring chemistry/Synonyms Tinidazole occurs as an almost white or pale yellow, crystalline powder. It is practically insoluble in water, soluble in acetone, and sparingly soluble in methyl alcohol. Tinidazole may also be known as CP-12574 or tinidazolum. International trade names include: Estovyn-T®, Fasigyn®, Tindamax®, Tiniba®, Tiniameb®, or Tinidazol®. Storage/Stability Store tinidazole tablets at controlled room temperature (20-25°C) protected from light. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None As tinidazole is a nitroimidazole, its use is prohibited in animals to be used for food. Human-Labe Le D PRo Duct S: Tinidazole Tablets (film-coated): 250 mg, 500 mg; Tindamax® (Pre-sutti); (Rx)tiopronin (tye-oh-proe-nin) Thiola®, 2-MPG antiurolithic (cy Stine) agent Prescriber Highlights Drug for prevention (& treatment) of cystine urolithiasis T T Cautions: Agranulocytosis, aplastic anemia, thrombo-T T cytopenia or other significant hematologic abnormality, impaired renal or hepatic function, or sensitivity to either tiopronin or penicillamine Adverse Effects: Coombs'-positive regenerative sphero-T T cyte anemia, aggressiveness, proteinuria, thrombocytope-nia, elevations in liver enzymes, dermatologic effects, & myopathy uses/indications Tiopronin is indicated for the prevention of cystine urolithiasis in patients where dietary therapy combined with urinary alkaliniza-tion is not completely effective. It may also be useful in combina-tion with urine alkalinization to dissolve stones. Pharmacology/actions Tiopronin is considered an antiurolithic agent. It undergoes thiol-disulfide exchange with cystine (cysteine-cysteine disulfide) to form tiopronin-cystine disulfide. This complex is more water-soluble and is readily excreted thereby preventing cystine calculi from forming. Pharmacokinetics Tiopronin has a rapid onset of action and in humans, up to 48% of a dose is found in the urine within 4 hours of dosing. Tiopronin has a relatively short duration of action and its effect in humans disap-pears in about 10 hours. Elimination is primarily via renal routes. contraindications/Precautions/Warnings Tiopronin's risks versus its benefits should be considered before using in patients with agranulocytosis, aplastic anemia, thrombo-cytopenia or other significant hematologic abnormality, impaired renal or hepatic function, or sensitivity to either tiopronin or pen-icillamine. adverse effects There is limited information available on the adverse effect profile of tiopronin in dogs. While tiopronin is thought to have fewer ad-verse effects than penicillamine in humans, it has been associated with Coombs'-positive regenerative spherocyte anemia in dogs. Should this effect occur, the drug should be discontinued and ap-propriate treatment started (corticosteroids, blood component therapy as needed). Other adverse effects noted in dogs include aggressiveness, proteinuria, thrombocytopenia, elevations in liver enzymes, dermatologic effects, and myopathy. Adverse effects noted in humans that occur more frequently include dermatologic effects (ecchymosis, itching, rashes, mouth ulcers, jaundice) and GI distress; less frequently allergic reactions (specifically adenopathy), arthralgias, dyspnea, fever, hematologic abnormalities, edema, and nephrotic syndrome have been noted. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
tob Ramycin Su LF ate 889 Reproductive/nursing Safety There is limited information on the reproductive safety of tiopronin. Skeletal defects, cleft palates and increased resorptions were noted when rats were given 10 times the human dose of penicillamine and, therefore, may also be of concern with tiopronin. Other animal studies have suggested that tiopronin may affect fetus viability at high doses. In humans, the FDA categorizes this drug as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) Because tiopronin may be excreted in milk, at present it is not recommended for use in nursing animals. overdosage/acute t oxicity There is little information available. It is suggested to contact an animal poison control center for further information in the event of an overdose situation. Drug interactions Potentially use of tiopronin with other drugs causing nephrotoxicity, hepatotoxicity, or bone marrow depression could cause additive toxic effects. Clinical significance is not clear. Doses Do GS:T! For treatment or prevention of recurrence of cystine urinary calculi: a) In conjunction with an alkalinizing, protein and sodium re-stricted diet (e. g., u/d®), 30-40 mg/kg PO divided into two daily doses. (Cowan 1994) b) Treatment: 20 mg/kg PO twice daily for 1-3 months; rela-tively high incidence of adverse effects; Prevention: 15 mg/kg PO twice daily. (Adams and Syme 2005) monitoring Efficacy (stone size)T! CBC with platelets T! Liver enzymes T! Urinalyses including urine p HT! client information Clients should be counseled on the importance of adequate com-T! pliance with this drug to maximize efficacy and detailed on the clinical signs to watch for regarding adverse effects. chemistry/Synonyms A sulfhydryl compound related to penicillamine, tiopronin has a molecular weight of 163. 2. It occurs as a white crystalline powder which is freely soluble in water. Tiopronin may also be known as: SF 522, N-(2-Mercaptopropionyl)-glycine (MPG), 2-MPG, thiopronine, Acadione®, Captimer®, Epatiol®, Mucolysin®, Mucosyt®, Sutilan®, Thiola®, Thiosol®, or Tioglis®. Storage/Stability Store tablets at room temperature in tight containers. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Tiopronin Tablets: 100 mg; Thiola® (Mission); (Rx)tobra Mycin Sulfate (toe-bra-mye-sin) Nebcin®, TOBI® aminoglyco Side antibiotic Prescriber Highlights Parenteral aminoglycoside antibiotic that has “good” ac-T T tivity against a variety of bacteria, predominantly gram-negative aerobic bacilli, also in ophthalmic preps Because of potential adverse effects usually reserved for T T serious infections when given systemically, may be less nephrotoxic than gentamicin Adverse Effects: Nephrotoxicity, ototoxicity, neuromuscu-T T lar blockade Cats may be more sensitive to toxic effects T T Risk factors for nephrotoxicity: Preexisting renal dis-T T ease, age (both neonatal & geriatric), fever, sepsis, & dehydration uses/indications While most veterinarians use gentamicin or amikacin and there are no approved veterinary tobramycin products in the U. S., tobramy-cin can be useful clinically to treat serious gram-negative infections in most species. It is often used in settings where gentamicin-re-sistant bacteria are a clinical problem. The inherent toxicity of the aminoglycosides limit their systemic use to serious infections when there is either a documented lack of susceptibility to other less toxic antibiotics or when the clinical situation dictates immediate treat-ment of a presumed gram-negative infection before culture and susceptibility results are reported. Whether tobramycin is less nephrotoxic than either gentamicin or amikacin when used clinically is controversial. Laboratory stud-ies indicate that in a controlled setting in laboratory animals, it may indeed be so. Pharmacology/actions T obramycin, like the other aminoglycoside antibiotics, act on sus-ceptible bacteria presumably by irreversibly binding to the 30S ri-bosomal subunit thereby inhibiting protein synthesis. It is consid-ered a bactericidal antibiotic. T obramycin's spectrum of activity includes coverage against many aerobic gram-negative and some aerobic gram-positive bacteria, including most species of E. coli, Klebsiella, Proteus, Pseudomonas, Salmonella, Enterobacter, Serratia, Shigella, Mycoplasma, and Staphylococcus. Antimicrobial activity of the aminoglycosides is enhanced in an alkaline environment. The aminoglycoside antibiotics are inactive against fungi, virus-es and most anaerobic bacteria. Pharmacokinetics T obramycin, like the other aminoglycosides, is not appreciably ab-sorbed after oral or intrauterine administration, but it is absorbed from topical administration (not skin or urinary bladder) when used in irrigations during surgical procedures. Patients receiving oral aminoglycosides with hemorrhagic or necrotic enteritises may absorb appreciable quantities of the drug. Subcutaneous injection results in slightly delayed peak levels and more variability than af-ter IM injection. Bioavailability from extravascular injection (IM or SC) is greater than 90%. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
890 tob Ramycin Su LF ate After absorption, aminoglycosides are distributed primarily in the extracellular fluid. They are found in ascitic, pleural, pericardial, peritoneal, synovial and abscess fluids, and high levels are found in sputum, bronchial secretions and bile. Aminoglycosides (other than streptomycin) are minimally protein bound (<20%) to plasma pro-teins. Aminoglycosides do not readily cross the blood-brain barrier nor penetrate ocular tissue. CSF levels are unpredictable and range from 0-50% those found in the serum. Therapeutic levels are found in bone, heart, gallbladder and lung tissues after parenteral dosing. Aminoglycosides tend to accumulate in certain tissues such as the inner ear and kidneys, which may help explain their toxicity. Aminoglycosides cross the placenta and fetal concentrations range from 15-50% those found in maternal serum. Elimination of aminoglycosides after parenteral administration occurs almost entirely by glomerular filtration. Patients with de-creased renal function can have significantly prolonged half-lives. In humans with normal renal function, elimination rates can be highly variable with the aminoglycoside antibiotics. contraindications/Precautions/Warnings Aminoglycosides are contraindicated in patients who are hyper-sensitive to them. Because these drugs are often the only effective agents in severe gram-negative infections, there are no other abso-lute contraindications to their use; however, they should be used with extreme caution in patients with preexisting renal disease with concomitant monitoring and dosage interval adjustments made. Other risk factors for the development of toxicity include age (both neonatal and geriatric patients), fever, sepsis, and dehydration. Because aminoglycosides can cause irreversible ototoxicity, they should be used with caution in “working” dogs (e. g., “seeing-eye”, herding, dogs for the hearing impaired, etc. ). Aminoglycosides should be used with caution in patients with neuromuscular disorders (e. g., myasthenia gravis) due to their neu-romuscular blocking activity. Because aminoglycosides are eliminated primarily through re-nal mechanisms, they should be used cautiously, preferably with serum monitoring and dosage adjustment in neonatal or geriatric animals. Aminoglycosides are generally considered contraindicated in rabbits/hares as they adversely affect the GI flora balance in these animals. adverse effects The aminoglycosides are infamous for their nephrotoxic and oto-toxic effects. The nephrotoxic (tubular necrosis) mechanisms of these drugs are not completely understood, but are probably relat-ed to interference with phospholipid metabolism in the lysosomes of proximal renal tubular cells, resulting in leakage of proteolytic enzymes into the cytoplasm. Nephrotoxicity normally manifests by increases in BUN, creatinine, nonprotein nitrogen in the se-rum and decreases in urine specific gravity and creatinine clear-ance. Proteinuria and cells or casts may also be seen in the urine. Nephrotoxicity is usually reversible once the drug is discontinued. While gentamicin may be more nephrotoxic than the other amino-glycosides, the incidences of nephrotoxicity with all of these agents require equal caution and monitoring. Ototoxicity (8th cranial nerve toxicity) of the aminoglycosides can manifest with either auditory and/or vestibular clinical signs and may be irreversible. Vestibular clinical signs are more frequent with streptomycin, gentamicin, or tobramycin. Auditory clinical signs are more frequent with amikacin, neomycin, or kanamycin, but either form can occur with any of the drugs. Cats are apparently very sensitive to the vestibular effects of the aminoglycosides. The aminoglycosides can also cause neuromuscular blockade, facial edema, pain or inflammation at the injection site, peripheral neuropathy, and hypersensitivity reactions. Rarely, GI clinical signs, hematologic, and hepatic effects have been reported. Reproductive/nursing Safety T obramycin can cross the placenta and concentrate in fetal kidneys and while rare, cause 8th cranial nerve toxicity or nephrotoxicity in fetuses. T otal irreversible deafness has been reported in some hu-man babies whose mothers received tobramycin during pregnancy. Because the drug should only be used in serious infections, the ben-efits of therapy may exceed the potential risks. In humans, the FDA categorizes this drug as category D for use during pregnancy (There is evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women may be acceptable despite its potential risks. ) In a separate system evaluating the safety of drugs in canine and feline pregnancy (Papich 1989), this drug is categorized as in class: C (These drugs may have potential risks. Studies in people or laboratory animals have uncovered risks, and these drugs should be used cautiously as a last resort when the benefit of therapy clearly out-weighs the risks. ) Small amounts of aminoglycoside antibiotics are excreted in milk, but are unlikely to cause clinically significant effects in nurs-ing offspring. overdosage/acute t oxicity Should an inadvertent overdosage be administered, three treat-ments have been recommended: 1) Hemodialysis is very effective in reducing serum levels of the drug, but is not a viable option for most veterinary patients; 2) Peritoneal dialysis also will reduce se-rum levels, but is much less efficacious; 3) Complexation of drug with either carbenicillin or ticarcillin (12-20 g/day in humans) is reportedly nearly as effective as hemodialysis. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving tobramycin and may be of significance in veterinary patients: beta-Lactam antibiotic S T! (penicillins, cephalosporins ): May have synergistic effects against some bacteria; some potential for inac-tivation of aminoglycosides in vitro (do not mix together) and in vivo (patients in renal failure) ce PHa Lo SPo Rin ST! : The concurrent use of aminoglycosides with cephalosporins is somewhat controversial. Potentially, cepha-losporins could cause additive nephrotoxicity when used with aminoglycosides, but this interac tion has only been well docu-mented with cephaloridine and cephalothin (both no longer marketed). Diu Retic S, Loo PT! (e. g., furosemide, torsemide ) or o Smotic (e. g., man-nitol): Concurrent use with loop or osmotic diuretics may increase the nephrotoxic or ototoxic potential of the aminoglycosides ne PHRotoxic DRu GS, ot He R T! (e. g., cisplatin, amphotericin b, polymyxin b, or vancomycin ): Potential for increased risk for nephrotoxicity neu Romu Scu La R b Lockin G a Gent S & ane St Hetic S, Gene Ra L T! : Con-comitant use with general anesthetics or neuromuscular block-ing agents could potenti ate neuromuscular blockade Laboratory considerations T obramycin serum concentrations may be falsely decreased if the T! patient is also receiving beta-lactam antibiotics and the serum is stored prior analysis. It is recommended that if assay is delayed, samples be frozen and, if possible, drawn at times when the beta-lactam antibiotic is at a trough level. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
tob Ramycin Su LF ate 891 Doses note : There is significant inter-patient variability with amino-glycoside pharmacokinetic parameters. T o insure therapeutic levels and to minimize the risks for toxicity development, con-sider monitoring serum levels for this drug. Like other amino-glycosides, most now recommend dosing mammals once daily; consider giving the total daily dose as a single dose (e. g., if dose listed is 2 mg/kg q8h, give 6 mg/kg once daily). Do GS & cat S:T! For small animals, one pair of authors (Aronson and Aucoin 1989) make the following recommendations with regard to min-imizing risks of toxicity, yet maximizing efficacy: 1) Dose according to animal size. The larger the animal, the smaller the dose (on a mg/kg basis). 2) The more risk factors (age, fever, sepsis, renal disease, dehy-dration) the smaller the dose. 3) In old patients or those suspected of renal disease, increase dosing interval from q8h to q16-24h. 4) Determine serum creatinine prior to therapy and adjust by changes in level even if it remains in “normal range. ” 5) Monitor urine for changes in sediment (e. g., casts) or con-centrating ability. Not very useful in patients with UTI. 6) Therapeutic drug monitoring is recommended when possible. a) 2 mg/kg IV, IM, or SC q8h (avoid use or reduce dosage in patients with renal failure; recommend therapeutic drug monitoring, particularly in young animals) (Vaden and Papich 1995) b) For susceptible UTI: 1-2 mg/kg SC q8h (Brovida 2003) c) For sepsis: 2-4 mg/kg IV three times daily (q8h) (T ello 2003b) d) Dogs: For soft tissue, systemic infections: 1-1. 7 mg/kg IV q8h or 3-5. 1 mg/kg IV q24h for less than 7 days; For systemic infections: 2 mg/kg SC q8-12h or 4-6 mg/ kg SC q24h for less than 7 days;For persistent bacteremia: 3-5 mg/kg IV, IM, SC q8h or 9-15 mg/kg IV, IM or SC q24h for 7 days or less. (Greene, Hartmannn et al. 2006) e) Cats:For soft tissue, systemic infections: 2 mg/kg IV, IM or SC q12h or 4 mg/kg IV, IM, SC q24h for 5 days or less; For persistent bacteremia: 2 mg/kg IV, IM, SC q8h or 6 mg/kg IV, IM or SC q24h for 5 days or less. (Greene, Hartmannn et al. 2006) Ho RSe S:T! For susceptible infections: a) 1-1. 7 mg/kg q8h IV (slowly) or IM ( note : This is a human dose and should be used as a general guideline only) (Walker 1992) LLama S:T! For susceptible infections: a) 4 mg/kg IV q24h; 0. 75 mg/kg IV q8h (Baird 2003) bi RDS:T! For susceptible infections:a) 5 mg/kg IM every 12 hours (Bauck and Hoefer 1993) b) 2. 5-5 mg/kg/day; must be given parenterally (Flammer 2003b)Re Pti Le S:T! For susceptible infections: a) 2. 5 mg/kg once daily IM (Gauvin 1993) monitoring Efficacy (cultures, clinical signs associated with infection)T! Renal toxicity; baseline urinalysis, and serum creatinine/BUN. T! Casts in the urine are often the initial sign of impending neph-rotoxicity. Frequency of monitoring during therapy is contro-versial, but daily urinalysis and serum creatinine may not be too frequent. Gross monitoring of vestibular or auditory toxicity is T! recommended Serum levels if possible T! client information With appropriate training, owners may give subcutaneous injec-T! tions at home, but routine monitoring of therapy for efficacy and toxicity must still be done Clients should understand that the potential exists for severe T! toxicity (nephrotoxicity, ototoxicity) developing from this medication chemistry/Synonyms An aminoglycoside derived from Streptomyces tenebrarius, to-bramycin occurs as a white to off-white, hygroscopic powder that is freely soluble in water and very slightly soluble in alcohol. The sulfate salt is formed during the manufacturing process. The com-mercial injection is a clear, colorless solution and the p H is adjusted to 6-8 with sulfuric acid and/or sodium hydroxide. T obramycin Sulfate may also be known as: tobramycin sul-phate, Brulamycin®, Gernebcin®, Mytobrin®, Nebcina®, Nebcine®, Nebicina®, Obracin®, Tobra ®, Tobra Gobens®, TOBI®, Tobra Laf®, Tobra-cell®, Tobracil®, Tobradistin®, Tobramina®, Tobraneg®, Tobrasix®, Tobrex ®, Tomycin ®, or Trazil®. Storage/Stability/compatibility T obramycin sulfate for injection should be stored at room tempera-ture (15-30°C); avoid freezing and temperatures above 40°C. Do not use the product if discolored. While the manufacturers state that tobramycin should not be mixed with other drugs, it is reportedly physically compatible and stable in most commonly used intravenous solutions (not com-patible with dextrose and alcohol solutions, Polysal, Polysal M, or Isolyte E, M or P) and compatible with the following drugs: az-treonam, bleomycin sulfate, calcium gluconate, cefoxitin sodium, ciprofloxacin lactate, clindamycin phosphate (not in syringes), floxacillin sodium, metronidazole (with or without sodium bicar-bonate), ranitidine HCl, and verapamil HCl. The following drugs or solutions are reportedly physically incompatible or only compatible in specific situations with to-bramycin: cefamandole naftate, furosemide and heparin sodium. Compatibility is dependent upon factors such as p H, concentra-tion, temperature, and diluent used; consult specialized references or a hospital pharmacist for more specific information. In vitro inactivation of aminoglycoside antibiotics by beta-lactam antibiotics is well documented; see the information in the Drug Interaction and Laboratory Consideration sections. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
892 tocaini De Hc L Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: T obramycin Sulfate Injection: 0. 8 mg/m L and 1. 2 mg/m L (as sulfate) in 100 m L & 50 m L single-dose containers; 10 mg/m L in 2 m L vials; and 40 mg/m L in 1. 5 m L and 2 m L syringes, 2 m L and 30 m L vials; T obramycin in 0. 9% Sodium Chloride (Hospira); generic (various); (Rx) T obramycin Sulfate Powder for Injection: 1. 2 g vials (40 mg/m L after reconstitution), preservative free in 50 m L bulk package vial; generic (American Pharmaceutical Partners); (Rx) T obramycin Nebulizer Solution: 60 mg/m L in 5 m L amps; TOBI® (Patho Genesis); (Rx)Also available in ophthalmic preparations. tocainide Hcl (toe-kay-nide) Tonocard® oral antiarrhythmic Prescriber Highlights Oral antiarrhythmic with similar activity as lidocaine; not T T commonly used in veterinary medicine Contraindications: Hypersensitivity reactions to it or T T amide-type local anesthetics, 2nd or 3rd degree AV block & not being artificially paced. Caution: Heart failure, hematologic abnormalities, or preexisting bone marrow failure. Adverse Effects: CNS effects (depression, ataxia, muscle T T tremors, etc. ), nausea & vomiting (usually transient), car-diovascular effects (hypotension, bradycardia, tachycar-dia, other arrhythmias, & exacerbation of CHF) Case reports of dogs on long-term therapy (>3 mos. ) de-T T veloping ocular & renal toxicity uses/indications Veterinary experience with tocainide is limited. At this time, dogs are the only veterinary species where enough clinical experience has been garnered to recommend its use. It is indicated for the oral ther-apy of ventricular arrhythmias, principally ventricular tachycardia and ventricular premature complexes. In humans, response to lido-caine can usually predict whether tocainide might be effective. Pharmacology/actions T ocainide is considered a class IB (membrane-stabilizing) antidys-rhythmic agent that demonstrates rapid rates of attachment and dissociation to sodium channels. Like lidocaine, tocainide produces a dose-dependent decrease in potassium and sodium conductance that results in decreased excitability of myocardial cells. Automaticity, conduction velocity, and effective refractory periods are decreased at therapeutic levels. Little or no increases in PR intervals, QRS com-plexes, or QT intervals are seen at therapeutic levels. Like lidocaine, tocainide has little, if any effect, on autonomic tone. Pharmacokinetics Following oral administration, tocainide is rapidly and almost completely absorbed. The presence of food in the stomach may al-ter the rate, but not the extent, of absorption. Unlike lidocaine, the hepatic first-pass effect is minimal with tocainide. In humans, peak plasma levels occur between 0. 5-2 hours when administered on an empty stomach. The distribution aspects of tocainide have not been fully de-scribed. In humans, the volume of distribution ranges from 1. 5-4 L/kg and has been reported to be 1. 7 L/kg in dogs. T ocainide is minimally bound to plasma proteins. It is unknown if it crosses the placenta or enters into the milk. T ocainide is metabolized by the liver, but up to 50% of a dose is excreted unchanged by the kidneys into the urine. Alkalinization of the urine may result in a substantial decrease in the amount of tocainide that is excreted unchanged into the urine, but acidifica-tion of the urine reportedly does not enhance the excretion rate. Elimination half-life is dose-dependent and at the clinical doses used for dogs, not well-described. contraindications/Precautions/Warnings T ocainide is contraindicated in patients who have demonstrated previous hypersensitivity reactions to it or amide-type local anes-thetics, or who have 2nd or 3rd degree A V block and are not being artificially paced. Use tocainide cautiously in patients with heart failure as it has the potential to aggravate the condition. Use with caution in pa-tients with hematologic abnormalities or preexisting bone marrow failure. adverse effects It is expected that tocainide would exhibit a similar adverse reaction profile as lidocaine with anorexia, and vomiting being most likely. In dogs, tocainide serum concentrations of greater than 12 mcg/m L have been associated with neurotoxicity (ataxia, head tremor). There are case reports of dogs receiving tocainide for more than 3 months developing ocular (corneal dystrophy) and renal toxicity. Although side effects are common in human patients, they are usually dose related, mild, and reversible upon discontinuation of the drug. CNS effects can include drowsiness, depression, ataxia, muscle tremors, etc. Nausea and vomiting may occur, but are usu-ally transient. Cardiovascular effects reported include hypotension, bradycardia, tachycardia, other arrhythmias, and exacerbation of CHF. Rarely (<1% incidence), clinical signs of bone marrow de-pression or pulmonary effects (pulmonary fibrosis, pneumonia, respiratory arrest, pulmonary edema, etc. ) have been reported in humans. Reproductive/nursing Safety In humans, the FDA categorizes this drug as category C for use dur-ing pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) T ocainide enters milk in significant quantities and may poten-tially cause adverse effects in nursing offspring. overdosage/acute t oxicity Dogs tend to be rather resistant to the acute toxic effects of the drug. In one study, dogs were administered 750 mg/kg over 6 hours and emesis was the only frequent effect seen, but ECG changes were also seen in some animals. There is no specific antidote for tocainide overdose and treat-ment tends to be supportive and symptomatic. For more informa-tion, see the Lidocaine monograph. T ocainide can be removed with hemodialysis. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
to Lazo Line Hc L 893 Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving tocainide and may be of significance in veterinary patients: antia RRHyt Hmic S, ot He R c La SS ib T! (e. g., lidocaine, phenytoin, mexi-letine ): T oxicities may be additive, with little or no therapeutic gain, if tocainide is used concurrently with other Class IB anti-dysrhythmics; use caution, when converting from one Class IB agent to another cimeti Dine T! (and other H2 blockers ): May reduce tocainide bio-availability meto PRo Lo LT! : T ocainide used concomitantly with metoprolol (a beta-adrenergic antagonist) can have additive effects on car-diac index and wedge pressure; may clinically significant, par-ticularly in patients with sick sinus syndrome and impaired A V conduction Ri Fam Pin T! : May decrease tocainide effects by increasing metabolism Doses Do GS:T! a) 10-20 mg/kg (up to 25 mg/kg) PO q8h (Ware 2000) b) 5-10 mg/kg PO three times daily (Atkins 2003a) c) 10-20 mg/kg PO q8h (Fox 2003a) d) 10-20 mg/kg PO two to three times a day (Tilley 2007) monitoring ECGT! Clinical signs of toxicity (see Adverse Reactions); may wish to T! monitor CBC's if treating chronically ( note: For human patients, the manufacturer recommends weekly CBC's with differential and platelets, be run at weekly intervals for the first 3 months of therapy and periodically thereafter) Serum levels (therapeutic levels in humans are usually 3-10 mi-T! crograms/m L), especially if clinical signs of toxicity or lack of ef-ficacy are noted. client information T o be effective, the animal must receive all doses as prescribed T! Notify veterinarian if the animal exhibits any abnormal bleeding T! or bruising, develops wheezing, shortness of breath, or a cough If dog vomits or becomes anorexic after dosing, give with food; T! if vomiting persists or animal develops a change in behavior or attitude, contact veterinarian chemistry/Synonyms An amide-type local anesthetic, tocainide HCl occurs as a bit-ter tasting, white, crystalline powder with a p K a of 7. 8. It is freely soluble in both water and alcohol. T ocainide is structurally related to lidocaine, but it is a primary amine where lidocaine is a tertiary amine. This modification allows tocainide to be resistant to exten-sive first-pass metabolism after oral administration. T ocainide HCl may also be known as W-36095, Tonocard® or Xylotocan®. Storage/Stability Protect tablets from light and store in well-closed containers. An expiration date of 4 years after manufacture is assigned to the com-mercially available tablets when packaged in high-density polyeth-ylene bottles. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: T ocainide HCl Oral Tablets: 400 mg, 600 mg; Tonocard® (Astra Mer-ck); (Rx) tolazoline Hcl (toe-laz-oh-leen) Tolazine® al Pha-adrenergic blocker Prescriber Highlights Alpha-adrenergic blocker used primarily as a reversal T T agent for xylazine Contraindications: Horses exhibiting signs of stress, de-T T bilitation, cardiac disease, sympathetic blockage, hypov-olemia or shock, hypersensitivity, or with coronary artery or cerebrovascular disease Adverse Effects: T T HORSES: Transient tachycardia; periph-eral vasodilatation presenting as sweating & injected mucous membranes of the gingiva & conjunctiva; hype-ralgesia of the lips (licking, flipping of lips); piloerection; clear lacrimal & nasal discharge; muscle fasciculations; apprehensiveness uses/indications T olazoline is approved and indicated for the reversal of effects asso-ciated with xylazine in horses. It has also been used for this purpose in a variety of other species as well, but less safety and efficacy data is available. In humans, the primary uses for tolazoline are: treatment of per-sistent pulmonary hypertension in newborns, adjunctive treatment and diagnosis of peripheral vasospastic disorders, and as a provoca-tive test for glaucoma after subconjunctival injection. Pharmacology/actions By directly relaxing vascular smooth muscle, tolazoline has periph-eral vasodilating effects and decreases total peripheral resistance. T olazoline also is a competitive alpha 1 and alpha 2-adrenergic blocking agent, explaining its mechanism for reversing the effects of xylazine. T olazoline is rapid acting (usually within 5 minutes of IV administration), but has a short duration of action and repeat doses may be required. Pharmacokinetics After IV injection in horses, tolazoline is widely distributed. Animal studies have demonstrated that tolazoline is concentrated in the liver and kidneys. Half-life in horses at recommended doses is ap-proximately 1 hour. contraindications/Precautions/Warnings The manufacturer does not recommend use in horses exhibiting signs of stress, debilitation, cardiac disease, sympathetic blockage, hypovolemia, or shock. Safe use for foals has not been established and some believe it should not be used in foals. as adverse reactions and fatalities have been reported. T olazoline should be considered contraindicated in patients known to be hypersensitive to it, or with coronary artery or cerebro-vascular disease. Humans having any of the above-contraindicated conditions should use extra caution when handling the agent. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
894 to Lazo Line Hc L adverse effects In horses adverse effects that may occur include: transient tachycar-dia; peripheral vasodilatation presenting as sweating and injected mucous membranes of the gingiva and conjunctiva; hyperalgesia of the lips (licking, flipping of lips); piloerection; clear lacrimal and nasal discharge; muscle fasciculations; apprehensiveness. Adverse effects should diminish with time and generally disappear within 2 hours of dosing. The potential for adverse effects increases if tola-zoline is given at higher than recommended dosages or if xylazine has not be previously administered. Reproductive/nursing Safety Safety during pregnancy, in breeding or lactating animals has not been established. It is unknown if the drug enters maternal milk. overdosage/acute t oxicity In horses given tolazoline alone (no previous xylazine), doses of 5X recommended resulted in gastrointestinal hypermotility with resultant flatulence and defecation or attempt to defecate. Some horses exhibited mild colic and transient diarrhea. Intraventricular conduction may be slowed when horses are overdosed, with a pro-longation of the QRS-complex noted. Ventricular arrhythmias may occur resulting in death with higher overdoses (5X). In humans, ephedrine (NOT epinephrine or norepinephrine) has been recom-mended to treat serious tolazoline-induced hypotension. A llama that received 4. 3 mg/kg IV and again 45 minutes later (approximately a 5X overdose) developed signs of anxiety, hyperes-thesia, profuse salivation, GI tract hypermotility, diarrhea, convul-sions, hypotension, and tachypnea. Treatment including IV diaz-epam, phenylephrine, IV fluids, and oxygen was successful. (Reed, Duke et al. 2000). Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving tolazoline and may be of significance in veterinary patients: a Lco Ho LT! : Accumulation of acetaldehyde can occur if tolazoline and alcohol are given simultaneously e Pine PHRine, no Re Pine PHRine T! : If large doses of tolazoline are given with either norepinephrine or epinephrine, a paradoxical drop in blood pressure can occur followed by a precipitous increase in blood pressure Doses Ho RSe S:T! For reversal of xylazine effects: a) 4 mg/kg slow IV (4 m L/220 lb. of body weight); administra-tion rate should approximate 1 m L/second (Package Insert; Tolazine®—Lloyd Laboratories) Do GS & cat S: T! For reversal of xylazine effects: a) 4 mg/kg slow IV (4 m L/220 lb. of body weight); administra-tion rate should approximate 1 m L/second (Package Insert; Tolazine®—Lloyd Laboratories; New Zealand) note : If reversal is warranted, the high concentration (100 mg/m L) of the veterinary drug may make accurate dosing difficult; yohimbine or the human-labeled tolazoline prod-uct (25 mg/m L) may be safer alternatives than Tolazine® (100 mg/m L). note : T olazoline is not approved for use in dogs and cats in the USA and the US manufacturer does not recom-mend its use LLama S/a LP aca S: T! For reversal of xylazine/ketamine effects: a) 2 mg/kg IM (Du Bois, Prado et al. 2004) b) 1-2 mg/kg IV or IM; Caution: acute death has been reported after rapid IV administration of tolazoline at high dosages. (Anderson 2005) bi RDS:T! As a reversal agent for alpha2-adrenergic agonists (e. g., xylazine, detomidine, etc. ): a) 15 mg/kg IV (Clyde and Paul-Murphy 2000) Dee R: T! note : Not approved in the USA for use in food animals For reversal of xylazine effects: a) 2-4 mg/kg slow IV; titrate to effect; Slaughter withdrawal: 30 days (Label Directions; Tolazine®—Lloyd Laboratories; New Zealand) catt Le: T! note : Not approved in the USA for use in food animals For reversal of xylazine effects: a) 2-4 mg/kg slow IV; titrate to effect; Slaughter withdrawal: 30 days (Label Directions; Tolazine®—Lloyd Laboratories; New Zealand) SHee P & Goat S:T! note : Not approved in the USA for use in food animals For reversal of xylazine effects:a) 2-4 mg/kg slow IV; titrate to effect; Slaughter withdrawal: 30 days (Label Directions; Tolazine®—Lloyd Laboratories; New Zealand) b) Goats: 1-2 mg/kg IV, inject slowly to effect (Hooper 2002) c) Sheep: 2. 2 mg/kg slowly IV. (Snyder 2006) monitoring/client information Reversal effects (efficacy)T! Adverse effects (see above). Because of the risks associated with T! the use of xylazine and reversal by tolazoline, these drugs should be administered and monitored by veterinary professionals only. chemistry/Synonyms An alpha-adrenergic blocking agent, tolazoline HCl is structurally related to phentolamine. It occurs as a white to off-white, crystal-line powder possessing a bitter taste and a slight aromatic odor. T olazoline is freely soluble in ethanol or water. The commercially available (human) injection has p H between 3-4. T olazoline HCl may also be known as: benzazoline hydrochlo-ride, tolazolinium chloratum, Priscol ®, Priscoline®, Tolazine® or Vaso-Dilatan®. Storage/Stability/compatibility Commercially available injection products should be stored be-tween 15-30°C and protected from light. The drug is reportedly physically compatible with the commonly used IV solutions. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: T olazoline HCl Injection: 100 mg/m L in 100 m L multi-dose vials; To-lazine® (Lloyd); (Rx). Approved for use in horses; not to be used in food-producing animals. Human-Labe Le D PRo Duct S: None | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
to LFenamic aci D 895 tolfena Mic acid (tole-fen-a-mik) Tolfedine® non Steroidal antiinflammatory agent Prescriber Highlights NSAID approved for dogs & cats in Canada, Europe T T Available (not in USA) in both oral & injectable dosage T T forms Relatively safe for short-term use T T uses/indications T olfenamic acid may be useful for the treatment of acute or chronic pain and/or inflammation in dogs and acute pain/inflammation in cats. In Europe, it is also approved for use in cattle. Pharmacology/actions T olfenamic acid exhibits pharmacologic actions similar to those of aspirin. It is a potent inhibitor of cyclooxygenase, thereby inhibiting the release of prostaglandins. It also has direct inhibition of prosta-glandin receptors. T olfenamic acid has significant anti-thrombox-ane activity and is not recommended for use pre-surgically because of its effects on platelet function. Pharmacokinetics T olfenamic acid is absorbed after oral administration. In dogs, peak levels occur from 2-4 hours after dosing. Enterohepatic recircula-tion is increased if given with food. This can increase the bioavail-ability, but also creates more variability in bioavailability than when given to fasted dogs. The volume of distribution in dogs is reported to be 1. 2 L/kg and it has an elimination half-life of about 6. 5 hours. Duration of antiinflammatory effect is 24-36 hours. contraindications/Precautions/Warnings T olfenamic acid is contraindicated in animals hypersensitive to it or to other drugs in its class (i. e., meclofenamic acid). Like other NSAIDs, it should not be used in animals with active GI bleeding or ulceration. Use with caution in patients with decreased renal or hepatic function. adverse effects T olfenamic acid is relatively safe when given as recommended in dogs and cats. Vomiting and diarrhea have been reported after oral use. Experimental studies did not demonstrate significant renal or GI toxicity until doses were more than 10 times labeled. Because of its anti-thromboxane activity and resultant effects on platelet function, tolfenamic acid is not recommended for use pre-surgically. Reproductive/nursing Safety No specific information was located; like other NSAIDs, tolfenamic acid should be used with caution in pregnancy. overdosage/acute t oxicity No specific information was located. It is suggested that if an acute, overdose occurs treatment follows standard overdose procedures (empty gut following oral ingestion, etc. ). Supportive treatment should be instituted as necessary and IV diazepam used to help control seizures. Monitor for GI bleeding. Because tolfenamic acid may cause renal effects, monitor electrolyte and fluid balance care-fully and manage renal failure using established guidelines. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving tolfenamic acid or other NSAIDs and may be of significance in veterinary patients: a SPi Rin T! : May increase the risk of gastrointestinal toxicity (e. g., ul-ceration, bleeding, vomiting, diarrhea) co Rtico Ste Roi DST! : As concomitant corticosteroid therapy may in-crease the occurrence of gastric ulceration, avoid the use of these drugs when also using tolfenamic acid Di Goxin T! : NSAIDS may increase serum levels FLuconazo Le T! : Administration has increased plasma levels of cele-coxib in humans and potentially could also affect tolfenamic acid levels in dogs Fu Ro Semi De T! : NSAIDs may reduce saluretic and diuretic effects met Hot Rexate T! : Serious toxicity has occurred when NSAIDs have been used concomitantly with methotrexate; use together with extreme caution ne PHRotoxic DRu GST! (e. g., furosemide, aminoglycosides, amphotericin b, etc. ): May enhance the risk of nephrotoxicity n Sai DS, ot He R T! : May increase the risk of gastrointestinal toxicity (e. g., ulceration, bleeding, vomiting, diarrhea) Wa RF a Rin T! : Closely monitor patients also receiving drugs that are highly bound to plasma proteins (e. g., warfarin), as tolfenamic acid and its active metabolite are 98-99% protein bound in the dog Doses Do GS:T! a) For acute pain: 4 mg/kg once daily SC, IM or PO for 3-5 days. For chronic pain: 4 mg/kg, PO once daily for 3-5 consecu-tive days per week. The injectable is suggested for the first dose only. (Dowling 2000) b) First dose: 4 mg/kg SC or IM; follow with tablets at 4 mg/kg PO once daily for 2-4 days. The treatment may be re-peated once a week as required, or as recommended by the veterinarian, PO once daily for 3-5 days. (Label informa-tion; Tolfedine®—Vetoquinol Canada) cat S:T! a) For acute pain: 4 mg/kg once daily SC, IM or PO for 3-5 days. The injectable is suggested for the first dose only. (Dowling 2000) b) 4 mg/kg PO once daily for 3-5 days or as recommended by the veterinarian. (Label information; Tolfedine®—Vetoquinol Canada) monitoring Clinical efficacy T! Adverse effects T! client information The weekly dosing regimen (3-5 consecutive days per week for T! dogs) is important to follow to minimize risks of adverse effects Report any changes in appetite, water consumption, or GI dis-T! tress to veterinarian chemistry/Synonyms A non-steroidal antiinflammatory agent in the anthranilic acid (fe-namate) category, tolfenamic acid is related chemically to meclofe-namic acid. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
896 to Lt Razu Ri L T olfenamic Acid may also be known as: acidum tolfenam-icum, Bifenac®, Clotam®, Clotan®, Fenamic®, Flocur®, Gantil®, Migea®, Polmonin®, Purfalox®, Rociclyn®, Tolfamic®, Tolfedine® or Turbaund®. Storage/Stability Unless otherwise labeled, store tolfenamic acid tablets and solution at room temperature. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None in the USA. In Canada and Europe: T olfenamic Acid Tablets: 6 mg, 30 mg, 60 mg and T olfenamic Acid Injection 40 mg/m L are available. Common trade name is Tolfedine® (Vetoquinol). Human-Labe Le D PRo Duct S: None in the USA toltrazuril (tole-traz-yoo-ril) Baycox® anti Protozoal/anticoccidial Prescriber Highlights Antiprotozoal labeled for treating coccidia in poultry (in T T Europe) May be considered as an alternative for treating coccidi-T T osis in dogs & cats, oocyst shedding stage of toxoplas-mosis in cats, etc. Not commercially available in the USA, must be legally T T imported Adverse effect profile not well described T T uses/indications T oltrazuril is an antiprotozoal agent that may be considered as an alternative treatment for coccidiosis in dogs and cats, Hepatazoon infections, or for treating the oocyst shedding stage of toxoplasmo-sis in cats. It has also been used as a treatment for overwhelming parasitic loads in lizards (Bearded Dragons). T oltrazuril has activity against parasites of the genus Hepatozoon, but other drugs (e. g., imidocarb, primaquine, doxycycline) are gen-erally used. While toltrazuril has been used to treat equine protozoal my-eloencephalitis (EPM) caused by Sarcocystis neurona, use of ap-proved products now available (e. g., nitazoxanide, ponazuril, py-rimethamine/sulfadiazine) is preferred. T oltrazuril has been used in some countries to treat Isospora suis in piglets. Pharmacology/actions T oltrazuril is the parent compound to ponazuril (toltrazuril sul-fone). Its mechanism of action is not well understood, but it ap-pears to inhibit protozoal enzyme systems. T oltrazuril has activity against Hepatozoon, Isospora, Sarcocystis, Toxoplasma, and all intracellular stages of coccidia. Pharmacokinetics Little information is available. T oltrazuril is about 50% absorbed after oral consumption in poultry. Highest concentrations are found in the liver; it is rapidly metabolized into the sulfone deriva-tive (ponazuril). contraindications/Precautions/Warnings T oltrazuril should not be used in patients who have had prior hy-persensitivity reactions to it or other triazinone (triazine) antipro-tozoals (e. g., ponazuril, diclazuril). The principle metabolite of toltrazuril reportedly persists in the environment and can contaminate groundwater, however there ap-pears to be little risk for significant environmental contamination when toltrazuril is used in dogs, cats, horses, or other companion animals (pet birds, reptiles). adverse effects T oltrazuril appears to be well tolerated in birds. An adverse effect profile in mammals is not well described. Potentially, GI signs could occur. Some horses receiving the related drug ponazuril, developed blisters on their nose and mouth, and some, a rash or hives during field trials. Reproductive/nursing Safety No reproductive or nursing safety information was located; weigh potential risks versus benefits of use during pregnancy or lactation. overdosage/acute t oxicity Very limited information is available. Doses of up to 10x in horses were tolerated without significant adverse effects. 5x overdoses in poultry have been tolerated without clinical signs noted. Decreased water intake has been seen if overdoses are greater than 5X. Drug interactions None reported Laboratory considerations No issues were noted. Doses Do GS:T! a) For coccidiosis (Cystoisosporosis): 10-20 mg/kg PO one time to all puppies at 3-4 weeks of age will help prevent problems associated with intestinal coccidiosis (Daugschies, Mundt et al. 2000) b) For coccidiosis: 15 mg/kg PO once daily for 3-6 days (Dubey and Greene 2006) cat S:T! a) For enteroepithelial cycle of toxoplasmosis (oocyst shed-ding): 5-10 mg/kg PO once daily for 2 days (Dubey and Lappin 2006) b) For coccidiosis: 30 mg/kg PO once daily for 2-3 days (Greene, Hartmannn et al. 2006) bi RDST! : a) For coccidiosis in raptors: 7 mg/kg PO once daily for 2-3 days (Jones 2004b) Re Pti Le S:T! a) For parasitism in Bearded Dragons: 5-15 mg/kg PO once daily for 3 days (Kramer 2006) monitoring Clinical efficacy T! client information Avoid direct contact with this medication; the manufacturer rec-T! ommends wearing synthetic rubber gloves when handling the 2. 5% solution. Wash exposed skin after use. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
to Pi Ramate 897 chemistry/Synonyms Related to other antiprotozoals such as ponazuril, toltrazuril is a triazinone (triazine) antiprotozoal (anticoccidial) agent. The com-mercially available (in Europe) 2. 5% oral solution is an alkaline, clear, colorless to yellow brown solution which also contains tri-ethanolamine 30 mg/m L and polyethylene glycol 80. 7 mg/m L. T oltrazuril has a molecular weight of 425. 4 T oltrazuril may also be known as Bay-Vi-9142, toltrazurilo, tol-trazurilum and Baycox ®. Storage/Stability The 2. 5% solution should be stored at temperatures at 25°C or b e l o w. Dilutions in drinking water more concentrated than 1:1000 (1 m L of the 2. 5% solution to 1 liter of water) may precipitate. After dilution, the resulting solution is stable for 24 hours. It is recom-mended that medicated drinking water not consumed after 24 hours be discarded. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None in the USA In some European countries: T oltrazuril 2. 5% (25 mg/m L) solu-tion for dilution in drinking water in 1 liter bottles; Baycox ® 2. 5% Solution (Bayer); (Rx). Approved for treatment of coccidiosis in poultry. In the UK, slaughter withdrawal is 18 days for poultry. Not for use in birds producing eggs for human consumption. The FDA may allow legal importation of this medication for com-passionate use in animals; for more information, see the Instructions for Legally Importing Drugs for Compassionate Use in the USA found in the appendix. Human-Labe Le D PRo Duct S: None topira Mate (toe-pie-rah-mate) Topamax® anticonvul Sant Prescriber Highlights Antiseizure medication that may be useful for seizure T T disorders in dogs, particularly partial seizure activity; may be of benefit in treating cats, but little information available Very short half-life in dogs (2-4 hours), but therapeutic T T activity may persist secondary to high affinity for recep-tors in brain Adverse effect profile may include GI distress, inap-T T petance, & irritability in dogs; in cats, sedation & inap-petance have been noted Expense may be an issue; generics now available T T uses/indications T opiramate may be useful for treating seizures in dogs, particularly partial seizure activity. It may also be of benefit in treating cats, but little information is available. Pharmacology/actions While the exact mechanism for its antiseizure action is not known, topiramate possesses three properties that probably play a role in its activity: T opiramate blocks in a time-dependent manner ac-tion potentials elicited repetitively by a sustained depolarization of neurons; it increases the frequency that GABA activates GABAA receptors; and it antagonizes the kainite/AMPA receptors without affecting the NMDA receptor subtype. T opiramate's actions are concentration-dependent; effects can first be seen at 1micro Mole and maximize at 200 micro Moles. T opiramate is a weak inhibitor of carbonic anhydrase isoenzymes CA-II and CA-IV, but it is believed that this effect does not contribute significantly to its antiepileptic actions. Pharmacokinetics In dogs, topiramate is rapidly absorbed after oral administration, but absolute bioavailability varies between 30-60%. Half-life rang-es from 2-4 hours after multiple doses. Comparatively, the half-life in humans is about 21 hours in adults, but shorter in children. In humans, the drug is not extensively metabolized and about 70% is excreted unchanged in the urine. contraindications/Precautions/Warnings T opiramate is contraindicated in patients hypersensitive to it. It should be used with caution (in humans) with impaired hepatic or renal function. adverse effects Because this drug rarely has been used in veterinary patients, an ac-curate adverse effect profile is not known. In dogs, most prevalent adverse effects reported include GI distress, inappetance, and irrita-bility. In cats, sedation and inappetance have been noted. In humans, the most likely adverse effects include somnolence, dizziness, nervousness, confusion, and ataxia. Very rarely, acute myopia with secondary angle closure glaucoma has been reported. Incidence of kidney stones is about 2-4 times higher in patients taking topiramate than in the general population. Reproductive/nursing Safety In humans, the FDA categorizes topiramate as a category C drug for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) T eratogenic effects were noted in mice and rats given topiramate at dosages equivalent to those used in humans. T opiramate enters maternal milk; use with caution in nursing patients. overdosage/acute t oxicity There were 132 exposures to topiramate reported to the ASPCA Animal Poison Control Center (APCC; www. apcc. aspca. org) dur-ing 2005-2006. In these cases 113 were dogs with 10 showing clini-cal signs and 19 were cats with 4 showing clinical signs. Common findings in dogs recorded in decreasing frequency included ataxia, lethargy, anxiety, disorientation and head shaking. Common find-ings in cats recorded in decreasing frequency included vomiting, ataxia and lethargy. Overdoses in humans have cause convulsions, drowsiness/leth-argy, slurred speech, blurred and double vision, impaired menta-tion/stupor, ataxia, metabolic acidosis, hypotension, agitation, and abdominal pain. Treatment consists of gut emptying protocols if the ingestion was recent, and supportive therapy. Hemodialysis is effective in en-hancing the elimination of topiramate from the body. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
898 to RSemi De Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving topiramate and may be of significance in veterinary patients: amit Ri Pty Line T! : T opiramate may increase levels ca Rbonic an Hy DRa Se in Hibito RST! (acetazolamide, dichlorphenamide, etc. ): Used concomitantly with topiramate, may increase the risk of renal stone formation cn S De PRe SSant DRu GS, ot He R T! : Other CNS depressant drugs may exacerbate the adverse effects of topiramate Lamot Ri Gine T! : May increase topiramate levels PHenytoin T! : May decrease topiramate levels; phenytoin levels may increase Va LPRoic aci DT! : May decrease topiramate and VPA levels Laboratory considerations No specific laboratory interactions or considerations were noted. Plasma concentrations of topiramate are usually not monitored in human patients, but therapeutic levels are thought to range from 2-25 mg/L. Doses Do GS:T! a) As an alternative second line anticonvulsant: 5-10 mg/kg PO q12h (Shell 2003c) b) As an alternative treatment for refractory generalized and fo-cal seizures: 5-10 mg/kg PO twice daily (Smith 2002b) c) Initial dose of 2-10 mg/kg PO q12h. (Podell 2006a) d) 5-10 mg/kg PO twice daily; start at the lower dosage to re-duce adverse effects. (Kortz 2005) cat S:T! a) 12. 5-25 mg PO (total dose) q8-12h. (Podell 2006a) monitoring Efficacy T! Adverse effects T! client information Clients must understand that the clinical use of this agent is T! relatively “investigational” in veterinary patients, that it must be dosed often in dogs, and the potential costs Caution clients not to stop therapy abruptly or “rebound” sei-T! zures may occur Have clients maintain a seizure diary to help determine efficacy T! chemistry/Synonyms A sulfamate-substituted derivative of D-fructose antiepileptic, topi-ramate occurs as a white crystalline powder with a bitter taste. Its solubility in water is 9. 8 mg/m L; it is freely soluble in alcohol. T opiramate may also be known as: Mc N-4853, RWJ-17021, Epitomax®, Topamac®, Topamax®, or Topimax®. Storage/Stability T opiramate tablets should be stored in tight containers at room tem-perature (15-30°C; 59-86°F); protect from moisture. T opiramate sprinkle capsules should be stored in tight containers at tempera-tures below 25°C (76°F); protect from moisture. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None The ARCI (Racing Commissioners International) has designated this drug as a class 2 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: T opiramate Tablets: 25 mg, 50 mg and 100 mg; Sprinkle Capsules: 15 mg & 25 mg; Topamax® (Ortho-Mc Neil); generic; (Rx) tor Se Mide (tor-she-myde) Demadex®, Torasemide loo P diuretic Prescriber Highlights Potent loop diuretic potentially useful for adjunctive T T treatment of CHF in dogs & cats; very little information available on clinical use in veterinary medicine Approximately 10X more potent, longer diuretic action, & T T more potassium-sparing (in dogs) than furosemide May be more expensive than furosemide, but tablets are T T now available generically uses/indications T orsemide is a loop diuretic similar to furosemide, but it is more potent, its diuretic effects persist for a longer period, and it does not cause as much potassium excretion (in dogs). While clinical use in dogs and cats thus far has been minimal, it potentially may be a useful adjunctive treatment for congestive heart failure in dogs and cats, particularly in patients that have become refractory to furosemide. Pharmacology/actions T orsemide, like furosemide inhibits sodium and chloride reabsorp-tion in the ascending loop of Henle via interference with the chlo-ride-binding site of the 1Na +, 1K+, 2Cl-cotransport system. T orsemide increases renal excretion of water, sodium, potassi-um, chloride, calcium, magnesium, hydrogen, ammonium, and bi-carbonate. In dogs, excretion of potassium is affected much less so than is sodium (20:1); this is approximately twice the ratio of Na:K excreted than with furosemide. In cats, torsemide's effects on potas-sium excretion appear to be similar to that of furosemide. In dogs, torsemide appears to have differing effects on aldosterone than fu-rosemide. When compared to furosemide, torsemide increases plas-ma aldosterone levels and inhibits the amount of receptor-bound aldosterone, however, additional research must be performed to determine the clinical significance of these effects. Pharmacokinetics/Pharmacodynamics Limited information is available. Oral bioavailability has been re-ported to be between 80-100% in dogs and cats. Elimination half-life in dogs is about 8 hours which is longer than furosemide. In dogs, diuretic activity begins within one hour of dosing, peaks at about 2 hours and persists for approximately 12 hours. In cats, peak diuresis occurs about 4 hours post-dose and per-sists for 12 hours. contraindications/Precautions/Warnings T orsemide should not be used in patients with known hypersensi-tivity to it or other sulfonylureas, or in anuric patients. Use torsemide cautiously in patients with significant hepatic dysfunction, hyperuricemia (may increase serum uric acid), or dia-betes mellitus (may increase serum glucose). The ARCI (Racing Commissioners International) has designat-ed this drug as a class 3 substance when used in horses. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
to RSemi De 899 The injection should be administered IV slowly over a period of 2 minutes. Ototoxicity has occurred in human patients receiving rapid IV administration of other loop diuretics. adverse effects Adverse effect profiles for dogs and cats have not been established due to the limited use of this drug in veterinary medicine. Furosemide, a related drug, can induce fluid and electrolyte abnormalities. Patients should be monitored for hydration status and electrolyte imbalances (especially potassium, calcium, magnesium and sodium). Prerenal azotemia may result if moderate to severe dehydration occurs. Hy-ponatremia is probably the greatest concern, but hypocalcemia, hy-pokalemia, and hypomagnesemia may all occur. Animals with nor-mal food and water intake are much less likely to develop water and electrolyte imbalances than those that do not. Other potential adverse effects include gas trointestinal distur-bances, hematologic effects (anemia, leukopenia), weakness, and restlessness. T orsemide, unlike furosemide, apparently only rarely causes significant ototoxic effects in humans; very high doses in laboratory animals have induced ototoxicity. Reproductive/nursing Safety No effects on fertility were noted when female and male rats were administered up to 25 mg/kg/day. No adverse teratogenic effects were seen when pregnant rats and rabbits were administered up to 15X (human dose) and 5X (hu-man dose), respectively. Larger doses did increase fetal resorptions, decreased average body weight, and delayed fetal ossification. In humans, the FDA categorizes torsemide as category B for use dur-ing pregnancy (Animal studies have not yet demonstrated risk to the fetus, but there are no adequate studies in pregnant women; or animal studies have shown an adverse effect, but adequate studies in pregnant women have not demonstrated a risk to the fetus in the first trimester of pregnancy, and there is no evidence of risk in later trimesters. ) It is unknown if torsemide enters milk, but furosemide is dis-tributed in milk. Clinical significance for nursing offspring is unknown. overdosage/acute t oxicity In dogs, the oral LD50 is >2 grams/kg. Fluid and electrolyte imbal-ance is the most likely risk associated with an overdose. Consider gut emptying protocols for very large or quantity unknown inges-tions. Acute overdoses should generally be managed by observation with fluid, electrolyte and acid-base monitoring; supportive treat-ment should be initiated if required. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving torsemide and may be of significance in veterinary patients: ace in Hibito RST! (e. g., enalapril, benazepril ): Increased risks for hy-potension, particularly in patients who are volume or sodium depleted secondary to diuretics amino GL yco Si De S T! (gentamicin, amikacin, etc. ): Other diuretics have been associated with increasing the ototoxic or nephrotoxic risks of aminoglycosides. It is unknown if torsemide can also have these effects and if so, what the clinical significance may be. am PHote Ricin b T! : Loop diuretics may increase the risk for nephro-toxicity development Di Goxin T! : Can increase the area under the curve of torsemide by 50%, but is unlikely to be of significance clinically; torsemide-induced hypokalemia may increase the potential for digoxin toxicity Lit Hium T! : T orsemide may reduce lithium clearancen Sai Ds T! : Some NSAIDs may reduce the natriuretic effects of torsemide PRobeneci DT! : Can reduce the diuretic efficacy of torsemide Sa Licy Late ST! : T orsemide can reduce the excretion of salicylates Laboratory considerations T orsemide can affect T! serum electrolytes, glucose, uric acid, and bun concentrations. Doses Do GS/cat S:T! While no referenced dosages were located, torsemide could be considered for use as an alternative to furosemide particularly in those patients that have become refractory to furosemide therapy. T orsemide is approximately 10 times more potent than furosemide, so a starting dose of 10% of furosemide could be considered. As torsemide has a more persistent diuretic ef-fect (approximately 12 hours), dosing frequency may also be reduced. monitoring Serum electrolytes, BUN, creatinine, glucose (if diabetic)T! Hydration status T! Blood pressure, if indicated T! Clinical signs of edema, patient weight, if indicated T! client information Contact veterinarian if clinical signs of water or electrolyte imbal-T! ance occur. Signs such as excessive thirst, lethargy, restlessness, increased urination, GI distress or rapid heart rate may indicate electrolyte or water balance problems. chemistry/Synonyms T orsemide is a pyridyl sulfonylurea loop diuretic that occurs as white to off-white, crystalline powder. It is practically insoluble in water and slightly soluble in alcohol. The injection has a p H >8. 3. T orsemide may also be known as torasemide, AC-3525, AC 4464, BM-02. 015, JDL-464, and Demadex®. International trade names include Torem ® and Unat®. Storage/Stability/compatibility T orsemide tablets and injectable solution should be stored be-low 40°C; preferably between 15-30°C (59-86°F). Protect from freezing. T orsemide injection is stable in Na Cl 0. 9%, Na Cl 0. 45%, or D5W. When given IV undiluted, the manufacturer recommends flushing the line to avoid incompatibilities with other drugs secondary to torsemide's high p H. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None The ARCI (Racing Commissioners International) has designated this drug as a class 3 substance. Human-Labe Le D PRo Duct S: T orsemide Tablets: 5 mg, 10 mg, 20 mg, & 100 mg; Demadex® (Roche), generic; (Rx) T orsemide Injection: 10 mg/m L in 2 and 5 m L amps; Demadex® (Roche) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
900 t Rama Do L Hc L tra Madol Hcl (tram-ah-doll) Ultram® o Piate (mu-rece Ptor) agoni St Prescriber Highlights Synthetic T T mu-receptor opiate agonist that also inhibits reuptake of serotonin & norepinephrine May be useful as an analgesic or antitussive T T Not a controlled drug in USA, but has some potential for T T human abuse Appears well tolerated in dogs; sedation most likely ad-T T verse effect Avoid use with SSRIs ( T T e. g., fluoxetine) or MAOIs (e. g., selegiline)Relatively inexpensive T T uses/indications Tramadol may be a useful alternative or adjunct for the treatment of pain or cough in dogs and, potentially, cats. When used in com-bination with NSAIDs, it may be particularly useful for chronic pain conditions in dogs. Epidurally administered tramadol may also be useful as an analgesic in horses, but no appropriate com-mercial dosage forms are presently available in the USA. Pharmacology/actions Tramadol is a centrally acting opiate agonist that has primarily mu-receptor activity, but also inhibits reuptake of serotonin and nor-epinephrine. These pharmacologic actions all contribute to its an-algesic properties. At least one metabolite (O-desmethyltramadol; ODT; M1) has activity. When compared to tramadol in lab animal studies, M1 is 6 times more potent an analgesic and has 20 times more potency in binding to mu-receptors. Naloxone only partially antagonizes the analgesic effects of tramadol. Pharmacokinetics In dogs after oral administration, bioavailability is about 65%, but there is significant interpatient variability. Volume of distribution is approximately 3. 8 L/kg. T otal body clearance and half-life are about 55 m L/kg/min and 1. 7 hours, respectively. Tramadol is extensively metabolized via several metabolic pathways. At least one metabolite (M1) has agonist activity, but is a minor metabolite in dogs; M1 has a half-life of about 2 hours after oral tramadol administration in dogs. One study in 8 cats using the immediate release oral tablet, showed high interpatient variability in absorption (with two cats there was not enough data to analyze). The elimination half-life for the parent compound was about 2. 5 hours; for the M1 metabolite, 4. 5 hours. Neurologic effects (mydriasis, dysphoria) were seen in 25% of cats (2 of 4 females) in the study group and the drug was observed to be unpalatable to cats. (Papich and Bledsoe 2007) In neonatal and weaned foals, tramadol has different pharma-cokinetics. After oral administration, higher bioavailability (53% vs. 20%), shorter time to peak concentration (1 hr. vs. 1. 25 hr. ), and peak levels occurred with neonatal (2 week old) versus weaned foals (4 months old). Elimination half-life did not significantly differ (ap-prox. 2 hours). The active metabolite (M1; ODT) remained above the reported therapeutic concentration for humans for 3 hours in neonatal foals and 8 hours in weaned foals. (Stewart, Boothe et al. 2006)contraindications/Precautions/Warnings Tramadol is contraindicated in patients hypersensitive to it or other opioids. The combination product containing acetaminophen is contraindicated in cats. Use with caution in conjunction with other drugs that can cause CNS or respiratory depression. Because tramadol has caused sei-zures in humans, it should be used with caution in animals with preexisting seizure disorders or receiving other drugs that may reduce the seizure threshold. Like other opiates, tramadol should be used with caution in geriatric or severely debilitated animals. Patients with impaired renal or hepatic function may need dosage adjustments. While the risk of physical dependence occurring is less than that of several other opiates, it has been reported in humans. The drug should be withdrawn gradually in animals that have received it chronically. While not a controlled substance in the USA, humans can potentially abuse tramadol and significant diversion of the drug reportedly occurs. Veterinarians should be alert to “clients” seeking tramadol for their animals. adverse effects Tramadol appears to be well tolerated in dogs. Potentially, it could cause a variety of adverse effects associated with its pharmacologic actions, including: CNS effects (excessive sedation, agitation, anxi-ety, tremor, dizziness), or GI (inappetence, vomiting, constipation to diarrhea). Very limited information is available on the adverse effects in cats. Dysphoria, mydriasis, and dose avoidance (unpalatability) have been reported. Approximately 10% of humans receiving the drug develop pruritus. Injectable tramadol may cause respiratory and cardiac depression. Reproductive/nursing Safety In humans, the FDA categorizes tramadol as a category C drug for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) At dosages 3-15 times usual, tramadol was embryotoxic and fe-totoxic in laboratory animals. Tramadol and its active metabolite enter maternal milk in very low levels, but the drug's safety in neo-nates has not been established. overdosage/acute t oxicity Acute oral overdosage may cause respiratory depression, lethargy, coma, seizure, cardiac arrest and death. There were 11 exposures to tramadol reported to the ASPCA Animal Poison Control Center (APCC; www. apcc. aspca. org) dur-ing 2005-2006. In these cases all 11 were dogs with 1 showing clini-cal signs (subdued). Treatment is primarily supportive (maintaining respiration, treating seizures with benzodiazepines or barbiturates, etc. ). Naloxone may NOT be useful in tramadol overdoses as it may only partially reverse some of the effects of the drug and may, in fact, increase the risk of seizures. Naloxone did not decrease the drug's lethality in tramadol overdoses given to mice. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving tramadol and may be of significance in veterinary patients: Di Goxin T! : In humans, tramadol has been rarely linked to digoxin toxicity mao in Hibito RST! (including amitraz and possibly, selegiline ): Poten-tial for serotonin syndrome; use together should be avoided | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
t Riamcino Lone acetoni De 901 quini Dine T! : May increase tramadol concentrations and decrease M1 (active metabolite) concentrations Sam T! e: Theoretically, concurrent use of SAMe with tramadol could cause additive serotonergic effects SSRi anti De PRe SSant ST! (fluoxetine, sertraline, paroxetine, etc. ): Po-tential for serotonin syndrome; use together should be avoided; fluoxetine or paroxetine may inhibit tramadol metabolism t Ricyc Lic anti De PRe SSant S T! (clomipramine, amitriptyline, etc. ): Increased risk for seizures; amitriptyline may inhibit tramadol metabolism Wa RF a Rin T! : In humans, increased PT and INR in patients taking tramadol has been reported (relatively rare) Laboratory considerations No specific laboratory interactions or considerations were noted. Doses Do GS:T! a) For analgesia: 1-4 mg/kg PO q8-12h (Hardie, Lascelles et al. 2003) b) For treating chronic cancer pain: 1-4 mg/kg PO q6h (Las-celles 2003) c) As an analgesic: Recent investigations and clinical use sug-gest a starting dose of 2-5 mg/kg four times daily. (Hellyer 2006) d) 5 mg/kg q6-8h PO (Papich 2006) cat S:T! a) For chronic pain: 4 mg/kg PO twice daily (Note: Dose ex-trapolated from human medicine. Tramadol has not been evaluated for toxicity in cats and has not been used exten-sively, but early results encouraging) (Lascelles, Robertson et al. 2003) b) Plumb's note : Several clinicians report anecdotally that they use 1/4 of a 50 mg tablet (12. 5 mg) orally twice daily in an average sized cat. monitoring Clinical efficacy T! Adverse effects T! client information May be given with or without food T! Keep out of reach of children T! May cause changes in alertness or behavior T! Clients should understand that the clinical experience with this T! drug in animals is limited and to report adverse effects to the veterinarian chemistry/Synonyms A mu-receptor opiate agonist, tramadol HCl occurs as a white crystalline powder that is freely soluble in water or alcohol, and very slightly soluble in acetone. Tramadol is not derived from opi-um nor is it a semi-synthetic opioid, but is entirely synthetically produced. Tramadol HCl may also be known as: CG-315; CG-315E; trama-doli hydrochloridum; U-26225A; many trade names are available. Storage/Stability/compatibility Unless otherwise labeled, tramadol tablets should be stored at room temperature 25°C (77°F); excursions permitted to 15-30°C (59-86°F). Dispense in tight, light-resistant containers. Tramadol HCl injection 50 mg/m L (not available commercially in the USA) is reportedly not compatible when mixed in the same sy-ringe with injectable diazepam, diclofenac sodium, indomethacin, midazolam, piroxicam, phenylbutazone, or lysine aspirin. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None The ARCI (Racing Commissioners International) has designated this drug as a class 2 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: Tramadol HCl Tablets (film-coated) 50 mg; Ultram® (Ortho-Mc-Neil); generic; (Rx) Tramadol HCl Extended-Release Tablets: 100 mg, 200 mg & 300 mg; Ultram ER® (Ortho-Mc Neil); (Rx). note : Dogs apparently do not ab-sorb this product as well as humans, and potentially could “overdose” if the tablet is chewed. Tramadol is also available in a fixed dose combination of tramadol HCl 37. 5 mg and acetaminophen 325 mg tablets. USA trade name is Ultracet® (Ortho-Mc Neil); (Rx). Warning : Be certain this combina-tion product is not dispensed for cats. In several countries (but not the USA), tramadol injection is available commercially. tria Mcinolone acetonide (trye-am-sin-oh-lone) Vetalog® glucocorticoid Prescriber Highlights Oral, parenteral, topical & inhaled glucocorticoid that is T T 4-10X more potent than hydrocortisone; no appreciable mineralocorticoid activity Contraindications (relatively): Systemic fungal infections, T T manufacturer lists: “in viral infections,... animals with arrested tuberculosis, peptic ulcer, acute psychoses, corneal ulcer, & Cushingoid syndrome. The presence of diabetes, osteoporosis, chronic psychotic reactions, pre-disposition to thrombophlebitis, hypertension, CHF, renal insufficiency, & active tuberculosis necessitates carefully controlled use. ” If using for therapy, goal is to use as much as is required T T & as little as possible for as short an amount of time as possible Primary adverse effects are “Cushingoid” in nature with T T sustained use Many potential drug & lab interactions T T uses/indications The systemic veterinary labeled product (Vetalog® Injection) is la-beled as “indicated for the treatment of inflammation and related disorders in dogs, cats, and horses. It is also indicated for use in dogs and cats for the management and treatment of acute arthritis, allergic and dermatologic disorders. ” Glucocorticoids have been used in an attempt to treat practically every malady that afflicts man or animal, but there are three broad uses and dosage ranges for use of these agents. 1) Replacement of glucocorticoid activity in patients with adrenal insufficiency, 2) as an antiinflammatory agent, and 3) as an immunosuppressive. Among some of the uses for glucocorticoids include treatment of: | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
902 t Riamcino Lone acetoni De endocrine conditions (e. g., adrenal insufficiency), rheumatic dis-eases (e. g., rheumatoid arthritis), collagen diseases (e. g., systemic lupus), allergic states, respiratory diseases (e. g., asthma), dermato-logic diseases (e. g., pemphigus, allergic dermatoses), hematologic disorders (e. g., thrombocytopenias, autoimmune hemolytic ane-mias), neoplasias, nervous system disorders (increased CSF pres-sure), GI diseases (e. g., ulcerative colitis exacerbations), and renal diseases (e. g., nephrotic syndrome). Some glucocorticoids are used topically in the eye and skin for various conditions or are injected intra-articularly or intra-lesionally. The above listing is certainly not complete. Pharmacology/actions Glucocorticoids have effects on virtually every cell type and system in mammals. An overview of the effects of these agents follows. cardiovascular System : Glucocorticoids can reduce capillary per-meability and enhance vasoconstriction. A relatively clinically in-significant positive inotropic effect can occur after glucocorticoid administration. Increased blood pressure can result from both the drugs' vasoconstrictive properties and increased blood volume that may be produced. cells : Glucocorticoids inhibit fibroblast proliferation, macrophage response to migration inhibiting factor, sensitization of lympho-cytes and the cellular response to mediators of inflammation. Glucocorticoids stabilize lysosomal membranes. cn S/autonomic nervous System : Glucocorticoids can lower sei-zure threshold, alter mood and behavior, diminish the response to pyrogens, stimulate appetite, and maintain alpha rhythm. Glucocorticoids are necessary for normal adrenergic receptor sensitivity. endocrine System : When animals are not stressed, glucocorticoids will suppress the release of ACTH from the anterior pituitary, thereby reducing or preventing the release of endogenous corticos-teroids. Stress factors (e. g., renal disease, liver disease, diabetes) may sometimes nullify the suppressing aspects of exogenously admin-istered steroids. Release of thyroid-stimulating hormone (TSH), follicle-stimulating hormone (FSH), prolactin and luteinizing hormone (LH) may all be reduced when glucocorticoids are ad-ministered at pharmacological doses. Conversion of thyroxine (T 4) to triiodothyronine (T 3) may be reduced by glucocorticoids; and plasma levels of parathyroid hormone increased. Glucocorticoids may inhibit osteoblast function. Vasopressin (ADH) activity is re-duced at the renal tubules and diuresis may occur. Glucocorticoids inhibit insulin binding to insulin-receptors and the post-receptor effects of insulin. Hematopoietic System : Glucocorticoids can increase the numbers of circulating platelets, neutrophils and red blood cells, but platelet aggregation is inhibited. Decreased amounts of lymphocytes (pe-ripheral), monocytes and eosinophils are seen as glucocorticoids can sequester these cells into the lungs and spleen and prompt de-creased release from the bone marrow. Removal of old red blood cells is diminished. Glucocorticoids can cause involution of lym-phoid tissue. Gi tract and Hepatic System : Glucocorticoids increase the secretion of gastric acid, pepsin, and trypsin. They alter the structure of mu-cin and decrease mucosal cell proliferation. Iron salts and calcium absorption are decreased while fat absorption is increased. Hepatic changes can include increased fat and glycogen deposits within he-patocytes, increased serum levels of alanine aminotransferase (ALT) and gamma-glutamyl transpeptidase (GGT). Significant increases can be seen in serum alkaline phosphatase levels. Glucocorticoids can cause minor increases in BSP (bromosulfophthalein) retention time. immune System (also see Cells and Hematopoietic System): Glucocorticoids can decrease circulating levels of T-lymphocytes; inhibit lymphokines; inhibit neutrophil, macrophage, and mono-cyte migration; reduce production of interferon; inhibit phagocyto-sis and chemotaxis; antigen processing; and diminish intracellular killing. Specific acquired immunity is affected less than nonspecific immune responses. Glucocorticoids can also antagonize the com-plement cascade and mask the clinical signs of infection. Mast cells are decreased in number and histamine synthesis is suppressed. Many of these effects only occur at high or very high doses and there are species differences in response. metabolic effects : Glucocorticoids stimulate gluconeogenesis. Lipogenesis is enhanced in certain areas of the body (e. g., abdomen) and adipose tissue can be redistributed away from the extremities to the trunk. Fatty acids are mobilized from tissues and their oxi-dation is increased. Plasma levels of triglycerides, cholesterol and glycerol are increased. Protein is mobilized from most areas of the body (not the liver). musculoskeletal : Glucocorticoids may cause muscular weakness (also caused if there is a lack of glucocorticoids), atrophy, and os-teoporosis. Bone growth can be inhibited via growth hormone and somatomedin inhibition, increased calcium excretion and inhibi-tion of vitamin D activation. Resorption of bone can be enhanced. Fibrocartilage growth is also inhibited. ophthalmic : Prolonged corticosteroid use (both systemic or topically to the eye) can cause increased intraocular pressure and glaucoma, cataracts and exophthalmos. Renal, Fluid, & electrolytes : Glucocorticoids can increase potas-sium and calcium excretion; sodium and chloride reabsorption and extracellular fluid volume. Hypokalemia and/or hypocalce-mia occur rarely. Diuresis may occur following glucocorticoid administration. Skin: Thinning of dermal tissue and skin atrophy can be seen with glucocorticoid therapy. Hair follicles can become distended and alopecia may occur. contraindications/Precautions/Warnings Systemic use of glucocorticoids is generally considered contrain-dicated in systemic fungal infections (unless used for replacement therapy in Addison's), when administered IM in patients with id-iopathic thrombocytopenia or hypersensitive to a particular com-pound. Sustained-release injectable glucocorticoids use is consid-ered contraindicated for chronic corticosteroid therapy of systemic diseases. Animals that have received glucocorticoids systemically, other than with “burst” therapy, should be tapered off the drugs. Patients who have received the drugs chronically should be tapered off slowly as endogenous ACTH and corticosteroid function may re-turn slowly. Should the animal undergo a “stressor” (e. g., surgery, trauma, illness, etc. ) during the tapering process or until normal adrenal and pituitary function resume, additional glucocorticoids should be administered. Corticosteroid therapy may induce parturition in large animal species during the latter stages of pregnancy. adverse effects Adverse effects are generally associated with long-term administra-tion of these drugs, especially if given at high dosages or not on an alternate day regimen. Effects generally are manifested as clini-cal signs of hyperadrenocorticism. When administered to young, growing animals, glucocorticoids can retard growth. Many of the potential effects, adverse and otherwise, are outlined above in the Pharmacology section. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
t Riamcino Lone acetoni De 903 In dogs, polydipsia (PD), polyphagia (PP) and polyuria (PU), may all be seen with short-term “burst” therapy as well as with alternate-day maintenance therapy on days when giving the drug. Adverse effects in dogs can include dull, dry haircoat, weight gain, panting, vomiting, diarrhea, elevated liver enzymes, pancreatitis, GI ulceration, lipidemias, activation or worsening of diabetes mellitus, muscle wasting and behavioral changes (depression, lethargy, vi-ciousness). Discontinuation of the drug may be necessary; chang-ing to an alternate steroid may also alleviate the problem. With the exception of PU/PD/PP, adverse effects associated with antiinflam-matory therapy are relatively uncommon. Adverse effects associated with immunosuppressive doses are more common and potentially, more severe. Cats generally require higher dosages than dogs for clinical effect, but tend to develop fewer adverse effects. Occasionally polydipsia, polyuria, polyphagia with weight gain, diarrhea, or depression can be seen. Long-term, high dose therapy can lead to “Cushingoid” ef-fects, however. Administration of dexamethasone or triamcinolone may play a role in the development of laminitis in horses. Reproductive/nursing Safety Glucocorticoids are probably necessary for normal fetal develop-ment. They may be required for adequate surfactant production, myelin, retinal, pancreas and mammary development. Excessive dosages early in pregnancy may lead to teratogenic ef-fects. In horses and ruminants, exogenous steroid administration may induce parturition when administered in the latter stages of pregnancy. In humans, the FDA categorizes this drug as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) Glucocorticoids unbound to plasma proteins will enter milk. High dosages or prolonged administration to mothers may poten-tially inhibit the growth of nursing newborns. overdosage/acute t oxicity Glucocorticoids when given short-term are unlikely to cause harm-ful effects, even in massive dosages. One incidence of a dog develop-ing acute CNS effects after accidental ingestion of glucocorticoids has been reported. Should clinical signs occur, use supportive treat-ment if required. Chronic usage of glucocorticoids can lead to serious adverse ef-fects. Refer to Adverse Effects above for more information. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving triamcinolone and may be of significance in veterinary patients: am PHote Ricin b T! : Administered concomitantly with glucocorti-coids may cause hypokalemia ana LGe Sic S, o Piate T! and/or ane St Hetic S, Loca L (epidural injections ): Combination with glucocorticoids in epidurals has caused seri-ous CNS injuries and death; do not use more volume than very small intrathecal test doses of these agents with glucocorticoids antic Ho Line Ste Ra Se a Gent S T! (e. g., pyridostigmine, neostigmine, etc. ): In patients with myasthenia gravis, concomitant gluco-corticoid and anticholinesterase agent administration may lead to profound muscle weakness. If possi ble, discontinue anticho-linesterase medication at least 24 hours prior to corticosteroid administration a SPi Rin T! : Glucocorticoids may reduce salicylate blood levelsba Rbitu Rate ST! : May increase the metabolism of glucocorticoids and decrease blood levels cyc Lo PHo SPHami De T! : Glucocorticoids may also inhibit the hepatic metabolism of cyclophos phamide; dosage adjustments may be required cyc Lo SPo Rine T! : Concomitant administration of glucocorticoids and cyclosporine may increase the blood levels of each, by mutu-ally inhibiting the hepatic metabolism of each other; the clinical significance of this interaction is not clear Diu Retic S, Pota SSium-De PLetin GT! (e. g., spironolactone, triamterene ): Administered concomitantly with glucocorticoids may cause hypokalemia e Ryt HRomycin, c La Rit HRomycin T! : May increase TMC levels e St Ro Gen ST! : The effects of TMC, and possibly other glucocorti-coids, may be potentiated by concomi tant administration with estrogens in Su Lin T! : Insulin requirements may increase in patients receiving glucocorticoids i Soniazi DT! : TMC may decrease isoniazid levels ketoconazo Le T! and other azo Le anti Fun Ga LS : May decrease the metabolism of glucocorticoids and increase TMC blood levels; ketoconazole may induce adrenal insufficiency when gluco-corticoids are withdrawn by inhibiting adrenal corticosteroid synthesis mitotane T! : May alter the metabolism of steroids; higher than usu-al doses of steroids may be neces sary to treat mitotane-induced adrenal insufficiency n Sai DST! : Administration of ulcerogenic drugs with gluco corticoids may increase the risk of gastrointestinal ulceration PHenoba Rbita LT! : May increase the metabolism of glucocorticoids and decrease TMC blood levels Ri Fam Pin T! : May increase the metabolism of glucocorticoids and decrease TMC blood levels Vaccine ST! : Patients receiving corticosteroids at immunosuppres-sive dosages should generally not receive live at tenuated-virus vaccines as virus replication may be augmented; a diminished immune response may occur after vaccine, toxoid, or bacterin administration in patients receiving glucocorticoid Wa RF a Rin T! : TMC may affect INR's; monitor Laboratory considerations Glucocorticoids may increase T! serum cholesterol Glucocorticoids may increase T! serum and urine glu cose levels Glucocorticoids may decrease T! serum potassium Glucocorticoids can suppress the release of thyroid stimulat-T! ing hormone (TSH) and reduce t3 & t4 values. Thyroid gland atrophy has been reported after chronic glucocorticoid ad-ministration. Uptake of i131 by the thyroid may be decreased by glucocorticoids. Reactions to T! skin tests may be suppressed by glucocorticoids False-negative results of the T! nitroblue tetrazolium test for systemic bacterial infections may be induced by glucocorticoids Glucocorticoids may cause T! neutrophilia within 4-8 hours after dosing and return to baseline within 24-48 hours after drug discontinuation Glucocorticoids can cause T! lymphopenia which can persist for weeks after drug discontinuation in dogs | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
904 t Riamcino Lone acetoni De Doses Do GS:T! For glucocorticoid effects: a) 2 mg PO once daily for 7 days; 0. 11-0. 22 mg/kg IM or SC (Kirk 1989) b) For antiinflammatory effects: 0. 05 mg/kg PO two to three times daily (Williamson 2003) c) For tablets: 0. 11 mg/kg PO initially once a day, may increase to 0. 22 mg/kg PO once daily if initial response is unsatisfac-tory. As soon as possible, but not later than 2 weeks, reduce dose gradually to 0. 028-0. 055 mg/kg/day. (Booth 1988), (Package insert; Vetalog® Tablets—Solvay) d) For injectable product: 0. 11-0. 22 mg/kg for inflammatory or allergic disorders, and 0. 22 mg/kg for dermatological dis-orders. Effects generally persist for 7-15 days; if symptoms recur, may repeat or institute oral therapy. For intralesional injection: Usual dose is 1. 2-1. 8 mg; inject around lesion at 0. 5-2. 5 cm intervals. Do not exceed 0. 6 mg at any one site or 6 mg total dose. May repeat as necessary. (Package insert; Vetalog® Injection—Solvay) e) T o prevent re-stricture after esophageal dilation: Using an endoscopically directed needle, inject 0. 5-1 m L of Vetalog® (2 mg/m L) submucosally at time of dilation procedure. In-filtration is done circumferentially at four points around the site. (Marks 2004b) cat S:T! For glucocorticoid effects:a) 0. 25-0. 5 mg PO once daily for 7 days (Kirk 1989) b) For pododermatitis, feline plasmacytic pharyngitis: 2-4 mg (total dose) PO once a day or every other day 0. 4-0. 6 mg/kg PO once daily, then taper. For pemphigus complex: 0. 4-0. 8 mg/kg/day PO (Williamson 2003) c) For tablets: 0. 11 mg/kg PO initially once a day, may increase to 0. 22 mg/kg PO once daily if initial response is unsatisfac-tory. As soon as possible, but not later than 2 weeks, reduce dose gradually to 0. 028-0. 055 mg/kg/day (Booth 1988), (Package insert; Vetalog® Tablets—Solvay) d) For injectable product: 0. 11-0. 22 mg/kg for inflammatory or allergic disorders, and 0. 22 mg/kg for dermatological dis-orders. Effects generally persist for 7-15 days; if symptoms recur, may repeat or institute oral therapy. For intralesional injection: Usual dose is 1. 2-1. 8 mg; inject around lesion at 0. 5-2. 5 cm intervals. Do not exceed 0. 6 mg at any one site or 6 mg total dose. May repeat as necessary. (Package insert; Vetalog® Injection—Solvay) T o prevent re-stricture after esophageal dilation: Using an endoscopically directed needle, inject 0. 5-1 m L of Vetalog® (2 mg/m L) submucosally at time of dilation procedure. In-filtration is done circumferentially at four points around the site. (Marks 2004b) For feline plasma cell gingivitis-pharyngitis: a) 2-4 mg PO once a day to every other day (De Novo, Potter, and Woolfson 1988) For feline polymyopathy: a) 0. 5-1 mg/kg PO once a day (Knaack 1988) catt Le:T! For glucocorticoid effects: a) 0. 02-0. 04 mg/kg IM; 6-18 mg intra-articularly (Howard 1986)Ho RSe S: T! (note : ARCI UCGFS Class 4 Drug) For glucocorticoid effects:a) 0. 1-0. 2 mg/kg IM or SC; 3-6 mg subconjunctivally (Robin-son 1987) b) 0. 011-0. 022 mg/kg PO twice daily; 0. 011-0. 022 mg/kg IM or SC; 6-18 mg intra-articularly or intrasynovially, may repeat after 3-4 days (Package inserts; Vetalog® Powder and Injection— Solvay) c) For intra-articular injection: 12 mg IA on days 0, 13, 27 (Mc-Clure 2002) monitoring Monitoring of glucocorticoid therapy is dependent on its reason for use, dosage, agent used (amount of mineralocorticoid activity), dosage schedule (daily versus alternate day therapy), duration of therapy, and the animal's age and condition. The following list may not be appropriate or complete for all animals; use clinical assess-ment and judgment should adverse effects be noted: Weight, appetite, signs of edema T! Serum and/or urine electrolytes T! T otal plasma proteins, albumin T! Blood glucose T! Growth and development in young animals T! ACTH stimulation test if necessary T! chemistry/Synonyms Triamcinolone acetonide, a synthetic glucocorticoid, occurs as slightly odorous, white to cream-colored, crystalline powder with a melting point between 290-294°C. It is practically insoluble in water, very soluble in dehydrated alcohol and slightly soluble in alcohol. The commercially available sterile suspensions have a p H range of 5-7. 5. Triamcinolone acetonide may also be known as: triamcinoloni acetonidum; many trade names are available. Storage/Stability Triamcinolone acetonide products should be stored at room tem-perature (15-30°C); the injection should be protected from light. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: Triamcinolone Acetonide Tablets: 0. 5 mg, 1. 5 mg; Cortalone Tablets® (Vedco), generic (Boehringer Ingelheim), Triacet® Tablets (Phoenix), Triamtabs® (Butler); (Rx). Approved for use in dogs and cats. Triamcinolone acetonide Suspension for Injection: 2 mg/m L; 6 mg/ m L; Vetalog® Parenteral (Fort Dodge); (Rx). Approved for use in dogs, cats, and horses not intended for food. The ARCI (Racing Commissioners International) has designated this drug as a class 4 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: Triamcinolone Acetonide Injection: 10 mg/m L suspension & 40 mg/m L suspension in 1 m L, 5 m L and 10 m L vials; Kenalog-10 &-40 (Bristol-Myers Squibb); (Rx) Triamcinolone Hexacetonide Injection: 5 mg/m L & 20 mg/m L sus-pension in 1 m L & 5 m L vials; Aristospan Intralesional® (Fujisawa); (Rx) Many topical preparations are available, alone and in combination with other agents. Oral mucosal paste & Inhaled products are also approved. All are Rx. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
t Riamte Rene 905 tria Mterene (trye-am-the-reen) Dyrenium® Pota SSium-SP aring diuretic Prescriber Highlights Potassium-sparing diuretic that may be considered as T T an alternative to spironolactone for treating CHF in dogs; limited clinical experience with this drug in dogs/cats Contraindications: Anuria, severe or progressive renal T T disease, severe hepatic disease, hypersensitivity to tri-amterene, preexisting hyperkalemia, concurrent therapy with another potassium-sparing agent (spironolactone, amiloride) or potassium supplementation Hyperkalemia possible; must monitor serum K+ T T uses/indications Triamterene is a potassium-sparing diuretic that potentially could be used as an alternative to spironolactone for the adjunctive treat-ment of congestive heart failure in dogs, however, there is little ex-perience associated with its use in dogs or cats. Pharmacology/actions By exerting a direct effect on the distal renal tubule, triamterene inhibits the reabsorption of sodium in exchange for hydrogen and potassium ions. Unlike spironolactone, it does not competitively inhibit aldosterone. Triamterene increases excretion of sodium, calcium, magnesium and bicarbonate; urinary p H may be slightly increased. Serum concentrations of potassium and chloride may be increased. When used alone, triamterene has little effect on blood pressure. Triamterene can reduce GFR slightly, probably by affect-ing renal blood flow. This effect is reversible when the medication is discontinued. Pharmacokinetics Pharmacokinetic data for dogs or cats was not located. In humans, triamterene is rapidly absorbed after oral administration and oral bioavailability is about 85%. Onset of diuresis occurs in 2-4 hours and diminishes after about 8 hours. Triamterene is metabolized in the liver to 6-p-hydroxytriamterine and its sulfate conjugate. These metabolites are eliminated in the bile/feces and urine; elimination half-life is about 2 hours. contraindications/Precautions/Warnings Triamterene is contraindicated for human patients (and presum-ably dogs and cats) with anuria, severe or progressive renal disease, severe hepatic disease, hypersensitivity to triamterene, preexisting hyperkalemia, history of triamterene-induced hyperkalemia, con-current therapy with another potassium-sparing agent (spironolac-tone, amiloride) or potassium supplementation. adverse effects Because triamterene has been infrequently used in veterinary medicine, an accurate adverse effect profile for small animals is not known, however, hyperkalemia is a definite possibility and moni-toring of electrolytes and renal function are necessary. In humans, hyperkalemia rarely occurs in patients with normal urine output and potassium intake. Less common adverse effects reported in humans include head-ache/dizziness, GI effects, hyponatremia, and an increased sensi-tivity to sunlight. Rarely, hypersensitivity reactions have occurred in human patients taking triamterene. Other rare adverse effects include triamterene-nephrolithiasis, agranulocytosis, thrombocy-topenia, or megaloblastosis. Reproductive/nursing Safety Studies to determine triamterene's effects on fertility have not been performed. Studies in pregnant rats given triamterene at 6-20X (human dose) did not show adverse effects to the fetuses. Triamterene cross-es the placental barrier. For humans, triamterene is either in FDA category B or category C, depending on the reference. Category C for use during pregnancy states: Animal studies have shown an ad-verse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. If considering use of this product in a pregnant animal, weigh the potential benefits of treatment versus the risks. Triamterene is distributed into milk. Although unlikely to pose much risk to nursing animals, safety during nursing cannot be assured. overdosage/acute t oxicity The oral LD50 for triamterene in mice is 380 mg/kg. Fluid and elec-trolyte imbalance is the most likely risk associated with an overdose. GI effects or hypotension are also possible. Consider gut empty-ing protocols for very large or quantity unknown ingestions. Acute overdoses should generally be managed by observation, with fluid, electrolyte (especially serum potassium) and acid-base monitoring. Supportive treatment should be initiated if required. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving triamterene and may be of significance in veterinary patients: ace in Hibito RST! (e. g., enalapril, benazepril ): Increased risks for hyperkalemia anti Diabetic a Gent ST! (insulin, oral hypoglycemic agents ): Triam-terene may increase blood glucose antihypertensive agents T! : Possible potentiation of hypotensive effects Diu Retic S, Pota SSium-SP a Rin G T! (spironolactone, amiloride ): Increase risk of hyperkalemia; use of these drugs with triamterene in hu-mans is contraindicated Lit Hium T! : Triamterene may reduce lithium clearance n Sai Ds T! : Triamterene with NSAIDs (esp. indomethacin ) may in-crease the risks of nephrotoxicity Pota SSium Su PPLement S T! or Hi GH Pota SSium Foo DS : Increased risk for hyperkalemia Laboratory considerations quinidine T! : Triamterene may interfere with fluorescent assay of quinidine Doses Do GS:T! a) For adjunctive treatment of recurrent heart failure associated with chronic mitral valve insufficiency: 1-2 mg/kg PO q12h. Documentation of use is limited; spironolactone is drug of choice. (Haggstrom, Kvart et al. 2005) b) As a diuretic for adjunctive treatment of CHF: 2-(4) mg/kg/ day PO (Ware 2003) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
906 t Rientine Hc L monitoring Serum electrolytes (especially potassium), BUN, creatinine T! Hydration status T! Blood pressure, if indicated T! Signs of edema; patient weight, if indicated T! client information Give this medication with food to help prevent stomach upset T! Urine may develop a bluish hue, this is normal T! Because this medication has not been used very much in dogs or T! cats; report any unusual effects to the veterinarian chemistry/Synonyms Triamterene is structurally related to folic acid and occurs as a yel-low, odorless, crystalline powder. It is practically insoluble in wa-ter and very slightly soluble in alcohol. At 50°C, it is slightly sol-uble in water. In acidified solutions, triamterene gives off a blue fluorescence. Triamterene may also be known as NSC-77625, KF-8542, FI-6143, triamteren, trimaterenum or triamtereen, Dyrenium®,. International trade names include Dytac®, Dyazide®, Maxzide-25® and Triteren ®. There are many international trade names for com-bination products with hydrochlorothiazide. Storage/Stability Triamterene capsules should be stored between 15-30°C (59-86°F) in tight, light-resistant containers. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None The ARCI (Racing Commissioners International) has designated this drug as a class 4 substance. Human-Labe Le D PRo Duct S: Triamterene Capsules: 50 mg, 100 mg; Dyrenium® (Wellspring); (Rx) In humans, triamterene is often prescribed as a fixed-dose combi-nation with hydrochlorothiazide. Products include: Triamterene 37. 5 mg/Hydrochlorothiazide 25 mg Tablets and Capsules; generic, Dyazide®, Maxzide-25®; (Rx) Triamterene 50 mg/Hydrochlorothiazide 25 mg Capsules; generic; (Rx) Triamterene 75 mg/Hydrochlorothiazide 50 mg Tablets; generic, Maxzide®; (Rx) trientine Hcl (trye-en-teen) Syprine® chelating agent Prescriber Highlights Oral copper chelating agent for copper hepatopathy T T Probably fewer adverse effects then penicillamine, but T T acute renal failure possible Very limited experience with this drug T T More expensive than penicillamine; may need to be com-T T pounded into smaller dosages Give on an empty stomach T Tuses/indications Trientine may be useful for the treatment of copper-associated he-patopathy in dogs, particularly when dogs cannot tolerate the ad-verse effects (e. g., vomiting) associated with penicillamine. Pharmacology/actions Trientine is an effective chelator of copper and increases its elimi-nation via urinary excretion. It apparently has a greater affinity for copper in plasma than penicillamine, but penicillamine has a great-er affinity for tissue copper. Pharmacokinetics No data was located. contraindications/Precautions/Warnings Trientine is contraindicated in patients hypersensitive to it. It is not indicated for cystinuria, rheumatoid arthritis, or biliary cirrhosis. adverse effects Albeit with limited veterinary experience, trientine has had relative-ly minimal adverse effects in dogs treated for copper hepatotoxic-ity, but acute renal failure has been reported. Human patients have developed iron deficiency anemia after taking trientine long-term. There is a chance for topical dermatitis developing if trientine gets on skin; wash off immediately. The drug should be given in a cap-sule (may need to be compounded) and not sprinkled on food. Reproductive/nursing Safety Trientine is a potential teratogen. It was teratogenic in rats given doses similar to those for humans and should only be used in preg-nancy when the benefits to the mother outweigh the risks to off-spring. In humans, the FDA categorizes this drug as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) It is not known whether this drug is excreted in breast milk. Exercise caution when administering to nursing patients. overdosage/acute t oxicity Little information is available; a case of a human ingesting 30 g of trientine without significant morbidity has been reported. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving trientine and may be of significance in veterinary patients: i Ron T! : Iron and trientine inhibit the absorption of one another; if iron therapy is needed, give doses at least 2 hours apart from one another zinc T! : Because trientine may also chelate zinc or other minerals, separate doses as above Doses Do GS:T! As a chelator for copper hepatotoxicity:a) 10-15 mg/kg PO twice daily; 1-2 hours before a meal (Twedt 1999) b) 10-15 mg/kg PO q12h; give one hour before meals (Johnson 2000) c) 15-30 mg/kg PO twice daily (q12h). Give prior to meals (Richter 2002) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
t Ri Lo Stane 907 monitoring Periodic quantitative hepatic copper levels T! client information While it is preferable to give on an empty stomach, if the drug T! causes vomiting or lack of appetite give with a small amount of food chemistry/Synonyms An oral copper chelator, trientine HCl occurs as a white to pale yellow crystalline powder. It is hygroscopic and freely soluble in water. Trientine HCl may also be known as: MK-0681, 2,2,2-tetramine, trien hydrochloride, triethylenetetramine dihydrochloride, trien-tine hydrochloride or Syprine®. Storage/Stability Store trientine capsules in the refrigerator (2-8°C) in tightly closed containers. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Trientine HCl Capsules: 250 mg; Syprine® (Merck); (Rx) trilo Stane (trye-loe-stane) Vetoryl® adrenal Steroid Synthe Si S inhibitor Prescriber Highlights Competitive inhibitor of 3-beta hydroxysteroid dehydroge-T T nase thereby reducing synthesis of cortisol, aldosterone, & adrenal androgens May be useful in dogs for treatment of pituitary-depen-T T dent hyperadrenocorticism, adrenal dependent hypera-drenocorticism, Alopecia X in Pomeranians & Alaskan malamutes; in cats for treatment of feline pituitary dependent hyperadrenocorticism, & in horses for equine hyperadrenocorticism (HAC) In USA, must presently be imported T T Potential adverse effects in dogs include lethargy, inap-T T petence, vomiting, electrolyte abnormalities, & diarrhea Rare case reports of hypoadrenocorticism & death T T Expense of treatment may be an issue T T uses/indications Trilostane may be useful for treating pituitary-dependent hypera-drenocorticism or adrenal dependent hyperadrenocorticism in dogs, feline pituitary-dependent hyperadrenocorticism, and equine hyperadrenocorticism (HAC). It may also be useful in treating Pomeranians with Alopecia X and Alaskan malamutes with adult-onset alopecia. Pharmacology/actions Trilostane is a competitive inhibitor of 3-beta hydroxysteroid de-hydrogenase thereby reducing synthesis of cortisol, aldosterone, and adrenal androgens. Inhibition is reversible and apparently dose dependent. Pharmacokinetics In dogs, orally administered trilostane is rapidly, but erratically ab-sorbed with peak levels occurring between 1. 5-2 hours post dose. It is unknown whether the presence of food in the gut significantly alters absorption characteristics. After 18 hours, the drug report-edly returns to baseline levels. Effects on cortisol production appar-ently last for no more than 20 hours, and more likely wane within 10 hours of dosing. Trilostane is metabolized in the liver to several metabolites including ketotrilostane, which is active. contraindications/Precautions/Warnings Trilostane is contraindicated in animals hypersensitive to it. It should be used with caution in patients with renal or hepatic impairment. adverse effects Trilostane appears to be relatively well tolerated in dogs. Lethargy, mild electrolyte abnormalities and inappetence are commonly not-ed during the first few days of therapy secondary to steroid with-drawal. Vomiting and diarrhea may also be seen. Withholding the drug for a few days and then giving it every other day for a week may alleviate lethargy and vomiting. Rarely, acute death or development of hypoadrencorticism (including adrenal necrosis) occurring in dogs after receiving trilostane have been anecdotally reported. In one study of trilostane given to 20 horses with equine Cushing's (Mc Gowan and Neiger 2003), no adverse effects were noted. Reproductive/nursing Safety Because trilostane can significantly reduce the synthesis of proges-terone in vivo, it should not be used in pregnancy. Trilostane report-edly (not confirmed) is classified by the FDA as a category X drug (Contraindicated in pregnancy). Information on trilostane levels in maternal milk were not lo-cated; use with caution in lactating animals. overdosage/acute t oxicity Specific information on trilostane acute toxicity was not located. One source states that trilostane overdoses would be unlikely to threaten life and no clinical signs would be expected. However, blood pressure, hydration status, and electrolyte balance should be monitored. If the animal is stressed, consider giving exogenous corticosteroids short-term. Because the drug's effects are relatively short lived, monitoring of patients without complications should only be required for a few days post ingestion. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving trilostane and may be of significance in veterinary patients: ace in Hibito RST! (e. g., benazepril, enalapril ): Could increase risk for hyperkalemia amino GLutet Himi De T! : May potentiate the effects of trilostane and lead to hypoadrenocorticism ketoconazo Le T! : May potentiate the effects of trilostane and lead to hypoadrenocorticism mitotane T! : May potentiate the effects of trilostane and lead to hy-poadrenocorticism Pota SSium-SP a Rin G Diu Retic S T! (e. g., spironolactone ): Could in-crease risk for hyperkalemia Pota SSium-Su PPLement S; Hi GH Pota SSium Foo DS T! : Could increase risk for hyperkalemia | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
908 t Ri Lo Stane Laboratory considerations No specific laboratory interactions or considerations were T! located. Doses Do GS:T! For treatment of canine hyperadrenocorticism (HAC): a) For treatment of canine hyperadrenocorticism (HAC) wheth-er due to adrenal tumor or PDH: Initial therapy at 2-10 mg/ kg PO once daily. Adjust dosage per monitoring parameters below. Doses of up to 50 mg/kg/day divided twice daily have been given without untoward side effects. Give with food. Some dogs require twice daily administration. ACTH stimulation test done at 10-14 days, 30 days and 90 days after starting therapy. ACTH stimulation tests should be performed 4-6 hours post-trilostane dose. Interpret ACTH test in light of physical exam. If ACTH Stim results are <20 nmol/L (0. 72 mcg/dl), then the drug is discontin-ued for 48-72 hours and then re-started at a lower dosage. If ACTH Stim results are >200 nmol/L (7. 2 mcg/dl), then the dose is increased. If the ACTH Stim results are between these two values and the dog is clinically well-controlled, then no change. If between these two results and the patient appears not to be clinically well-controlled, then the drug may need to be given twice daily. Once the dog is stable, repeat ACTH Stim test every 3-6 months. (Neiger 2004) b) Author's (Feldman) experience is that trilostane is not more effective or safer than mitotane and that trilostane is less pre-dictable (under dose, over dose, resolution of signs, or the need for dosing more than once per day) than mitotane. If using trilostane current recommendation is: Initiate at 1 mg/kg PO once daily and continue for about one week until a veterinary recheck can occur. Have owners collect a small urine sample from their dog before leaving home the morn-ing of the scheduled recheck prior to trilostane administra-tion. Trilostane should then be given and the dog should be seen by veterinarian 2 to 3 hours later. The goal of therapy is an owner who is completely pleased with the response. The urine should be checked, at a minimum, for specific grav-ity, glucose and urine cortisol:creatinine ratio (UCCR). An ACTH stimulation test should be started at the time that the dog is seen (about 2 to 3 hours after trilostane dose). The UCCR result should be within the reference interval and the post-ACTH serum cortisol concentration should be between 1. 5 and 5. 5 mcg/d L. If the serum cortisol concentration is within that goal and the UCCR is abnormal, the medication should be given twice daily. If the serum cortisol concentra-tion is too high, the trilostane dose should be increased and if the serum cortisol concentration is too low, the dose should be decreased. This approach should be utilized at each re-check until the dog is doing well. (Feldman 2007) For treatment of Alopecia X:a) In Alaskan Malamutes: 3-3. 6 mg/kg PO twice a day for 4-6 months. Three dogs treated; no adverse effects reported. (Le-one, Vercelli et al. 2005) b) In Miniature poodles and Pomeranians: Average dose was 10. 85 mg/kg per day given either once a day or divided twice a day for 4-8 weeks. (Cerundolo, Lloyd et al. 2004)cat S:T! a) For treatment of feline hyperadrenocorticism: 7 mg/kg/day divided and given twice daily. Doses of up to 60 mg per cat per day have been used in a small number of cats with PDH. (Greco 2007a) Ho RSe S:T! a) For treatment of equine Cushing's syndrome: 0. 4-1 mg/ kg (total dose 120-240 mg) PO once daily. (Mc Gowan and Neiger 2003) monitoring Clinical effects T! Adverse effects T! Serum electrolytes T! Urinalysis including specific gravity, glucose and urine T! cortisol:creatinine ratio (UCCR) ACTH stimulation tests (see doses for recommendations)T! client information Keep out of reach of children and pets T! Wear gloves or wash hands thoroughly after handling T! Clients should report any adverse effects to the veterinarian T! Give the drug with food, unless otherwise directed by T! veterinarian Clients should understand that trilostane is a treatment for the T! condition and not a cure chemistry/Synonyms A synthetic steroid analog, trilostane has a molecular weight of 329. 4 and its chemical name is 4-alpha, 5-alpha-Epoxy-17-beta-hydroxy-3-oxoandrostane-2-alpha-carbonitrile. It reportedly is relatively insoluble in water. Trilostane may also be known as: WIN 24540, Vetor yl ®, Desopan®, Modrastane® or Modrenal®. Storage/Stability/compatibility Commercially available trilostane capsules should be stored at room temperature in tight, light-resistant containers. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None in the USA. In the UK, Trilostane Oral Capsules 60 mg, 120 mg are available. Trade name is Vetoryl® (Arnolds Veterinary Products, Cartmel Drive, Harlescott, Shrewsbury, Shropshire SY1 3TB, U. K. ; FAX Number: +44 0174346211). Vetoryl® can be legally imported into the USA by obtaining prior approval from the FDA. See the appendix for step-wise instructions. One source that has been recommended for obtaining trilostane af-ter obtaining FDA approval is: www. mastersmarketing. com (Mealey 2007) Human-Labe Le D PRo Duct S: Modrastane® is reportedly still an approved human drug, but was withdrawn from the market in the USA in 1994. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
t Rime PRazine ta R t Rate Wit H PRe Dni So Lone 909 tri Meprazine t artrate Wit H predni Solone (trye-mep-ra-zeen) Temaril-P® Phenothiazine antihi Stamine & cortico Steroid Prescriber Highlights Combination phenothiazine antihistamine & corticoster-T T oid used for pruritus & potentially as an antitussive Relatively Contraindicated: Systemic fungal infections, T T hypovolemia, or shock & in patients with tetanus or strychnine intoxication. Caution: Hepatic dysfunction, car-diac disease, active bacterial or viral infections, peptic ul-cer, acute psychoses, corneal ulcer, Cushingoid syndrome, diabetes, osteoporosis, chronic psychotic reactions, pre-disposition to thrombophlebitis, hypertension, CHF, renal insufficiency, general debilitation, very young animals Goal is to use as much as is required & as little as pos-T T sible for as short an amount of time as possible Primary adverse effects: Sedation, may cause significant T T hypotension, cardiac rate abnormalities, hypo-or hyper- thermia, “Cushingoid” effects with sustained use Many potential drug & lab interactions T T uses/indications Trimeprazine with prednisolone is used for the treatment of pru-ritic conditions, especially if induced by allergic conditions. Many dermatologists believe that when prednisolone is combined with trimeprazine (Temaril-P®), less prednisolone is required to control pruritus. The manufacturer suggests the drug is for use in dogs ei-ther for pruritic conditions or as an antitussive. Pharmacology/actions Trimeprazine has antihistaminic, sedative, antitussive, and antipru-ritic qualities. The veterinary-approved product also has predniso-lone in its formulation that provides additional antiinflammatory effects. Pharmacokinetics The pharmacokinetics of trimeprazine have apparently not been studied. contraindications/Precautions/Warnings The contraindications and precautions of this product follow those of the other phenothiazines and antihistaminic agents. For more information, it is suggested to review the acepromazine and chlo-rpheniramine monographs. adverse effects For trimeprazine, possible adverse reactions include: sedation, de-pression, hypotension and extrapyramidal reactions (rigidity, trem-ors, weakness, restlessness, etc. ). Additional adverse effects, if using the product containing ste-roids include: elevated liver enzymes, weight loss, polyuria/poly-dipsia, vomiting, and diarrhea. If used chronically, therapy must be withdrawn gradually and Cushing's syndrome may develop. The manufacturer of the veterinary combination product (Temaril®-P) includes the following adverse effects in its package insert: sodium retention and potassium loss, negative nitrogen bal-ance, suppressed adrenocortical function, delayed wound healing, osteoporosis, possible increased susceptibility to and/or exacerba-tion of bacterial infections, sedation, protruding nictitating mem-brane, blood dyscrasias. In addition, intensification and prolonga-tion of the action of sedatives, analgesics or anesthetics can be noted and potentiation of organophosphate toxicity and of procaine HCl activity. Reproductive/nursing Safety The manufacturer of the veterinary combination product (Temaril®-P) warns that corticosteroids can induce the first stages of parturition if administered during the last trimester of pregnancy. overdosage/acute t oxicity Acute overdosage should be handled as per the acepromazine monograph found at the beginning of the book. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving promethazine (a related phenothiazine antihistamine) or prednisolone and may be of sig-nificance in veterinary patients: ace in Hibito RST! : Phenothiazines may increase effects am PHote Ricin b T! : When administered concomitantly with gluco-corticoids may cause hypokalemia antaci DST! : May cause reduced GI absorption of oral phenothiazines anti Dia RRHea L mixtu Re ST! (e. g., kaolin/pectin, bismuth subsali-cylate mixtures ): May cause reduced GI absorption of oral phenothiazines antic Ho Line Ste Ra Se a Gent ST! (e. g., pyridostigmine, neostigmine, etc. ): In patients with myasthenia gravis, concomitant glucocor-ticoid with these agents may lead to profound muscle weakness. If possible, discontinue anticholinesterase medication at least 24 hours prior to corticosteroid administration. a SPi Rin T! (salicylates ): Glucocorticoids may reduce salicylate blood levels ci Sa PRi De T! : Increased risk for cardiac arrhythmias when used with phenothiazines cn S De PRe SSant a Gent S T! (barbiturates, narcotics, anesthetics, etc. ): May cause additive CNS depression if used with phenothiazines cyc Lo PHo SPHami De T! : Glucocorticoids may also inhibit the hepatic metabolism of cyclophosphamide; dosage adjustments may be required. cyc Lo SPo Rine T! : Concomitant administration of may increase the blood levels of each, by mutually inhibiting the hepatic metabo-lism of each other; clinical significance of this interaction is not clear Di Goxin T! : Secondary to hypokalemia, increased risk for arrhythmias Diu Retic S, Pota SSium-De PLetin G T! (furosemide, thiazides ): When administered concomitantly with glucocorticoids may cause hypokalemia e PHe DRine T! : May increase metabolism e St Ro Gen ST! : The effects of hydrocortisone, and possibly other glu-cocorticoids, may be potentiated by concomitant administration with estrogens in Su Lin T! : Requirements may increase in patients receiving glucocorticoids ketoconazo Le T! : May decrease metabolism | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
910 t Ri Pe Lennamine Hc L mitotane T! : May alter the metabolism of steroids; higher than usu-al doses of steroids may be necessary to treat mitotane-induced adrenal insufficiency n Sai DST! : Administration of other ulcerogenic drugs with gluco-corticoids may increase risk Pa Roxetine T! : May increase phenothiazine plasma levels PHenoba Rbita LT! : May increase the metabolism of glucocorticoids PHenytoin T! : May increase the metabolism of glucocorticoids Ri Fam Pin T! : May increase the metabolism of glucocorticoids Vaccine ST! : Patients receiving corticosteroids at immunosuppres-sive dosages should generally not receive live attenuated-virus vaccines as virus replication may be augmented; a diminished immune response may occur after vaccine, toxoid, or bacterin administration in patients receiving glucocorticoids Laboratory considerations Glucocorticoids may increase serum T! cholesterol and urine glucose levels. Glucocorticoids may decrease serum T! potassium. Glucocorticoids can suppress the release of thyroid stimulat-T! ing hormone (TSH) and reduce t3 & t4 values. Thyroid gland atrophy has been reported after chronic glucocorticoid admin-istration. Uptake of I131 by the thyroid may be decreased by glucocorticoids. Reactions to T! skin tests may be suppressed by glucocorticoids or trimeprazine. False-negative results of the T! nitroblue tetrazolium test for systemic bacterial infection s may be induced by glucocorticoids. Doses Do GS:T! a) For antipruritic and antitussive therapy: Weight up to 10 lb = 1/2 tab PO twice daily; 11-20 lb = 1 tablet twice daily; 21-40 lb = 2 tablets twice daily; over 40 lb = 3 tablets twice daily. Af-ter 4 days reduce dose to 1/2 of initial dose or to an amount just sufficient to maintain remission of symptoms; adjust as necessary. (Package Insert; Temaril®-P—Pfizer) b) For treatment of pruritus: 1 tablet per 10 kg of body weight once daily for 3-5 days, then every other day. Giving with an EFA (essential fatty acid) may reduce the dose and frequency, if not the need for, glucocorticoids. (White 2003a) c) For atopic dermatitis: 1 tablet of Temaril®-P per 5 kg body weight q12h for one week, then once daily for one week, then q48h (every other day). (Hillier 2006e) monitoring Efficacy T! Degree of sedation, and anticholinergic effects T! Adverse effects associated with corticosteroids T! client information Follow veterinarians dosage recommendations carefully T! Dog's appetite and water consumption may increase T! If side effects are worrisome, contact veterinarian T! chemistry/Synonyms A phenothiazine antihistamine related to promethazine, trimepra-zine tartrate occurs as an odorless, white, to off-white crystalline powder with a melting range of 160-164°C. Approximately 0. 5 gm is soluble in 1 m L water, and 0. 05 gm is soluble in 1 m L of alcohol. Trimeprazine Tartrate may also be known as: trimeprazine tar-trate, alimemazine tartrate, Chemists Own Peetalix®, Nedeltran®, Panectyl®, Repeltin®, Temaril®, Theralen®, Theralene®, Theralene®, Vallergan®, or Variargil®. Storage/Stability Store trimeprazine products at room temperature (15-30°C); pro-tect tablets from light. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: No single agent trimeprazine products are approved for veterinary medicine. Trimeprazine Tartrate 5 mg; Prednisolone 2 mg Tablets; Temaril-P® Tablets (Pfizer); (Rx). Approved for use in dogs. Trade name in Can-ada is Vanectyl-P®. The ARCI (Racing Commissioners International) has designated this drug as a class 4 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: None Trimethoprim/Sulfa — See Sulfadiazine/Trimethoprim tripelenna Mine Hcl (tri-pel-ehn-a-meen) Re-Covr® antihi Stamine Prescriber Highlights Oral & injectable antihistamine T T Contraindications: Do not give IV to horses T T Adverse Effects: CNS stimulation (if given IV to horses), T T sedation, depression, ataxia, GI effects (oral use) uses/indications Antihistamines are used in veterinary medicine to reduce or help prevent histamine mediated adverse effects. Tripelennamine has been used as a CNS stimulant in “Downer cows” when adminis-tered slow IV. Pharmacology/actions Antihistamines (H 1-receptor antagonists) competitively inhibit histamine at H 1 receptor sites. They do not inactivate or prevent the release of histamine, but can prevent histamine's action on the cell. Besides their antihistaminic activity, these agents also have varying degrees of anticholinergic and CNS activity (sedation). Tripelennamine is considered to have moderate sedative activ-ity and minimal anticholinergic activity when compared to other antihistamines. Pharmacokinetics The pharmacokinetics of tripelennamine have apparently not been thoroughly studied in domestic animals or humans. contraindications/Precautions/Warnings Do not administer Tripelennamine IV in horses (see Adverse Effects). adverse effects CNS stimulation (hyperexcitability, nervousness, and muscle trem-ors) lasting up to 20 minutes, has been noted in horses after receiv-ing tripelennamine intravenously. Other effects seen (in all species) include CNS depression, incoordination, and GI disturbances. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
tu Lat HRomycin 911 overdosage/acute t oxicity Overdosage of tripelennamine reportedly can cause CNS excita-tion, seizures and ataxia. Treat symptomatically and supportively if clinical signs are severe. Phenytoin (IV) is recommended in the treatment of seizures caused by antihistamine overdose in humans; barbiturates and diazepam are generally avoided. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving tripelennamine and may be of significance in veterinary patients: cn S De PRe SSant S, ot He R T! : Increased sedation can occur if chlo-rpheniramine is combined with other CNS depressant drugs He Pa Rin, Wa RF a Rin T! : Antihistamines may partially counteract the anti-coagulation effects of heparin or warfarin. Laboratory considerations Antihistamines can decrease the wheal and flare response to T! anti-gen skin testing. In humans, it is suggested that antihistamines be discontinued at least 4 days prior to testing. Doses It is recommended to warm the solution to near body temperature before injecting; give IM injections into large muscle areas. Do GS:T! a) 1mg/kg PO q12h; 1 mg/kg IM (Kirk 1986) cat S:T! a) 1 mg/kg PO q12h; 1 mg/kg IM (Kirk 1986) catt Le:T! a) 1. 1 mg/kg (2. 5 m L per 100 lbs body weight) IV (for more immediate effect) or IM q6-12h as needed (Package Insert; Re-Covr®—Solvay) b) As adjunctive treatment in “Downer Cow Syndrome” as a CNS stimulant: 0. 5 mg/kg slow IV in conjunction with par-enteral mineral treatment (Caple 1986) c) 1 mg/kg IV or IM (Howard 1986) Ho RSe S:T! (note: ARCI UCGFS Class 3 Drug) a) 1. 1 mg/kg (2. 5 m L per 100 lbs body weight) IM q6-12h as needed (Package Insert; Re-Covr®—Solvay) b) 1 mg/kg IM (Robinson 1987) SWine: T! a) 1 mg/kg IV or IM (Howard 1986) monitoring Clinical efficacy T! Adverse effects T! chemistry/Synonyms An ethylenediamine-derivative antihistamine, tripelennamine HCl occurs as a white, crystalline powder that will slowly darken upon exposure to light. It has a melting range of 188-192°C and p K as of 3. 9 and 9. 0. One gram is soluble in 1 m L of water or 6 m L of alcohol. Tripelennamine HCl may also be known as: tripelennamin-ium chloride, Azaron®, Etono®, Fenistil®, PBZ®, Pelamine®, Pyribenzamine®, Re-Covr® or Vaginex®. Storage/Stability Store the injection at room temperature and protect from light; avoid freezing or excessive heat. Tablets should also be stored at room temperature in tight containers. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: Tripelennamine HCl for Injection: 20 mg/m L in 20 m L, 100 m L, and 250 m L vials; Re-Covr® (Fort Dodge), generic (various manufacturers and trade names); (Rx). Tripelennamine HCl injection is approved for use in cattle and horses. Treated cattle must not be slaughtered for food purposes for 4 days following the last treatment. Milk must not be used for food for 24 hours (2 milkings) after treatment. No specific tolerance for residues has been published. The ARCI (Racing Commissioners International) has designated this drug as a class 3 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: None TSH — See Thyrotropin tulat Hro Mycin (too-la-throe-mye-sin) Draxxin® injectable macrolide antibiotic Prescriber Highlights Injectable macrolide antibiotic for cattle & swine T T Very long tissue half-lives; one dose treatment T T Not for lactating dairy cattle or veal calves T T Local injection site reactions most likely adverse effect T T Monograph by Elaine Lust, Pharm D uses/indications In beef and non-lactating dairy cattle, tulathromycin is indicated for the treatment of bovine respiratory disease (BRD) associated with Mannheimia haemolytica, Pasteurella multocida, Histophilus somni ( Haemophilus somnus) and Mycoplasma bovis; and for the control of respiratory disease in cattle at high risk of developing BRD, associated with Mannheimia haemolytica, Pasteurella multo-cida and Histophilus somni (Haemophilus somnus). In swine, tulathromycin is indicated for the treatment of swine respiratory disease (SRD) associated with Actinobacillus pleuro-pneumoniae, Pasteurella multocida, Bordetella bronchiseptica, and Haemophilus parasuis. Pharmacology/actions While tulathromycin is a macrolide antibiotic such as erythromycin or azithromycin, it is structurally unique in that it has three amine groups (tribasic), while erythromycin and azithromycin have one (monobasic) and two (dibasic) groups, respectively. The tribasic group of compounds are called triamilide macrolides. It is believed that tulathromycin's tribasic structure allows it to better penetrate gram-negative pathogenic bacteria and its low af-finity for bacterial efflux pumps may allow the drug to remain and accumulate within the bacteria. The mechanism of action of tulathromycin is similar to other macrolides in that it inhibits protein synthesis by pene trating the cell wall and binding to the 50S ribosomal subunits in susceptible bacteria. It is consid ered a bacteriostatic antibiotic, but it possesses some bactericidal activity as well, particularly for Mannheimia hae-molytica and Pasteurella multocida. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
912 tu Lat HRomycin Tulathromycin's efficacy is probably enhanced by its ability to accumulate and be released by host phagocytic cells. Neither time-dependent nor concentration-dependent models may accurately predict or describe the drug's efficacy. Some modern macrolides (e. g., azithromycin) efficacy may be more predictive by assessing the total drug exposure to the pathogen; the AUC:MIC ratio may be helpful. Pharmacokinetics In feeder calves given 2. 5 mg/kg SC (in the neck), tulathromycin is rapidly and nearly completely absorbed (bioavailability >90%). Peak plasma concentrations generally occur within 15 minutes af-ter dosing. Volume of distribution is very large (approximately 11 L/kg) and total systemic clearance is approximately 170 m L/hr/kg. This extensive volume of distribution is largely responsible for the long elimination half-life of this compound. In plasma, elimination half life is approximately 2. 75 days, but in lung tissue it is about 8. 75 days. Tulathromycin is eliminated from the body primarily un-changed via biliary excretion. Following intramuscular administration to feeder pigs at a dos-age of 2. 5 mg/kg, tulathromycin is readily and rapidly absorbed (bioavailability 88%) with peak levels occurring in about 15 min-utes. Tulathromycin rapidly distributes into body tissues, and the volume of distribution is 13-15 L/kg. Plasma half-life is approxi-mately 60-90 hours, but lung tissue half life is about 5. 9 days. Tulathromycin is eliminated from the body primarily unchanged via the feces and urine. contraindications/Precautions/Warnings Tulathromycin is contraindicated in animals with a prior hypersen-sitivity reaction to the drug. Cattle intended for human consumption must not be slaugh-tered within 18 days from the last treatment. Do not use in female dairy cattle 20 months of age or older. A withdrawal period has not been established for this product in pre-ruminating calves. Do not use in calves to be processed for veal. Swine intended for human consumption must not be slaugh-tered within 5 days from the last treatment. adverse effects At labeled doses, adverse effects appear to be minimal in cattle and swine. Transient hypersalivation has been reported and one feeder calf in field studies developed transient dyspnea. Injection site reac-tions are most commonly reported and there have been some re-ports to the FDA 's Adverse Drug Reporting database of anorexia in cattle. Hypersensitivity reactions are possible, but no reports were located. Subcutaneous or intramuscular injection can cause a transient local tissue reaction that may result in trim loss at slaughter. Reproductive/nursing Safety Reproductive safety is not known, the product is labeled: “The ef-fects of Draxxin® on bovine (and porcine) reproductive perfor-mance, pregnancy and lactation have not been determined. overdosage/acute t oxicity In cattle (feeder calves), single subcutaneous doses of up to 25 mg/kg caused transient indications of pain at the injection, including head shaking and pawing at the ground. Injection site swelling, discoloration of the subcutaneous tissues at the injection site and corresponding histopathologic changes were seen in animals in all dosage groups. In swine, single IM doses of up to 25 mg/kg caused transient indications of pain at the injection site, restlessness, and excessive vocalization. Tremors occurred briefly in one animal receiving 7. 5 mg/kg BW. No systemic treatment for single overdoses should be necessary, localized treatment at the injection site (e. g., ice pack) to reduce swelling and pain as well as approved analgesic medications can be considered. Drug interactions No drug interactions are noted in the manufacturer's label and none could be found in other references for tulathromycin. Laboratory considerations No concerns were noted Doses catt Le:T! For labeled indications:a) Inject subcutaneously as a single dose in the neck at a dos-age of 2. 5 mg/kg (1. 1 m L/100 lb) body weight (BW). Do not inject more than 10 m L per injection site. (Label directions; Draxxin®—Pfizer) SWine:T! For labeled indications:a) Inject intramuscularly as a single dose in the neck at a dosage of 2. 5 mg/kg (0. 25 m L/22 lb) BW. Do not inject more than 2. 5 m L per injection site. (Label directions; Draxxin®—Pfizer) monitoring Clinical efficacy T! client information Follow dosing guidelines exactly; adhere to withdrawal times T! Not for female dairy cattle (20 months or older) or veal calves T! Cattle are dosed subcutaneously in the neck, not more than 10 T! m L per injection site Swine are dosed intramuscularly in the neck, not more than 2. 5 T! m L per injection site chemistry/Synonyms Tulathromycin is a semi-synthetic macrolide antibiotic of the sub-class triamilide. It occurs as white to of-white-crystalline powder that is readily soluble in water at p H<8. At a p H of 7. 4 (physiologi-cal p H), tulathromycin (a weak base) is approximately 50 times more soluble in hydrophilic than hydrophobic media. The commercially available injection contains 100 mg/m L of tu-lathromycin in an equilibrated mixture of the two isomeric forms of tulathromycin in a 9:1 ratio. The injectable vehicle consists of 50% propylene glycol, monothioglycerol (5 mg/m L); citric and hydrochloric acids are added to adjust p H. It has a relatively low viscosity. Tulathromycin may also be known as tulathromycine, tulathro-mycinum, CP-472295 (component A), CP-547272 (component B), or Draxxin®. Storage/Stability/compatibility Tulathromycin injection should be stored at, or below 25°C (77°F). The product is stable at room temperature for up to 36 months. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
ty Lo Sin 913 Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: Tulathromycin Injection 100 mg/m L in 50, 100, 250, & 500 m L vi-als: Draxxin® (Pfizer); Approved for use in cattle and swine. Cattle intended for human consumption must not be slaughtered within 18 days from the last treatment. Do not use in female dairy cattle 20 months of age or older. A withdrawal period has not been es-tablished for this product in pre-ruminating calves. Do not use in calves to be processed for veal. Swine intended for human consumption must not be slaughtered within 5 days from the last treatment. Human-Labe Le D PRo Duct S: None tylo Sin (tye-loe-sin) Tylan® macrolide antibiotic Prescriber Highlights Macrolide antibiotic related to erythromycin, used primar-T T ily in cattle & swine; sometimes used orally in cats/dogs for chronic colitis Contraindications: hypersensitivity to it or other mac-T T rolide antibiotics; probably contraindicated in horses Adverse Effects: Pain & local reactions after IM injection, T T GI upset (anorexia, & diarrhea). May cause severe diar-rheas if administered PO to ruminants or by any route to horses. SWINE: edema of rectal mucosa & mild anal protrusion with pruritus, erythema, & diarrhea uses/indications Although the injectable form of tylosin is approved for use in dogs and cats, it is rarely used parenterally in those species. Oral tylosin is sometimes recommended for the treatment of chronic colitis in small animals (see Doses), but controlled studies documenting its efficacy have not been performed. Tylosin is also used clinically in cattle and swine for infections caused by susceptible organisms. Pharmacology/actions Tylosin is thought to have the same mechanism of action as eryth-romycin (binds to 50S ribosome and inhibits protein synthesis) and exhibits a similar spectrum of activity. It is a bacteriostatic anti-biotic. Tylosin may also have immunomodulatory effects on cell-mediated immunity. In dogs, tylosin increases concentrations of enterococci (Enterococcus fecalis) in the jejunum. Enterococci are thought to have probiotic effects. For more specific information on organisms where tylosin is usually active, refer to the erythromycin monograph; cross-resis-tance with erythromycin occurs. Pharmacokinetics Tylosin tartrate is well absorbed from the GI tract, primarily from the intestine. The phosphate salt is less well absorbed after oral ad-ministration. Tylosin base injected SC or IM is reportedly rapidly absorbed. Like erythromycin, tylosin is well distributed in the body after systemic absorption, with the exception of penetration into the CSF. The volume of distribution of tylosin is reportedly 1. 7 L/kg in small animals and 1-2. 3 L/kg in cattle. In lactating dairy cattle, the milk to plasma ratio is reported to be between 1-5. 4. Tylosin is eliminated in the urine and bile apparently as un-changed drug. The elimination half-life of tylosin is reportedly 54 minutes in small animals, 139 minutes in newborn calves, and 64 minutes in calves 2 months of age or older. contraindications/Precautions/Warnings Tylosin is contraindicated in patients hypersensitive to it or other macrolide antibiotics (e. g., erythromycin). Most clinicians feel that tylosin is contraindicated in horses, as severe and sometimes fatal diarrheas may result from its use in that species. adverse effects Most likely adverse effects with tylosin are pain and local reactions at intramuscular injection sites, and mild GI upset (anorexia and di-arrhea). Tylosin may induce severe diarrheas if administered orally to ruminants or by any route to horses. In swine, adverse effects reported include edema of rectal mucosa and mild anal protrusion with pruritus, erythema, and diarrhea. Reproductive/nursing Safety In a system evaluating the safety of drugs in canine and feline preg-nancy (Papich 1989), this drug is categorized as in class: B (Safe for use if used cautiously. Studies in laboratory animals may have uncov-ered some risk, but these drugs appear to be safe in dogs and cats or these drugs are safe if they are not administered when the animal is near term. ) overdosage/acute t oxicity Tylosin is relatively safe in most overdose situations. The LD 50 in pigs is greater than 5 g/kg orally, and approximately 1 g/kg IM. Dogs are reported to tolerate oral doses of 800 mg/kg. Long-term (2 year) oral administration of up to 400 mg/kg produced no organ toxicity in dogs. Shock and death have been reported in baby pigs overdosed with tylosin, however. Drug interactions Drug interactions with tylosin have not been well documented. It has been suggested that tylosin may increase digoxin blood levels with resultant toxicity. It is suggested to refer to the erythromycin monograph for more information on potential interactions. Laboratory considerations Macrolide antibiotics may cause falsely elevated values of T! a St (SGOT), and a Lt (SGPT) when using colorimetric assays. Fluorometric determinations of T! urinary catecholamines can be al-tered by concomitant macrolide administration. Doses Do GS: T! When using Tylan® Soluble (100 grams per bottle) powder: Us-ing volumetric containers to measure powders is not necessar-ily accurate, but 1 level teaspoonful (5 m L) of powder contains approximately 2. 5-2. 7 grams of tylosin; 1/8th of a teaspoonful contains approximately 325 mg tylosin. a) For small intestinal bacterial overgrowth: 10-20 mg/kg PO q12h; recommended for chronic cases, may require therapy for as long as 6 weeks. (Ludlow and Davenport 2000) b) For adjunctive treatment of IBD: 10 mg/kg PO three times daily. Therapeutic trial for 21 days to evaluate efficacy. (Simp-son 2003a) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
914 ty Lo Sin c) For clostridial colitis: 10-40 mg/kg PO twice daily. Practical-ly (using the wettable powder): 1/16th of teaspoon 2-3 times daily for dogs (<7kg); Jth of a teaspoon 2-3 times a day for medium dogs (7-15 kg); and 1/4 teaspoon 2-3 times a day for larger dogs (>15 kg). Mix with food to hide unpleasant taste or put into capsules. Animals with chronic clostridial colitis can often be controlled with one treatment every 2-3 days. (Willard 2006a) d) For IBD and antibiotic responsive diarrhea: 20-40 mg/kg PO q12h (Marks 2007b) cat S: T! When using Tylan® Soluble (100 grams per bottle) powder: Us-ing volumetric containers to measure powders is not necessar-ily accurate, but 1 level teaspoonful (5 m L) of powder contains approximately 2. 5-2. 7 grams of tylosin; 1/8th of a teaspoonful contains approximately 325 mg tylosin. a) For adjunctive treatment of IBD: 10 mg/kg PO three times daily. Therapeutic trial for 21 days to evaluate efficacy. (Simp-son 2003a) b) For treatment of IBD or diarrheas caused by C. perfringens: 20-40 mg/kg PO twice daily (Marks 2002) c) For IBD: 40 mg/kg PO q12h (Zoran 2007) d) For clostridial colitis: 10-40 mg/kg PO twice daily. Practi-cally (using the wettable powder): 1/16th of teaspoon 2-3 times daily. Mix with food to hide unpleasant taste or put into capsules. Animals with chronic clostridial colitis can of-ten be controlled with one treatment every 2-3 days. (Wil-lard 2006a) Fe RRet S:T! For susceptible infections: a) 10 mg/kg PO once to twice daily (Williams 2000) Rabbit S, Ro Dent S, Sma LL mamma LS:T! a) Rabbits: 10 mg/kg PO, SC, IM q12-24h (Ivey and Morrisey 2000) b) Gerbils, Hamsters, Rats: 10 mg/kg SC q24h (Adamcak and Otten 2000) catt Le:T! For susceptible infections:a) 17. 6 mg/kg IM once daily. Continue treatment for 24 hours after symptoms have stopped, not to exceed 5 days. Do not inject more than 10 m L per site. Use the 50 mg/m L formula-tion in calves weighing less than 200 pounds. (Package insert; Tylosin® Injection—T ech America) b) For bronchopneumonia and fibrinous pneumonia in cattle associated with penicillin G-refractory C. pyogenes infections or other bacteria sensitive to tylosin and resistant to sulfas, penicillin G and tetracyclines: using Tylosin 200 mg/m L: 44 mg/kg IM q24h. Recommend a 21-day slaughter withdrawal at this dosage. (Hjerpe 1986) c) 5-10 mg/kg IM or slow IV once daily; not to exceed 5 days (Huber 1988a) d) Tylosin base injectable: 10 mg/kg IM initially, then 6 mg/kg IM q8h (q8-12h in calves) (Baggot 1983) SWine:T! For susceptible infections:a) 8. 8 mg/kg IM twice daily. Continue treatment for 24 hours after symptoms have stopped, not to exceed 3 days. Do not inject more than 5 m L per site. (Package insert; Tylosin® In-jection—T ech America)b) 5-10 mg/kg until 24 hours after remission of disease signs; not to exceed 3 days therapy (Huber 1988a) c) Tylosin base injectable: 12. 5 mg/kg IM q12h (Baggot 1983) SHee P & Goat S:T! For susceptible infections: a) 10 mg/kg, treatment not to exceed 5 days (Huber 1988a) bi RDS:T! For susceptible infections:a) For initial therapy in caged birds for upper respiratory infec-tions (especially if mycoplasma suspected). Using 200 mg/m L injectable: 40 mg/kg IM. Used in combi-nation with aminoglycosides. (Mc Donald 1989) b) For initial therapy of upper respiratory infections and air sacculitis. Using 50 mg/m L or 200 mg/m L injectable: 10-40 mg/kg IM twice daily or three times daily (Clubb 1986) c) 30 mg/kg IM q12h (Hoeffer 1995) Re Pti Le S:T! For susceptible infections:a) For tortoises: 5 mg/kg IM once daily for at least 10 days. Used primarily for chronic respiratory infections or when Myco-plasma is suspected (Gauvin 1993) b) All species: 5 mg/kg IM once daily (Jacobson 1999) monitoring Clinical efficacy T! Adverse effects T! chemistry/Synonyms A macrolide antibiotic related structurally to erythromycin, tylosin is produced from Streptomyces fradiae. It occurs as an almost white to buff-colored powder with a p K a of 7. 1. It is slightly soluble in wa-ter and soluble in alcohol. Tylosin is considered highly lipid soluble. The tartrate salt is soluble in water. The injectable form of the drug (as the base) is in a 50% propylene glycol solution. Tylosin may also be known as Desmycosin, tilosina, tylozin, ty-losiini, tylosinum, tylozyna or Tylan®. Storage/Stability/compatibility Unless otherwise instructed by the manufacturer, injectable tylosin should be stored in well-closed containers at room temperature. Tylosin, like erythromycin, is unstable in acidic (p H <4) media. It is not recommended to mix the parenteral injection with other drugs. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S : note : The product Tylan® Plus Vitamins was used extensively orally in companion animals, but has been withdrawn from the market. Tylan® Soluble may be substituted, but is significantly more concen-trated than Tylan® Plus Vitamins and dosage sizes (teaspoons are not equivalent) will be different. Tylosin Injection: 50 mg/m L, 200 mg/m L; Tylan® (Elanco); generic; (OTC). Approved for use in nonlactating dairy cattle, beef cattle, swine, dogs, and cats. Slaughter withdrawal (at labeled doses): cattle = 21 days; swine = 14 days. note : Although this author (Plumb) was unable to locate parenteral products approved for use in lactating dairy animals, one source (Huber 1988a) states that tylosin has a 72 hour milk withdrawal for dairy cattle, and 48 hour milk withdrawal in dairy goats and sheep. Contact FARAD for more information be-fore using in lactating dairy animals. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
u RSo Dio L 915 Tylosin Tartrate Powder: (approximately 2. 5-2. 7 grams/level tea-spoonsful) in 100 g bottles; Tylan® Soluble (Elanco); (OTC). Ap-proved for use in turkeys (not layers), chickens (not layers) and swine. Slaughter withdrawal swine = 2 days; chickens = 1 day; turkeys = 5 days. There are many approved tylosin products for addition to feed or wa-ter for use in beef cattle, swine, and poultry. Many of these products have other active ingredients included in their formulations. Human-Labe Le D PRo Duct S: None. ur Sodiol (ur-soe-dye-ole) Actigall®, Ursodeoxycholic acid bile acid Prescriber Highlights Bile acid that may be useful for treatment of hepatobil-T T iary disease in dogs/cats. May also be used for choles-terol containing gallstones Contraindications: Rabbits & other hindgut fermenters. T T Caution: Complications associated with gallstones (e. g., biliary obstruction, biliary fistulas, cholecystitis, pancrea-titis, cholangitis) Adverse Effects: Appears to be well tolerated in T T dogs/cats uses/indications In small animals, ursodiol may be useful as adjunctive therapy for the medical management of cholesterol-containing gallstones and/or in patients with chronic liver disease, particularly where cholestasis (bile toxicity) plays an important role. Ursodiol's benefit in treating canine or feline hepatobiliary disease is unknown at the time of writing (studies are ongoing), but it may be of help in slow-ing the progression of inflammatory hepatic disorders, particularly autoimmune hepatitis and acute hepatotoxicity. Pharmacology/actions After oral administration, ursodiol suppresses hepatic synthesis and secretion of cholesterol. Ursodiol also decreases intestinal absorp-tion of cholesterol. By reducing cholesterol saturation in the bile, it is thought that ursodiol allows solubilization of cholesterol-con-taining gallstones. Ursodiol also increases bile flow and in patients with chronic liver disease, it apparently reduces the hepatocyte toxic effects of bile salts by decreasing their detergent action, and may protect hepatic cells from toxic bile acids (e. g., lithocholate, deoxy-cholate, and chenodeoxycholate). Pharmacokinetics Ursodiol is well absorbed from the small intestine after oral admin-istration. In humans, up to 90% of dose is absorbed. After absorp-tion, it enters the portal circulation. In the liver, it is extracted and combined (conjugated) with either taurine or glycine and secreted into the bile. Only very small quantities enter the systemic circula-tion and very little is detected in the urine. After each entero-he-patic cycle, some quantity of conjugated and free drug undergoes bacterial degradation; eventually most of the drug is eliminated in the feces after being oxidized or reduced to less soluble compounds. Ursodiol detected in the systemic circulation is highly bound to plasma proteins. contraindications/Precautions/Warnings Ursodiol is contraindicated in rabbits and other hindgut ferment-ers as it is converted into lithocholic acid (toxic). Patients sensi-tive to other bile acid products may also be sensitive to ursodiol. The benefits of using ursodiol should be weighed against its risks in patients with complications associated with gallstones (e. g., biliary obstruction, biliary fistulas, cholecystitis, pancreatitis, cholangitis). While ursodiol may be useful in treating patients with chronic liver disease, some patients may experience further impairment of bile acid metabolism. adverse effects While ursodiol use in animals has been limited, it appears to be well tolerated in dogs and cats. Although hepatotoxicity has not been associated with ursodiol therapy, some human patients have an in-ability to sulfate lithocholic acid (a naturally occurring bile acid and also a metabolite of ursodiol). Lithocholic acid is a known hepa-totoxin; veterinary significance is unclear. Diarrhea and other GI effects have rarely been noted in humans taking ursodiol. Ursodiol will not dissolve calcified radiopaque stones or radiolucent bile pig-ment stones. Reproductive/nursing Safety In humans, the FDA categorizes this drug as category B for use dur-ing pregnancy (Animal studies have not yet demonstrated risk to the fetus, but there are no adequate studies in pregnant women; or animal studies have shown an adverse effect, but adequate studies in pregnant women have not demonstrated a risk to the fetus in the first trimester of pregnancy, and there is no evidence of risk in later trimesters. ) It is not known whether ursodiol is excreted in breast milk. overdosage/acute t oxicity Overdosage of ursodiol would most likely cause diarrhea. Treatment, if required, could include supportive therapy; oral administration of an aluminum-containing antacid (e. g., aluminum hydroxide sus-pension); gastric emptying (if large overdose) with concurrent ad-ministration of activated charcoal or cholestyramine suspension. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving ursodiol and may be of significance in veterinary patients: a Luminum-containin G antaci DST! : May bind to ursodiol, thereby reducing its efficacy c Ho Le Sty Ramine Re Sin T! : May bind to ursodiol, thereby reducing its efficacy Laboratory considerations As ursodiol is detected by many T! serum bile acid tests, bile acids may remain falsely elevated. One study in normal dogs did not show any effects, however. Doses Do GS:T! For adjunctive treatment of chronic hepatitis: a) 5-15 mg/kg PO divided q12h, with immunosuppressive therapy. ( note: Use of this drug at this dose is preliminary, but promising) (Johnson and Sherding 1994) b) 10-15 mg/kg PO once daily (Leveille-Webster and Center 1995); (Twedt 1999) c) For use in chronic active hepatitis, fibrosis and cirrhosis. May use as primary or adjunctive therapy. Dose: 11-15. 4 mg/kg PO either once daily or divided twice daily (Tams 2000) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
916 Va LPRoic aci D/V a LPRoate So Dium/Di V a LPRoex So Dium cat S:T! For adjunctive treatment of chronic hepatitis: a) 10-15 mg/kg PO once daily (Leveille-Webster and Center 1995); (Trepanier 1999) b) For use in chronic active hepatitis, fibrosis, and cirrhosis. May use as primary or adjunctive therapy. Dose: 11-15. 4 mg/kg PO either once daily or divided twice daily. Cats usu-ally get 1/6th of a capsule mixed with a small amount of food. Cats may still eat their food even if drug is sprinkled on top. (Tams 2000) c) 10 mg/kg/day PO (Zoran 2006b) monitoring Efficacy (ultrasonography for gallstones; improved liver function T! tests for chronic hepatic disease) Monitoring of SGPT/SGOT (AST/ALT) on a routine basis (in T! humans these tests are recommended to be performed at the ini-tiation of therapy and at 1 and 3 months after starting therapy; then every 6 months). client information Because ursodiol dissolves more rapidly in the presence of bile or T! pancreatic juice, it should be given with food. chemistry/Synonyms A naturally occurring bile acid, ursodiol, also known as ursodeoxy-cholic acid has a molecular weight of 392. 6. Ursodiol may also be known as: acidum ursodeoxycholicum, UDCA, ursodesoxycholic acid; many trade names are available. Storage/Stability Unless otherwise specified by the manufacturer, ursodiol cap-sules should be stored at room temperature (15-30°C) in tight containers. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Ursodiol Capsules: 300 mg; Actigall® & generic (Watson); (Rx) Ursodiol Tablets: 250 mg & 500 mg; URSO® 250 &-Forte (Axcan Pharma); (Rx)valproic acid valproate Sodiu M divalproex Sodiu M (val-proe-ik; val-proe-ayte; die-val-proe-ex) Depakene®, Depakote®, Depacon® Prescriber Highlights 2nd to 4th line anticonvulsant that may be useful as T T adjunctive treatment in some dogs; most do not recom-mend its use in veterinary patients Contraindications: Significant hepatic disease or dysfunc-T T tion, previous hypersensitivity Caution: Thrombocytopenia or altered platelet aggrega-T T tion function Adverse Effects: GI effects (may be diminished by giv-T T ing with food) most likely; hepatotoxicity, CNS (sedation, ataxia, behavioral changes, etc. ), dermatologic reactions, (alopecia, rash, etc. ), hematologic reactions, (thrombocy-topenia, reduced platelet aggregation, leukopenias, ane-mias, etc. ), pancreatitis, & edema are possible May be teratogenic T T uses/indications Because of its cost, apparent unfavorable pharmacokinetic profile, and potential hepatotoxicity, valproic acid must be considered at best, a third or fourth line drug in the treatment of seizures in the dog. Some clinicians feel it is of benefit when added to phenobar-bital in patients not adequately controlled with that drug alone. Additionally, it is less protein bound in dogs than in humans, so the human serum therapeutic range of the drug (40-100 mcg/ m L) may be too high in dogs. The drug (free form) actually may concentrate in the CSF, and anticonvulsant effects may persist even after valproate levels are non-detectable in CSF, lending to the idea that serum levels do not accurately reflect clinical efficacy. Clearly, additional studies are needed to determine the clinical role, if any, for this drug. Pharmacology/actions The mechanism of the anticonvulsant activity of valproic acid is not understood. Animal studies have demonstrated that valproic acid inhibits GABA transferase and succinic aldehyde dehydroge-nase causing increased CNS levels of GABA. Additionally, one study has demonstrated that valproic acid inhibits neuronal activity by increasing potassium conductance. Pharmacokinetics Sodium valproate is rapidly converted to valproic acid in the acidic environment of the stomach where it is rapidly absorbed from the GI tract. The bioavailability reported in dogs following oral admin-istration is approximately 80%; peak levels occur in approximately 1-hour. Food may delay absorption, but does not alter the extent of it. Divalproex in its enteric-coated form has an approximately 1-hour delay in its oral absorption. Patients' who exhibit GI (nau-sea, vomiting) adverse effects may benefit from this dosage form. Valproic acid is rapidly distributed throughout the extracellu-lar water spaces and plasma. It is approximately 80-95% plasma protein bound in humans, and 78-80% plasma protein bound in | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Va LPRoic aci D/V a LPRoate So Dium/Di V a LPRoex So Dium 917 dogs. CSF levels are approximately 10% those found in plasma. Milk levels are 1-10% those found in plasma; it readily crosses the placenta. Valproic acid is metabolized in the liver and is conjugated with glucuronide. These metabolic conjugates are excreted in the urine; only very small amounts of unchanged drug are excreted in the urine. The elimination half-life in humans ranges from 5-20 hours; in dogs from 1. 5-2. 8 hours. contraindications/Precautions/Warnings Valproic acid is contraindicated in patients with significant hepatic disease or dysfunction, or exhibiting previous hypersensitivity to the drug. It should be used with caution in patients with thrombo-cytopenia or altered platelet aggregation function. adverse effects Because of the limited experience with this agent, the following ad-verse effects may not be complete nor valid for dogs: Gastrointestinal effects consisting of nausea, vomiting, anorexia, and diarrhea are the most common adverse effects seen in people and also appar-ently,, in dogs. GI effects may be diminished by administration with food. Hepatotoxicity is the most serious potential adverse (human) reaction reported and must be considered for canine patients also. Dose related increases in liver enzymes may be seen and, rarely, he-patic failure and death may occur. In humans, incidences of hepa-totoxicity are greater in very young (<2 yr. old) patients, those on other anticonvulsants, or with multiple congenital abnormalities. Other potential adverse effects include: CNS (sedation, ataxia, behavioral changes, etc. ), dermatologic (alopecia, rash, etc. ), hema-tologic (thrombocytopenia, reduced platelet aggregation, leukope-nias, anemias, etc. ), pancreatitis, and edema. Reproductive/nursing Safety A 1-2% incidence of neural tube defects in children born of moth-ers taking valproic acid during the first trimester of pregnancy has been reported. Use in pregnant dogs only when the benefits out-weigh the risks of therapy. In humans, the FDA categorizes this drug as category D for use during pregnancy (There is evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women may be acceptable despite its potential risks. ) In a separate system evaluating the safety of drugs in canine and fe-line pregnancy (Papich 1989), this drug is categorized as in class: C (These drugs may have potential risks. Studies in people or laboratory animals have uncovered risks, and these drugs should be used cau-tiously as a last resort when the benefit of therapy clearly outweighs the risks. ) Concentrations of valproic acid in maternal milk are 1-10% of serum concentrations. It is unknown if this would have any detri-mental effect on nursing offspring. overdosage/acute t oxicity Severe overdoses can cause profound CNS depression, asterixis, motor restlessness, hallucinations, and death. One human patient recovered after a serum level of 2000 micrograms/m L (20 times over therapeutic) was measured. Treatment consists of supportive measures and maintenance of adequate urine output is considered mandatory. Because the drug is rapidly absorbed, emesis or gastric lavage may be of limited value. Because of its delayed absorptive characteristics, the divalproex form may be removed by lavage or emesis if ingestion occurred recently. Naloxone is reported to be of benefit in reversing some of the CNS effects of valproic acid, but may also reverse the anticonvulsant properties of the drug. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving valproic acid and may be of significance in veterinary patients: anticoa Gu Lant ST! : Valproic acid may have effects on platelet aggre-gation; use with caution with other drugs that affect coagulation status a SPi Rin T! : Salicylates may displace valproic acid from plasma pro-tein sites, thus increasing valproic acid levels c Lonaze P am T! : The sedative effects of clonazepam may be en-hanced by valproic acid and the anticonvulsant efficacy of both may be diminished cn S De PRe SSant S, ot He R T! : VPA may enhance the CNS depressant effects of other CNS active drugs. PHenoba Rbita L, PRimi Done T! : Valproic acid may increase serum lev-els of phenobarbital and primidone Laboratory considerations A keto-metabolite of valproic acid is excreted into the urine and T! may yield false positive urine ketone tests. Altered T! thyroid function tests have been reported in humans with unknown clinical significance. Doses note : Because of its very short half-life in dogs, most neurologists do not recommend using VPA in dogs. Do GS:T! a) Add on therapy with phenobarbital or bromide: 60 mg/kg PO q8h (Thomas 2000) monitoring Anticonvulsant efficacy T! If used chronically, routine CBC's and liver enzymes at least every T! 6 months client information Compliance with therapy must be stressed to clients for success-T! ful epilepsy treatment. Encourage administering daily doses at same time each day, preferably with food. Veterinarian should be contacted if animal develops significant T! adverse reactions (including clinical signs of anemia and/or liver disease) or if seizure control is unacceptable. chemistry/Synonyms Structurally unrelated to other anticonvulsant agents; valproic acid, valproate sodium, divalproex sodium are derivatives of carboxylic acid. Valproic acid occurs as a colorless to pale yellow clear liquid. It is slightly viscous; has a characteristic odor, a p K a of 4. 8, is slightly soluble in water and freely soluble in alcohol. It is also known as Dipropylacetic acid, DPA, 2-propylpentanoic acid, and 2-propyl-valeric acid. Valproate sodium occurs as a white, crystalline, saline tasting, very hygroscopic powder. It is very soluble in water or alcohol. The commercially available oral solution has a p H of 7-8. Divalproex sodium is a stable compound in a 1:1 molar ratio of valproic acid and valproate sodium. It occurs as a white powder with a characteristic odor. It is insoluble in water and very soluble in alcohol. Valproate sodium may also be known as: Abbott-44090, natrii valproas; many trade names are available. Valproic acid may also be known as: Abbott-44089, acidum val-proicum; many trade names are available. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
918 Vana Dium/V ana Dy L Su LF ate Storage/Stability Valproic acid capsules should be stored at room temperature (15-30°C) and in tight containers; avoid freezing. Valproate so-dium oral solution should be stored at room temperature and in tight containers; avoid freezing. Divalproex sodium enteric-coated tablets should be stored at room temperature in tight, light resistant containers. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Valproic Acid Capsules: 250 mg; Depakene® (Abbott); (Rx); generic; (Rx) Valproate Sodium Syrup: 50 mg/m L in 473 m L; Depakene® (Abbott); generic; (Rx)Divalproex Sodium Delayed/Extended Release Tablets: 125 mg, 250 mg, 500 mg; Depakote® and Depakote ER® (Abbott); (Rx) Divalproex Sodium Capsules (Sprinkle): 125 mg; Depakote® (Ab-bott); (Rx)Valproate Sodium Injection: 100 mg/m L in 5 m L single-dose vials (regular and preservative free); Depacon® (Abbott); generic; (Bed-ford); (Rx) vanadiu M vanadyl Sulfate (van-aye-dee-um; van-ah-dil) Vanadyl Fuel® trace metal Prescriber Highlights Trace metal “nutraceutical” that may be useful as an ad-T T junctive treatment for diabetes mellitus in cats Efficacy questionable, but probably safe T T uses/indications Vanadium supplementation may be useful in the adjunctive treat-ment of diabetes mellitus, particularly in cats. There is controversy whether or not this treatment is beneficial. Pharmacology/actions In humans with non-insulin dependent diabetes mellitus (NIDDM), vanadium can reduce fasting blood glucose and glycosylated hemo-globin levels, reduces hepatic glucose release, and increases periph-eral glucose disposal and uptake into skeletal muscle mediated by insulin. Vanadium does not influence blood glucose levels in normal patients. While the exact mechanism of action of vanadium is un-known, it apparently inhibits protein tyrosine phosphatase (PTP). PTP is important in signal transduction and allows vanadium to act via both insulin-dependent and insulin-independent pathways. Pharmacokinetics Little information on the pharmacokinetics of vanadium was lo-cated. Only about 5% is absorbed from foodstuffs. In vivo it is converted to the vanadyl cation and forms complexes with ferri-tin and transferrin. Highest vanadium concentrations are found in the liver, bone and kidney. Vanadium is eliminated via renal routes. Effects on glucose in NIDDM humans may persist for weeks after discontinuation of therapy. contraindications/Precautions/Warnings Vanadium supplements could potentially exacerbate renal insuffi-ciency; use with caution in these patients. adverse effects Gastrointestinal effects have been reported in some cats receiv-ing vanadium supplements; anorexia and vomiting is most com-monly reported. It has been reported that cats initially unable to tolerate vanadium, can have therapy re-instituted without ill effect. Vanadium in high dosages may have renal toxic effects. Reproductive/nursing Safety It is unknown if supplemental vanadium is safe in pregnancy. Vanadium is unlikely to have negative effects in nursing kittens. overdosage/acute t oxicity Vanadyl sulfate may be mildly toxic. The oral LD50 in rats is 450 mg/kg. Consider gut removal protocols if an acute overdose oc-curs. Contact an animal poison control center for further guidance. Chronic overdoses may cause kidney damage. Drug interactions No specific interactions of note were located. When used with other agents for diabetes management, effects may be additive. Laboratory considerations No specific laboratory interactions or considerations were noted Doses note : Because vanadium is given as a salt, do not confuse dosages for vanadium with vanadyl sulfate. Vanadyl sulfate reportedly con-tains 31% elemental vanadium, but labeled amounts of vanadium vary considerably. cat S:T! a) Using Super Vanadyl Fuel® (Twin Labs; also contains chromi-um): 1/2 capsule PO once daily with food. (Dowling 2000) b) For adjunctive use in treating feline type 2 diabetes: Vana-dium (Note: salt not specified, assume elemental vanadium) 0. 2 mg/kg PO once daily in food or water. (Greco 2002a) c) For diabetes mellitus: Vanadyl sulfate 1 mg/kg PO once daily or vanadium 0. 2 mg/kg PO once daily. (Wynn 2002) d) For early NIDDM using Vanadyl Fuel® (Twin Labs; also con-tains chromium): One capsule PO once daily (q24h) (Me-lendez and Lorenz 2002) monitoring As there is no reliable way to measure vanadium in the body, a T! clinical trial is the only way to determine whether vanadium is effective in helping to control blood glucose. Standard methods for monitoring efficacy of diabetes treatment should be followed (e. g., fasting blood glucose, appetite, attitude, body condition, PU/PD resolution and, perhaps, serum fructosamine and/or gly-cosylated hemoglobin levels). client information Clients should give the medication only as prescribed and not T! change brands without their veterinarian's guidance Give with food T! chemistry/Synonyms A trace element, vanadium (V, atomic number 23) is usually given in the form of the inorganic salt, vanadyl sulfate. Vanadyl sulfate occurs as blue crystals and is very soluble in water. Vanadyl sulfate reportedly contains 31% elemental vanadium. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Vancomycin Hc L 919 Vanadyl sulfate may also be known as: vanadium (IV) sulfate oxide; vanadium oxysulfate, oxo[sulfato(2-)-O]-vanadium, oxy-sulfato vanadium (IV); vanadyl (IV) sulfate, or vanadyl (IV)-sulfate hydrate. Storage/Stability/compatibility While vanadyl sulfate is stable under ordinary conditions, refer to the label for each product used. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: No oral products are approved as pharmaceuticals. Oral vanadyl sulfate products are considered nutritional supplements by the FDA. No standards have been accepted for potency, purity, safety or efficacy by regulatory bodies. Supplements are available from a wide variety of sources. Common products include 7. 5 mg, and 10 mg tablets or 15 mg capsules. One proprietary product that has been used in cats is Super Vanadyl Fuel® (Twin Labs). This is a combination product that contains per capsule (among many other ingredients): 150 mcg chromium (from chro-mium nicotinate and picolinate) and 1. 25 mg of elemental vanadium (from BMOV [bi (maltolato) oxovanadium] and vanadyl sulfate). Bioequivalence between products cannot be assumed. vanco Mycin Hcl (van-koe-mye-sin) Vancocin® glyco Pe Ptide antibiotic Prescriber Highlights Glycopeptide antibiotic reserved for IV use for multi-drug T T resistant Staph or Enterococcus infections; can also be used PO to treat Clostridium difficile diarrhea When used systemically, must be given IV; severe pain & T T tissue injury occurs with SC or IM injection May be synergistic with aminoglycoside therapy, but in-T T creased risk of nephrotoxicity, ototoxicity & neutropenia also possible If decreased renal dysfunction, adjust dosage T T uses/indications Vancomycin should only be used to treat infections that are docu-mented resistant to other antibiotics and susceptible to vancomy-cin, usually methicillin-resistant Staphylococcus spp. (MRSA) or multidrug-resistant Enterococcus spp. It potentially is useful for oral treatment of pseudomembranous colitis caused by Clostridia difficile. Pharmacology/actions Vancomycin inhibits cell-wall synthesis and bacterial cell-mem-brane permeability. It also affects bacterial RNA synthesis. It is only effective against gram-positive bacteria, including many strains of streptococci, staphylococci, and enterococci. Vancomycin is gener-ally a bactericidal antibiotic, but is bacteriostatic against entero-cocci. Vancomycin also has activity against Clostridium difficile, Listeria monocytogenes, Corynebacterium, and Actinomyces spp.. Vancomycin and aminoglycosides can have synergistic action against susceptible bacteria. Resistance to vancomycin by certain strains of enterococci and staphylococci is an increasing concern in human medicine and po-tentially, for veterinary patients. Pharmacokinetics When given orally, vancomycin is not appreciably absorbed. After intravenous administration, vancomycin is widely distributed. Therapeutic levels can be found in pleural, ascitic, pericardial, and synovial fluids. At usual serum levels, it does not readily distribute into the CSF. The elimination half-life of vancomycin in patients with normal renal function is approximately 4-6 hours. Prolonged dosing can allow the drug to accumulate. The drug is eliminated primarily via glomerular filtration; small amounts are excreted into the bile. contraindications/Precautions/Warnings Vancomycin is an important antibiotic for treating multi-drug re-sistant infections in humans. It should not be used in veterinary patients when other antibiotics can be used to successfully treat the infection. Patients with decreased renal function that require vancomycin should have dosages reduced or dosing interval increased. Serum levels should be monitored. adverse effects When given parenterally, nephrotoxicity and ototoxicity are the most serious potential adverse effects of vancomycin. Unlike amin-oglycosides, these effects are believed to be uncommon. In humans, dermatologic reactions and hypersensitivity can occur; it is un-known if these effects are issues for veterinary patients. Reversible neutropenia has been reported in humans, particularly when dos-age is high and prolonged. Do not administer IV rapidly or as a bolus; thrombophlebitis, severe hypotension or cardiac arrest (rare) have been reported. Vancomycin must be given over at least 30 minutes as a dilute solution. Do not give IM, SC, or IP. Severe tissue damage and pain may occur. Oral therapy may cause GI effects (nausea, inappetence). Reproductive/nursing Safety When used orally, vancomycin is relatively safe to use during preg-nancy (FDA category B). When used IV, it is not known whether vancomycin can cause fetal harm. A limited study performed in humans did not detect fetal harm, but the numbers studied were small. In humans, the FDA categorizes IV vancomycin as a category C drug for use during pregnancy (Animal studies have shown an ad-verse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate stud-ies in humans. ) Because in veterinary patients, vancomycin should only be used for serious infections, the potential benefits of therapy will probably outweigh the risks in most circumstances. Vancomycin is excreted into milk. Because the drug is not ap-preciably absorbed, it is unlikely to pose significant harm to nursing animals, although diarrhea could occur. overdosage/acute t oxicity Patients with colitis associated with Clostridia difficile taking an oral overdose, could potentially absorb enough drug to cause adverse effects. The IV LD50 for vancomycin in mice and rats is 400 mg/kg and 319 mg/kg, respectively. Intravenous overdoses of vancomycin may cause an increased risk of adverse effects, particularly ototox-icity and nephrotoxicity. Supportive care is advised. Hemodialysis does not appear to remove the drug in significant amounts. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
920 Va So PRe SSin Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving vancomycin and may be of significance in veterinary patients: amino GL yco Si De S T! : Vancomycin may increase the risk of aminogly-coside-related ototoxicity or nephrotoxicity. Because this combi-nation of drugs may be medically required (there is evidence of synergy against staphylococci and enterococci), only enhanced monitoring is suggested. ane St Hetic a Gent S T! : In children, vancomycin used with anesthetic agents has caused erythema and a histamine-like flushing ne PHRotoxic DRu GS, ot He R T! (e. g., amphotericin b, cisplatin ): Use with caution with other nephrotoxic drugs Laboratory considerations No specific concerns were noted T! Doses T o prepare parenteral solution using vancomycin 500 mg or 1 g powder for injection: Reconstitute the 500 mg for injection vial by adding 10 m L of sterile water for injection. Add 20 m L to the 1 gm vial. Before administering to patient, further dilute reconstituted solutions with (at least 100 m L for 500 mg; 200 m L for 1 gram vial) a compatible diluent (e. g., D5W, lactated Ringer's, 0. 9% Na Cl). Do GS:T! For susceptible infections:a) For confirmed bacteremia/septicemia for enterococci or staphylococci resistant to other commonly used antibiotics: 15 mg/kg IV over 30-60 minutes q6-8h. (Ford 2005) b) 15 mg/kg IV over 30-60 minutes q6h. For successful therapy of serious infections, an aminoglycoside such as gentamicin or amikacin should also be administered. (Papich 2003b) c) For oral use to treat C. difficile enterocolitis: 10-20 mg/kg PO q6h for 5-7 days; For IV use to treat skin, urinary, soft tissue infections: 10-20 mg/kg IV q12h for 7-10 days; For IV use to treat systemic infections, bacteremia: 15 mg/kg IV q6h for 10 days. (Greene, Hartmannn et al. 2006) cat S:T! For susceptible infections:a) For confirmed bacteremia/septicemia for enterococci or staphylococci resistant to other commonly used antibiotics: 15 mg/kg IV over 30-60 minutes q6-8h. (Ford 2005) b) 15 mg/kg IV over 30-60 minutes q6h. For successful therapy of serious infections, an aminoglycoside such as gentamicin or amikacin should also be administered. (Papich 2003b) monitoring When used parenterally: Renal function, baseline and periodic T! Vancomycin levels, maintain trough level above 5 mcg/m L (some T! say troughs between 10-15 mcg/m L) Periodic CBC if therapy is prolonged T! client information Parenteral vancomycin is used in an inpatient setting T! Oral vancomycin may be used for outpatient therapy; clients T! should be counseled to give as prescribed May give oral dosage forms with a small amount of food T!chemistry/Synonyms A glycopeptide antibiotic, vancomycin HCl occurs as an odorless, tan to brown free-flowing powder. It is freely soluble in water. A 5% aqueous solution has a p H of 2. 5-4. 5. Vancomycin may also be known as: vanco, vancomycini, or Vancocin®; there are many registered international trade names available. Storage/Stability/compatibility Vancomycin should be stored at room temperature in tight con-tainers that are protected from light. Once reconstituted (see direc-tions in package insert or in the Doses section), the injectable or oral solutions are stable for 14 days if refrigerated. If diluted further with D5W or sodium chloride 0. 9% for parenteral administration, solutions are stable for 24 hours at room temperature and 2 months if refrigerated. Vancomycin is compatible with D5W, 0. 9% Na Cl, and lactated Ringer's injection. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Vancomycin HCl Capsules: 125 mg & 250 mg; Vancocin® (Viro P-harma); (Rx) Vancomycin HCl Powder for Oral Solution: 1 gram bottles; generic (ESI Lederle); (Rx) Vancomycin HCl Powder for Injection: 500 mg, 1, 5, & 10 g; Vanco-cin® (Viro Pharma); Vancoled® (Lederle); generic (various); (Rx) va Sopre SSin (vay-soe-press-in) Pitressin® hormone Prescriber Highlights Hormone used primarily as a diagnostic agent & some-T T times for treatment of diabetes insipidus; it may be use-ful for the adjunctive treatment of shock syndromes Contraindications: Chronic nephritis until nitrogen reten-T T tion is resolved to reasonable levels, or patients hyper-sensitive to it; Caution: Vascular disease, seizure disor-ders, heart failure, or asthma Adverse Effects: Local irritation at the injection site T T (including sterile abscesses), skin reactions, abdominal pain, hematuria, &, rarely, a hypersensitivity (urticarial) reaction Overdosage can lead to water intoxication T T uses/indications Vasopressin is used in veterinary medicine as a diagnostic agent and in the treatment of diabetes insipidus in small animals. In recent years, there has been significant interest in using vasopressin for treating shock syndromes in humans and animals. Ongoing re-search is being conducted. In human medicine, vasopressin has been used to treat acute GI hemorrhage and to stimulate GI peristalsis. Vasopressin CRI is also being used for treatment of hypotensive septic patients unrespon-sive to conventional vasopressor. Prior to radiographic procedures, it has been used to dispel interfering gas shadows or help concen-trate contrast media. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Va So PRe SSin 921 Pharmacology Vasopressin or antidiuretic hormone (ADH) promotes the renal re-absorption of solute-free water in the distal convoluted tubules and collecting duct. ADH increases cyclic adenosine monophosphate (c AMP) at the tubule which increases water permeability at the lu-minal surface resulting in increased urine osmolality and decreased urine flow. Without vasopressin, urine flow can be increased up to 90% greater than normal. At doses above those necessary for antidiuretic activity, vaso-pressin can cause smooth muscle contraction. Capillaries and small arterioles are most affected, with resultant decreased blood flow to several systems. Hepatic flow may actually be increased, however. Vasopressin can cause contraction of smooth muscle of the bladder and gall bladder and increase intestinal peristalsis, particu-larly of the colon. Vasopressin may decrease gastric secretions and increase GI sphincter pressure; gastric acid concentration remains unchanged. Vasopressin possesses minimal oxytocic effects, but at large dos-es may stimulate uterine contraction. Vasopressin also causes the release of corticotropin, growth hormone, and follicle-stimulating hormone (FSH). Pharmacokinetics Vasopressin is destroyed in the GI prior to being absorbed and therefore must be administered either intranasally or parenterally. After IM or SC administration in dogs, aqueous vasopressin has antidiuretic activity for 2-8 hours. Vasopressin is distributed throughout the extracellular fluid. The hormone apparently is not bound to plasma proteins. Vasopressin is rapidly destroyed in the liver and kidneys. The plasma half-life has been reported to be only 10-20 minutes in humans. contraindications/Precautions/Warnings In humans, vasopressin is contraindicated in patients hypersensi-tive to it or with chronic nephritis until nitrogen retention is re-solved to reasonable levels. Because of its effects on other systems, particularly at high doses, vasopressin should be used with caution in patients with vascular disease, seizure disorders, heart failure, or asthma. adverse effects Adverse effects that can be seen include local irritation at the in-jection site (including sterile abscesses), skin reactions, abdominal pain, hematuria, and, rarely, a hypersensitivity (urticarial) reaction. Overdosage can lead to water intoxication (see below). Reproductive/nursing Safety Although the drug has minimal effects on uterine contractions at usual doses, it should be used with caution in pregnant animals. In humans, the FDA categorizes this drug as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) overdosage/acute t oxicity Early clinical signs of overdose-induced water intoxication can in-clude listlessness or depression. More severe intoxication clinical signs can include coma, seizures, and eventually death. Treatment for mild intoxication is stopping vasopressin therapy and restrict-ing water access until resolved. Severe intoxication may require the use of osmotic diuretics (mannitol, urea, or dextrose) with or with-out furosemide. Drug interactions The following drugs may inhibit the antidiuretic activity of vasopressin: a Lco Ho L!! Demec Locyc Line!! e Pine PHRine !! (large doses ) He Pa Rin T! no Re Pine PHRine T! (large doses ) The following drugs may potentiate the antidiuretic effects of vasopressin: anti De PRe SSant S, t Ricyc Lic!! ca Rbamaze Pine!! c HLo RPRo P ami De !! c Lo Fib Rate!! FLu DRoco R ti Sone !! PHen Fo Rmin!! u Rea T! Doses Do GS:T! As a diagnostic agent after the water deprivation test (WDT); monitor carefully. The WDT is considered contraindicated in animals that are dehydrated or have known renal disease and is used to characterize whether DI is central or nephrogenic in ori-gin. Refer to a current small animal internal medicine text for further information. a) Exogenous vasopressin test: After WDT, empty bladder and start IV catheter and slowly reintroduce water. Give aque-ous vasopressin in D 5W IV at a dose of 2. 5 m U/kg over one hour. T o make one liter of a 5 m U/m L solution add 5 Units of vasopressin to one liter of D 5W. Empty bladder and col-lect urine at 30 minutes, 60 minutes, and 90 minutes. If urine specific gravity >1. 1015 = ADH-responsive DI; if <1. 015 = either nephrogenic DI or medullary washout effect. (Nichols and Miller 1988) For adjunctive treatment of shock:a) Dogs with persistent hypotension after optimal fluid thera-py; Vasopressin (1-4 micro Units/kg/minute) and/or norepi-nephrine (0. 1-2 mcg/kg/minute). Goal of pressor therapy is to maintain mean arterial blood pressure between 70-90 mm Hg. (Hansen 2007a) For treatment of central diabetes insipidus: note : Because vaso-pressin tannate in oil is no longer commercially available; most clinicians are using desmopressin (DDA VP) for treating central DI. Refer to that monograph for more information. cat S:T! As a diagnostic agent after the water deprivation test (WDT): The WDT is generally considered contraindicated in animals that are dehydrated or have known renal disease and is used to characterize whether DI is central or nephrogenic in origin. a) Immediately after the end-point of the WDT, give aqueous vasopressin 0. 5 U/kg IM; continue to withhold food and water. At 30, 60, and 120 minutes after vasopressin, empty bladder and determine specific gravity (osmolality). Upon completion, the cat is gradually allowed access to water. In-ability to concentrate urine during the water deprivation test followed by a rise in urine specific gravity above 1. 025 after vasopressin is indicative of central DI. (Peterson and Ran-dolph 1989) For treatment of central diabetes insipidus: note : Because vaso-pressin tannate in oil is no longer commercially available; most | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
922 Vecu Ronium b Romi De clinicians are using desmopressin (DDA VP) for treating central DI. Refer to that monograph for more information. monitoring Urine output/frequency T! Water consumption T! Urine specific gravity &/or osmolality T! chemistry/Synonyms A hypothalamic hormone stored in the posterior pituitary, vaso-pressin is a 9-amino acid polypeptide with a disulfide bond. In most mammals (including dogs and humans), the natural hormone is arginine vasopressin, while in swine the arginine is replaced with lysine. Lysine vasopressin has only about 1/2 the antidiuretic activ-ity of arginine vasopressin. The commercially available vasopressin products may be a combination of arginine or lysine vasopressin derived from natural sources or synthetically prepared. The prod-ucts are standardized by their pressor activity in rats [USP posterior Pituitary (pressor) Units]; their antidiuretic activity can be variable. Commercially available vasopressin has little, if any, oxytocic activ-ity at usual doses. Vasopressin injection occurs as a clear, colorless or practically colorless liquid with a faint, characteristic odor. Vasopressin is sol-uble in water. Vasopressin may also be known as: ADH, antidiuretic hor-mone, 8-arginine vasopressin, beta-hypophamine, Neo-Lidocaton®, Pitressin® or Pressyn®. Storage/Stability/compatibility Vasopressin (aqueous) injection should be stored at room tempera-ture; avoid freezing. If the aqueous injection is to be administered as an intravenous or intra-arterial infusion, it may be diluted in either D 5W or nor-mal saline. For infusion use in humans, it is usually diluted to a concentration of 0. 1-1 Unit/m L. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Vasopressin Injection: 20 pressor Units/m L in 0. 5 m L, 1 m L and 10 m L vials; and 1 m L ampules; Pitressin® (Monarch); generic; (Rx) Vasopressin Tannate Sterile Suspension in oil is no longer commer-cially available. vecuroniu M bro Mide (vek-yew-roe-nee-um) Norcuron® nonde Polarizing neuromu Scular blocker Prescriber Highlights Nondepolarizing neuromuscular blocking agent T T Contraindications: Hypersensitive to it. Caution: Severe T T renal dysfunction, hepatic, or biliary disease; extreme caution: myasthenia gravis Adverse Effects: None, other than pharmacologic actions T T No analgesia or anesthetic effects T Tuses/indications Vecuronium is indicated as an adjunct to general anesthesia to pro-duce muscle relaxation during surgical procedures or mechanical ventilation and to facilitate endotracheal intubation. It causes very minimal cardiac effects and generally does not cause the release of histamine. Pharmacology/actions Vecuronium is a nondepolarizing neuromuscular blocking agent and acts by competitively binding at cholinergic receptor sites at the motor endplate, thereby inhibiting the effects of acetylcholine. The potency of vecuronium when compared to pancuronium (on a weight basis) has been described as being equipotent to up to 3 times as potent. Pharmacokinetics The onset of neuromuscular blockade after IV injection is depen-dent upon the dose administered. In dogs administered 0. 1 mg/kg IV, full neuromuscular block occurs within 2 minutes and the duration of action at this dose is approximately 25 minutes (also receiving halothane anesthesia). Vecuronium has a shorter duration of action than pancuronium (approx. 1/3-1/2 as long), but is very similar to that of atracurium. Vecuronium is partially metabolized; it and its metabolites are excreted into the bile and urine. Prolonged recovery times may re-sult in patients with significant renal or hepatic disease. contraindications/Precautions/Warnings Vecuronium is contraindicated in patients hypersensitive to it. It should be used with caution in patients with severe renal dysfunc-tion. Lower doses may be necessary in patients with hepatic or bil-iary disease. Vecuronium has no analgesic or sedative/anesthetic ac-tions. In patients with myasthenia gravis, neuromuscular blocking agents should be used with extreme caution, if at all. One case of successful use in a dog with myasthenia gravis has been reported. adverse effects In human studies and one limited dog study, adverse effects other than what would be seen pharmacologically (skeletal muscle weak-ness to profound, prolonged musculoskeletal paralysis) have not been reported. Reproductive/nursing Safety In humans, the FDA categorizes this drug as category C for use dur-ing pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) overdosage/acute t oxicity No cases of vecuronium overdosage have yet been reported (hu-man or veterinary). Should an inadvertent overdose occur, treat conservatively (mechanical ventilation, O 2, fluids, etc. ). Reversal of blockade might be accomplished by administering an anticholin-esterase agent (edrophonium, physostigmine, or neostigmine) with an anticholinergic (atropine or glycopyrrolate). A suggested dose for neostigmine is 0. 06 mg/kg IV after atropine 0. 02 mg/kg IV. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Ve Ra P ami L Hc L 923 Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving vecuronium and may be of significance in veterinary patients: non-De Po La Rizin G mu Sc Le Re Laxant DRu GS, ot He R T! : May have a synergistic effect if used with vecuronium Succiny Lc Ho Line T! : May speed the onset of action and enhance the neuromuscular blocking actions of vecuronium; do not give vecuronium until succinylcholine effects have subsided The following agents may enhance or prolong the neuromuscular blocking activity of vecuronium: amino GL yco Si De S !! ane St Hetic S !! (halothane, isoflurane, sevoflurane ) c Lin Damycin, Lincomycin!! Dant Ro Lene!! ma Gne Sium Sa L t S !! Pi Pe Raci LLin, mez Loci LLin!! quini Dine!! tet Racyc Line S!! Ve Ra P ami LT! Doses Do GS:T! a) 0. 1 mg/kg IV initially (after meperidine and/or acepromazine pre-op 30 minutes before); may give subsequent incremental doses of 0. 04 mg/kg IV. Duration of action after initial dose averages 25 minutes. (Jones and Seymour 1985) b) 10-20 mcg/kg IV (Morgan 2003) c) If using CRI propofol-fentanyl anesthesia: CRI maintenance infusion rate of vecuronium at 0. 2 mg/kg/hr; If using CRI fentanyl-isoflurane or fentanyl-sevoflurane an-esthesia: CRI maintenance infusion rate of vecuronium at 0. 1 mg/kg/hr. (Nagahama, Nishimura et al. 2006) cat S:T! a) 20-40 mcg/kg (0. 02-0. 04 mg/kg) IV (Morgan 2003) monitoring Level of neuromuscular relaxation T! client information This drug should only be used by professionals familiar with T! its use chemistry/Synonyms Structurally similar to pancuronium, vecuronium bromide is a syn-thetic, nondepolarizing neuromuscular blocking agent. It contains the steroid (androstane) nucleus, but is devoid of steroid activity. It occurs as white to off-white, or slightly pink crystals or crystalline powder. In aqueous solution, it has a p K a of 8. 97, and the commer-cial injection has a p H of 4 after reconstitution. 9 mg are soluble in 1 m L of water; 23 mg are soluble in 1 m L of alcohol. Vecuronium Bromide may also be known as: Org-NC-45, Curlem®, Norcuron®, Rivecrum®, Vecural®, or Vecuron®. Storage/Stability/compatibility The commercially available powder for injection should be stored at room temperature and protected from light. After reconstitution with sterile water for injection, vecuronium bromide is stable for 24 hours at either 2-8°C or at room temperature (less than 30°C) if stored in the original container. As it contains no preservative, un-used portions should be discarded after reconstitution. The drug is stable for 48 hours at room temperature or refrigerated when stored in plastic or glass syringes, but the manufacturer recommends that it be used within 24 hours. Vecuronium bromide has been shown to be physically compat-ible with D 5W, normal saline, D 5 in normal saline, and lactated Ringer's. It should not be mixed with alkaline solutions (e. g., thiobarbiturates). Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Vecuronium Bromide Powder for Injection: 10 mg and 20 mg; in 10 m L and 20 m L vials, with and without diluent; Norcuron® (Or-ganon); (Rx) verapa Mil Hcl (ver-ap-a-mill) Calan®, Isoptin®, Verelan® calcium-channel blocker Prescriber Highlights Calcium channel blocking agent used for supraventricular T T tachycardias in dogs & cats Contraindications: Cardiogenic shock or severe CHF T T (unless secondary to a supraventricular tachycardia), hypotension, sick sinus syndrome, 2nd or 3rd degree AV block, digoxin intoxication, or hypersensitive to vera-pamil. IV is contraindicated within a few hours of IV beta-adrenergic blockers. Caution: Heart failure, hypertrophic cardiomyopathy, T T & hepatic or renal impairment. Use very cautiously in patients with atrial fibrillation & Wolff-Parkinson-White (WPW) syndrome. Adverse Effects: Hypotension, bradycardia, tachycardia, T T exacerbation of CHF, peripheral edema, AV block, pulmo-nary edema, nausea, constipation, dizziness, headache, or fatigue Drug Interactions T T uses/indications Veterinary experience with this agent is somewhat limited, but in dogs and cats verapamil may be useful for supraventricular tachy-cardias and, possibly, treatment of atrial flutter or fibrillation. Pharmacology/actions A slow-channel calcium blocking agent, verapamil is classified as a class IV antiarrhythmic drug. Verapamil exerts its actions by block-ing the transmembrane influx of extracellular calcium ions across membranes of vascular smooth muscle cells and myocardial cells. The result of this blocking is to inhibit the contractile mechanisms of vascular and cardiac smooth muscle. Verapamil has inhibitory effects on the cardiac conduction system and these effects produce its antiarrhythmic properties. Electrophysiologic effects include in-creased effective refractory period of the A V node, decreased auto-maticity and substantially decreased A V node conduction. On ECG, heart rate and RR intervals can be increased or decreased; PR and A-H intervals are increased. Verapamil has negative effects on myo-cardial contractility and decreases peripheral vascular resistance. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
924 Ve Ra P ami L Hc L Pharmacokinetics In humans, about 90% of a dose of verapamil is rapidly absorbed after oral administration, but because of a high first-pass effect, only about 20-30% is available to the systemic circulation. Patients with significant hepatic dysfunction may have considerably higher per-centages of the drug systemically bioavailable. Food will decrease the rate and extent of absorption of the sustained-release tablets, but less so with the conventional tablets. Verapamil's volume of distribution is between 4. 5-7 L/kg in hu-mans and has been reported to be approximately 4. 5 L/kg in dogs. In humans, approximately 90% of the drug in the serum is bound to plasma proteins. Verapamil crosses the placenta and milk levels may approach those in the plasma. Verapamil is metabolized in the liver to at least 12 separate me-tabolites, with norverapamil being the most predominant. The majority of the amounts of these metabolites are excreted into the urine. Only 3-4% is excreted unchanged in the urine. In humans, the half-life of the drug is 2-8 hours after a single IV dose, but it can increase after 1-2 days of oral therapy (presumably due to a saturable process of the hepatic enzymes). Serum half-lives of 0. 8 hours and 2. 5 hours have been reported in the dog. contraindications/Precautions/Warnings Verapamil is contraindicated in patients with cardiogenic shock or severe CHF (unless secondary to a supraventricular tachycardia amenable to verapamil therapy), hypotension (<90 mm Hg sys-tolic), sick sinus syndrome, 2nd or 3rd degree A V block, digoxin intoxication, or hypersensitive to verapamil. IV verapamil is contraindicated within a few hours of IV beta-adrenergic blocking agents (e. g., propranolol) as they both can de-press myocardial contractility and A V node conduction. Use of this combination in patients with wide complex ventricular tachycardia (QRS >0. 11 seconds) can cause rapid hemodynamic deterioration and ventricular fibrillation. Verapamil should be used with caution in patients with heart failure, hypertrophic cardiomyopathy, and hepatic or renal impair-ment. T oxicity may be potentiated in patients with hepatic dys-function. It should be used very cautiously in patients with atrial fibrillation and Wolff-Parkinson-White (WPW) syndrome as fatal arrhythmias may result. Because verapamil may increase blood glucose in dogs, it should be used with caution in diabetic animals. Verapamil is potentially a neurotoxic substrate of P-glycoprotein; use with caution in those herding breeds (e. g., Collies) that may have the gene mutation that causes a nonfunctional protein. adverse effects The following adverse reactions may occur: hypotension, bradycar-dia, tachycardia, exacerbation of CHF, peripheral edema, A V block, pulmonary edema, nausea, constipation, dizziness, headache or fatigue. Reproductive/nursing Safety Oral verapamil in rats with doses 1. 5-6 times the human dose was embryocidal and retarded fetal growth and development, probably due to reduced weight gains in dams. Verapamil crosses the pla-centa and can be detected in umbilical vein blood at delivery. In humans, the FDA categorizes this drug as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) Verapamil is excreted in milk. Consider discontinuing nursing if the dam requires verapamil therapy. overdosage/acute t oxicity Clinical signs of overdosage may include bradycardia, hypoten-sion, hyperglycemia, junctional rhythms, and 2nd or 3rd degree A V block. If overdose is secondary to a recent oral ingestion, emptying the gut and charcoal administration may be considered. Treatment is generally supportive in nature; vigorously monitor cardiac and re-spiratory function. Intravenous calcium salts (1 m L of 10% solu-tion per 10 kgs of body weight) have been suggested to treat the negative inotropic clinical signs, but may not adequately treat clini-cal signs of heart block. Use of fluids and pressor agents (e. g., do-pamine, norepinephrine, etc. ) may be utilized to treat hypotensive clinical signs. The A V block and/or bradycardia can be treated with isoproterenol, norepinephrine, atropine, or cardiac pacing. Patients that develop a rapid ventricular rate after verapamil due to ante-grade conduction in flutter/fibrillation with WPW syndrome, have been treated with D. C. cardioversion, lidocaine, or procainamide. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving verapamil and may be of significance in veterinary patients: ace in Hibito RST! : May cause additive hypotensive effects a LPHa-a DRene RGic b Locke RS T! (e. g., prazosin ): May cause additive hypotensive effects beta-a DRene RGic b Locke RST! (e. g., propranolol ): May cause additive negative cardiac inotrope and chronotrope effects Doxo Rubicin T! : Verapamil may increase concentrations co PP c Hemot He Ra Py T! (cyclophosphamide, vincristine, procarbazine, prednisone ): May decrease oral absorption of verapamil cyc Lo SPo Rine T! : Verapamil may increase levels Dant Ro Lene T! : Cardiovascular collapse reported in animals when used with verapamil Di Goxin T! : Verapamil may increase the blood levels of digoxin; monitoring of digoxin levels recommended Di So Py Rami De T! : May cause additive effects; impair left ventricular function; use together within 24-48 hours not recommended Diu Retic ST! : May cause additive hypotensive effects e Ryt HRomycin, c La Rit HRomycin T! : May increase verapamil levels FLecaini De T! : Possible additive effects; use is together with vera-pamil is to be avoided in humans neu Romu Scu La R b Locke RST! : Neuromuscular blocking effects of nondepolarizing muscle relaxants may be enhanced by verapamil PHenoba Rbita LT! : May reduce verapamil levels quini Dine T! : Additive alpha-adrenergic blocking activity; increased hypotensive effect; verapamil can block quinidine's A V conduc-tive effects and increase quinidine levels Ri Fam Pin T! : May reduce verapamil levels t Heo PHy LLine T! : Verapamil may increase serum levels of theophyl-line and lead to toxicity Vinc Ri Stine T! : Calcium channel blockers may increase intracellular vincristine by inhibiting the drug's outflow from the cell Laboratory considerations Verapamil may elevate blood glucose in dogs and confuse T! blood glucose determinations | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Vinb La Stine Su LF ate 925 Doses Do GS:T! a) Initial dose of 0. 05 mg/kg IV slowly, can repeat every 5 min-utes up to a total dose of 0. 15-0. 2 mg/kg; Oral Dose: 0. 5-2 mg/kg PO q8h (Ware 2000) b) For treatment of hypertension: 1-5 mg/kg PO q8h (Brovida 2002) c) 0. 05-0. 15 mg/kg slow IV to effect (Fox 2003a) d) 1-5 mg/kg PO three times daily; 0. 05-0. 25 mg/kg IV slowly (Kramer 2003c) e) For the acute termination of supraventricular tachycardia: Initial dose of 0. 05 mg/kg should be administered over 1-2 minutes while ECG is monitored; if not effective, may repeat in 5-10 minutes. If arrhythmia still not terminated, may give one last dose of 0. 05 mg/kg (total = 0. 15 mg/kg). Effect may persist for 30 minutes or less. For longer control, may give as a CRI at 2-10 mcg/kg/minute. (Kittleson 2006c) cat S:T! a) Initial dose of 0. 025 mg/kg IV slowly, can repeat every 5 min-utes up to a total dose of 0. 15-0. 2 mg/kg; Oral Dose: 0. 5-1 mg/kg PO q8h (Ware 2000) Ho RSe S: T! (note: ARCI UCGFS Class 4 Drug) a) T o control ventricular rate in atrial fibrillation: 0. 025-0. 05 mg/kg IV q 30 minutes; give less than 0. 2 mg/kg total dose (Reimer 2002) monitoring ECGT! Clinical signs of toxicity (see Adverse Effects);T! Blood pressure, during acute IV therapy T! Serum concentration, if efficacy or toxicity warrant (100-300 T! ng/m L is considered therapeutic) client information T o be effective, the animal must receive all doses as prescribed T! If animal becomes lethargic or becomes exercise intolerant, be-T! gins wheezing, has shortness of breath or cough, or develops a change in behavior or attitude, notify veterinarian. chemistry/Synonyms A calcium channel blocking agent, verapamil HCl occurs as a bitter-tasting, nearly white, crystalline powder. It is soluble in water and the injectable product has a p H of 4-6. 5. Verapamil HCl tablets should be stored at room temperature (15-30°C); the injectable product should be stored at room tem-perature (15-30°C) and protected from light and freezing. Verapamil HCl for injection is physically compatible when mixed with all commonly used intravenous solutions. However, a crystal-line precipitate may form if verapamil is added to an infusion line with 0. 45% sodium chloride with sodium bicarbonate running. Verapamil is reported to be physically compatible with the following drugs: amikacin sulfate, aminophylline, ampicillin sodium, ascor-bic acid, atropine sulfate, bretylium tosylate, calcium chloride/gluconate, carbenicillin disodium, cefamandole naftate, cefazolin sodium, cefotaxime sodium, cefoxitin sodium, cephapirin sodium, chloramphenicol sodium succinate, cimetidine HCl, clindamycin phosphate, dexamethasone sodium phosphate, diazepam, digoxin, dobutamine HCl (slight discoloration due to dobutamine oxida-tion), dopamine HCl, epinephrine HCl, furosemide, gentamicin sulfate, heparin sodium, hydrocortisone sodium phosphate, hydro-morphone HCl, insulin, isoproterenol, lidocaine HCl, magnesium sulfate, mannitol, meperidine HCl, metaraminol bitartrate, methi-cillin sodium, methylprednisolone sodium succinate, metoclopr-amide HCl, morphine sulfate, multivitamin infusion, nitroglycerin, norepinephrine bitartrate, oxytocin, pancuronium Br, penicillin G potassium/sodium, pentobarbital sodium, phenobarbital sodium, phentolamine mesylate, phenytoin sodium, potassium chloride/phosphate, procainamide HCl, propranolol HCl, protamine sulfate, quinidine gluconate, sodium bicarbonate, sodium nitroprusside, ti-carcillin disodium, tobramycin sulfate, vasopressin, and vitamin B complex with C. The following drugs have been reported to be physically incom-patible with verapamil: albumin injection, amphotericin B, hydrala-zine HCl, nafcillin sodium, and trimethoprim/sulfamethoxazole. Compatibility is dependent upon factors such as p H, concentra-tion, temperature, and diluent used; consult specialized references for more specific information. Verapamil may also be known as: CP-16533-1, D-365, iprover-atril hydrochloride, verapamili hydrochloridum; many trade names are available. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None The ARCI (Racing Commissioners International) has designated this drug as a class 4 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: Verapamil HCl Tablets: 40 mg, 80 mg & 120 mg; Calan® (Searle); generic; (Rx) Verapamil HCl Sustained/Extended-Release Tablets and Capsules: 100 mg, 120 mg, 180 mg, 200 mg, 240 mg, 300 mg and 360 mg; Calan® SR & Covera-HS® (Searle); Isoptin® SR (Abbott); Verelan® and Verelan® PM (Schwarz Pharma); generic; (Rx) Verapamil HCl for Injection: 2. 5 mg/m L in 2 m L, and 4 m L vials, amps and syringes, 2 m L fill in single-use Carpuject syringe; generic; (Rx) vinbla Stine Sulfate (vin-blas-teen) Velban® antineo Pla Stic Prescriber Highlights A Vinca alkaloid antineoplastic used for a variety of tu-T T mors in dogs (& sometimes cats) Contraindications: Preexisting leukopenia or granulocy-T T topenia (unless a result of the disease being treated) or active bacterial infection; reduce dose if hepatic disease Adverse Effects: Gastroenterocolitis (nausea/vomiting), T T myelosuppression (more so than with vincristine); may also cause constipation, alopecia, stomatitis, ileus, inap-propriate ADH secretion, jaw & muscle pain, & loss of deep tendon reflexes CATS T T can develop neurotoxicity causing constipation or paralytic ileus & aggravating anorexia; can also develop reversible axon swelling & paranodal demyelination Potentially teratogenic T T Avoid extravasation; wear gloves & protective clothing T T when preparing or administering Drug Interactions T T | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
926 Vinb La Stine Su LF ate uses/indications Vinblastine may be employed in the treatment of lymphomas, car-cinomas, mastocytomas, and splenic tumors in small animals. It is more effective than vincristine in the treatment of canine mast cell tumors. Pharmacology/actions Vinblastine apparently binds to microtubular proteins (tubulin) in the mitotic spindle, thereby preventing cell division during meta-phase. It also interferes with amino acid metabolism by inhibiting glutamic acid utilization and preventing purine synthesis, citric acid cycle, and urea formation. Pharmacokinetics Vinblastine is administered IV. After injection, it is rapidly distrib-uted to tissues. In humans, approximately 75% is bound to tissue proteins and the drug does not appreciably enter the CNS. Vinblastine is extensively metabolized by the liver and is primar-ily excreted in the bile/feces; lesser amounts are eliminated in the urine. contraindications/Precautions/Warnings Vinblastine is contraindicated in patients with preexisting leukope-nia or granulocytopenia (unless a result of the disease being treat-ed), or active bacterial infection. Doses of vinblastine should be reduced in patients with hepatic disease. A 50% reduction in dose should be considered if serum bilirubin levels are greater than 2 mg/dl. Because vinblastine is potentially a neurotoxic substrate of P-glycoprotein, it should be used with caution in those herding breeds (e. g., Collies) that may have the gene mutation that causes a nonfunctional protein. As vinblastine may be a skin irritant, gloves and protective cloth-ing should be worn when preparing or administering the medica-tion. If skin/mucous membrane exposure occurs, thoroughly wash area with soap and water. adverse effects Vinblastine can cause gastroenterocolitis (nausea/vomiting) which generally lasts less than 24-hours. It can be myelosuppressive at usual dosages (nadir at 4-9 days after treatment; recovery at 7-14 days). Vinblastine is considered more myelosuppressive than is vincristine. Vinblastine may not possess the degree of peripheral neurotoxic effects seen with vincristine, but at high doses, these effects may be seen. Additionally, vinblastine may cause constipation, alope-cia, stomatitis, ileus, inappropriate ADH secretion, jaw and muscle pain, and loss of deep tendon reflexes. Cats can develop neurotoxicity that can be associated with con-stipation or paralytic ileus thereby aggravating anorexia. They may develop reversible axon swelling and paranodal demyelination. Extravasation of vinblastine may cause significant tissue irrita-tion and cellulitis. Because of the vesicant action of this drug, it is recommended to use a different needle for injecting the drug than the one used to withdraw the drug from the vial. Should clinical signs of extravasation be noted, discontinue infusion immediately at that site and apply moderate heat to the area to help disperse the drug. Injections of hyaluronidase have also been suggested to help diffuse the drug. Reproductive/nursing Safety Little is known about the effects of vinblastine on developing fe-tuses, but it is believed that the drug possesses some teratogenic and embryotoxic properties. It may also cause aspermia in males. In humans, the FDA categorizes this drug as category D for use during pregnancy (There is evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women may be acceptable despite its potential risks. ) It is not known whether vinblastine is excreted in milk. Because of the potential for serious adverse reactions in nursing offspring, consider using milk replacer if dams are being given this drug. overdosage/acute t oxicity In dogs, the lethal dose for vinblastine has been reported as 0. 2 mg/kg. Effects of an overdosage of vinblastine are exacerbations of the adverse effects outlined above. Additionally, neurotoxic effects sim-ilar to those associated with vincristine may also be noted. In humans, cardiovascular and hematologic monitoring are per-formed after an overdose. Treatment can include anticonvulsants, and prevention of ileus. Additionally, an attempt is made to prevent the effects associated with the syndrome of inappropriate antidi-uretic hormone (SIADH) with fluid restriction and loop diuretics to maintain serum osmolality. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving vinblastine and may be of significance in veterinary patients: ototoxic DRu GST! (e. g., cisplatin, carboplatin ): May cause additive risk for ototoxicity Caution is advised if using other drugs that can inhibit p-glycopro-tein particularly in those dogs at risk for MDR1-allele mutation (Collies, Australian Shepherds, Shelties, Long-haired Whippet, etc. “white feet”), unless tested “normal”. Drugs and drug classes in-volved include: amio Da Rone!! azo Le anti Fun Ga LS !! (e. g., ketoconazole ) ca RVe Di Lo L!! cyc Lo SPo Rine!! Di Ltiazem!! e Ryt HRomycin; c La Rit HRomycin!! quini Dine!! SPi Rono Lactone!! tamoxi Fen T! Ve Ra P ami L!! Laboratory considerations Vinblastine may significantly increase both blood and urine con-T! centrations of uric acid Doses For more information on using vinblastine as part of chemotherapy protocols, refer to the protocols found in the appendix or other dos-ages/protocols found in numerous references, including: Withrow and Mac Ewen's Small Animal Clinical Oncology, 4th Ed. (Withrow and Vail 2007); Canine and Feline Geriatric Oncology (Villalobos 2007); Small Animal Internal Medicine, 3rd Edition (Nelson and Couto 2003); Textbook of Veterinary Internal Medicine: Diseases of the Dog and Cat 6th Edition (Ettinger and Feldman 2005); and The 5-Minute Veterinary Consult Canine & Feline, 3rd Ed. (Tilley and Smith 2004). Do GS:T! For susceptible neoplastic diseases:a) 2 mg/m2 IV every 7-14 days (O'Keefe and Harris 1990), (Thompson 1989a) b) For mast cell tumors after surgical removal: vinblastine at 2 mg/m2 IV, weekly for four weeks then every two weeks for | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Vinc Ri Stine Su LF ate 927 eight weeks. Prednisolone is given concurrently starting at 2 mg/kg/day, tapering to 0. 5 mg/kg day. (Davies, Wyatt et al. 2002) c) For lymphoma and mastocytoma: 2 mg/m2 weekly. For lym-phosarcoma and various carcinomas: 2. 5 mg/m2 IV weekly (Mac Ewen and Rosenthal 1989), (Rosenthal 1985) cat S:T! For susceptible neoplastic diseases:a) For lymphosarcoma and mast cell neoplasms: 2 mg/m2 IV every 7-14 days (Couto 1989b) b) 2 mg/m2 slow IV every 7-14 days (Golden and Langston 1988) monitoring Efficacy T! T oxicity (complete blood counts with platelets; liver function tests T! prior to therapy and repeated as necessary; serum uric acid) client information Clients must be briefed on the possibilities of severe toxicity de-T! veloping from this drug, including drug-related mortality Contact the veterinarian if the patient exhibits any symptoms of T! profound depression, abnormal bleeding (including bloody diar-rhea) and/or bruising chemistry/Synonyms Commonly referred to as a Vinca alkaloid, vinblastine sulfate is isolated from the plant Cantharanthus roseus (Vinca rosea Linn) and occurs as a white or slightly yellow, hygroscopic, amorphous or crystalline powder that is freely soluble in water. The commercially available injection has a p H of 3-5. 5. Vinblastine may also be known as: 29060-LE, NSC-49842, sulf-ato de vimblastina, vinblastini sulfas, vincaleukoblastine sulphate, VBL, Alkaban®, Blastovin®, Cellblastin®, Cytoblastin®, Ifabla®, Lemblastine®, Periblastine®, Serovin®, Solblastin®, Velban®, Velbe ®, Velsar®, or Xintoprost®. Storage/Stability/compatibility The sterile powder for injection, solution for injection and reconsti-tuted powder for injection should all be protected from light. The powder for injection and injection should be stored in the refrig-erator (2-8°C). The intact powder for injection is stable at room temperature for at least one month. After reconstituting with bac-teriostatic saline, the powder for injection is stable for 30 days if refrigerated. Vinblastine sulfate is reportedly physically compatible with the following intravenous solutions and drugs: D 5W and bleomycin sulfate. In syringes or at Y-sites with: bleomycin sulfate, cisplatin, cyclophosphamide, droperidol, fluorouracil, leucovorin calcium, methotrexate sodium, metoclopramide HCl, mitomycin, and vin-cristine sulfate. Vinblastine sulfate compatibility information conflicts or is depen-dent on diluent or concentration factors with the following drugs or solutions: doxorubicin HCl and heparin sodium (in syringes). Vinblastine sulfate is reportedly physically incompatible with furosemide. Compatibility is dependent upon factors such as p H, concentration, temperature and diluent used; consult specialized references or a hospital pharmacist for more specific information. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Vinblastine Sulfate Injection: 1 mg/m L in 10 m L and 25 m L vials; generic; (Rx) Vinblastine Powder for Injection: 10 mg in vials; Velban® (Lilly); ge-neric; (Rx) vincri Stine Sulfate (vin-kris-teen) Oncovin® antineo Pla Stic Prescriber Highlights A Vinca alkaloid antineoplastic used for a variety of tu-T T mors in dogs & cats (primarily lymphoid & hematopoietic neoplasms); also used for the treatment of immune-mediated thrombocytopenia Caution: Hepatic disease, leukopenia, infection, or pre-T T existing neuromuscular disease; reduce dose if hepatic disease Adverse Effects: Much less myelosuppressive than vin-T T blastine, but may cause more peripheral neurotoxic effects; neuropathic clinical signs can include propriocep-tive deficits, spinal hyporeflexia, or paralytic ileus with resulting constipation; CATS can develop neurotoxicity causing constipation or paralytic ileus & aggravating an-orexia; can also develop reversible axon swelling & para-nodal demyelination Potentially teratogenic T T Avoid extravasation; wear gloves & protective clothing T T when preparing or administering Drug Interactions T T uses/indications Vincristine is used as an antineoplastic primarily in combination drug protocols in dogs and cats in the treatment of lymphoid and hematopoietic neoplasms. In dogs, it may be used alone in the ther-apy of transmissible venereal neoplasms. Because vincristine can induce thrombocytosis (at low doses) and has some immunosuppressant activity, it may also be employed in the treatment of immune-mediated thrombocytopenia. Pharmacology/actions Vincristine apparently binds to microtubular proteins (tubulin) in the mitotic spindle, thereby preventing cell division during meta-phase. It also interferes with amino acid metabolism by inhibiting glutamic acid utilization and preventing purine synthesis, citric acid cycle and urea formation. Tumor resistance to one Vinca alka-loid does not imply resistance to another. Vincristine can induce thrombocytosis (mechanism unknown) and has some immunosuppressant activity. Pharmacokinetics Vincristine is administered IV as it is unpredictably absorbed from the GI tract. After injection it is rapidly distributed to tissues. In humans, approximately 75% is bound to tissue proteins and the drug does not appreciably enter the CNS. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
928 Vinc Ri Stine Su LF ate Vincristine is extensively metabolized, presumably by the liver and primarily excreted in the bile/feces; lesser amounts are elimi-nated in the urine. The elimination half-life in dogs is reportedly biphasic with an alpha half-life of 13 minutes and a beta half-life of 75 minutes. contraindications/Precautions/Warnings Vincristine should be used with caution in patients with hepatic dis-ease, leukopenia, infection, or preexisting neuromuscular disease. Doses of vincristine should be reduced in patients with hepatic disease. A 50% reduction in dose should be considered if serum bilirubin levels are greater than 2 mg/dl. Because vincristine is potentially a neurotoxic substrate of P-glycoprotein, it should be used with caution in those herding breeds (e. g., Collies) that may have the gene mutation that causes a nonfunctional protein As vincristine may be a skin irritant, gloves and protective cloth-ing should be worn when preparing or administering the medica-tion. If skin/mucous membrane exposure occurs, thoroughly wash area with soap and water. adverse effects Although structurally related to and having a similar mechanism of action as vinblastine, vincristine has a different adverse reaction profile. Vincristine is much less myelosuppressive (mild leukope-nia) at usual doses than is vinblastine, but may cause more pe-ripheral neurotoxic effects. Neuropathic clinical signs may include proprioceptive deficits, spinal hyporeflexia, or paralytic ileus with resulting constipation. In humans, vincristine commonly causes mild sensory impairment and peripheral paresthesias. These may also occur in animals, but are not usually noted due to difficulty in detection. Cats, however, can develop neurotoxicity that can be associated with constipation or paralytic ileus thereby aggravating anorexia. They can develop reversible axon swelling and paranodal demyelination. Additionally, in small animals, vincristine may cause impaired platelet aggregation, increased liver enzymes, inappropriate ADH secretion, jaw pain, alopecia, stomatitis, or seizures. Extravasation injuries associated with perivascular injection of vincristine can range from irritation to necrosis and tissue slough-ing. Because of the vesicant action of this drug, it is recommended to use a different needle for injecting the drug than the one used to withdraw it from the vial. Recommendations of therapy for ex-travasation include discontinuing the infusion immediately at that site and applying moderate heat to the area to help disperse the drug. Injections of hyaluronidase have been suggested to help dif-fuse the drug. Others have suggested applying ice to the area to limit the drug's diffusion and minimize the area affected. T opical dim-ethyl sulfoxide (DMSO) has also been recommended by some to treat the area involved. Reproductive/nursing Safety Little is known about the effects of vincristine on developing fe-tuses, but it is believed that the drug possesses some teratogenic and embryotoxic properties. It may also cause aspermia in males. In humans, the FDA categorizes this drug as category D for use during pregnancy (There is evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women may be accept-able despite its potential risks. ) In a separate system evaluating the safety of drugs in canine and feline pregnancy (Papich 1989), this drug is categorized as in class: C (These drugs may have potential risks. Studies in people or laboratory animals have uncovered risks, and these drugs should be used cautiously as a last resort when the benefit of therapy clearly outweighs the risks. ) It is not known whether this drug is excreted in milk. Because of the potential for serious adverse reactions in nursing offspring, consider using milk replacer if dams are being given this drug. overdosage/acute t oxicity In dogs, it is reported that the maximally tolerated dose of vincris-tine is 0. 06 mg/kg every 7 days for 6 weeks. Animals receiving this dose showed signs of slight anemia, leukopenia, increased liver en-zymes, and neuronal shrinkage in the peripheral and central ner-vous systems. In cats, the lethal dose of vincristine is reportedly 0. 1 mg/kg. Cats receiving toxic doses showed clinical signs of weight loss, sei-zures, leukopenia, and general debilitation. In humans, cardiovascular and hematologic monitoring are per-formed after an overdose. Treatment can include anticonvulsants, and prevention of ileus. Additionally, an attempt is made to prevent the effects associated with the syndrome of inappropriate antidi-uretic hormone (SIADH) with fluid restriction and loop diuretics to maintain serum osmolality. There have been some reports of leucovorin calcium being used to treat vincristine overdoses in hu-mans, but efficacy of this treatment has not yet been confirmed. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving vincristine and may be of significance in veterinary patients: a SPa Ra Gina Se T! : Additive neurotoxicity may occur; is appar-ently less common when asparaginase is administered after vincristine mitomycin T! : In humans who have previously or simultaneously received mitomycin-C with Vinca alkaloids, severe bronchos-pasm has occurred Caution is advised if using other drugs that can inhibit p-glycopro-tein particularly in those dogs at risk for MDR1-allele mutation (Collies, Australian Shepherds, Shelties, Long-haired Whippet, etc. “white feet”), unless tested “normal”. Drugs and drug classes in-volved include: amio Da Rone!! azo Le anti Fun Ga LS !! (e. g., ketoconazole ) ca RVe Di Lo L!! cyc Lo SPo Rine!! Di Ltiazem!! e Ryt HRomycin; c La Rit HRomycin!! quini Dine!! SPi Rono Lactone!! tamoxi Fen!! Ve Ra P ami L!! Laboratory considerations Vincristine may significantly increase both blood and urine con-T! centrations of uric acid Doses For more information on using vincristine as part of chemother-apy protocols such as COP, VELCAP, etc, refer to the protocols found in the appendix or other dosages/protocols found in numer-ous references, including: Withrow and Mac Ewen's Small Animal Clinical Oncology, 4th Ed. (Withrow and Vail 2007); Canine and Feline Geriatric Oncology (Villalobos 2007); Small Animal Internal Medicine, 3rd Edition (Nelson and Couto 2003); Textbook of Veterinary Internal Medicine: Diseases of the Dog and Cat 6th Edition (Ettinger and Feldman 2005); and The 5-Minute Veterinary Consult Canine & Feline, 3rd Ed. (Tilley and Smith 2004). | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Vitamin e/Se Lenium 929 Do GS:T! For neoplastic diseases (usually used in combination protocols with other drugs; see the appendix for sample protocols):a) 0. 5-0. 75 mg/m2 IV every 7-14 days (O'Keefe and Harris 1990) b) 0. 5 mg/m2 every 7-14 days (Coppoc 1988) c) 0. 5 mg/m2 IV weekly (Mac Ewen and Rosenthal 1989) d) For transmissible venereal tumor: 0. 025 mg/kg (maximum dose 1 mg) IV once weekly. Generally requires 3-6 weeks of therapy. Usually tumor regression noted within 2 weeks of initial treatment. (Herron 1988) e) For transmissible venereal tumor: 0. 5 mg/m2 (maximum dose 1 mg) IV every 7 days until there is no evidence of dis-ease. Generally requires 4-6 weeks of therapy. (Rosenthal 1985) For immune-mediated thrombocytopenia:a) Used only when other therapies are ineffective and bone marrow aspirate demonstrates adequate megakaryocytopoi-esis: 0. 02 mg/kg IV once weekly (Feldman 1989) b) If refractory to prednisone (3-5 days), give vincristine at 0. 5-0. 7 mg/m2 IV bolus or as an infusion over 4-6 hours (Trepanier 1999) c) 0. 02 mg/kg IV once; generally single use (Cohn 2004) cat S:T! For neoplastic diseases (usually used in combination proto-cols with other drugs; see the appendix for additional sample protocols): a) 0. 5-0. 75 mg/m2 IV once a week (Couto 1989b) b) For feline lymphoma: A neutrophil count over 4,500 cells/UL is required. Cats should be well hydrated before treatment and fluid therapy should be continued for 24-36 hours. On day 1 give vincristine at 0. 5 mg/m2 IV and cyclophosphamide at 250 mg/m2 IV or orally. These drugs may be administered by slow IV push. If no adverse reactions and neutrophil count is over 4,500, may repeat on day 21. On day 42, premedicate with diphenhydramine (2. 2. mg/kg SC) and give doxorubi-cin at 1 mg/kg IV over 20 minutes into the injection port of an IV drip set. This regimen is repeated until a total of six cycles have been administered. If cat is in complete remission at the end of the of the 6 cycles, consider stopping therapy. Treatment is delayed if neutropenia of thrombocytopenia occur. If hemorrhagic cystitis occurs, discontinue cyclophos-phamide. Monitor renal function throughout therapy. (Leg-endre 2003) monitoring Efficacy (tumor burden reduction or platelet count)T! T oxicity (peripheral neuropathic clinical signs; complete blood T! counts with platelets; liver function tests prior to therapy and re-peated as necessary; serum uric acid) client information Clients must be briefed on the possibilities of severe toxicity de-T! veloping from this drug, including drug-related mortality Clients should contact the veterinarian if the patient exhibits T! any signs of profound depression, abnormal bleeding (including bloody diarrhea) and/or bruising, severe constipation, or severe peripheral neuropathic signs chemistry/Synonyms Commonly referred to as a Vinca alkaloid, vincristine sulfate is iso-lated from the plant Cantharanthus roseus ( Vinca rosea Linn) and occurs as a white or slightly yellow, hygroscopic, amorphous or crystalline powder that is freely soluble in water and slightly soluble in alcohol. The commercially available injection has a p H of 3-5. 5. Vincristine sulfate has p K as of 5 and 7. 4 Vincristine Sulfate may also be known as: leurocristine sulfate, VCR, LCR compound 37231, leurocristine sulphate, NSC-67574, 22-oxovincaleukoblastine sulphate, sulfato de vincristina, vincris-tini sulfas and Oncovin®; many other trade names are available. Storage/Stability/compatibility Vincristine sulfate injection should be protected from light and stored in the refrigerator (2-8°C). Vincristine sulfate is reportedly physically compatible with the following intravenous solutions and drugs: D 5W, bleomycin sul-fate, cytarabine, fluorouracil, and methotrexate sodium. In syringes or at Y-sites with: bleomycin sulfate, cisplatin, cyclophosphamide, doxorubicin HCl, droperidol, fluorouracil, heparin sodium, leuco-vorin calcium, methotrexate sodium, metoclopramide HCl, mito-mycin, and vinblastine sulfate. Vincristine sulfate is reportedly physically incompatible with furosemide. Compatibility is dependent upon factors such as p H, concentration, temperature, and diluent used; consult specialized references or a hospital pharmacist for more specific information. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Vincristine Sulfate Injection: 1 mg/m L in 1 m L, 2 m L and 5 m L vials and flip-top vials; Vincasar® PFS (Genesia Sicor); generic; (Rx) vita Min e/Seleniu M vita Min e (se-lee-nee-um) nutritional; f at Soluble vitamin Prescriber Highlights Lipid-soluble vitamin (E) with or without selenium used T T alone for discoid lupus erythematosus, canine demodi-cosis, acanthosis nigricans, hepatic fibrosis, or adjunctive therapy of exocrine pancreatic deficiency or hepatopathy in dogs & cats; used in combination for selenium-tocoph-erol deficiency (white muscle disease) Contraindications: Vitamin E/selenium products should T T only be used in the species for which they are approved Selenium overdoses can be extremely toxic T T Adverse Effects: Anaphylactoid reactions; IM injections T T may cause transient muscle soreness. Selenium OD's can cause depression, ataxia, dyspnea, blindness, diar-rhea, muscle weakness, & a “garlic” odor on the breath uses/indications Depending on the actual product and species, vitamin E/selenium is indicated for the treatment or prophylaxis of selenium-tocoph-erol deficiency (STD) syndromes in ewes and lambs (white muscle disease), sows, weanling and baby pigs (hepatic necrosis, mulber-ry heart disease, white muscle disease), calves and breeding cows (white muscle disease), and horses (myositis associated with STD). Vitamin E may be useful as adjunctive treatment of discoid lu-pus erythematosus, canine demodicosis, and acanthosis nigricans | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
930 Vitamin e/Se Lenium in dogs. It may also be of benefit in the adjunctive treatment of he-patic fibrosis or adjunctive therapy of copper-associated hepatopa-thy in dogs. Pharmacology/actions Both vitamin E and selenium are involved with cellular metabolism of sulfur. Vitamin E has antioxidant properties and, with selenium, protects against red blood cell hemolysis and prevents the action of peroxidase on unsaturated bonds in cell membranes. Pharmacokinetics After absorption, vitamin E is transported in the circulatory system via beta-lipoproteins. It is distributed to all tissues and stored in adipose tissue. Vitamin E is only marginally transported across the placenta. Vitamin E is metabolized in the liver and excreted primar-ily into the bile. Pharmacokinetic parameters for selenium were not located. contraindications/Precautions/Warnings Vitamin E/selenium products should only be used in the species for which they are approved. Because selenium can be extremely toxic, the promiscuous use of these products cannot be condoned. Give slowly when administering intravenously to horses. adverse effects Anaphylactoid reactions have been reported. Intramuscular in-jections may be associated with transient muscle soreness. Other adverse effects are generally associated with overdoses of selenium (see below). overdosage/acute t oxicity Selenium is quite toxic in overdose quantities, but has a fairly wide safety margin. Cattle have tolerated chronic doses of 0. 6 mg/kg/day with no adverse effects (approximate therapeutic dose is 0. 06 mg/kg). Clinical signs of selenium toxicity include depression, ataxia, dyspnea, blindness, diarrhea, muscle weakness, and a “garlic” odor on the breath. Horses suffering from selenium toxicity may become blind, paralyzed, slough their hooves, and lose hair from the tail and mane. Dogs may exhibit clinical signs of anorexia, vomiting, and diarrhea at high dosages. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving vitamin E/selenium and may be of significance in veterinary patients: i Ron T! : Large doses of vitamin E may delay the hematologic re-sponse to iron therapy in patients with iron deficiency anemia. mine Ra L oi LT! : May reduce the absorption of orally administered vitamin E Vitamin a T! : Absorption, utilization and storage may be enhanced by vitamin E Doses (Vitamin e alone): For doses of vitamin E/selenium products see the Dosage Form section Do GS:T! For adjunctive treatment of discoid lupus erythematosus, canine demodicosis or acanthosis nigricans: a) 200-400 IU PO three times daily; variable efficacy, but rela-tively innocuous at these dosages (White 2000) For adjunctive treatment of hepatic fibrosis: a) 100-400 IU q12h PO (Rutgers 2000)For adjunctive treatment of copper-associated hepatopathy: a) 400-600 IU PO per day (Johnson 2000) For treatment of tocopherol deficiency associated with exocrine pancreatic disease: a) 100-400 IU PO once daily for one month then every 1-2 weeks as needed (Williams 2000) cat S:T! For treatment of tocopherol deficiency associated with exocrine pancreatic disease: a) 30 IU PO once daily for one month then every 1-2 weeks as needed (Williams 2000) For adjunctive treatment of hepatic lipidosis: a) 10 IU/kg once PO once daily) (Scherk and Center 2005) Ho RSe S:T! For adjunctive treatment of ionophore (monensin) toxicity: a) 4-12 Units/kg PO once daily (Mogg 1999) For adjunctive therapy for EPM: a) 8000-9000 IU PO per day (Dowling 1999) For adjunctive therapy for metabolic syndrome: a) 10,000 IU PO once daily (Johnson 2003b) For adjunctive treatment of perinatal asphyxia syndrome (hy-poxic ischemic encephalopathy): a) Foals: 4,000 IU PO once daily; Mares: 10,000 IU PO once daily (Slovis 2003b) monitoring Clinical efficacy T! Blood selenium levels (when using the combination prod-T! uct). Normal values for selenium have been reported as: >1. 14 micromol/L in calves, >0. 63 micromol/L in cattle, >1. 26 micromol/L in sheep, and >0. 6 micromol/L in pigs. Values in-dicating deficiency are: <0. 40 micromol/L in cattle, <0. 60 micromol/L in sheep, and <0. 20 micromol/L in pigs. Intermedi-ate values may result in suboptimal production Optionally, glutathione peroxidase activity may be monitored T! chemistry/Synonyms Vitamin E is a lipid soluble vitamin that can be found in either liq-uid or solid forms. The liquid forms occur as clear, yellow to brown-ish red, viscous oils that are insoluble in water, soluble in alcohol and miscible with vegetable oils. Solid forms occur as white to tan-white granular powders that disperse in water to form cloudy sus-pensions. Vitamin E may also be known as alpha tocopherol. Selenium in commercially available veterinary injections is found as sodium selenite. Each mg of sodium selenite contains ap-proximately 460 micrograms (46%) of selenium. Storage/Stability Vitamin E/Selenium for injection should be stored at temperatures less than 25°C (77°F). Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: Vitamin E (Alone) Injection Vitamin E Injection: 300 mg/m L in 250 m L vials; Emulsivit® E-300 (Vedco); Vital E®-300 (Schering-Plough); (OTC or Rx) Vitamin E/Selenium Oral Equ-Se E® (Vet-A-Mix) (one teaspoonful contains 1 mg selenium and 220 IU vitamin E) and Equ-Se5E® (one teaspoonful contains 1 mg se-lenium and approximately 1100 IU vitamin E); (Vet-a-Mix); (OTC) Approved for oral use in horses. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Vo Riconazo Le 931 Other top dress equine products containing Vitamin E and Selenium include: Vitamin E and Selenium Powder (Farnam, Horse Health), Vitamin E and Selenium Crumbles® (Horse Health) Vitamin E/Selenium Injection Mu-Se® (Schering); (Rx): Each m L contains: selenium 5 mg (as so-dium selenite); Vitamin E 68 IU; 100 m L vial for injection. Approved for use in non-lactating dairy cattle and beef cattle. Slaughter with-drawal (at labeled doses) = 30 days. Dose: For weanling calves: 1 m L per 200 lbs. body weight IM or SC. For breeding beef cows: 1 m L per 200 lbs. body weight during middle third of pregnancy and 30 days before calving IM or SC. Bo-Se® (Schering); (Rx): Each m L contains selenium 1 mg (as sodium selenite) and Vitamin E 68 IU; 100 m L vial for injection. Approved for use in calves, swine and sheep. Slaughter withdrawal (at labeled doses) = 30 days (calves); 14 days (lambs, ewes, sows, and pigs). Dose: Calves: 2. 5-3. 75 m L/100 lbs body weight (depending on severity of condition and geographical area) IM or SC. Lambs (2 weeks of age or older): 1 m L per 40 lbs. body weight IM or SC (1 m L minimum). Ewes: 2. 5 m L/100 lbs. body weight IM or SC. Sows and weanling pigs: 1 m L/40 lbs. body weight IM or SC (1 m L minimum). Do not use on newborn pigs. L-Se® (Schering); (Rx): Each m L contains: selenium 0. 25 mg (as so-dium selenite) and Vitamin E 68 IU in 30 m L vials. Approved for use in lambs and baby pigs. Slaughter withdrawal (at labeled doses) = 14 days. Dose: Lambs: 1 m L SC or IM in newborns and 4 m L SC or IM in lambs 2 weeks of age or older; Baby Pigs: 1 m L SC or IM. E-Se® (Schering); (Rx): Each m L contains selenium 2. 5 mg (as so-dium selenite) and Vitamin E 68 IU in 100 m L vials. Approved for use in horses. Dose: Equine: 1 m L/100 lbs. body weight slow IV or deep IM (in 2 or more sites; gluteal or cervical muscles). May be repeated at 5-10 day intervals. Seletoc® (Schering); (Rx): Each m L contains selenium 1 mg (as so-dium selenite) and Vitamin E 68 IU in 10 m L vials. Approved for use in dogs. Dose: Dogs: Initially, 1 m L per 20 pounds of body weight (minimum 0. 25 m L; maximum 5 m L) SC, or IM in divided doses in 2 or more sites. Repeat dose at 3 day intervals until satisfactory results then switch to maintenance dose. If no response in 14 days reevalu-ate. Maintenance dose: 1 m L per 40 lbs body weight (minimum 0. 25 m L) repeat at 3-7 day intervals (or longer) to maintain. Human-Labe Le D PRo Duct S: Vitamin E Tablets: 100 IU, 200 IU, 400 IU, 500 IU & 800 IU; generic (various; OTC) Vitamin E Capsules: 100 IU, 200 IU, 400 IU & 1000 IU; Mixed E 400 Softgels® & d'ALPHA E 1000 Softgels® (Naturally); Vita-Plus E® (Scot-Tussin); generic; (OTC)Vitamin E Drops: 15 IU/0. 3 m L in 12 m L & 30 m L; Aquasol E® (Mayne Pharma); Aquavit-E® (Cypress); (OTC)Vitamin E Liquid: 15 IU/30 m L in 30 m L, 60 m L & 120 m L; 798 IU/30 m L in 473 m L; Vitamin E (Freeda); Nutr-E-Sol® (Advanced Nutri-tional T echnology); (OTC) T opicals are available. There are no approved vitamin E/selenium products, but there are many products that contain either vitamin E (alone, or in combination with other vitamins ± minerals) or sele-nium (as an injection alone or in combination with other trace ele-ments) available. voriconazole (vor-ih-koh-nah-zohl) Vfend® Second generation triazole antifungal Prescriber Highlights Broad-spectrum oral/parenteral triazole antifungal T T Very little clinical experience thus far in veterinary medi-T T cine; extremely expensive Like other compounds in this class, there are many po-T T tential drug interactions uses/indications Voriconazole may be a useful treatment for a variety of fungal in-fections in veterinary patients, particularly against Blastomyces, Cryptococcus, and Aspergillus. It has high oral bioavailability in a variety of species and can cross into the CNS. Currently available human dosage forms are extremely expensive, however, and little clinical experience has occurred using voriconazole in veterinary patients. There is considerable interest in using voriconazole for treating aspergillosis in pet birds as their relative small size may allow the drug to be affordable; additional research must be per-formed before dosing regimens are available. Pharmacology/actions Voriconazole a synthetic derivative of fluconazole, has broad-spectrum antifungal activity against a variety of organisms, includ-ing Candida, Aspergillus, Trichosporon, Histoplasma, Cryptococcus, Blastomyces, and Fusarium species. Like the other azole/triazole an-tifungals it inhibits cytochrome P-450-dependent 14-alpha-sterol demethylase which is required for ergosterol biosynthesis in fungal cell walls. Unlike fluconazole, voriconazole also inhibits 24-methyl-ene dehydrolanosterol demethylation in molds such as Aspergillus giving it more activity against these fungi. Pharmacokinetics In dogs, voriconazole is rapidly and essentially completely absorbed after oral administration. Peak levels occur about 3 hours after oral dosing. Voriconazole is only moderately (51%) bound to canine plasma proteins and volume of distribution is about 1. 3 L/kg. It is metabolized in the liver to a variety of metabolites with the N-oxide metabolite being the primary circulating metabolite. This metabo-lite has only weak (<100X as active as the parent) antifungal activity. The elimination pharmacokinetics of voriconazole in dogs is very complex. Both dose-dependent non-linear elimination and auto-induced metabolism after multiple dosages are seen complicating any dosage regimen scenarios; dosages may need to be increased over time. Auto-induction of metabolism apparently does not oc-cur in humans, rabbits or guinea pigs. In horses, voriconazole is well absorbed after oral administra-tion with peak levels occurring at approximately 3 hours post-dose. Voriconazole has low protein binding (31%); volume of distribu-tion is about 1. 35 L/kg. Elimination half-life is quite long—approx-imately 13 hours after oral dosing. It is not known if voriconazole self-induces hepatic metabolism after multiple doses in the horse. contraindications/Precautions/Warnings Voriconazole is contraindicated in patients hypersensitive to it oth-er azole antifungals. It should be given with caution to patients with hepatic dysfunction, or proarrhythmic conditions. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
932 Vo Riconazo Le The intravenous product contains 3200 mg of sulfobutyl ether beta-cyclodextrin sodium (SBECD) per vial. This compound can accumulate in patients with decreased renal function. adverse effects Accurate adverse effect profiles are unknown for veterinary species. Liver enlargement and up to a 2-3 fold increase in cytochrome P450 hepatic microsomal enzyme concentrations were noted in dogs orally dosed for 30 days. This may significantly impact the metabolism of other drugs that are hepatically metabolized (See Drug Interactions). In humans, commonly encountered adverse effects include visu-al disturbances (blurring, spots, wavy lines) usually within 30 min-utes of dosing or if higher drug concentrations are attained, and rashes (usually mild to moderate in severity). Less frequent adverse effects include gastrointestinal effects (nausea, vomiting, diarrhea), hepatotoxicity (jaundice, abnormal liver function tests), hyperten-sion/hypotension, tachycardia, peripheral edema, hypokalemia, and hypomagnesemia. Rarely, eye hemorrhage, anemia, leukope-nia, thrombocytopenia, pancytopenia, QT prolongation, torsade de pointes, and nephrotoxicity have been reported. Reproductive/nursing Safety Voriconazole was teratogenic in rats at low dosages (10 mg/kg) and embryotoxic in rabbits at higher dosages (100 mg/kg). In humans, the FDA categorizes voriconazole as category D for use during preg-nancy (There is evidence of human fetal risk, but the potential benefits from the use of the drug in pregnant women may be acceptable despite its potential risks. ) Weigh the risks of treatment versus the benefits when considering use in pregnant patients. It is unknown if voriconazole enters milk. overdosage/acute t oxicity The minimum lethal dose in rats and mice was 300 mg/kg (4-7X maintenance dose). T oxic effects included increased salivation, my-driasis, ataxia, depression, dyspnea, and seizures. Accidental single overdoses of up to 5X in human pediatric patients caused only brief photophobia. No antidote is known for voriconazole overdoses. Gut emptying should be considered for very large oral overdoses, fol-lowed by close observation and supportive treatment if required. Drug interactions There are many potential drug interactions involving voriconazole. The following partial listing includes reported or theoretical in-teractions in humans receiving voriconazole that may also be of significance in veterinary patients. Because, in dogs, voriconazole induces hepatic microsomal enzymes (in humans it does not) ad-ditional interactions and further clarification may be reported as clinical use increases in veterinary patients. anti Diabetic a Gent ST! (sulfonylureas ): Voriconazole may increase serum concentrations of these drugs and increase risk for hypoglycemia ba Rbitu Rate ST! (phenobarbital ): Decreased voriconazole concentra-tions; use together contraindicated benzo Diaze Pine ST! : Voriconazole may increase benzodiazepine concentrations ca Lcium-c Hanne L b Locke RS T! (amlodipine, diltiazem, verapamil ): Voriconazole may increase serum concentrations, dosage adjust-ment may be required ca Rbamaze Pine T! : Decreased voriconazole concentrations; use to-gether contraindicated ci Sa PRi De T! : Potential for serious cardiac arrhythmias; use is contraindicatedco Rtico Ste Roi DST! (prednisolone ): Potentially increased AUC for prednisolone immuno Su PPRe SSi Ve a Gent S T! (systemic : cyclosporine, tacrolimus ): Increased cyclosporine and tacrolimus concentrations; decrease cyclosporine dosage by 50% when starting voriconazole; decrease tacrolimus dosage by 33% when starting voriconazole met Ha Done T! : Voriconazole may increase plasma concentrations of R-methadone; monitor for methadone toxicity and adjust dosage if necessary PHenytoin T! : Can decrease voriconazole concentrations and vori-conazole can increase phenytoin concentrations; monitoring and dosage adjustment may be required Pimozi De T! : Potential for serious cardiac arrhythmias; use is contraindicated PRoton-Pum P in Hibito RS T! (omeprazole ): Voriconazole may increase omeprazole (and potentially other PPI's) concentrations quini Dine T! : Potential for serious cardiac arrhythmias; use is contraindicated Ri Fam Pin, Ri F abutin T! : Decreased voriconazole concentrations; use together contraindicated Vinca a Lka Loi DST! (vincristine, vinblastine ): Possible increased Vinca alkaloid concentrations; monitor for toxicity Wa RF a Rin T! : Voriconazole may potentiate warfarin's effects Laboratory considerations No specific concerns were noted; see Monitoring for additional information. Doses At the time of writing (March 2007) there is little data or clinical ex-perience with voriconazole to support science-or experience-based dosing regimens for systemic use in veterinary species, particularly in small animals. The drug's pharmacokinetic profile can vary con-siderably across species and in some species (dogs) the drug induc-es hepatic microsomal enzymes that increase its own metabolism. A single-dose pharmacokinetic study in horses (Davis, Salmon et al. 2006) gives support to a dose of 4 mg/kg PO once daily for sus-ceptible fungi with an MIC ≤1 mcg/m L, but it is unknown if this dose will be adequate after repeated dosing. One respected refer-ence (Greene, Hartmannn et al. 2006), has listed a dose for treat-ing fungal infections in dogs extrapolated from the human dose: Loading dose: 6 mg/kg IV or PO q12h for days, then 3-4 mg/kg PO q12h for a duration as necessary. monitoring Efficacy T! Liver function tests, serum electrolytes T! client information Inform clients of the investigational nature of using this drug in T! veterinary species and the associated expense Give at least one hour before or one hour after feeding T! Because experience with this medication has been limited, report T! any possible adverse effects to the veterinarian immediately, in-cluding itching/rash, yellowing of whites of the eyes, reduced ap-petite, etc. chemistry/Synonyms A triazole antifungal, voriconazole occurs as a white to light colored powder with a molecular weight of 349. 3. Aqueous solubility is 0. 7 mg/m L. Voriconazole may also be known as UK-109496, voriconazol, voraconazolum, or Vfend®. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Wa RFa Rin So Dium 933 Storage/Stability/compatibility Voriconazole tablets should be stored at 15-30°C. The unreconstituted powder for oral suspension should be stored in the refrigerator (2-8°C); it has a shelf-life of approxi-mately 18 months. Once reconstituted, it should be stored in tightly closed containers at room temperature (15-30°C); do not refriger-ate or freeze. After reconstitution, the suspension is stable for 14 days. The suspension should be shaken well for 10 seconds prior to each administered dose. The powder for injection should be stored at room temperature (15-30°C). After reconstituting with 19 m L of sterile water for in-jection, the manufacturer recommends using immediately; how-ever, chemical and physical stability remain for up to 24 hours if stored in the refrigerator (2-8°C). Discard solution if it is not clear or particles are visible. The injectable solution must be further diluted to a concentra-tion of 5mg/m L or less for administration over 1-2 hours. Suitable diluents for IV infusion include (partial list): NS, LRS, D5LRS, and D5W. Voriconazole is not compatible with simultaneous infusion with blood products. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Voriconazole Tablets: 50 mg, 200 mg; Vfend® (Pfizer); (Rx) Voriconazole Powder for Oral Suspension: 45 g (40 mg/m L after re-constitution; orange flavor in 100 m L bottles; Vfend® (Pfizer); (Rx) Voriconazole Powder for Injection, Lyophilized: 200 mg/vial (single use); Vfend I. V. ® (Pfizer); (Rx). Also contains 3200 mg of sulfobutyl ether beta-cyclodextrin sodium (SBECD) per vial (See Warnings) to solubolize the drug for IV administration. Warfarin Sodiu M (war-far-in) Coumadin® anticoagulant Prescriber Highlights Coumarin derivative anticoagulant used primarily for T T long-term treatment (or prevention of recurrence) of thrombotic conditions, primarily in cats, dogs, or horses Contraindications: Preexistent hemorrhage, pregnancy, T T those undergoing or contemplating eye or CNS surgery, major regional lumbar block anesthesia, surgery of large, open surfaces, active bleeding from the GI, respiratory, or GU tract; aneurysm, acute nephritis, cerebrovascular hemorrhage, blood dyscrasias, uncontrolled or malignant hypertension, hepatic insufficiency, pericardial effusion, & visceral carcinomas Adverse Effects: Dose-related hemorrhage T T Teratogenic; contraindicated in pregnancy T T Must actively monitor coagulation status T T Drug Interactions T Tuses/indications In veterinary medicine, warfarin is used primarily for the oral, long-term treatment (or prevention of recurrence) of thrombotic conditions, primarily in cats, dogs, or horses. Use of warfarin in veterinary species is somewhat controversial and due to unproven benefit in reducing mortality, increased expense associated with monitoring, and potential for serious effects (bleeding), many do not recommend its use. Pharmacology/actions Warfarin acts indirectly as an anticoagulant (it has no direct an-ticoagulant effect) by interfering with the action of vitamin K 1 in the synthesis of the coagulation factors II, VII, IX, and X. Sufficient amounts of vitamin K 1 can override this effect. Warfarin is ad-ministered as a racemic mixture of S (+) and R (-) warfarin. The S enantiomer is a significantly more potent vitamin K antagonist than the R enantiomer in species studied. Pharmacokinetics Warfarin is administered as a racemic mixture of S (+) and R (-) warfarin. Warfarin is rapidly and completely absorbed in humans after oral administration. In cats, warfarin is also rapidly absorbed after oral administration. After absorption, warfarin is highly bound to plasma proteins in humans, with approximately 99% of the drug bound. In cats, more than 96% of the drug is protein bound. It is reported that there are wide species variations with regard to protein binding; horses have a higher free (unbound) fraction of the drug than do rats, sheep or swine. Only free (unbound) warfarin is active. While other coumarin and indanedione anticoagulants are distributed in milk, warfarin does not enter milk in humans. Warfarin is principally metabolized in the liver to inactive me-tabolites that are excreted in urine and bile (and then reabsorbed and excreted in the urine). The plasma half-life of warfarin may be several hours to several days, depending on the patient (and spe-cies?). In cats, the terminal half-life of the S enantiomer is approxi-mately 23-28 hours and the R enantiomer approximately 11-18 hours. contraindications/Precautions/Warnings Warfarin is contraindicated in patients with preexistent hemor-rhagic tendencies or diseases, those undergoing or contemplating eye or CNS surgery, major regional lumbar block anesthesia, or sur-gery of large, open surfaces. It should not be used in patients with active bleeding from the GI, respiratory, or GU tract. Other con-traindications include: aneurysm, acute nephritis, cerebrovascular hemorrhage, blood dyscrasias, uncontrolled or malignant hyper-tension, hepatic insufficiency, pericardial effusion, pregnancy, and visceral carcinomas. adverse effects The principal adverse effect of warfarin use is dose-related hemor-rhage, which may manifest with clinical signs of anemia, throm-bocytopenia, weakness, hematomas and ecchymoses, epistaxis, hematemesis, hematuria, melena, hematochezia, hemathrosis, he-mothorax, intracranial and/or pericardial hemorrhage, and death. Reproductive/nursing Safety Warfarin is embryotoxic, can cause congenital malformations and considered contraindicated during pregnancy. If anticoagulant therapy is required during pregnancy, most clinicians recommend using low-dose heparin. In humans, the FDA categorizes this drug as category X for use during pregnancy (Studies in animals or hu-mans demonstrate fetal abnormalities or adverse reaction; reports in-dicate evidence of fetal risk. The risk of use in pregnant women clearly | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
934 Wa RFa Rin So Dium outweighs any possible benefit. ) In a separate system evaluating the safety of drugs in canine and feline pregnancy (Papich 1989), this drug is categorized as in class: D (Contraindicated. These drugs have been shown to cause congenital malformations or embryotoxicity. ) Based on very limited published data, warfarin has not been de-tected in the breast milk of humans treated, but there are reports of some breast-fed infants whose mothers were treated having pro-longed prothrombin times. Use with caution in nursing patients. overdosage/acute t oxicity Acute overdosages of warfarin may result in life-threatening hem-orrhage. In dogs and cats, single doses of 5-50 mg/kg have been as-sociated with toxicity. It must be remembered that a lag time of 2-5 days may occur before signs of toxicity occur, and animals must be monitored and treated accordingly. Cumulative toxic doses of warfarin have been reported as 1-5 mg/kg for 5-15 days in dogs and 1 mg/kg for 7 days in cats. If overdosage is detected early, prevent absorption from the gut using standard protocols. If clinical signs are noted, they should be treated with blood products and vitamin K 1 (phytonadione). Refer to the phytonadione monograph for more information. Drug interactions Drug interactions with warfarin are perhaps the most important in human medicine. The following drug interactions have either been reported or are theoretical in humans or animals receiving warfarin and may be of significance in veterinary patients: A multitude of drugs have been documented or theorized to interact with warfarin. The following drugs or drug classes may increase the anticoagulant response of warfarin (not necessarily complete): acetamino PHen!! a LLo Pu Rino L!! amio Da Rone!! anabo Lic Ste Roi DS!! azit HRomycin!! c HLo Ram PHenico L!! cimeti Dine!! ci Sa PRi De!! co-t Rimoxazo Le !! (trimethoprim/sulfa ) Danazo L!! Diazoxi De!! e Ryt HRomycin!! et Hac R ynic aci D !! FLuo Roquino Lone S!! FLuoxetine!! He Pa Rin!! met Roni Dazo Le!! n Sai DS!! Pentoxi Fy LLine !! PRo Py L t Hiou Raci L !! quini Dine!! Sa Licy Late S!! Se Rt Ra Line!! Su LFonami De S!! t Hy Roi D me Dication S!! za Fi RLuka St!!The following drugs or drug classes may decrease the anticoagulant response of warfarin (not necessarily complete): ba Rbitu Rate S !! (phenobarbital, etc. ) co Rtico Ste Roi DS!! e St Ro Gen S!! GRi Seo Fu LVin!! me Rca Pto Pu Rine!! Ri Fam Pin!! SPi Rono Lactone!! Suc Ra LF ate !! Vitamin k!! Should concurrent use of any of the above drugs with warfarin be necessary, enhanced monitoring is required. Refer to other refer-ences on drug interactions for more specific information. Laboratory considerations Warfarin may cause falsely decreased T! theophylline values if using the Schack and Waxler ultraviolet method of assay Doses Do GS:T! For adjunctive therapy of thromboemboli:a) 0. 22 mg/kg PO q12h; target dosage to prolong PT by 1. 25-1. 5 times the pretreatment value (Brooks 2000) b) For pulmonary thromboembolism: 0. 2 mg/kg PO once daily then 0. 05-0. 1 mg/kg PO once daily. Adjust dosage to increase PT to 1. 5-2. 5 times baseline. Heparin may be stopped once appropriate warfarin dosage is established. If PT exceeds 2. 5 times baseline, reduce dose. If bleeding develops, stop dose and institute blood or phytonadione therapy as appropriate. (Roudebush 1985) c) For prophylactic use in patients with glomerular disease and severe proteinuria: Initially, 0. 22 mg/kg, PO once daily. Mon-itor PT and adjust dose so that PT is maintained at 1. 5 times normal. (Grauer and Di Bartola 2000) cat S:T! For adjunctive therapy of thromboembolism:a) For feline aortic thromboembolism: 0. 06-0. 1 mg/kg once daily PO. Evaluate using PT, a PTT, or preferably PIVKA (pro-teins induced by vitamin K antagonists) daily during initial titration (3 days), then every other day (2 times) and weekly thereafter until stable. New steady state may require one week after dosage adjustments. Long-term therapy should be monitored at least once monthly. (Pion and Kittleson 1989) b) For chronic management/prevention of recurrence: 0. 1-0. 2 mg/kg PO once daily. Adjust dosage to prolong PT to 2-2. 5 times normal. Collect blood sample 8 hours after dosing. Requires 48-72 hours to achieve effective anticoagulation. Monitor PT weekly for 1 month, then at monthly intervals. Also determine hematocrit with each PT. (Harpster 1988) c) For thromboembolism: 0. 5 mg per cat PO once daily; target dosage to prolong PT by 1. 25-1. 5 times the pretreatment value (Brooks 2000) d) For long-term thromboprophylaxis: Initially warfarin at 0. 06-0. 09 mg/kg per day PO. Due to unequal drug distribu-tion, tablets should be crushed and mixed well. PT, adjusted to international normalized ratio (INR) is used to monitor therapy, but may not be applicable to cats. Overlap heparin and warfarin therapy by at least 4-5 days. Reevaluate antico-agulation status with any change in concurrent drug therapy. (Smith 2004) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
xy Lazine Hc L 935 e) Initially, 0. 25-0. 5 mg (total dose) per cat PO once daily. Ad-just dosage to prolong PT to twice normal value, or INR to be between 2-3. Overlap therapy with heparin. (Fox 2007a) Ho RSe S:T! (note : ARCI UCGFS Class 5 Drug) As an anticoagulant:a) For adjunctive treatment of laminitis: 0. 0198 mg/kg PO once daily; monitor OSPT (one-step prothrombin time) until prolonged 2-4 seconds beyond baseline (Brumbaugh, Lopez et al. 1999) b) Initially, 0. 018 mg/kg PO once daily and increase dose by 20% every day until baseline PT is doubled. Final dose rates may be from 0. 012 mg/kg to 0. 57 mg/kg daily. (Vrins, Carl-son, and Feldman 1983) monitoring note : The frequency of monitoring is controversial, and is dependent on several factors including dose, patient's condition, concomitant problems, etc. See the Dosage section above for more information. While Prothrombin Times (PT) or International Normalized Ra-T! tio (INR) are most commonly used to monitor warfarin, PIVKA (proteins induced by vitamin K antagonists) has been suggested as being more sensitive. PT's are usually recommended to be 1. 5-2X normal and INR's to be between 2-3. Platelet counts and hematocrit (PCV) should be done T! periodically Occult blood in stool and urine; other observations for bleeding T! Clinical efficacy T! client information Clients must be counseled on both the importance of adminis-T! tering the drug as directed Immediately report any signs or symptoms of bleeding T! chemistry/Synonyms A coumarin derivative, warfarin sodium occurs as a slightly bitter tasting, white, amorphous or crystalline powder. It is very soluble in water and freely soluble in alcohol. The commercially available products contain a racemic mixture of the two optical isomers. Warfarin Sodium may also be known as: sodium warfarin, war-farinum natricum, Coumadin®, Jantoven ®, or Panwarfin®; there are many other trade names internationally. Storage/Stability Warfarin sodium tablets should be stored in tight, light-resistant containers at temperatures less than 40°C, preferably at room tem-perature. Warfarin sodium powder for injection should be protect-ed from light and used immediately after reconstituting. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None The ARCI (Racing Commissioners International) has designated this drug as a class 5 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: Warfarin Sodium Tablets (scored): 1 mg, 2 mg, 2. 5 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7. 5 mg & 10 mg; Coumadin® (Bristol-Myers Squibb), Jantoven® (Upsher-Smith), generic; (Rx) Warfarin Sodium Powder for Injection, lyophilized: 5. 4 mg (2 mg/ m L when reconstituted) preservative-free in 5 mg vials; Coumadin® (Bristol-Myers Squibb); (Rx)A method of suspending warfarin tablets in an oral suspension has been described (Enos 1989). T o make 30 m L of a 0. 25 mg/m L suspen-sion: Crush three 2. 5 mg tablets with a mortar and pestle. Add 10 m L glycerin to form a paste; then 10 m L of water; add sufficient amount of dark corn syrup (Karo®) to obtain a final volume of 30 m L. Warm gently; shake well and use within 30 days. xylazine Hcl (zye-la-zeen) Rompun® al Pha 2-adrenergic agoni St Prescriber Highlights Alpha T T 2-adrenergic agonist used for its sedative & analge-sic in a variety of species; sometimes used as an emetic in cats Contraindications: Animals receiving epinephrine or hav-T T ing active ventricular arrhythmias. Extreme caution: pre-existing cardiac dysfunction, hypotension or shock, respi-ratory dysfunction, severe hepatic or renal insufficiency, preexisting seizure disorders, or if severely debilitated. Should generally not be used in the last trimester of pregnancy, particularly in cattle. Do not give to ruminants that are debilitated, dehydrated, or with urinary tract obstruction. Horses may kick after a stimulatory event (usually auditory); use caution. Avoid intra-arterial injec-tion; may cause severe seizures & collapse. Caution in patients treated for intestinal impactions. Use cautiously in horses during the vasoconstrictive development phase of laminitis. Adverse Effects: T T CATS: emesis, muscle tremors, bradycar-dia with partial A-V block, reduced respiratory rate, move-ment in response to sharp auditory stimuli, & increased urination. Adverse Effects: T T DOGS: Muscle tremors, bradycardia with partial A-V block, reduced respiratory rate, movement in response to sharp auditory stimuli, emesis, bloat from aerophagia which may require decompression. Adverse Effects: T T HORSES: Muscle tremors, bradycardia with partial A-V block, reduced respiratory rate, move-ment in response to sharp auditory stimuli, sweating, increased intracranial pressure, or decreased mucociliary clearance. Adverse Effects: T T CATTLE: Salivation, ruminal atony, bloat-ing, regurgitation, hypothermia, diarrhea, bradycardia, premature parturition, & ataxia. Yohimbine, atipamezole, & tolazoline may be used alone T T or in combination to reverse effects or speed recovery times Dosages between species can be very different; be cer-T T tain of product concentration when drawing up into sy-ringe, especially if treating ruminants Drug Interactions T T | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
936 xy Lazine Hc L uses/indications Xylazine is approved for use in dogs, cats, horses, deer, and elk. It is indicated in dogs, cats, and horses to produce a state of sedation with a shorter period of analgesia, and as a preanesthetic before lo-cal or general anesthesia. Because of the emetic action of xylazine in cats, it is occasionally used to induce vomiting after ingesting toxins. Pharmacology/actions A potent alpha 2-adrenergic agonist, xylazine is classified as a seda-tive/analgesic with muscle relaxant properties. Although xylazine possesses several of the same pharmacologic actions as morphine, it does not cause CNS excitation in cats, horses or cattle, but causes sedation and CNS depression. In horses, the visceral analgesia pro-duced has been demonstrated to be superior to that produced by meperidine, butorphanol or pentazocine. Xylazine causes skeletal muscle relaxation through central medi-ated pathways. Emesis is often seen in cats, and occasionally in dogs receiving xylazine. While thought to be centrally mediated, neither dopaminergic blockers (e. g., phenothiazines) nor alpha-blockers (yohimbine, tolazoline) block the emetic effect. Xylazine does not cause emesis in horses, cattle, sheep or goats. Xylazine depresses thermoregulatory mechanisms and either hypothermia or hyper-thermia is a possibility depending on ambient air temperatures. Effects on the cardiovascular system include an initial increase in total peripheral resistance with increased blood pressure fol-lowed by a longer period of lowered blood pressures (below base-line). A bradycardic effect can be seen with some animals develop-ing a second-degree heart block or other arrhythmias. An overall decrease in cardiac output of up to 30% may be seen. Xylazine has been demonstrated to enhance the arrhythmogenic effects of epi-nephrine in dogs with or without concurrent halothane. Xylazine's effects on respiratory function are usually clinically insignificant, but at high dosages it can cause respiratory depression with decreased tidal volumes and respiratory rates, and an overall decreased minute volume. Brachycephalic dogs and horses with up-per airway disease may develop dyspnea. Xylazine can increase blood glucose secondary to decreased se-rum levels of insulin; in non-diabetic animals, there appears to be little clinical significance associated with this effect. In horses, sedatory signs include a lowering of the head with relaxed facial muscles and drooping of the lower lip. The retractor muscle is relaxed in male horses, but unlike acepromazine, no re-ports of permanent penile paralysis have been reported. Although, the animal may appear to be thoroughly sedated, auditory stimuli may provoke arousal with kicking and avoidance responses. With regard to the sensitivity of species to xylazine, definite dif-ferences are seen. Ruminants are extremely sensitive to xylazine when compared with horses, dogs, or cats. Ruminants generally require approximately 1/10th the dosage that is required for hors-es to exhibit the same effect. In cattle (and occasionally cats and horses), polyuria is seen following xylazine administration, prob-ably because of decreased production of vasopressin (anti-diuretic hormone, ADH). Bradycardia and hypersalivation are also seen in cattle and diminished by pretreating with atropine. Because swine require 20-30 times the ruminant dose, it is not routinely used. Pharmacokinetics Absorption is rapid following IM injection, but bioavailabilities are incomplete and variable. Bioavailabilities of 40-48% in horses, 17-73% in sheep, and 52-90% in dogs have been reported after IM administration. In horses, the onset of action following IV dosage occurs within 1-2 minutes with a maximum effect 3-10 minutes after injection. The duration of effect is dose dependent but may last for approxi-mately 1. 5 hours. The serum half-life after a single dose of xylazine is approximately 50 minutes in the horse; recovery times generally take from 2-3 hours. In dogs and cats, the onset of action following an IM or SC dose is approximately 10-15 minutes, and 3-5 minutes following an IV dose. The analgesic effects may persist for only 15-30 minutes, but the sedative actions may last for 1-2 hours depending on the dose given. The serum half-live of xylazine in dogs has been reported as averaging 30 minutes. Complete recovery after dosing may take 2-4 hours in dogs and cats. Xylazine is not detected in milk of lactating dairy cattle at 5 and 21 hours post-dose, but the FDA has not approved its use in dairy cattle and no meat or milk withdrawal times have been specified. contraindications/Precautions/Warnings Xylazine is contraindicated in animals receiving epinephrine or having active ventricular arrhythmias. It should be used with ex-treme caution in animals with preexisting cardiac dysfunction, hypotension or shock, respiratory dysfunction, severe hepatic or renal insufficiency, preexisting seizure disorders, or if severely de-bilitated. Because it may induce premature parturition, it should generally not be used in the last trimester of pregnancy, particularly in cattle. Be certain of product concentration when drawing up into sy-ringe, especially if treating ruminants. Do not give to ruminants that are dehydrated, debilitated, or with urinary tract obstruction. It is not approved for any species to be consumed for food purposes. Horses have been known to kick after a stimulatory event (usu-ally auditory); use caution. The addition of opioids (e. g., butorpha-nol) may help temper this effect, but may cause increased risks for hypotension or ileus development. Avoid intra-arterial injection; may cause severe seizures and collapse. The manufacturers warn against using xylazine in conjunction with other tranquilizers. Because this drug may inhibit gastrointestinal motility, use with caution in patients treated for intestinal impactions. Use cautiously in horses during the vasoconstrictive development phase of lamini-tis as xylazine has been shown to reduce digital flow of blood for about 8 hours after administration. adverse effects Emesis is generally seen within 3-5 minutes after xylazine admin-istration in cats and occasionally in dogs. T o prevent aspiration, do not induce further anesthesia until this time has lapsed. Other ad-verse effects listed in the package insert (Gemini®, Butler) for dogs and cats include: muscle tremors, bradycardia with partial A-V block, reduced respiratory rate, movement in response to sharp au-ditory stimuli, and increased urination in cats. Dogs may develop bloat from aerophagia that may require de-compression. Because of gaseous distention of the stomach, xyla-zine's use before radiography can make test interpretation difficult. Adverse effects listed in the package insert (Ana Sed®, Lloyd) for horses include: muscle tremors, bradycardia with partial A-V block, reduced respiratory rate, movement in response to sharp auditory stimuli, and sweating (rarely profuse). Additionally, horses may develop increased intracranial pressure or decreased mucociliary clearance rates when xylazine is used. Adverse reactions reported in cattle include: salivation, rumi-nal atony, bloating and regurgitation, hypothermia, diarrhea, and bradycardia. Hypersalivation and bradycardia may be alleviated by pretreating with atropine. Large animals may become ataxic following dosing and caution should be observed. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
xy Lazine Hc L 937 Reproductive/nursing Safety Limited information was located on the safety of xylazine in preg-nancy; apparently, there are no reports of teratogenicity in animals. Xylazine may induce premature parturition in cattle. Xylazine does not appear to be excreted in detectable quantities in cows' milk. overdosage/acute t oxicity In the event of an accidental overdosage, cardiac arrhythmias, hy-potension, and profound CNS and respiratory depression may oc-cur. Seizures have also been reported after overdoses. There has been much interest in using alpha-blocking agents as antidotes or reversal agents to xylazine. Y ohimbine, atipamezole, and tolazoline have been suggested for use alone and in combination to reverse the effects of xylazine or speed recovery times. Separate mono-graphs for yohimbine and atipamezole are available with suggested doses, etc. T o treat the respiratory depressant effects of xylazine toxicity, mechanical respiratory support with respiratory stimulants (e. g., doxapram) have been recommended for use. Drug interactions The manufacturers warn against using xylazine in conjunction with other tranquilizers. ace PRomazine T! : The combination use of acepromazine with xyla-zine is generally considered safe, but there is potential for addi-tive hypotensive effects and this combination should be used cau-tiously in animals susceptible to hemodynamic complications. cn S De PRe SSant a Gent S, ot He R T! (barbiturates, narcotics, anesthet-ics, phenothiazines, etc. ): May cause additive CNS depression if used with xylazine. Dosages of these agents may need to be reduced. e Pine PHRine T! : The use of epinephrine with or without the concur-rent use of halothane with xylazine may induce the development of ventricular arrhythmias. Re Se RPine T! : A case of a horse developing colic-like clinical signs after reserpine and xylazine has been reported. Until more is known about this potential interaction, use of these two agents together should be avoided. Doses Do GS:T! a) 1. 1 mg/kg IV, 1. 1-2. 2 mg/kg IM or SC (Package Insert; Rompun®—Miles) b) 0. 6 mg/kg IV, IM as a sedative (Morgan 1988) c) T o treat a hypoglycemic crises (with IV dextrose): 1. 1 mg/kg IM (Schall 1985) d) For epidural injection: 0. 02-0. 25 mg/kg; dilute with suffi-cient quantity of sterile saline to a volume of 0. 26 m L/kg. Onset of action 20-30 minutes; 2-5 hour duration. Xylazine 0. 02 mg/kg with morphine 0. 1 mg/kg; dilute with sufficient quantity of sterile saline to a volume of 0. 26 m L/kg. Onset of action 30-60 minutes; 10-20 hour duration. As an analgesic: 0. 1-1 mg/kg IV, IM or SC. For post-opera-tive anxiety: 0. 1-0. 5 mg/kg IV, IM or SC (Carroll 1999) cat S:T! a) 1. 1 mg/kg IV, 1. 1-2. 2 mg/kg IM or SC (Package Insert; Rompun®—Miles) b) As an emetic: 0. 44 mg/kg IM (Morgan 1988), (Riviere 1985) c) As an analgesic: 0. 1-1 mg/kg IV, IM or SC. For post-opera-tive anxiety: 0. 1-0. 5 mg/kg IV, IM or SC (Carroll 1999) d) 0. 55 mg/kg IM (Mandsager 1988)Rabbit S, Ro Dent S, Sma LL mamma LS:T! a) Rabbits: For minimally invasive procedures lasting less than 30-45 minutes: 5 mg/kg once SC or IM in combination with ketamine (35 mg/kg). Mice/Rats: General anesthesia 13 mg/kg once IP in combina-tion with ketamine (87 mg/kg). Hamsters/Guinea pigs: General anesthesia 8-10 mg/kg once IP in combination with ketamine (200 mg/kg for hamsters and 60 mg/kg for Guinea pigs) (Huerkamp 1995) Fe RRet S:T! a) As a sedative/analgesic: Xylazine: 0. 5-2 mg/kg IM or SC. Usually combined with atropine (0. 05 mg/kg) or glycopyrro-late (0. 01 mg/kg IM) or Butorphanol/Xylazine: Butorphanol 0. 2 mg/kg plus Xylazine (2 mg/kg) IM (Finkler 1999) b) Xylazine (2 mg/kg) plus butorphanol (0. 2 mg/kg) IM; T elazol (1. 5 mg/kg) plus xylazine (1. 5 mg/kg) IM; may re-verse xylazine with yohimbine (0. 05 mg/kg IM) T elazol (1. 5 mg/kg) plus xylazine (1. 5 mg/kg) plus butorpha-nol (0. 2 mg/kg) IM; may reverse xylazine with yohimbine (0. 05 mg/kg IM) (Williams 2000) bi RDS:T! a) As a sedative/analgesic: 1-4 mg/kg IM, provides sedation for ketamine anesthesia. Has been used at dosages of up to 10 mg/kg in small psittacines (Clyde and Paul-Murphy 2000) catt Le:T! caution : Cattle are extremely sensitive to xylazine's effects; be cer-tain of dose and dosage form. Pretreatment with atropine can decrease bradycardia and hypersalivation. a) 0. 05-0. 15 mg/kg IV; 0. 10- 0. 33 mg/kg IM. If administering IM use an 18 or 20 gauge needle at least 1. 5 inches long. In-travenous route may stress cardiovascular function. (Thur-mon and Benson 1986) b) 0. 044-0. 11 mg/kg IV; 0. 22 mg/kg IM (Mandsager 1988) c) 0. 1-0. 3 mg/kg IM; 0. 05-0. 15 mg/kg IV; 0. 05-0. 07 mg/kg epidurally. When used IV/IM, analgesia can be very short-lived (1/2 hour). (Walz 2006b) Ho RSe S:T! (note: ARCI UCGFS Class 3 Drug) a) 1. 1 mg/kg IV; 2. 2 mg/kg IM. Allow animal to rest quietly un-til full effect is reached. (Package Insert; Rompun®—Bayer) b) Sedative/analgesic for colic: 0. 2-0. 5 mg/kg IV (will provide analgesia for 20-30 minutes); or 0. 6-1 mg/kg IM (effects for 1-2 hours). Evaluate heart rate prior to therapy. (Moore 1999) c) For sedation/analgesia: Xylazine 0. 5-1 mg/kg IV or IM with or without butorphanol (0. 02-0. 03 mg/kg) (Taylor 1999) d) Prior to guaifenesin/thiobarbiturate anesthesia: 0. 55 mg/kg IV; Prior to ketamine induction: 1. 1 mg/kg IV; In combi-nation with opioid/tranquilizers (all IV doses): 1) Xylazine 0. 66 mg/kg and meperidine 1. 1 mg/kg; 2) Xylazine 1. 1 mg/ kg and butorphanol 0. 01-0. 02 mg/kg; 3) Xylazine 0. 6 mg/ kg; and acepromazine 0. 02 mg/kg. note : The manufacturers state that xylazine should not be used in conjunction with tranquilizers (Thurmon and Benson 1987) e) For field anesthesia: Sedate with xylazine (1 mg/kg IV; 2 mg/kg IM) given 5-10 minutes (longer for IM route) before induction of anesthesia with ketamine (2 mg/kg IV). Horse must be adequately sedated (head to the knees) before giving the ketamine (ketamine can cause muscle rigidity and sei-zures). If adequate sedation does not occur, either: 1) Redose xylazine: up to half the original dose, 2) Add butorphanol (0. 02-. 04 mg/kg IV). Butorphanol can be given with the | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
938 yo Himbine Hc L original xylazine if you suspect that the horse will be difficult to tranquilize (e. g., high-strung Thoroughbreds) or added before the ketamine. This combination will improve induc-tion, increase analgesia and increase recumbency time by about 5-10 minutes. 3) Diazepam (0. 03 mg/kg IV). Mix the diazepam with the ketamine. This combination will improve induction when sedation is marginal, improve muscle re-laxation during anesthesia and prolong anesthesia by about 5-10 minutes. 4) Guaifenesin (5% solution administered IV to effect) can also be used to increase sedation and muscle relaxation. (Mathews 1999) SHee P & Goat S:T! note : Use xylazine with extreme caution in these species. a) 0. 05-0. 1 mg/kg IV; 0. 1-0. 22 mg/kg IM (Thurmon and Ben-son 1986) b) 0. 044-0. 11 mg/kg IV; 0. 22 mg/kg IM (Mandsager 1988) exotic S:T! a) An extensive list of suggested dosages can be found on page 359 of Veterinary Pharmacology and Therapeutics, 6th Ed., Booth, NH and Mc Donald, LE, Eds. 1988; Iowa State Univer-sity Press; Ames, Iowa monitoring Level of anesthesia/analgesia T! Respiratory function; cardiovascular status (rate, rhythm, BP if T! possible) Hydration status if polyuria present T! client information Xylazine should only be used by individuals familiar with its use T! chemistry/Synonyms Xylazine HCl is a alpha 2-adrenergic agonist structurally related to clonidine. The p H of the commercially prepared injections is ap-proximately 5. 5. Dosages and bottle concentrations are expressed in terms of the base. Xylazine HCl may also be known as Bay-Va-1470, Rompun®, Ana Sed®, Sedazine®, X-Ject®, or Xyla-Ject®. Storage/Stability/compatibility Do not store above 30°C (86°F). Xylazine is reportedly physically compatible in the same syringe with several compounds, including: acepromazine, buprenorphine, butorphanol, chloral hydrate, and meperidine. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: Xylazine Injection: 20 mg/m L in 20 m L vials or 100 mg/m L in 50 m L vials: Ana Sed® (Lloyd); X-Ject® (Butler); Xyla-Ject® (Phoenix); Sedazine® (Fort Dodge); Tranqui Ved® (Vedco); generic; (Rx); Ap-proved for use (depending on strength and product) in dogs, cats, horses, deer, and elk. While xylazine is not approved for use in cattle in the USA, at labeled doses in Canada it reportedly has been assigned withdrawal times of 3 days for meat and 48 hours for milk. FARAD has reportedly sug-gested a withdrawal of 7 days for meat and 72 hours for milk for extra-label use. The ARCI (Racing Commissioners International) has designated this drug as a class 3 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: Noneyo Hi Mbine Hcl (yo-him-been) Yobine®, Antagonil® al Pha 2-adrenergic antagoni St Prescriber Highlights Alpha T T 2-adrenergic antagonist used to reverse xylazine & potentially amitraz; may be used prophylactically before amitraz dips Contraindications: Hypersensitivity to it. Caution: Renal T T disease, seizure disorders Adverse Effects: Transient apprehension or CNS excite-T T ment, muscle tremors, salivation, increased respiratory rates, & hyperemic mucous membranes; more likely in small animals Drug interactions T T uses/indications Y ohimbine is indicated to reverse the effects of xylazine in dogs, but it is being used clinically in several other species as well. Y ohimbine may be efficacious in reversing some of the toxic ef-fects associated with other agents (e. g., amitraz) and can be used prophylactically before amitraz dips. Pharmacology/actions Y ohimbine is an alpha 2-adrenergic antagonist that can antagonize the effects of xylazine. Alone, yohimbine increases heart rate, blood pressure, causes CNS stimulation and antidiuresis, and has hyper-insulinemic effects. By blocking central alpha 2-receptors, yohimbine causes sympa-thetic outflow (norepinephrine) to be enhanced. Peripheral alpha 2-receptors are also found in the cardiovascular system, genitourinary system, GI tract, platelets, and adipose tissue. Pharmacokinetics The pharmacokinetics of this drug have been reported in steers, dogs, and horses (Jernigan et al. 1988). The apparent volume of distribution (steady-state) is approximately 5 L/kg in steers, 2-5 L/ kg in horses, and 4. 5 L/kg in dogs. The total body clearance is ap-proximately 70 m L/min/kg in steers, 35 m L/min/kg in horses, and 30 m L/min/kg in dogs. The half-life of the drug is approximately 0. 5-1 hours in steers, 0. 5-1. 5 hours in horses, and 1. 5-2 hours in dogs. Y ohimbine is believed to penetrate the CNS quite readily and, when used to reverse the effects of xylazine, onset of action gener-ally occurs within 3 minutes. The metabolic fate of the drug is not known. contraindications/Precautions/Warnings Y ohimbine is contraindicated in patients hypersensitive to it. In hu-mans, yohimbine is contraindicated in patients with renal disease. Y ohimbine should be used cautiously in patients with seizure disorders. When used to reverse the effects xylazine, normal pain perception may result. adverse effects Y ohimbine may cause transient apprehension or CNS excitement, muscle tremors, salivation, increased respiratory rates, and hyper-emic mucous membranes. Adverse effects appear to be more prob-able in small animals than in large animals. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
za Fi RLuka St 939 Reproductive/nursing Safety Safe use of yohimbine in pregnant animals has not been established. No information on safety during lactation was located. overdosage/acute t oxicity Dogs receiving 0. 55 mg/kg (5 times recommended dose) exhibited clinical signs of transient seizures and muscle tremors. There were 51 exposures to yohimbine reported to the ASPCA Animal Poison Control Center (APCC; www. apcc. aspca. org) dur-ing 2005-2006. In these cases 46 were dogs with 9 showing clinical signs and the remaining 5 cases were cats with 1 showing clinical signs. Common findings in dogs recorded in decreasing frequency included panting, tachycardia, agitation, hypertension and anxiety. Common findings in cats recorded in decreasing frequency includ-ed hyperactivity, tachycardia, tachypnea and tremors. Drug interactions Little information is available, use with caution with other alpha 2-adrenergic antagonists or other drugs that can cause cn S stimulation. The following drug interaction has been reported in humans receiv-ing yohimbine and may be of significance in veterinary patients: t Ricyc Lic anti De PRe SSant S T! : In humans, yohimbine is not rec-ommended for use with antidepressants or other mood-altering agents; hypertension has been reported with tricyclics Doses Do GS:T! For xylazine reversal:a) 0. 11 mg/kg IV slowly (Package insert; Yobine®—Lloyd) b) 0. 1 mg/kg IV (Gross and Tranquilli 1989) c) As an antiemetic: 0. 25-0. 5 mg/kg q12h SC or IM (Washabau and Elie 1995) For reversal or prevention of amitraz effects: a) T o reverse centrally mediated bradycardia and hypotension associated with amitraz ingestion: 0. 1 mg/kg IV; repeat as necessary (Manning 2000) b) In cases of toxicity or to prevent a dog from having an acute episode of toxicity associated with demodicosis treatment: Y ohimbine at 0. 11 mg/kg IV or 0. 25 mg/kg IM with atipam-ezole (50 mcg/kg IM). (T orres 2007b) c) For treatment or prevention of side effects associated with amitraz dips: 0. 1 mg/kg IV; may give prior to, or after bathing to prevent effects. (Hillier 2006g) Rabbit S, Ro Dent S, Sma LL mamma LST! : T o reverse the effects of xylazine and to partially antagonize the effects of ketamine and acepromazine: a) Rabbits: 0. 2 mg/kg IV as needed b) Mice/Rats: 0. 2 mg/kg IP as needed (Huerkamp 1995) bi RDS:T! As a reversal agent for alpha2-adrenergic agonists (e. g., xyla-zine): a) 0. 1 mg/kg IV (Clyde and Paul-Murphy 2000) catt Le:T! For xylazine reversal: a) 0. 125 mg/kg IV (Gross and Tranquilli 1989) Ho RSe S:T! (note: ARCI UCGFS Class 2 Drug) For xylazine reversal: a) 0. 075 mg/kg IV (Gross and Tranquilli 1989) LLama S:T! For xylazine reversal: a) 0. 25 mg/kg IV or IM (Fowler 1989)Dee R:T! For xylazine reversal: a) In wild, exotic and ranched deer: 0. 2-0. 3 mg/kg IV (Package Insert; Antagonil®—Wildlife Labs) note : Y ohimbine has also been used as a reversal agent in several exotic species. Several dosages are listed in the chapter on Stimu-lants by Booth in Veterinary Pharmacology and Therapeutics, 6th Edition. Booth, NH and Mc Donald, LE Eds., Iowa State Uni-versity Press. Ames. 1988 monitoring CNS status (arousal level, etc. )T! Cardiac rate; rhythm (if indicated), blood pressure (if indicated T! and practical) Respiratory rate T! client information This agent should be used with direct professional supervision T! only chemistry/Synonyms A Rauwolfia or indolealkylamine alkaloid, yohimbine HCl has a molecular weight of 390. 9. It is chemically related to reserpine. Y ohimbine may also be known as: aphrodine hydrochloride, chlorhydrate de quebrachine, corynine hydrochloride, Aphrodyne®, Dayto Himbin®, Pluriviron mono®, Prowess Plain®, Urobine®, Virigen®, Yobine®, Yocon®, Yocoral®, Yohimex®, Yohydrol, Yomax®, or Zumba®. Storage/Stability/compatibility Y ohimbine injection should be stored at room temperature (15-30°C) and protected from light and heat. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: Y ohimbine Sterile Solution for Injection: 2 mg/m L in 20 m L vials; Yobine® (Lloyd); (Rx). Approved for use in dogs. Human-Labe Le D PRo Duct S: Oral 5. 4 mg tablets are available, but would unlikely to be of veteri-nary benefit. zafirlu Ka St (zah-fur-luh-kast) Accolate® leukotriene-rece Ptor antagoni St Prescriber Highlights Leukotriene-receptor antagonist used primarily for feline T T asthma; appears to have very limited efficacy Not for treatment of acute bronchospasm T T Well tolerated T T Dose on an empty stomach T T uses/indications While zafirlukast potentially could be useful in treating feline asth-ma, including allowing dose reductions of corticosteroid therapy, its efficacy has been disappointing to this point and most do not recommend its use. Potentially, it could be of benefit in allergy-mediated (where leukotrienes play a role) dermatologic condi- | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
940 zi Do Vu Dine (azt) tions, such as atopy in dogs, but evidence has been that it is not very effective. Pharmacology/actions Zafirlukast selectively and competitively inhibits leukotriene recep-tors, specifically receptors for leukotriene D 4 and E 4 (LTD 4 and LTE4). Additionally, it competes for receptors with some compo-nents of slow-reacting substance of anaphylaxis (SRS-A). These substances have all been implicated in the inflammatory and bron-choconstrictive aspects of bronchial asthma. Pharmacokinetics No specific veterinary data was located. In humans, zafirlukast is rapidly absorbed after oral administration. Food may impair the absorption of the drug, therefore, give on an empty stomach. Peak plasma levels occur about 3 hours after dosing. Zafirlukast is highly bound to plasma proteins (>99%). The drug is extensively metabo-lized; less than 10% of a dose is excreted in the urine, the rest in the feces. Half lives in humans average about 10 hours. contraindications/Precautions/Warnings Zafirlukast is contraindicated in patients hypersensitive to it. Zafirlukast is not indicated for, and is ineffective for treating bronchospasm associated with acute asthma attacks. Patients with significantly decreased hepatic function may have reduced clearances (and increased plasma levels) of zafirlukast. adverse effects Veterinary experience is very limited and no adverse effects have been reported thus far. In humans, the adverse effect profile seems to be minimal; headache was noted most often, but incidence is not much different than placebo. Reproductive/nursing Safety In humans, the FDA categorizes this drug as category B for use dur-ing pregnancy (Animal studies have not yet demonstrated risk to the fetus, but there are no adequate studies in pregnant women; or animal studies have shown an adverse effect, but adequate studies in pregnant women have not demonstrated a risk to the fetus in the first trimester of pregnancy, and there is no evidence of risk in later trimesters. ) Zafirlukast is excreted in milk, but it is probably safe to adminis-ter to nursing veterinary patients. overdosage/acute t oxicity In dogs, doses of up to 500 mg/kg were tolerated without mortality. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving zafirlukast and may be of significance in veterinary patients: a SPi Rin!! : May significantly increase zafirlukast plasma levels e Ryt HRomycin!! : May decrease the bioavailability of zafirlukast t Heo PHy LLine!! : May decrease plasma levels of zafirlukast Wa RF a Rin T! : Zafirlukast may significantly increase the prothrom-bin time of patients taking warfarin. Laboratory considerations None were noted Doses Do GS:T! a) For adjunctive treatment of atopic dermatitis: 20 mg (total dose) PO twice daily; only moderate success (Foil 2003a) cat S:T! a) For adjunctive treatment of feline bronchial asthma: 1-2 mg/kg PO once to twice daily (Noone 1999) monitoring Clinical efficacy T! client information Preferably give on an empty stomach. T! Give this medication even if animal appears well; do not use to T! treat acute asthma clinical signs. Because experience in veterinary medicine is minimal, report any T! untoward effects to the veterinarian. chemistry/Synonyms A leukotriene-receptor antagonist, zafirlukast occurs as a white to pale yellow, fine amorphous powder. It is practically insoluble in water. Zafirlukast may also be known as: ICI-204219, Accolate®, Accoleit®, Aeronix®, Azimax®, Olmoran®, Resma®, Vanticon®, Zafarismal®, Zafirst®, or Zuvair®. Storage/Stability Zafirlukast tablets should be stored at room temperature and protected from light and moisture. The manufacturer states that the tablets should be dispensed only in the original, unopened container. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None The ARCI (Racing Commissioners International) has designated this drug as a class 4 substance. See the appendix for more information. Human-Labe Le D PRo Duct S: Zafirlukast Tablets (film-coated): 10 mg & 20 mg; Accolate® (Astra-Zeneca); (Rx) zidovudine (azt) (zid-o-vew-den) Retrovir® antiretroviral Prescriber Highlights Antiretroviral agent that may be useful for adjunctive T T treatment of Fe LV or FIV in cats Limited experience T T Use with caution if renal, hepatic, or bone marrow dys-T T function present Anemia (non-regenerative) most common adverse effect T T in cats | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
zi Do Vu Dine (azt) 941 uses/indications In veterinary medicine, zidovudine may be useful for treating fe-line immunodeficiency virus (FIV) or feline leukemia virus (Fe LV). While zidovudine can reduce the viral load in infected cats and im-prove clinical signs, it may not alter the natural course of the disease to a great extent. Pharmacology/actions Zidovudine is considered an antiretroviral agent. While its exact mechanism of action is not fully understood, zidovudine is con-verted in vivo to an active metabolite (triphosphate) that interferes with viral RNA-directed DNA polymerase (reverse transcriptase). This causes a virustatic effect in retroviruses. Zidovudine has some activity against gram-negative bacteria and can be cytotoxic as well. Pharmacokinetics Zidovudine is well absorbed after oral administration. In cats, oral bioavailability is approximately 95%. When administered with food, peak levels may be decreased, but total area under the curve may not be affected; peak levels occur about one hour post-dosing in cats. The drug is widely distributed, including into the CSF. It is only marginally bound to plasma proteins. Zidovudine is rapidly metabolized and excreted in the urine. Half-life in cats is about 1. 5 hours. contraindications/Precautions/Warnings Zidovudine is considered contraindicated in patients who have de-veloped life threatening hypersensitivity reactions to it in the past. Use zidovudine with caution in patients with bone marrow, re-nal or hepatic dysfunction. Dosage adjustment may be necessary in cats with renal or hepatic dysfunction. adverse effects In cats, reductions in RBC's, PCV and hemoglobin are the most common adverse effects reported. Anemia may be non-regenerative and is most commonly seen with the higher end of the dosage range (10-15 mg/kg). Diarrhea and weakness have also been reported. While there are many adverse effects reported in humans, granulo-cytopenia and GI effects appear to be the most likely to occur. Reproductive/nursing Safety In humans, the FDA categorizes this drug as category C for use dur-ing pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) Zidovudine is excreted in milk. Clinical significance is not clear for nursing offspring. overdosage/acute t oxicity Human adults and children have survived oral overdoses of up to 50 g without permanent sequelae. Vomiting and transient hemato-logic effects are the most consistent adverse effects reported with overdoses. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving zidovudine and may be of significance in veterinary patients: anti Fun Ga LS, azo Le T! (ketoconazole, etc. ): May increase zidovudine levels ato Vaquone T! : May increase zidovudine levels Doxo Rubicin T! : May antagonize each other's effects; avoid use togetherinte RFe Ron a LFa T! : Increased risk for hematologic and hepato-toxicity PRobeneci DT! : May increase zidovudine levels mye Lo-/cytotoxic DRu GS T! (e. g., chloramphenicol, doxorubicin, flucy-tosine, vincristine, vinblastine ): Administered with zidovudine may increase the risk of hematologic toxicity Ri Fam Pin T! : May decrease blood levels (AUC) of zidovudine Laboratory considerations None were noted. T! Doses cat S:T! For adjunctive therapy of Fe LV and FIV: a) For FELV: 5 mg/kg PO or SC q12h. If giving SC dilute in sterile normal saline to prevent local irritation. Check CBC weekly the first month as anemia (non-regenerative) can be seen. If values are stable; may monitor monthly. Some cats develop mild decreases in hematocrit that resolves even if treatment is continued. (Hartmannn 2007) b) 5 mg/kg PO three times daily for five weeks, then a 4-week rest interval (Gomez, Gisbert et al. 2002) c) For FIV encephalopathy: 20 mg/kg PO q12h (Taylor 2003b) monitoring CBC; PCV. If PCV drops below 20% stop drug for a few days and T! then resume at a lower dosage (Levy 2000) CD4/CD8 rates, if possible T! Clinical efficacy T! client information Must be considered “experimental” therapy for cats T! Must be administered as prescribed for efficacy T! Regular blood tests required T! chemistry/Synonyms A thymidine analog, zidovudine is synthetically produced and occurs as a white to beige-colored, odorless, crystalline solid. Approximately 20 mg are soluble in one m L of water. Zidovudine may also be known as: ZDV, azidodeoxythymi-dine, 3'-azido-2',3'-dideoxythymidine, azidothymidine, AZT, BW-A509U, BW-509U, compound-S, zidovudinum or Retrovir ®; many other trade names are available. Storage/Stability Zidovudine oral tablets or capsules should be stored at room tem-perature. Protect from heat, light and moisture. The oral solution should be stored at room temperature. Zidovudine injection (for IV infusion) should be store at room temperature and protected from light. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Zidovudine Tablets: 300 mg; Retrovir® (Glaxo Smith Kline); generic; (Rx) Zidovudine Capsules: 100 mg; Retrovir® (Glaxo Smith Kline); (Rx)Zidovudine Oral Syrup/Solution: 10 mg/m L in 240 m L; generic (Au-robindo); (Rx) Zidovudine Injection: 10 mg/m L in 20 m L single-use vials; Retrovir® (Glaxo Smith Kline); (Rx) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
942 zinc zinc acetate zinc Sulfatezinc gluconate (zink) nutritional; trace element Prescriber Highlights Metal nutritional agent that may be used for zinc de-T T ficiency, to reduce copper toxicity in susceptible dog breeds (Bedlington Terriers, West Highland White Terri-ers) with hepatic copper toxicosis, & treat hepatic fibrosis in dogs. Has astringent & antiseptic activity topically. Contraindications: None; consider obtaining zinc & cop-T T per levels before treating. Adverse Effects: Large doses may cause GI disturbances T T or hematologic abnormalities (usually hemolysis), par-ticularly if a coexistent copper deficiency exists Zinc overdoses (T T e. g., U. S. Pennies) can be serious uses/indications Zinc sulfate is used systemically as a nutritional supplement in a variety of species. Oral zinc acetate has been shown to reduce cop-per toxicity in susceptible dog breeds (Bedlington T erriers, West Highland White T erriers) with hepatic copper toxicosis. Zinc ther-apy may also be of benefit in the treatment of hepatic fibrosis in the dog. Zinc sulfate is used topically as an astringent and as a weak antiseptic both for dermatologic and ophthalmic conditions. Pharmacology/actions Zinc is a necessary nutritional supplement; it is required by over 200 metalloenzymes for proper function. Enzyme systems that require zinc include alkaline phosphatase, alcohol dehydrogenase, carbonic anhydrase, and RNA polymerase. Zinc is also necessary to main-tain structural integrity of cell membranes and nucleic acids. Zinc dependent physiological processes include sexual maturation and reproduction, cell growth and division, vision, night vision, wound healing, immune response, and taste acuity. When administered orally, large doses of zinc can inhibit the ab-sorption of copper. Pharmacokinetics About 20-30% of dietary zinc is absorbed, principally from the duodenum and ileum. Bioavailability is dependent upon the food in which it is present. Phytates can chelate zinc and form insoluble complexes in an alkaline p H. Zinc is stored mostly in red and white blood cells, but is also found in the muscle, skin, bone, retina, pan-creas, liver, kidney, and prostate. Elimination is primarily via the feces, but some is also excreted by the kidneys and in sweat. Zinc found in feces may be reabsorbed in the colon. contraindications/Precautions/Warnings Zinc supplementation should be carefully considered before ad-ministering to patients with copper deficiency. adverse effects Large doses may cause GI disturbances. Hematologic abnormali-ties (usually hemolysis) may occur with large doses or serum levels greater than 1000 mcg/d L, particularly if a coexistent copper defi-ciency exists. Zinc acetate or methionine may be less irritating to the stomach. Mixing the contents of the capsule with a small amount of tuna or hamburger may minimize vomiting. Reproductive/nursing Safety Although zinc deficiency during pregnancy has been associated with adverse perinatal outcomes, other studies report no such oc-currences. In humans, since zinc deficiency is very rare, the routine use of zinc supplementation during pregnancy is not recommend-ed. In humans, the FDA categorizes this drug as category C for use during pregnancy (Animal studies have shown an adverse effect on the fetus, but there are no adequate studies in humans; or there are no animal reproduction studies and no adequate studies in humans. ) overdosage/acute t oxicity Signs associated with overdoses of zinc include hemolytic ane-mia, hypotension, jaundice, vomiting, and pulmonary edema. Suggestions for treatment of overdoses of oral zinc include remov-ing the source, dilution with milk or water, and chelation therapy using edetate calcium disodium (Calcium EDTA). Refer to that monograph for possible doses and usage information. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving zinc and may be of sig-nificance in veterinary patients: co PPe RT! : Large doses of zinc can inhibit copper absorption in the intestine; if this interaction is not desired, separate copper and zinc supplements by at least two hours FLuo Roquino Lone S T! (e. g., enrofloxacin, ciprofloxacin ): Zinc salts may reduce the oral absorption of some fluoroquinolones Penici LLamine T! : May potentially inhibit zinc absorption; clinical significance is not clear tet Racyc Line ST! : Zinc salts may chelate oral tetracycline and re-duce its absorption; separate doses by at least two hours u RSo Dio LT! : May potentially inhibit zinc absorption; clinical sig-nificance is not clear Doses Do GS:T! For adjunctive treatment and prophylaxis of hepatic copper toxicosis:a) Initially, give a loading dose of 100 mg elemental zinc (zinc acetate used in this study) twice daily (separate doses by at least 8 hours) for about 3 months; then reduce dose to 50 mg (elemental zinc) twice daily. If animal vomits, give doses with a small piece of meat. Do not give within one hour of a meal. Monitoring of zinc levels every 2-3 months initially is recommended. Target zinc levels are 200-500 micrograms/ dl. Do not allow levels to increase higher than 1000 micro-grams/dl. May require 3-6 months of therapy before signifi-cant efficacy is noted. (Brewer, Dick et al. 1992) b) 5-10 mg/kg elemental zinc q12h; use high end of dosage range initially for 3 months, then 50 mg PO q12h for main-tenance. Separate dosage from meals by 1-2 hours. Zinc ace-tate or methionine may be less irritating to the GI than other salts. Mixing the contents of the capsule with a small amount of tuna or hamburger may also minimize vomiting. In dogs with active copper-induced hepatitis, do not use zinc alone, but in combination with a chelator (e. g., D-penicillamine, trientine). Target zinc plasma levels >200 micrograms/dl but <400 micrograms/dl. Monitor levels every 2-3 months and adjust dosage as necessary. (Johnson 2000) c) 10 mg/kg elemental zinc (given as zinc acetate or zinc glucon- | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
zoni Sami De 943 ate) PO twice daily. Give one hour before each meal. (Rothu-izen 2003) d) 1. 5-2. 5 mg/kg zinc gluconate PO three times daily; 0. 67 mg/kg zinc sulfate PO three times daily; or 100 mg (total dose) elemental zinc (as zinc acetate) PO twice daily. Goal is to achieve zinc plasma concentrations of 200-600 mcg/ dl. After a 3-6 month loading period, dose is decreased to approximately half the original dose. Serum zinc concentra-tions are measured every 4-6 months. If serum level drops below 150 mcg/dl, increase dose to original level. If vomiting a problem, may mix dosage with a tablespoonful of tuna fish (in oil). (Richter 2002) For hepatic fibrosis: a) 200 mg of elemental zinc PO once daily for a 10-25 kg dog. Keep zinc plasma levels between 200-300 mcg/dl. (Rutgers 2000) For zinc-related dermatoses:a) Rapidly growing dogs: 10 mg/kg, day PO of zinc sulfate (Wil-lemse 1992) b) For zinc-responsive dermatoses found in Siberian huskies, Alaskan malamutes, Great Danes, and Doberman pinschers: Zinc sulfate: 10 mg/kg PO with food either once daily or di-vided q12h. Alternatively, zinc methionine: 2 mg/kg PO once daily. Correct any dietary imbalances (high calcium and phytate). Lifetime therapy usually required. If vomiting oc-curs, lower dose or give with food. For syndrome seen in puppies: Dietary corrections alone usually resolve the syndrome, but zinc supplementation as above, can expedite process. Some puppies require supple-mentation until maturity. (Kwochka 1994) As an appetite stimulant: a) 1 mg/kg of elemental zinc PO once a day (Bartges 2003b) cat S:T! For adjunctive therapy of severe hepatic lipidosis: a) 7-10 mg/kg PO once daily, in B-Complex mixture if pos-sible (Center 1994) As an appetite stimulant: a) 1 mg/kg of elemental zinc PO once a day (Bartges 2003b) monitoring; client information See information in individual doses above T! client information Although it is best to give oral zinc acetate on an empty stomach, T! if vomiting occurs mix with hamburger or tuna fish to decrease this side effect chemistry/Synonyms Zinc acetate occurs as white crystals or granules. It has a faint acet-ous odor and effloresces slightly. One gram is soluble in 2. 5 m L of water or 30 m L of alcohol. Zinc acetate contains 30% elemental zinc (100 mg zinc acetate = 30 mg elemental zinc). Zinc sulfate occurs as a colorless granular powder, small needles, or transparent prisms. It is odorless but has an astringent metal-lic taste. 1. 67 grams are soluble in one m L of water. Zinc sulfate is insoluble in alcohol and contains 23% zinc by weight (100 mg zinc sulfate = 23 mg elemental zinc). Zinc gluconate occurs as white or practically white powder or granules. It is soluble in water; very slightly soluble in alcohol. Zinc gluconate contains 14. 3% zinc (100 mg zinc gluconate = 14. 3 mg elemental zinc). Zinc acetate may also be known as: E650, or zinci acetas dihydricus. Zinc sulfate may also be known as: zinc sulphate; zinci sulfas, zincum sulfuricum; many trade names are available. Storage/Stability Store zinc acetate crystals in tight containers. Unless otherwise rec-ommended by the manufacturer, store zinc sulfate products in tight containers at room temperature. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None as single-ingredient products for systemic use; several vitamin/ mineral supplements contain zinc, however. Human-Labe Le D PRo Duct S: Zinc Acetate is available from chemical supply houses. An oral or-phan medication Galzin® is available. Zinc Injection: 1 mg/m L (as sulfate; as 4. 39 mg heptahydrate or 2. 46 mg anhydrous) in 10 m L and 30 m L vials; 5 mg/m L (as 21. 95 mg sul-fate) in 5 m L and 10 m L vials; 1 mg/m L (as 2. 09 mg chloride) in 10 m L vials; Zinca-Pak® (Smith and Nephew Solo Pak); generic; (Rx) Zinc Sulfate Tablets: 66 mg (15 mg zinc), 110 mg (25 mg zinc) & 200 mg (45 mg zinc); Zinc 15® and Orazinc® (Mericon); generic; (OTC) Zinc Sulfate Capsules: 220 mg (50 mg zinc); Orazinc® (Mericon); Ve-razinc® (Forest); Zinc-220® (Alto); Zincate® (Paddock); generic; (Rx or OTC depending on product)Zinc sulfate is also available in topical ophthalmic preparations. Zolazepam-see Tiletamine HCl/Zolazepam HCl zoni Sa Mide (zoh-niss-a-mide) Zonegran® anticonvul Sant Prescriber Highlights Antiseizure medication that may be useful as an “add-T T on” drug for refractory epilepsy Half-life of 15 hours makes twice daily dosing possible T T Adverse effect profile not fully elucidated for dogs; seda-T T tion, ataxia, & inappetence have been reported Known teratogen in dogs T T Contraindicated in patients hypersensitive to sulfon-T T amides Expense may be an issue T T uses/indications Zonisamide may be useful as an “add-on” drug for refractory epi-lepsy in dogs. Pharmacology/actions The exact mechanism of action for zonisamide is not known. It may produce its antiseizure activity by blocking sodium channels and reducing transient inward currents, thereby stabilizing neu-ronal membranes and suppressing neuronal hypersynchronization. It does not appear to potentiate GABA. Zonisamide has weak car-bonic anhydrase inhibitory activity. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
944 zoni Sami De Pharmacokinetics In dogs, zonisamide is well absorbed after oral administration and has low protein binding. The elimination half-life in dogs is about 15 hours. Most of the drug is excreted via the kidneys into the urine, but about 20% is metabolized, primarily in the liver. contraindications/Precautions/Warnings Zonisamide is contraindicated in patients hypersensitive to it or to any of the sulfonamide drugs. adverse effects Because there has been limited use of this drug in veterinary pa-tients the adverse effect profile is not fully known. Adverse ef-fects that have been reported in dogs include sedation, ataxia, and inappetence. In humans, the most common adverse effects associated with zonisamide include anorexia, nausea, dizziness, somnolence, agita-tion and headache. Rarely, serious dermatologic reactions (Stevens-Johnson syndrome, TEN), blood dyscrasias, oligohidrosis, and hy-perthermia have been reported in humans. Reproductive/nursing Safety When zonisamide was administered to pregnant dogs at 10 or 30 mg/kg/day (approximate therapeutic dosages in dogs), ventricu-lar septal defects, cardiomegaly and various valvular and arterial anomalies were seen at the higher dose. A plasma level of 25 mcg/m L was the threshold level for malformation. If this drug is to be used in pregnant dogs, the owner must accept the significant risks associated with its use. It is not known if zonisamide enters maternal milk; use with caution in nursing animals. overdosage/acute t oxicity The LD50 of zonisamide in dogs is reportedly 1 g/kg. In human overdoses, effects reported include coma, bradycardia, hypoten-sion, and respiratory depression. Treatment recommendations in-clude GI evacuation, if ingestion was recent, and supportive thera-py. Because of the drug's long half-life, support may be required for several days. Drug interactions The following drug interactions have either been reported or are theoretical in humans or animals receiving zonisamide and may be of significance in veterinary patients: PHenoba Rbita LT! : While there is concern that drugs that induce liv-er enzymes (e. g., phenobarbital) can increase the metabolism and clearance of zonisamide, it is not known if this significantly alters the pharmacokinetics of zonisamide in dogs. Since most dogs subsequently receiving zonisamide have been on phenobarbital chronically and only about 20% of a dose of drug is biotrans-formed, it may not be significant. Laboratory considerations No specific laboratory interactions or considerations were noted T! While plasma concentrations of zonisamide are not routinely T! monitored in human patients, in dogs, the therapeutic range has been suggested to be from 10-40 mcg/m LDoses Do GS:T! a) For refractory epilepsy: 10 mg/kg q12h PO twice daily (Dew-ey, Guiliano et al. 2003) b) As a secondary anticonvulsant for refractory epilepsy: 8-12 mg/kg PO q8h (Inzana 2004) c) 8-12 mg/kg PO q8-12h (Knipe 2006a) d) Initial dose: 5-10 mg/kg PO q12h; gradual adaptation in dosing is recommended. Reduce phenobarbital doses by 25% at the time of starting zonisamide. (Podell 2006a) monitoring Efficacy T! Adverse effects T! client information Clients must understand that the clinical use of this agent is T! relatively “investigational” in veterinary patients, that it must be dosed often in dogs and, also, the potential costs Caution clients not to stop therapy abruptly or “rebound” sei-T! zures may occur Have clients maintain a seizure diary to help determine efficacy T! chemistry/Synonyms A sulfonamide unrelated to other antiseizure drugs, zonisamide oc-curs as a white powder with a p Ka of 10. 2. It is moderately soluble in water (0. 8 mg/m L). Zonisamide may also be known as: AD-810, CI-912, PD-110843, Excegran®, or Zonegran®. Storage/Stability Zonisamide capsules should be stored at 25°C (76°F); excursions permitted to 15-30°C (59-86°F). Store in a dry place and protect-ed from light. Dosage Forms/Regulatory Status Vete Rina R y-Labe Le D PRo Duct S: None Human-Labe Le D PRo Duct S: Zonisamide Capsules: 25 mg, 50 mg & 100 mg; Zonegran® (Eisai); generic; (Rx) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
The following section lists the majority of veterinary-labeled oph-thalmic topical products and some of the more commonly used human-labeled products in veterinary medicine; written by Gigi Davidson, Dip ICVP w ith input from Michael Davidson, DVM, Dip ACVO. Drugs are listed by therapeutic class. For additional information, an excellent review on veterinary ophthalmic pharmacology and therapeutics can be found in both of the following textbooks: Slatter's Fundamentals of Veterinary Ophthalmology, 4th. Edition. David Maggs, Paul Miller, Ron Ofri, Editors, Elsevier, 2007, 496 pages, and Veterinary Ophthalmology, 4th Edition; Kirk N Gelatt, Editor; Lippincott Williams & Wilkins, Media, Pennsylvania, 2007. 1568 pp. Routes of Administration for Ophthalmic Drugs The route of administration selected to delivery therapy for an ocu-lar condition is critical to successful therapy. The following table lists advantages and disadvantages of each route of administration for ocular medications. 945Appendix Ophthalmic Products, Topical Route Tissues Reached Dosage Forms Advantages Disadvantages Comments Topical Conjunctiva; Cornea; Anterior uvea; Lids Solutions Suspensions Easier administration for small animals; minimal interference with vision; lower incidence of contact dermatitis; less toxic to interior of eye if penetrating wound More difficult to administer to horses; less contact time with eye; requires more frequent application than ointment; diluted by tearing; generally more expensive than ointment; more systemic absorption Doses >1 drop rarely indicated (maximum tear capacity is 10 - 20µl, volume of a drop is 25 - 50µl); allow 5 min utes between drops; instill in order of least viscous to most; instill in order of aqueous prior to oil base Ointments Longer contact time; less frequent administration; protect cornea from drying; not diluted by tearing; generally less expensive than solutions/ suspensions Contribute to volume of ocular discharge; temporary blurring of vision; more difficult for client administration; more contact dermatitis; should not be applied to penetrating corneal wounds as oils will cause a granulomatous uveitis; difficult to determine exact dose; metal tubes often fatigue and split before all medication is used Owners should be counseled to avoid contact of application tube with eye; observe patient for short while after application due to temporarily blurred vision Subconjunctival injection Cornea;Anterior uvea Sterile solutions and suspensions Longer duration of action; higher anterior chamber concentrations than topical; Limited number of injections can be performed; may create scar tissue; cannot be removed once applied; temporary pain; drug vehicle residues Indicated for poorly compliant owners, uncooperative patients; indicated for drugs with poor corneal penetration Retrobulbar injection Posterior segment; Optic nerve Sterile solutions and suspensions Primarily used for local anesthetic prior to enucleation of the eye Intracameral injection Anterior chamber; Posterior segment Sterile solutions and suspensions Allows very high drug concentrations for intraocular infections Risk of hemorrhage, retinal detachment, cataract formation, and retinal degeneration Rarely used except for severe intraocular infections or for administration of t PA to dissolve fibrin clots in the anterior chamber Systemic Drugs Lids; Posterior segment; Optic nerve; Anterior uvea (occasion-ally)Oral Intramuscular Subcutaneous Intravenous Allows drug penetration to areas where topical therapy will not reach Systemic toxicity; Does not reach cornea; expense directly proportional to body weight in most cases See monographs for use of systemic agents. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Diagnostic Agents Note: A logical sequence of diagnostic tests must be used to perform ocular examination based on the special needs of each diagnostic agent and test. For example, evaluation of the tear film is performed with the Schirmer T ear T est and must be done before the eye is ma-nipulated or any drug agents are instilled in order to provide a true picture of tear production. Likewise, cultures of the external ocular structures must be done prior to extensive cleaning or administra-tion of any drugs that may alter bacterial culture. The use of mydri-atics is essential to examination of the interior elements of the eye, but must not be given prior to measuring intraocular pressure as these agents will likely affect aqueous humor outflow. Intraocular pressure determination requires topical anesthetic, but must quick-ly be recorded prior to excessive manipulation of the eye or before the patient becomes anxious and uncooperative. Fluorescein sodium (flure-e-seen) Indications/Pharmacology Fluorescein sodium is a yellow water-soluble dye that fluoresces under a Wood's Lamp, but is plainly visible after binding to cor-neal stroma through an ophthalmic examination light source. It is used most commonly to delineate full thickness loss of corneal epi-thelium indicating the presence of a corneal ulceration. In this in-stance it will stain the corneal stroma. The epithelium is not stained because its outer lipid cell membrane repels the stain. Descemet's membrane will not stain with fluorescein stain and this is used to indicate descemetocele formation, an ocular emergency. Fluorescein stain is applied to the precorneal tear film in dogs and cats and the break-up of this stain with time, as observed through a slit lamp biomicroscope using a cobalt blue light source, is used to determine the tear film break-up time (normal 19 sec-onds), an indicator of tear film quality. Fluorescein stain is applied to the tear film of dogs to determine patency of the nasolacrimal outflow system. The normal wait time is 2 - 5 minutes in dogs and up to 10 minutes in cats. A positive test indicates patency of the system. A negative test is not indicative of disease as the test is negative in a large percentage of normal ani-mals. Fluorescein stain, then, can be added to irrigating solution to flush the nasolacrimal system, making detecting the irrigation solu-tion at the nose more obvious during flushing of the system. Suggested Dosages/Precautions/Adverse Effects Fluorescein stain is applied by dropping a drop of irrigating so-lution onto the sterile strip and then allowing the drop to fall on the eye. The strip should not contact the cornea or it will cause false positive stain retention at the site of contact with the epithelial cells. Fluorescein impregnated paper strips are preferred to fluo-rescein solution to insure sterility. After a few seconds, the excess fluorescein is irrigated from the eye, staining areas of full thickness epithelial loss. For procedures requiring topical anesthesia as well as a disclos-ing agent, benoxinate is added to fluorescein solutions in a ratio of 0. 25% fluorescein to 0. 4% benoxinate. These solutions are useful for removal of foreign bodies or sutures, but are not commonly used in veterinary medicine. Conjunctival or corneal epithelial cells for fluorescent antibody testing should be collected prior to application of fluorescein stain, which can cause a false positive test for several days after applica-tion of the stain. Fluorescein may rarely cause hypersensitivity reactions. T emporary staining of fur and skin may result. Do not use during intraocular surgery. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Sterile strips of paper impregnated with fluorescein sodium are the most commonly used form in veterinary medicine. Solutions (2%) of fluorescein are available, however they are not popular following one study indicating that Pseudomonas is readily grown in such solutions. Injectable products are also available (for ophthalmic an-giography), but are not routinely used in veterinary medicine. Fluorescein Sodium Strips: 0. 6 mg, Ful-Glo® (Barnes Hind); 1 mg, Fluor-I-Strip®-A. T. (W-A); 9 mg, Fluor-I-Strip® (W-A); (all Rx); 1 mg Bio-Glo®, 100 ct or 300 ct (Wilson Ophthalmic,) AK Flor 10% Injection (Akorn) 5 m L ampules Fluorescein Sodium:Benoxinate: Fluress® (Akorn) 0. 25:0. 4% Drops in 5 m L, Flurox® (Hub) 0. 25:0. 4% Drops in 5 m L, Flurate® (Bausch and Lomb) 0. 25:0. 4% Drops in 5 m L. liss Amine Green (lis-ah-meen) Indications/Pharmacology Lissamine green is used for diagnosis of corneal damage and to quantify tear production. These strips work by staining the cornea blue upon instillation, resulting in a “speckling” of the cornea. This speckling marks any corneal ulcerations as well as dry patches from any muco-deficient or damaged corneal cells. A white or blue light may be used on sthe slit lamp during detection. Lissamine green possesses a therapeutic advantage in that it does not sting the eye like Rose Bengal; however, as interpretation of lissamine green results requires broader experience than that of Rose Bengal and fluorescein, fluorescein staining is considered to be a more reliable indicator of corneal damage. Suggested Dosages/Precautions/Adverse Effects Lissamine Green impregnated strips are placed in the conjunctival sac and staining is scored based on 6 areas of staining. Dosage Forms/Regulatory Status VETERINAR y-APPROVED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Lissamine Green Ophthalmic Strips (Imperial Chemical Industries—available through distributors such as Wilson Ophthalmic) 1. 5 mg, 100 individually wrapped strips per box. 946 OPHTHALm IC PRODu CTS | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Phenol red Thre Ad (fee-nol) Indications/Pharmacology Measurement of tear production is an important diagnostic test when deficiency of the lacrimal system is suspected. T ear produc-tion is evaluated qualitatively by assessment of the corneal surface for moistness and luster. T ear production is measured quantitative-ly with either the Schirmer T ear T est or the Phenol Red Thread T est. The Phenol Red Thread (PRT) test is a new, fast and equally ac-curate method to test tear production as compared to the Schirmer T ear T est. The PRT test has a 75mm long yellow-colored thread that is impregnated with phenol red, a p H sensitive indicator. Suggested Dosages/Precautions/Adverse Effects The 3mm indentation at the end of the thread is inserted into the inferior conjunctival sac for 15 seconds. As tears travel up the thread, the alkaline p H of the tears turns the thread red. The PRT requires only 15 seconds for diagnostic results as opposed to 1 minute for the Schirmer T ear T est in dogs. Normal tear production via PRT in cats at 15 seconds is 18. 4 to 27. 7 mm/15 seconds and, in dogs, 29. 7 to 38. 6 mm/15 seconds. Dosage Forms/Regulatory Status VETERINAR y-APPROVED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Phenol Red Thread T est: Zone-Quick Diagnostic Threads®, 100 per box, (Menicon—available through distributors such as Wilson Ophthalmic) Pro PAr Ac Aine hcl (proe-par-a-kane) Indications/Pharmacology Proparacaine is a rapid acting topical anesthetic useful for a variety of ophthalmic procedures including tonometry (intraocular pres-sure measurement), relief of corneal pain to facilitate examination, biopsy/sample collection, and to distinguish between corneal and uveal pain. Proparacaine primarily anesthetizes the cornea; with limited penetration into conjunctiva. Anesthesia is of short dura-tion (5 - 10 minutes). Suggested Doses/Precautions/Adverse Effects Usual dose is 1-2 drops prior to examination or procedure. For prolonged procedures only requiring local anesthesia; may repeat 1 drop doses every 5-10 minutes for 5-7 doses. T opical anesthetics should not be used to treat painful eye dis-ease. Prolonged use may retard wound healing and cause corneal epithelial ulcers. Because the blink reflex may be suppressed, the eye should be protected from external injury during use. Repeated use may lead to rapid development of tolerance. Local allergic-type reactions have been rarely reported in humans. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Proparacaine HCl Solution: 0. 5% in 15 m L bottles; Ophthaine® (Solvay); (Rx). Protect from light. Refrigerate. Hum AN-LAb ELED PRODu CTS: Proparacaine HCl Solution: 0. 5% in 2 & 15 m L bottles; Ophthetic® (Allergan), Alcaine® (Alcon), Ophthaine® (Squibb), AK-Taine® (Akorn), Generic; (Rx). Protect from light. Some products should be refrigerated; check label. rose Ben GAl (rose ben-gall) Indications/Pharmacology Rose bengal is a vital stain and stains dead epithelial cells and mu-cus. Full thickness loss of the corneal epithelium is not necessary (only dead cells need be present) to obtain rose bengal stain uptake. It does not stain epithelial defects and does not pass into intercel-lular spaces. Rose bengal stain is most commonly employed in the detection of the presence of viral keratitis in the cat. Because feline herpes vi-rus tends to infect one cell, moving then to an adjacent cell (causing the so called dendritic tracts in the cornea) without full thickness loss of corneal epithelium initially, rose bengal is an ideal diagnostic agent for this infection. Rose Bengal can also be used to detect dam-aged corneal epithelium on the dorsal cornea in early cases of kera-toconjunctivitis sicca. Rose bengal stain is virucidal although no information is available relative to its use as a therapeutic agent. Suggested Dosages/Precautions/Adverse Effects Rose Bengal is applied as a solution (1-2 drops in conjunctival sac before examination) or from an impregnated strip (saturate tip of strip with sterile irrigating solution; touch bulbar conjunctiva or lower fornix with moistened strip; cause patient to blink several times to distribute the stain). Rose bengal is apparently toxic to the cornea and conjunctiva and should be thoroughly flushed from the eye after use to pre-vent irritation. Hypersensitivity reactions are possible. May stain clothing. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Rose Bengal Solution: 1% in 5 m L dropper bottles (Spectrum); (Rx) Rose Bengal Strips: 1. 3 mg per strip; Rosets® (Akorn), Generic (Barnes-Hind); (Rx) schirmer Te Ar Tes T (shir-mer) Indications/Dosages/Precautions Measurement of tear production is an important diagnostic test when deficiency of the lacrimal system is suspected. T ear produc-tion is evaluated qualitatively by assessment of the corneal surface for moistness and luster. T ear production is measured quantita-OPHTHALm IC PRODu CTS 947 | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
tively by the Schirmer T ear T est or the Phenol Red Thread T est. The Schirmer T ear T est measures the aqueous aspect of tears and is the most commonly used test for measuring tear production. Suggested Dosages/Precautions/Adverse Effects Because of the risk of false readings, the following should be avoid-ed prior to conducting a Schirmer T ear T est: excessive manipula-tion of the eyelids, topical anesthesia, and topical or systemic drugs (e. g., tranquilizers and atropine). The round end of the test paper is bent while still in the envelope and positioned to avoid contamina-tion. The bent end should be positioned in the lacrimal lake at the junction of the lateral and middle thirds of the lower eyelid. Most animals will close the eye during the test but this does not affect results. The Schirmer T ear T est should be left in position for one minute as results are not linear and cannot be extrapolated from shorter test times. Schirmer tear test values are as follows for the fol-lowing species: Dogs: 21. 9 +/-4. 0 mm wetting per minute, Rabbits: 5. 3 +/-2. 9 mm wetting per minute, Cats: 20. 2 +/-4. 5 mm wetting per minute. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Schirmer Tear Test®: 300 individually wrapped strips, (Schering Plough Animal Health) Hum AN-LAb ELED PRODu CTS: Clemente Clarke® Schirmer Tear Test Strips: 50 pair/box, Schirmer Tear Test Strips® (Alcon) Te Tr Ac Aine (tet-ra-kane) Indications/Pharmacology T etracaine is more irritating than proparacaine but is sometimes used in veterinary medicine. It is indicated to produce local anes-thesia of short duration for ophthalmic procedures including mea-surement of intraocular pressure (tonometry), removal of foreign bodies and sutures, and conjunctival and corneal scraping in diag-nosis and gonioscopy. T etracaine is also indicated to produce local anesthesia prior to surgical procedures in humans such as cataract extraction and pterygium excision, usually as an adjunct to locally injected anesthetics. Ophthalmic solutions used for intraocular procedures should be preservative-free. Preservatives may cause damage to the corneal epithelium if a significant quantity of solu-tion enters the eye through the incision. Suggested Dosages/Precautions/Adverse Effects Usual dose is 1-2 drops prior to examination or procedure. The onset of action is about 15 seconds. The duration of action usually extends with repeated applications. T opical anesthetics should not be used to treat painful eye dis-ease. Prolonged use may retard wound healing and cause corneal epithelial ulcers. Because the blink reflex may be suppressed, the eye should be protected from external injury during use. Repeated use may lead to rapid development of tolerance. Local allergic-type reactions have been rarely reported in humans. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: T etracaine Solution 0. 5%: 15 m L; Ak-Taine® (Akorn), Alcaine® (Al-con), Ocu-Caine®, Ophthaine®, Ophthetic®, Spectro-Caine®; (Rx) T etracaine Solution 2%; 15 m L and 30 m L bottles; Pontocaine® (Hospira); (Rx)T etracaine Injection 10 mg/m L; 2 m L ampules; Pontocaine ® (Hos-pira); (Rx) Glaucoma, Topical Agents Note: It is important to review the basic pathophysiology of glau-coma in order to understand drug therapy of this disease. Aqueous humor production results from ciliary body secretion and ultra-filtration of plasma. Carbonic anhydrase is a vital enzyme in the production of aqueous humor. Outflow of aqueous humor flows from the posterior chamber into the anterior chamber and exits at the iridocorneal angle, or exits through the iris, ciliary body, chor-oids, and sclera. The balance of generation and outflow of aque-ous humor maintains the intraocular pressure at between 15 and 25 mm Hg. By definition, glaucoma is an increase in intraocular pressure with resulting visual deficits. Delayed, inadequate or inap-propriate therapy can result in severe pain and irreversible blind-ness as well as a cosmetically unappealing eye. Generally, once acute congestive primary glaucoma (generally breed-related and heredi-tary) is noted in one eye in the dog, it is treated as an emergency using a topical prostaglandin such as latanoprost. Surgery may be considered for lasting control of intraocular pressure. The follow-ing topical drugs are used “in general” as a preventative measure to prevent the occurrence of primary glaucoma in the unaffected eye in canine patients. T opical ocular antihypertensive medica-tions are sometimes employed for pressure control with secondary glaucomas also. Because primary glaucoma in dogs is a progressive disorder, many patients are initially treated with single agents but combinations of drugs are often ultimately necessary to maintain pressure control. Primary glaucoma in the feline species is increasingly being recognized in several forms. Although breed-related glaucoma in Siamese and Persian cat breeds has been noted, many veterinary ophthalmologists feel that domestic short-haired cats are most like-ly affected. One form involving misdirected flow of aqueous humor into the vitreous, secondarily resulting in a forward displacement of the lens-iris diaphragm, has been described in the literature. The forward displacement of the iris has resulted in an average intraoc-ular pressure of 30 mm Hg in most patients. T opical medications have been successful in preventing progressive vision loss in most of these cats. Other forms of feline glaucomas which are presumably genetic are being noted sporadically in clinical practice and most of these cases, in complete contrast with primary glaucoma in the canine, are managed successfully with medications. Pharmacologic agents utilized for medical treatment of glaucoma are noted below categorized by therapeutic class but not by therapeutic priority. 948 OPHTHALm IC PRODu CTS | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
Parasmpathomimetics (miotics) Piloc Ar Pine hcl (pye-loe-kar-peen) Indications/Pharmacology Pilocarpine is a miotic agent that is rarely used in the treatment of canine primary glaucoma. Pilocarpine causes the ciliary body muscle to constrict placing posteriorly directed tension on the base of the iris to mechanically pull open the iridocorneal angle struc-tures. By causing miosis, it may prevent closure of the iridocorneal angle by preventing excess iris tissue from peripherally compromis-ing the outflow of aqueous humor. Pilocarpine has also been used for diagnostic localization of parasympathetic denervation of the iris sphincter caused by lesions or trauma to Cranial Nerve III. The popularity of treatment of KCS with ophthalmic cy-closporine and tacrolimus has been associated with a decline in the use of pilocarpine for this disease; however, pilocarpine is still used orally as the primary treatment of neurogenic keratoconjunctivitis sicca in dogs as this condition does not respond to cyclosporine or tacrolimus. Suggested Dosages/Precautions/Adverse Effects One drop in affected eye(s) 3 times daily. Usually 1% or 2% is most commonly used in veterinary medicine. Pilocarpine can cause local irritation initially. In humans, this irritation reportedly diminishes after 3 days of therapy. It may also cause inflammation of the uveal tract, especially with repeated applications and can cause hyphema. Pilocarpine should not be used in secondary glaucoma cases. With repeated use, pilocarpine may cause systemic effects (vomiting, di-arrhea, and increased salivation). For diagnosis of parasympathetic denervation or other conditions caused by cranial nerve III lesions, a 0. 2% solution of pilocarpine is applied topically. For neurogenic keratoconjunctivitis sicca, a 2% solution of pilocarpine is given orally (in food) at a dose of 2 drops per 20 lbs of body weight twice daily. The dose is increased weekly until signs of toxicity or until control of symptoms is achieved. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Pilocarpine HCl Ophthalmic Solution: 0. 25%, 0. 5%, 1%, 2%, 3%, 4%, and 6% (in addition there are 8% and 10% solutions and a 4% gel is available from Alcon) in 15 m L and 30 m L containers; Isopto Carpine® (Alcon); Ocu-Carpine® (Iomed); Piloptic® (Optopics); Pilostat® (Bausch and Lomb), generic; (Rx) See also the epinephrine monograph for information on epineph-rine/pilocarpine fixed dose combination products. demec Arium Bromide (deh-meh-kar-ee-um) Indications/Pharmacology Demecarium is a potent carbamate inhibitor that may reduce in-traocular pressures for up to 48 hours in canines. Demecarium reversibly inhibits anticholinesterase thereby causing miosis. Demecarium is generally used in preventive management of the contralateral eye in canine patients after the diagnosis of an acute congestive crisis of primary glaucoma in the other eye. It is not used in secondary glaucoma. Demecarium has the advantage of once or twice daily dosing. Suggested Dosages/Precautions/Adverse Effects One drop once or twice daily. Demecarium is contraindicated dur-ing pregnancy. Because of additive effects, demecarium should be used with caution with other cholinesterase inhibitors (e. g., car-bamate/organophosphate antiparasiticides), or succinylcholine. Demecarium may cause local inflammation (alleviated by addition of topical corticosteroids) and systemic adverse effects (vomiting, diarrhea, increased salivation, cardiac effects) are possible, particu-larly with high dosages or in very small dogs. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Formerly available as: Demecarium 0. 125% or 0. 25% in 5 m L drop-per bottles; Humorsol® (Merck); (Rx). Do not freeze and protect from heat. Demecarium must be obtained from a compounding pharmacy. echo Thio Ph ATe iodide (ek-oh-thye-oh-fate eye-oh-dide) Indications/Pharmacology Echothiophate iodide for ophthalmic solution is a long-acting cho-linesterase inhibitor for topical use that enhances the effect of en-dogenously liberated acetylcholine in iris, ciliary muscle, and other parasympathetically innervated structures of the eye. It thereby causes miosis, increase in facility of outflow of aqueous humor, fall in intraocular pressure, and potentiation of accommodation. Echothiophate iodide for ophthalmic solution will depress both plasma and erythrocyte cholinesterase levels in most patients after a few weeks of eye drop therapy. Suggested Doses/Precautions/Adverse Effects One drop twice daily. Echothiophate is contraindicated in the presence of active uveal inflammation, and in most cases of angle-closure glaucoma, due to the possibility of increasing angle block. T emporary or permanent discontinuation of the drug may be re-quired if cardiac irregularities, urinary incontinence, diarrhea, muscle weakness or respiratory difficulties occur. Echothiophate should be avoided in patients with asthma, gastric ulcers, brady-cardia, hypotension, epilepsy or other disorders that may respond adversely to vagotonic effects. Carbamate and organophosphate pesticides should not be used on patients receiving echothiophate. OPHTHALm IC PRODu CTS 949 | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
950 OPHTHALm IC PRODu CTS Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Echothiophate Iodide Solution: 0. 125% in 5 m L; Phospholine Io-dide® (Wyeth); (Rx). Stored under refrigeration. Once reconstitut-ed, may be stored at room temperature for up to 4 weeks. Sympathomimetics APr Aclonidine (a-pra-kloe-ni-deen) Indications/Pharmacology Apraclonidine is an alpha2 adrenergic agonist used to reduce aque-ous humor secretion. Apraclonidine is a relatively selective, alpha-adrenergic agonist and does not have significant membrane stabi-lizing (local anesthetic) activity. The onset of action is within 3-5 hours of a single dose. It apparently is less effective than brimoni-dine in dogs and is very potent, causing vomiting and diarrhea in cats and dogs. Apraclonidine will reduce aqueous production but must be combined with other agents for adequate control. Neither the beta-blockers nor alpha-agonists are as effective as the carbonic anhydrase inhibitors in decreasing aqueous production. Suggested Dosage/Precautions/Adverse Effects 1% solution applied as 1 drop 2-3 times daily. Apraclonidine should be used with caution in the face of hepatic and renal func-tion impairment (since a structurally related medication, clonidine, is partly metabolized in the liver and undergoes a significant in-crease in half life in humans with renal impairment). Ironically, in humans the 0. 5% concentration is more likely to cause cardiovas-cular adverse effects than the 1% solution. In humans the following side effects have been noted: For 0. 5% ophthalmic apraclonidine: Allergic reaction, abnormal coordination, arrhythmia, asthma, blepharitis, blepharoconjunctivitis, conjunctivitis, blurred vision or change in vision, chest pain, contact dermatitis, corneal erosion, corneal infiltrate, foreign body sensation, keratitis, keratopathy, de-pression, dizziness, dyspnea, edema of eye, eyelid, or conjunctiva, eye discharge, facial edema, lid retraction, paresthesia, or periph-eral edema. For 1% ophthalmic apraclonidine: Allergic reaction, arrhythmia, or ocular inflammation or injection. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Apraclonidine 0. 5% Solution: 5 m L & 10 m L; 1% Iopidine® (Al-con); (Rx). Supplied as follows: 0. 1 m L in plastic ophthalmic dis-pensers, packaged two per pouch. These dispensers are enclosed in a foil overwrap as an added barrier to evaporation. Brimonidine (bri-moe-ni-deen) Indications/Pharmacology Brimonidine is an alpha-adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that brimonidine tartrate has a dual mechanism of action by reducing aqueous humor production and by and increasing uveoscleral out-flow. After ocular administration of either a 0. 1% or 0. 2% solution, plasma concentrations peaked within 0. 5 to 2. 5 hours and declined with a systemic half-life of approximately 2 hours. In humans, sys-temic metabolism of brimonidine is extensive. It is metabolized primarily by the liver. Urinary excretion is the major route of elimi-nation of the drug and its metabolites. Approximately 87% of an orally-administered radioactive dose was eliminated within 120 hours, with 74% found in the urine. Suggested Dosages/Precautions/Adverse Effects The usual dosage is 1 drop in the affected eye twice daily. Adverse events in humans include: allergic conjunctivitis, conjunctival hype-remia, and eye pruritus, burning sensation, conjunctival folliculo-sis, hypertension, oral dryness, and visual disturbance. Brimonidine appears to be better tolerated in animals than apraclonidine. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Brimonidine 0. 15% solution: 5 m L, 10 m L, & 15 m L; Alphagan P® (Allergan); various generics as 0. 1% and 0. 2% solutions; (Rx) Brimonidine 0. 2%/Timolol maleate: 0. 5% in 5 m L & 10 m L; Com-bigan® (Allergan); (Rx) beta-Adrenergic Antagonists Be TAxolol (be-tax-oh-lol) Indications/Pharmacology Betaxolol HCl is a specific Beta 1 adrenergic blocking agent which reduces aqueous humor production by decreasing cyclic-AMP synthesis in the ciliary body. This drug is a suitable substitute for timolol and because of its specific Beta 1 activity, might be a first choice Beta blocking agent for patients with concurrent respiratory disease. Either levobunolol HCl or betaxolol HCl would be the first choice Beta blocking agent in a feline patient with glaucoma and asthma, although a topical carbonic anhydrates inhibitor should be considered before a Beta blocking agent in this situation. Betaxolol and the other Beta blockers should be used with caution in patients with cardiac disease. Suggested Dosages/Precautions/Adverse Effects Like timolol maleate, betaxolol HCl is supplied in a 0. 50% and 0. 25% solution. Because in animal patients, minimal pressure re-duction is noted with concentrations below 0. 5% with timolol maleate, many veterinary ophthalmologists only consider use of the 0. 5% betaxolol HCl product. One drop of the 0. 5% betaxolol HCl solution is instilled twice daily alone or in combination with other glaucoma medications. While problems have rarely been noted in veterinary medicine, ophthalmic beta blockers should be used with caution in patients with bronchoconstrictive disease or congestive heart failure, although the selective B1 blocking properties of this particular drug would tend to minimize these risks for patients with pulmonary disease. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 951 Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Betaxolol HCl 0. 5% and 0. 25% Solution: 2. 5, 5, 10, & 15 m L bottles; Betoptic ® & Betoptic-S® (Alcon); (Rx) c Ar Teolol (kar-tee-oh-lole) Indications/Pharmacology Carteolol HCl is a nonspecific beta adrenergic blocking agent and it reduces aqueous humor production by decreasing cyclic-AMP synthesis in the ciliary body. Carteolol is a suitable substitute for timolol maleate or any of the other beta blocking agents although it is rarely used in veterinary medicine. In humans, similar IOP reducing effects have been shown for all members of this class. Substitutes are necessary when one particular product induces topical irritation upon application. As noted above, beta blocking agents seem to be particularly useful in the management of primary glaucoma in cats. Suggested Dosages/Precautions/Adverse Effects One drop twice daily of the 1% solution. While problems have rarely been noted in veterinary medicine, ophthalmic beta blockers should be used with caution in patients with bronchoconstrictive disease or congestive heart failure. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Carteolol HCl 1% Solution: 5, 10 & 15 m L bottles; Ocupress® (Ot-suka America); (Rx) levo Bunolol hcl (lee-voe-byoo-noe-lole) Indications/Pharmacology Levobunolol HCl is a beta1-and beta2-blocking agent similar to timolol and metipranolol above but without the potential for myo-cardial depression or airway constriction noted rarely in veterinary medicine and occasionally in human patients. Levobunolol is used in humans with glaucoma responsive to beta adrenergic blocking agents but who suffer cardiac and respiratory side effects associated with timolol. Levobunolol HCl and then carteolol HCl would be suitable Beta blocking agents for feline patients with glaucoma and asthma, although carbonic anhydrase inhibitors should be used in such cases prior to adding a Beta blocking agent. Suggested Dosages/Precautions/Adverse Effects One drop twice daily of the 0. 5% concentration. Miosis may devel-op in veterinary patients after application of topical beta blocking antiglaucoma medications. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Levobunolol HCl 0. 25% or 0. 5% solution: 5, 10, & 15 m L. Betagan® (Allergan); (Rx) me Ti Pr Anolol (meti-pran-oh-lol) Indications/Pharmacology Metipranolol HCl can be used as a substitute for timolol maleate (see above). Metipranolol is a nonselective beta blocking agent and reduces intraocular pressure minimally in animals by decreasing cyclic-AMP synthesis in the ciliary body. Pilot studies have suggest-ed that metipranolol is as effective as timolol maleate, but is signifi-cantly less expensive then trade name timolol preparations, but not the generically labeled products. Metipranolol has been useful for the management of primary open angle glaucoma in cats. Suggested Dosages/Precautions/Adverse Effects One drop twice daily of the 0. 3% solution. While problems have rarely been noted in veterinary medicine, ophthalmic beta blockers should be used with caution in patients with bronchoconstrictive disease or congestive heart failure. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Metipranolol Solution 0. 3%: 2, 5, & 10 m L; Opti Pranolol® (Bausch & Lomb); (Rx) Timolol m Ale ATe (tye-moe-lole) Indications/Pharmacology Timolol maleate is used primarily to prevent the development of primary glaucoma in the contralateral eye of a dog which has de-veloped primary glaucoma in one eye. It only reduces intraocular pressure 3-10 mm Hg and, therefore is of minimal usefulness in patients requiring treatment of primary acute congestive glaucoma. Timolol's mechanism of action: decreases cyclic-AMP synthesis in non-pigmented ciliary epithelium resulting in decreased aqueous humor production. It may also cause slight miosis in dogs and cats. Timolol maleate is rarely used alone but is combined with dor-zolamide solution (Cosopt®). Caution is advised with use of Beta blocking agents in cats with concurrent asthma. As timolol maleate is now available in generic form, it is the primary Beta blocker agent now used. Suggested Dosages/Precautions/Adverse Effects One drop twice daily of the 0. 5% solution. The 0. 25% concentra-tion has minimal efficacy in animals and is not worth using. While problems have rarely been noted in veterinary medicine, ophthal-mic beta blockers should be used with caution in patients with bronchoconstrictive disease or congestive heart failure. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
952 OPHTHALm IC PRODu CTS Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Timolol Maleate 0. 25% (see dosage above) or 0. 5% Solution: 2. 5, 5, 10, & 15 m L Ocumeter® bottles; Timoptic® (MSD); Istalol® (ISTA Pharmaceuticals); generic; (Rx) Timolol Maleate 0. 5% and Dorzolamide 2% Solution: 5 m L & 10 m L Ocumeter® bottles, Cosopt ® (MSD); (Rx) Carbonic Anhydrase Inhibitors Brinzol Amide hcl (brin-zoh-la-mide) Indications/Pharmacology Brinzolamide is chemically similar to dorzolamide and reduces aqueous humor production by altering H+/Na+ active transport mechanisms associated with aqueous humor production in the cili-ary epithelial cells. It can be used as a substitute for dorzolamide and some patients that exhibit excessive topical irritation following application of dorzolamide drops, tolerate brinzolamide better or vice versa. Cats seem to be particularly sensitive to irritation from topical dorzolamide and often brinzolamide can be used in these patients. Comparative data is available suggesting that brinzol-amide and dorzolamide are equally effective in animal patients. Suggested Dosages/Precautions/Adverse Effects One drop three times daily is the standard treatment frequency, adjusted based on clinical response. May also cause stinging upon application like dorzolamide. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Brinzolamide HCl 1% solution: 2. 5, 5, 10 & 15 m L containers; Azopt ® (Alcon); (Rx) dorzol Amide hcl (dor-zole-a-mide) Indications/Pharmacology Dorzolamide is often used in the contralateral eye of a dog with primary glaucoma to prevent development of bilateral disease. It is also an excellent agent to consider for most secondary glauco-mas in dogs and cats because it has no effect on pupil size. Like the related oral carbonic anhydrase inhibitors (dichlorphenamide or Daranide®, methazolamide or Neptazane®), dorzolamide decreases aqueous humor production by the ciliary body epithelium by alter-ing p H and affecting the H+/Na+ active transport exchange mecha-nism. Oral carbonic anhydrase inhibitors cause numerous systemic side effects such as metabolic acidosis and panting, diarrhea, vomit-ing, anorexia and others, all of which can be avoided with topical carbonic anhydrase inhibitors. Suggested Dosages/Precautions/Adverse Effects One drop three times daily is the standard treatment frequency, adjusted based on clinical response. Dorzolamide may cause sting-ing upon topical application, particularly in cats. Approximately 5-10% of humans will experience irritation with use of topical dorzolamide. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Dorzolamide HCl 2% Solution: 5, 10 & 15 m L; Trusopt® (Merck); (Rx) Timolol Maleate 0. 5% and Dorzolamide 2% Solution: 5 & 10 m L Ocumeter® bottles, Cosopt ® (Merck); (Rx) Prostaglandins (Ophthalmic) l ATAn APros T, Bim ATo Pros T, Tr Avo Pros T (la-ta-noe-prost), (bi-ma-toe-prost), (tra-voe-prost) Indications/Pharmacology Prostaglandin analog drugs reduce intraocular pressure by increas-ing outflow of aqueous humor via the uveoscleral pathway. The major outflow mechanism in animals and people is through the iridocorneal angle, termed the “conventional outflow mechanism”. A species variable alternative pathway directly across the surface of the iris into the iridal venous supply accounts for some outflow in people and animals. The horse apparently has the highest uveo-scleral outflow of the domestic species studied. Latanoprost was the first drug marketed in this class. Prostaglandin analogues are an exiting class of topical medications for patients with glaucoma be-cause they increase the alternative outflow of aqueous which logi-cally would seem superior to reducing production or attempting to increase outflow through a failing conventional outflow system. Latanoprost is marketed for once daily usage in people and clini-cal studies show reduced effectiveness when once daily treatment is exceeded. Despite this report in people, many canines are started on once daily treatment but with the progression of their glauco-ma, further pressure management can be noted with twice daily administration. The canine uveal tract apparently metabolizes la-tanoprost at a rate higher than humans because the IOP reduction is profound, but only for 12-15 hours in most dogs. Latanoprost will provide the greatest amount of pressure reduction in canine primary glaucoma cases compared with any other single oral or topical agent. It is even more effective in combination with topical or oral carbonic anhydrase inhibitors. Latanoprost has been used in veterinary ophthalmology to treat primary and select secondary glaucomas in the dog although clinicians should assess the possibil-ity of profound miosis associated with the use of this medication in their secondary glaucoma cases. Latanoprost has not been found to be useful in the management of glaucoma in cats. 0. 003% bimatoprost (Lumigan®) and 0. 004% travoprost (Travatan®) are similar to latanoprost both in mechanism of ac-tion and clinical indications. Since latanoprost does not seem to be effective for most forms of feline glaucoma, it is not likely bimato-prost or travoprost will prove effective in these cases either. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 953 Suggested Dosages/Precautions/Adverse Effects One drop of latanoprost is applied in the PM initially, but with progression of the glaucoma, twice daily treatment schedules will provide additional reduction in intraocular pressure. Latanoprost may cause topical irritation. Conjunctival hyperemia is commonly noted in patients using this medication. A direct stimulation of iris melanocytes results in excess melanin production in the iris of people using this medication, causing a dark brown color change to the iris. Profound miosis is noted with the use of latanoprost in dogs and cats. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Latanoprost 0. 005% Solution: 2. 5 m L; Xalatan® (Pharmacia & Up-john); (Rx). Store under refrigeration until use; at room temp for 6 weeks after opened. Bimatoprost 0. 03% Solution; Lumigan® (Allergan); (Rx) Travoprost 0. 004% Solution; Travatan® (Alcon); (Rx) miscellaneous Agents For Treatment of Glaucoma e Pine Phrine, To Pic Al (OPHTHALm IC) (ep-i-nef-rin) Indications/Pharmacology Epinephrine (usually in combination with pilocarpine due to epi-nephrine's mydriatic effects) is usually used as a preventative mea-sure to prevent glaucoma in the unaffected eye. Epinephrine acts on both alpha and beta adrenergic receptors, thereby causing con-junctival decongestion, transient mydriasis (less so in cats) and de-creased IOP (intraocular pressure). Decreased IOP is probably due primarily to increased aqueous humor outflow, but decreased aque-ous humor production may occur secondary to vasoconstriction. Suggested Dosages/Precautions/Adverse Effects One drop 2-3 times daily in the unaffected eye. Epinephrine may cause ocular discomfort upon instillation. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Epinephrine (HCl) Solution: 0. 25%, 0. 5%, 1% & 2%: 10 or 15 m L btls; Epifrin® (Allergan), Glaucon® (Alcon); (Rx) Epinephrine (Borate) Solution: 0. 5%, 1% & 2%: 7. 5 m L btls; Eppy/N ® (Pilkington/Barnes-Hind), Epinal® (Alcon); (Rx) Epinephrine Bitartrate 1% in combination with Pilocarpine HCl Solution: 1%, 2%, 3%, 4% or 6%; E-Pilo-1®-2,-3,-4,-6 (Iolab); P1 E1® (Alcon); (Rx)mydriatic-Cycloplegic-Vasoconstrictors cyclo Pen Tol ATe (sye-kloe-pen-toe-late) Indications/Pharmacology Cyclopentolate is an anticholinergic agent that induces relaxation of the sphincter of the iris and the ciliary muscles. When applied topically to the eyes, it causes a rapid, intense cycloplegic and my-driatic effect that is maximal in 15-60 minutes; recovery usually occurs within 24 hours. The cycloplegic and mydriatic effects are slower in onset and longer in duration in animal patients who have darkly pigmented irises. Cyclopentolate is used mainly to produce mydriasis and cycloplegia for diagnostic purposes. Suggested Dosages/Precautions/Adverse Effects 1 drop instilled in the eye(s), followed by a second drop 5 minutes later, if necessary. Drops should be administered 40-50 minutes prior to diagnostic procedure. Cyclopentolate increases intraocular pressure and should not be used in animals with glaucoma. Slight stinging is noted with the higher (1%) concentration of the drug. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Cyclopentolate Solution 0. 5, 1, & 2%: in 2, 5 & 15 m L bottles: AK-Pentolate® (Akorn); Cyclogyl® (Alcon); generic; (Rx) Phenyle Phrine hcl (OPHTHALm IC) (fen-il-ef-rin) Indications/Pharmacology Phenylephrine is a vasoconstrictor used to differentiate conjunc-tival vascular injection (blanches with phenylephrine application) versus deep episcleral injection (blanches incompletely) associated with uveitis, glaucoma, or scleritis. It is also used prior to conjunc-tival surgery to reduce hemorrhage and in combination with at-ropine prior to cataract or other intraocular surgeries that require maximal pupillary dilation. Phenylephrine can be used to confirm the diagnosis of Horner's syndrome. Dilution of 2. 5% phenyleph-rine solution with saline (1:10) produces a 0. 25% solution. Normal eyes will not demonstrate mydriasis in response to this low concen-tration of phenylephrine. Third order Horner's syndrome of greater than two weeks duration is associated with receptor up regulation and therefore a response to 0. 25% phenylephrine is noted. In this way, the diagnosis of Horner's is confirmed and a suggestion as to whether or not the condition is 2nd or 3rd order in nature. In dogs, maximum mydriasis persists for about 2 hours and effects may last for up to 18 hours. Phenylephrine has significant alpha adrenergic effects (vasoconstriction and pupillary dilation) and minimal effects on beta receptors. When used alone, phe-nylephrine is reportedly not efficacious in the cat unless used with other mydriatics. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
954 OPHTHALm IC PRODu CTS Suggested Dosages/Precautions/Adverse Effects For diagnosis and characterization of Horner's syndrome: Apply 0. 25% solution (see above) in both eyes. If there is a response in the miotic eye; 3rd order. If no response in 20-30 minutes, apply 2. 5% solution; if there is a response in both eyes it confirms Horner's and probably is 2nd order. For treatment of Horner's syndrome: Treatment is indicated only if patient experiences visual difficulty because third eyelid is elevated over pupil; then given on an as needed basis with an aver-age duration of effect of 3-6 hours. Prior to cataract or intraocular surgery: 2. 5% or 10% given ev-ery 15 minutes for two hours. Smaller animals (e. g., cats and dogs weighing <5kg) are more susceptible to life-threatening systemic effects on blood pressure and cardiac rhythm and preoperative use of phenylephrine in these animals is generally not recommended. In larger animals, repeated dosing is also associated with cardiovas-cular adverse effects. Local discomfort may occur after instillation and chronic use may lead to inflammation. In some species (cat, rabbit, humans) transient stromal clouding may occur if used when corneal epithe-lium is damaged. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Phenylephrine HCl 0. 12% Solution: 15 m L or 20 m L bottles; ge-neric; (OTC) Phenylephrine HCl 2. 5% Solution: 2, 5 or 15 m L bottles; generic; (Rx) Phenylephrine HCl 10% Solution: 1, 2, 5 or 15 m L bottles; Neo-Synephrine® (Sanofi Winthrop), generic; (Rx) ATro Pine sul FATe (OPHTHALm IC) (a-troe-peen) Indications/Pharmacology Atropine, when used topically on the eye, acts by blocking the cho-linergic receptors of the sphincter muscle of the iris and the ciliary body to cause mydriasis (pupillary dilation) and accommodation paralysis (cycloplegia). Atropine controls pain secondary to corneal and uveal disease; to maximally dilate the pupil prior to intraocular surgery; to dilate the pupil and prevent pupillary block in glaucoma and uveitis. In the dog, atropine causes maximal mydriasis in about 1 hour and it may persist for up to 120 hours. Cats also show a de-layed onset of action and mydriasis may persist for up to 144 hours (dose dependent). Atropine is particularly long acting in horses and may last days to weeks. Atropine may be used in combination with 10% phenylephrine to achieve mydriasis and cycloplegia in cases of anterior uveitis. Atropine may also be used in uveitis to break up synechiae. Suggested Dosages/Precautions/Adverse Effects Ointments or drops are routinely used in dogs. One percent is com-monly used, but 2% solutions may be required in severe cases of uveitis. Ointments are generally used in cats to prevent hypersaliva-tion associated with the bitter taste of this medication. Dosage fre-quencies are variable depending on the condition and its severity. Commonly, atropine is given as one drop 2-3 times a day or every other day until pupillary dilation is achieved and once daily there-after to maintain this response. Atropine may precipitate acute, congestive primary glaucoma in dogs predisposed to primary glaucoma; do not use in primary glau-coma. Repeated topical application prior to surgery can result in systemic atropine toxicosis (mania, hyperthermia, etc. ). Salivation may result in dogs as well as cats (see above) secondary to the bitter taste. Atropine may also decrease tear production in small animals. Reportedly, very frequent treatment with atropine may induce colic in horses secondary to systemic absorption and atropine's va-gal parasympathetic effects. However, clinically this effect is only rarely noted. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Atropine Sulfate Ophthalmic Ointment: 10 mg/gm (1%) in 3. 5 gm tubes; Atrophate® (Schering-Plough); (Rx) Hum AN-LAb ELED PRODu CTS: Atropine Sulfate Ophthalmic Ointment: 5 mg/gm (0. 5%), & 10 mg/ gm (1%) in 3. 5 gm tubes; various trade names & generic; (Rx) Atropine Sulfate Ophthalmic Solution: 0. 5%, 1%, and 2% in unit dose droppers, 2, 5, & 15 m L bottles; various trade names & generic; (Rx) Tro Pic Amide (troe-pik-a-mide) Indications/Pharmacology Tropicamide, like atropine, causes mydriasis and cycloplegia, but has more mydriatic than cycloplegic activity. Tropicamide has a more rapid onset (maximum mydriasis in 15-30 minutes) of ac-tion and a shorter duration of action (pupil returns to normal in 6-12 hours in most animals) than does atropine, thereby making it more useful for funduscopic examinations. In dogs, intraocular pressure is apparently not affected by tropicamide. Tropicamide is also indicated following cataract removal to prevent synechiae for-mation that is associated with post-cataract atropine administra-tion. As the half-life of tropicamide is shorter than that of atropine, this allows iris contraction preventing synechial adhesions. Suggested Dosages/Precautions/Adverse Effects Once or twice application to eye, prior to exam. Following cataract surgery: apply 2-3 times daily to keep pupil constantly changing in size and reduce formation of synechiae associated with prolonged pupillary dilation (atropine). Tropicamide is less effective in pain control (cycloplegia) than atropine. Tropicamide may cause salivation, particularly in cats and may also sting when applied. Tropicamide may precipitate acute conges-tive glaucoma in predisposed patients. Dosage Forms/Regulatory Status VETERINAR y APPROVED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Tropicamide Solution 0. 5% and 1%: 2 m L & 15 m L bottles; Mydri-acyl® (Alcon), Opticyl® (Optopics), Tropicacyl® (Akorn), generic; (Rx) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 955 Anti-inflammatory/Analgesic Ophthalmic Agents mast Cell Stabilizers, Antihistamines, Decongestants cromolyn sodium (OPHTHALm IC) (kroe-moe-lin) Indications/Pharmacology Cromolyn sodium is a mast cell stabilizing agent that blocks re-lease of histamine and slow-reacting substance of anaphylaxis from mast cells following antigen recognition. Similar to lodoxamine tromethamine, cromolyn sodium has no intrinsic vasoconstrictor, antihistaminic, cyclooxygenase inhibition or other anti-inflamma-tory properties. Mast cell stabilizing agents are most useful in ani-mal patients suffering from allergic conjunctivitis. Suggested Dosages/Precautions/Adverse Effects For relief of seasonal allergy, one drop 2-6 times daily. A sting-ing sensation is noted in a low percentage of people using this medication. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Cromolyn Sodium 4% Solution: 2. 5, & 10 m L; Crolom® (Bausch & Lomb); (Rx) lodox Amine Trome Th Amine (loe-dox-a-mide) Indications/Pharmacology Lodoxamine tromethamine is a mast cell stabilizer that inhibits Type I hypersensitivity responses by preventing antigen medi-ated histamine release. Lodoxamine stabilizes mast cells by block-ing calcium influx into the cell upon antigen recognition, thereby blocking histamine release. Lodoxamine has no intrinsic vasocon-strictor, antihistaminic, cyclooxygenase inhibition or other anti-in-flammatory properties. Lodoxamine is used in people for manage-ment of conjunctivitis associated with seasonal allergy and other histamine mediated disorders. In veterinary medicine, lodoxamine tromethamine has been used in horses and small animal patients with presumed allergic conjunctivitis. Suggested Dosages/Precautions/Adverse Effects Prior to surgery: One drop 2-4 times daily. A stinging sensation is noted in a low percentage of people using this medication. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Lodoxamine Tromethamine 0. 1%: 10 m L; Alomide® (Alcon); (Rx)olo PAT Adine hcl (oh-loe-pa-ta-deen) Indications/Pharmacology Olopatadine HCl is a selective H 1 receptor antagonist and inhibitor of histamine release from mast cells. It is marketed for topical use to alleviate symptoms of allergic conjunctivitis in humans and is thought to be safe for use in children three years of age and older. Olopatadine, upon topical application in humans, was shown to have very limited systemic absorption. It was detectable in the milk of nursing rats, after topical application, and like most medications should be avoided in pregnant or nursing animals. Suggested Doses/Precautions/Adverse Effects Olopatadine eye drops are applied as needed in people for tempo-rary relief of itchiness associated with seasonal allergy. They can be used in dogs two to three times daily for allergic conjunctivitis. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Olopatadine HCl ophthalmic solution 0. 1%; Patanol® (Alcon); (Rx) Non-Steroidal Antiinflammatory Agents Brom Fen Ac (brome-fen-ak) Indications/Pharmacology Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) by virtue of its ability to block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. Bromfenac is indicated for treatment of postoperative inflammation in patients who have undergone cata-ract extraction. Suggested Doses/Precautions/Adverse Effects One drop twice daily. Bromfenac is contraindicated in patients with known hypersensitivity to any ingredient in the formulation. Bromfenac ophthalmic solution contains sodium sulfite, a sulfite known to cause allergic reactions especially in asthmatic patients. Caution should be exercised when utilizing bromfenac in patients who have previously exhibited sensitivity to other NSAID drugs as there is potential for cross-sensitivity. There have been reports that ocularly applied NSAIDs may cause increased belled of ocu-lar tissues (including hyphema) in conjunction with ocular surgery due to interference with platelet aggregation. All topical NSAIDs may slow or delay healing. Concomitant use with topical steroidal agents may increase the potential for delayed healing. Use of topical NSAIDs may result in keratitis due to epithelial breakdown, cor-neal thinning, corneal erosion, corneal ulceration or corneal per-foration. Use of bromfenac should be discontinued immediately in patients exhibiting evidence of corneal epithelial breakdown. Post marketing experience with topical NSAIDs suggests that use more than 24 hours prior to surgery or use beyond 14 days after sur-gery may increase patient risk for the occurrence of corneal adverse events. Bromfenac should be used with caution in patients with known bleeding tendencies or who are receiving other medications, which may prolong bleeding time. The most commonly reported adverse experiences reported following use of bromfenac include: | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
956 OPHTHALm IC PRODu CTS abnormal sensations in the eye, conjunctival hyperemia, eye irrita-tion (including burning/stinging), eye pain, eye pruritus, eye red-ness, headache, and iritis. These events were reported in 2-7% of human patients. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Bromfenac 0. 09% solution: 7. 5 m L, 10 m L; Xibrom® (ISTA Pharma-ceuticals) (Rx). Store at room temperature. diclo Fen Ac sodium (OPHTHALm IC) (dye-kloe-fen-ak) Indications/Pharmacology Diclofenac sodium is a phenylacetic acid that inhibits cyclooxyge-nase, inhibiting prostaglandin synthesis. Diclofenac sodium topi-cal solution reduces inflammation following cataract extraction in people and counteracts photophobia in humans having refrac-tive corneal surgery. In veterinary medicine, diclofenac sodium is used for treatment of uveitis following surgery on the eye or other causes of uveitis especially when corneal infection is suspected or in diabetic patients whose insulin regulation could be altered by the systemic uptake of topical corticosteroids. Diclofenac can be com-bined with topical corticosteroids for better control of uveitis in animals when the condition is severe. Suggested Dosages/Precautions/Adverse Effects Prior to surgery: One drop 4 times at 20 minute intervals. One drop four times daily following cataract surgery or for the treatment of uveitis. Caution should be used when applying any anti-inflamma-tory agent on the cornea in the face of corneal stromal infection because of the positive role inflammation plays in the immune re-sponse to microbial invasion of tissue. A stinging sensation is noted in 15% of people using this medication. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Diclofenac Sodium 0. 1% Solution: 2. 5 & 5 m L; Voltaren® (Novar-tis); (Rx) Flur Bi Pro Fen sodium (flure-bi-proe-fen) Indications/Pharmacology Flurbiprofen is a non-steroidal anti-inflammatory agent that prob-ably acts by inhibiting the cyclo-oxygenase enzyme system, thereby reducing the biosynthesis of prostaglandins. Prostaglandins may mediate certain kinds of ocular inflammation. They may disrupt the blood-aqueous humor barrier, cause vasodilation, increase intraoc-ular pressure and leukocytosis, and increase vascular permeability. Prostaglandins may also cause iris sphincter constriction (miosis) independent of cholinergic mechanisms. Flurbiprofen can inhibit this intraocular miosis and may also be useful in the management of uveal inflammation (usually in addition to topical steroids). Suggested Dosages/Precautions/Adverse Effects Prior to surgery: One drop 4 times at 20 minute intervals. Because flurbiprofen may be as immunosuppressive as topical corticosteroids, it should not be used in patients with infected cor-neal ulcers. By blocking prostaglandin synthesis, arachidonic acid metabolites may be shunted into leukotriene pathways and this ef-fect may result in a transient increase in intraocular pressure com-monly noted after intraocular surgery. Postoperative pressure spikes following cataract surgery have been the subject of much study in recent years and a general trend away from the use of flurbiprofen prior to cataract surgery has resulted from these studies. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Flurbiprofen Sodium 0. 03% Solution: 2. 5, 5 & 10 m L btls; Ocufen® (Allergan); generic; (Rx) Ke Torol Ac Trome Th Amine (OPHTHALm IC) (kee-toe-role-ak) Indications/Pharmacology Ketorolac tromethamine is a pyrrolol-pyrrole nonsteroidal an-ti-inflammatory agent that inhibits prostaglandin formation. Prostaglandins mediate inflammation within the eye by disrupting the blood-aqueous barrier, inducing vasodilation and increasing intraocular pressure. Prostaglandins may also cause iris sphinc-ter constriction (miosis) independent of cholinergic mechanisms. Ketorolac tromethamine is marketed for use before cataract extrac-tion in human patients (to prevent miosis during surgery) and for control of post surgical inflammation, especially following cataract surgery. It is also approved for management of conjunctivitis as-sociated with seasonal allergy in people. In veterinary medicine, ketorolac tromethamine is primarily used to control surgical or nonsurgical uveitis particularly in cases with concurrent corneal bacterial infection or ulceration when topical corticosteroids are contraindicated. It is also used in diabetic patients, especially smaller patients, adversely affected by systemic uptake of topically applied corticosteroids. Nonsteroidal agents like ketorolac tromethamine can be combined with topical steroids in patients with severe uveal inflammation. Suggested Dosages/Precautions/Adverse Effects Prior to surgery: One drop 4 times at 20 minute intervals. One drop four times daily following cataract surgery or for the treatment of uveitis or management of allergic conjunctivitis. The manufacturer indicates that ketorolac tromethamine does not enhance the spread of preexisting corneal fungal, viral or bac-terial infections in animal models. Ketorolac tromethamine does not in and of itself induce postoperative pressure elevation other then that which frequently follows cataract extraction in people and animals. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Ketorolac Tromethamine Solution 0. 5%: 3, 5, & 10 m L; Acular® (Allergan); (Rx) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 957 ne PAFen Ac (ne-pa-fen-ak) Indications/Pharmacology Nepafenac is a nonsteroidal anti-inflammatory and analgesic prod-rug. After topical ocular dosing, nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a nonsteroidal anti-inflammatory drug. Amfenac is thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production. Nepafenac is indicated for the treat-ment of pain and inflammation associated with cataract surgery. Suggested Dosages/Precautions/Adverse Effects One drop three times daily. Shake well before use. Nepafenac is contraindicated in patients who have demon-strated hypersensitivity to any of the ingredients in the formulation or to other NSAIDs. Caution should be exercised when utilizing bromfenac in patients who have previously exhibited sensitivity to other NSAID drugs as there is potential for cross-sensitivity. There have been reports that ocularly applied NSAIDs may cause increased bleeding of ocular tissues (including hyphema) in con-junction with ocular surgery due to interference with platelet aggre-gation. All topical NSAIDs may slow or delay healing. Concomitant use with topical steroidal agents may increase the potential for de-layed healing. Use of topical NSAIDs may result in keratitis due to epithelial breakdown, corneal thinning, corneal erosion, corneal ul-ceration or corneal perforation. Use of bromfenac should be discon-tinued immediately in patients exhibiting evidence of corneal epi-thelial breakdown. Post marketing experience with topical NSAIDs suggests that use more than 24 hours prior to surgery or use beyond 14 days after surgery may increase patient risk for the occurrence of corneal adverse events. Bromfenac should be used with caution in patients with known bleeding tendencies or who are receiving other medications, which may prolong bleeding time. In controlled clinical studies, the most frequently reported ocular adverse events following cataract surgery were capsular opacity, decreased visual acuity, foreign body sensation, increased intraocular pressure, and sticky sensation. These events occurred in approximately 5-10% of patients. Other ocular adverse events occurring at an incidence of approximately 1-5% included conjunctival edema, corneal edema, dry eye, lid margin crusting, ocular discomfort, ocular hyperemia, ocular pain, ocular pruritus, photophobia, tearing and vitreous detachment. Some of these events may be the consequence of the cataract surgical procedure. Non-ocular adverse events reported at an incidence of 1-4% included headache, hypertension, nausea/ vomiting, and sinusitis. Nepafenac ophthalmic suspension may be administered in conjunction with other topical ophthalmic medi-cations such as beta-blockers, carbonic anhydrase inhibitors, alpha-agonists, cycloplegics, and mydriatics. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Nepafenac Ophthalmic Suspension: 0. 1% in 3 m L; Nevanac® (Al-con); (Rx). Shake well and store at room temperature. su Pro Fen (su-pro-phen) Indications/Pharmacology Suprofen is a non-steroidal anti-inflammatory agent similar to flurbiprofen. Suprofen and flurbiprofen are phenylalkanoic acids that inhibit the cyclo-oxygenase enzymes responsible for conver-sion of arachadonic acid from cell membranes into various pros-taglandins. These prostaglandins mediate certain aspects of ocular inflammation including disruption of the blood-aqueous barrier, uveal vasodilation, increases in intraocular pressure, and leakage of white blood cells and protein from uveal vessels into the aqueous humor. Prostaglandins cause iris sphincter constriction (miosis) independent of cholinergic mechanisms. Suprofen can inhibit this intraocular miosis and may also be useful in the management of uveal inflammation (usually in addition to topical steroids). Suggested Dosages/Precautions/Adverse Effects Prior to surgery: One drop 4 times at 20 minute intervals. Because suprofen may be as immunosuppressive as topical cor-ticosteroids, it should not be used in patients with bacterial corneal ulcers. By blocking prostaglandin synthesis, arachidonic acid me-tabolites may be shunted into leukotriene pathways and this effect may result in a transient increase in intraocular pressure commonly noted after intraocular surgery. Postoperative pressure spikes fol-lowing cataract surgery have been the subject of much study in re-cent years and a general trend away from the use of suprofen or flur-biprofen prior to cataract surgery has resulted from these studies. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Suprofen Sodium 1% Solution in 2. 5 m L btls; Profenal® (Alcon); (Rx) Steroidal Anti-inflammatory Agents cor Ticos Teroids, To Pic Al (OPHTHALm IC) Prednisolone Ace TATe dex Ame Th Asone lo Te Prednol e TABon ATe (see also Antibiotic & Corticosteroid Combinations) Indications/Dosages/Precautions T opical corticosteroids are used to treat diseases of the eye involving the conjunctiva, sclera, cornea, and anterior chamber. Penetration of topically applied corticosteroids into the eyelids is poor as is penetration to the posterior segment of the eye. Corticosteroid-responsive conditions affecting these areas are usually managed with systemically administered agents (with or without adjunctive topically applied medications). Conjunctivitis in animals is often treated symptomatically, par-ticularly during the first occurrence of the condition for any partic-ular patient. Antibiotic agents with hydrocortisone or dexametha-sone, or antibiotic agents alone initially, are used for conjunctivitis | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
958 OPHTHALm IC PRODu CTS in the dog and the horse. Allergic and eosinophilic conjunctivitis are rare diagnoses in the cat. T opically applied corticosteroids should not be used to treat conjunctivitis in cats. Herpes virus is the most common feline conjunctival pathogen and topically applied steroids can induce prolonged disease, steroid dependency and cor-neal complications including ulcerative keratitis and/or corneal se-questrum formation. Inflammatory conditions of the canine sclera and episclera include episcleritis, scleritis, nodular granulomatous episclero-keratitis, Collie granuloma and others. Potency and penetration of corticosteroid agents is important in the management of these con-ditions. Dexamethasone sodium phosphate ointment is often em-ployed and the relatively reduced penetration of the fibrous ocular tunics of this medication compared with that of 1% prednisolone acetate ophthalmic suspension is made up for by increased contact time of the ointment form of this drug and by the increased po-tency of dexamethasone (30X cortisone) relative to prednisolone (4-5X cortisone). Dexamethasone products alone (without antibi-otics) are becoming increasingly scarce in the marketplace and be-cause of this, dexamethasone is often used in combination with an antibiotic for availability reasons only. Four times daily treatment is often the initial frequency with tapering paralleled to clinical re-sponse. T opical treatment is often used following subconjunctival injection of corticosteroid agents into or adjacent to the lesion (if focal). Systemic steroid treatment is usually not necessary. Non-ulcerative inflammatory conditions of the cornea of ani-mals include chronic superficial keratitis (pannus) of the German Shepherd and other breeds, eosinophilic keratitis of the cat and cer-tain, often poorly understood, keratopathies of the equine, includ-ing Onchocerca related keratitis. German Shepherd pannus may be better managed using cyclosporine ophthalmic solution or oint-ment with or without concurrent topical steroids initially followed by long term management with cyclosporine ophthalmic alone (see cyclosporine ophthalmic). Eosinophilic keratitis is often treated with subconjunctival corticosteroids in addition to topical 0. 1% dexamethasone ophthalmic ointment or solution or 1% predniso-lone acetate ophthalmic suspension 4 times daily, tapering the dos-age frequency based on clinical response. Recent research reveals that eosinophilic keratitis may be an unusual immune response to latent feline herpes virus in the corneal stroma, calling into question the value of topical steroids in the management of a disease with an infectious etiology. Despite new information pertaining to possible causes of eosinophilic keratitis in the cat, the condition continues to be well managed in most cases with infrequent topical corticoster-oid treatment. Non-ulcerative, immune mediated and/or parasitic equine keratopathies are treated with 0. 1% dexamethasone oint-ment 4 times daily with tapering of the treatment frequency based on the clinical response. Corticosteroids are also used to manage anterior uveal inflam-matory disease of companion animals. In small animals, 1% pred-nisolone acetate ophthalmic suspension is generally used for this purpose because of superior penetration into the anterior seg-ment of the eye in comparison with dexamethasone products. The frequency of treatment depends on the severity of the condition. Severe anterior uveitis can be treated with subconjunctival corti-costeroids given in combination with hourly topical corticosteroids with reevaluation performed again 24 hours after beginning treat-ment. Moderate to mild uveitis and that found following surgery of the anterior segment is often treated initially at the QID level with tapering based on clinical response. Anterior uveitis in animals can often be associated with an underlying systemic infectious or neoplastic condition in animals. Clinicians are advised to evaluate the patient for generalized infectious or neoplastic conditions prior to or concurrent with a course of corticosteroid antiinflammatory therapy, particularly if the condition dictates systemic treatment with these agents in combination with subconjunctival and topical treatment. Uveitis has also been successfully treated utilizing sub-conjunctival injections of triamcinolone acetonide. As commer-cially available triamcinolone injections are preserved with benzyl alcohol, veterinary ophthalmologists centrifuge triamcinolone in-jections and remove the alcohol-containing supernatant vehicle. An equal volume of non-preserved sodium chloride injection is then utilized to reconstitute the remaining triamcinolone to provide for an acceptable subconjunctival injection. Uveitis in the equine spe-cies is often treated with either 1% prednisolone acetate ophthalmic suspension or with 0. 1% dexamethasone ointment. Many clini-cians prefer to use the ointment because of increased contact time and potency and the logistics of frequent treatment of this species. 1% prednisolone acetate can be passed through a subpalpebral la-vage catheter very frequently to treat equine patients with anterior uveitis when necessary. Pred Forte®, Econopred Plus® or generic 1% prednisolone ac-etate ophthalmic suspension are the prednisolone products most used by veterinary ophthalmologists. There are few indications for Econopred® or Pred Mild® in veterinary ophthalmology. Inflammatory conditions of the posterior segment require sys-temic treatment because of poor penetration of topically applied agents. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Prednisolone Acetate Drops: 0. 12% Suspension: Pred Mild® (Al-lergan); 0. 125% Suspension: Econopred® (Alcon); 1% Suspension: Econopred Plus® (Alcon); Pred Forte® (Allergan), generic; (Rx) Prednisolone Sodium Phosphate Drops: 0. 125 & 1% Solution; (var-ious); (Rx) Prednisolone (0. 25%) and Atropine (1%) Drops in 5 m L btls; My-drapred® (Alcon); (Rx)Loteprednol Etabonate Ophthalmic Suspension: 0. 2% in 5 m L, 10 m L; Alrex ® (Bausch and Lomb); (Rx). Shake well and store at room temperature. Do not freeze. Also available: Fluorometholone or Medrysone drops Other routes of administration: Systemically administered corti-costeroids (usually orally) may be indicated for non-infectious in-flammatory ocular conditions and following intraocular surgery. Subconjunctival steroids are useful in anterior segment inflamma-tory disease and following cataract surgery and intraocular glauco-ma surgery. Subconjunctival steroids may be absorbed systemically and should be used with caution in patients with endocrinopathies (e. g., diabetes mellitus) or infectious diseases. Even frequent topical steroid application in small animal patients under 20 kg can cause difficulties with diabetes mellitus regulation and after the peak inflammatory response has been suppressed, nonsteroidal antiin-flammatory drugs should be considered for ongoing maintenance treatment. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 959 Ophthalmic Analgesics (Topical) mor Phine sul FATe (To Pic Al) (mor-feen) Indications/Pharmacology A recent study showed that topical use of 1% morphine sulfate so-lution in dogs with corneal ulcers provided analgesia and did not interfere with normal wound healing. Both mu and delta opioid re-ceptors were identified in normal corneas of dogs, although the mu receptors were present only in small numbers. Dogs treated with morphine sulfate 1% topical solution had significantly less blephar-ospasm and lower esthesiometer readings than did control dogs. Morphine sulfate is a Schedule II controlled substance. Suggested Dosages/Precautions/Adverse Effects 1 drop of 1% morphine sulfate solution in the affected eye(s) three times daily. Preserved solutions of morphine should not be used. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None A 1% morphine sulfate ophthalmic solution may be compounded by utilizing the preservative-free morphine 2. 5% injectable solution diluted with sterile saline observing appropriate aseptic technique. n Al Bu Phine (To Pic Al) (nal-byoo-feen) Indications/Pharmacology A review of the literature reveals that solutions of topical nalbu-phine were used clinically to provide analgesia and reduce ophthal-mic pain in humans as early as 1983. Nalbuphine hydrochloride is a potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis. Receptor studies show that nalbuphine hydrochloride binds to mu, kappa, and delta receptors, but not to sigma receptors. Nalbuphine hydrochloride is primar-ily a kappa agonist/partial mu antagonist analgesic. Nalbuphine hydrochloride by itself has potent opioid antagonist activity at doses equal to or lower than its analgesic dose. When administered following or concurrent with mu agonist opioid analgesics (e. g., morphine, oxymorphone, fentanyl), nalbuphine hydrochloride may partially reverse or block opioid-induced activity from the mu agonist analgesic. Nalbuphine hydrochloride may precipitate with-drawal in patients dependent on opioid drugs. Nalbuphine hydro-chloride should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis. Nalbuphine is not commercially available for ophthalmic use, but may be prepared through compounding. Suggested Dosages/Precautions/Adverse Effects One drop two to six times daily as needed for corneal pain. Do not use in conjunction with topical morphine as nalbuphine will re-verse the effects of morphine at the mu receptor. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None. The 10 mg/m L (1%) nalbuphine injection may be applied as an ophthalmic solution. A 1% nalbuphine ophthalmic solution may also be compounded by utilizing nalbuphine 20 mg/m L injectable solution diluted with 1:1 with sterile saline observing appropriate aseptic technique. Antimicrobial Ophthalmic Therapy Antibiotics, Single & Combination Agents Indications/Pharmacology; General use Considerations T opical antibiotic agents are commonly used to treat conjuncti-vitis and ulcerative keratitis complicated by bacterial infection of the corneal stroma. These agents are also used to prevent infection following surgery of the eyelids, conjunctiva, cornea, and the ante-rior segment. Conjunctivitis in animals is a common clinical entity. Because in most instances the condition does not threaten vision, it is often treated symptomatically with antibiotic agents or anti-biotic agents in combination with topical steroids (see antibiotic/corticosteroid combination agents). Conjunctivitis is an exclusion diagnosis in animals, ruling out other causes for ocular discomfort and discharge, including anterior uveitis, glaucoma and inflam-matory disease of the sclera, episclera and cornea. Triple antibiotic products (neomycin, bacitracin and polymyxin B) are often em-ployed for this purpose, with or without hydrocortisone, because these drugs are not used systemically and because the combination of antibiotics is broad spectrum. Triple antibiotic or triple antibi-otic HC is often used in dogs 4 times daily for 1 to 2 weeks for conjunctivitis. Chronic or recurrent cases of conjunctivitis would indicate further diagnostic evaluation to determine an underly-ing cause. Oxytetracycline ophthalmic ointment is often used QID in cats for nonspecific or undiagnosed conjunctivitis; how-ever, anaphylaxis from Polymyxin B in the commercially available product ( Terramycin ®) has been reported. The rationale for topi-cal treatment is the efficacy of tetracycline for Chlamydia spp. and Mycoplasma spp., two infectious agents reported to cause conjunc-tivitis in the cat. Research evidence suggests that cats will not be cleared of Chlamydia spp. organisms dormant in the nasal and GI passages unless treated systemically with doxycycline at 25 mg twice daily by mouth for three weeks. Research evidence also shows that solid dosage forms of doxycycline are likely to become lodged in the esophagus of cats and result in esophageal erosions and subse-quent strictures. Consequently, liquid dosage forms of doxycycline should be used when treating cats. Because cats may carry the or-ganism in a dormant fashion it is recommended to treat all cats in a household when chlamydial conjunctivitis is diagnosed in one or more cats. Antibiotic agents with corticosteroids should not be used for the treatment of conjunctivitis in the cat. The majority of cases are related to primary or recurring infection with feline herpes virus and recent evidence indicates that topical or systemic steroid therapy can potentially prolong the duration of the viral infection and result in corneal complications in cases which other-wise may have remained a conjunctival infection. Veterinary oph-thalmologists are becoming increasingly concerned about sporadic reports of cats developing anaphylactic shock and death following application of triple antibiotic ointment to their eyes. Presumably this rare idiosyncratic reaction results from topical neomycin ir- | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
960 OPHTHALm IC PRODu CTS ritation and massive histamine release. Because of this often fatal anaphylactic reaction, many veterinary ophthalmologists do not use neomycin-containing products in cats. Triple antibiotic with or without hydrocortisone is often used to treat conjunctivitis in the equine species. Antibiotic therapy for corneal disease varies from prophylactic therapy to prevent infection to treatment of established corneal in-fections. Following an acute superficial injury to the cornea in the dog or horse, treatment with triple antibiotic ointment or drops 4 times daily is usually sufficient to prevent bacterial infection of the corneal stroma. Because of the potential for anaphylactic reactions in cats, gentamicin has become the first choice antibiotic for pre-venting microbial infection following injury or surgery in the feline species. Reevaluation of the patient 24-48 hours after the injury is indicated. Progressive edema, pain, and white opacification of the cornea (cellular infiltrate) would suggest that the antibiotic proto-col (agent and frequency) has failed to prevent bacterial infection. Post surgical prophylactic medical treatment usually involves triple antibiotic agents (except in cats in which gentamicin is gen-erally used) because of their broad spectrum and because they are not agents used systemically. Four times daily treatment is recom-mended. Ointments are commonly used after surgery of the eyelids, conjunctiva or cornea. Eye drops are usually used following surgery of the cornea or anterior segment. Bacterial infection of the ante-rior chamber alone is uncommon. Bacterial endophthalmitis car-ries a poor prognosis for saving vision or the globe in animals and is usually managed surgically in people. Gentamicin is sometimes used for prophylactic therapy of the equine species because of a greater number of gram negative organisms in the environment of this species. T obramycin and the quinolones would not be consid-ered for prophylactic treatment following surgery performed under sterile conditions. chlor Am Phenicol (OPHTHALm IC) (klor-am-fen-i-kole) Indications/Pharmacology A broad spectrum antibiotic, chloramphenicol has the ability to cross the corneal barrier and enter the anterior chamber. However, there are very few infections that occur in the anterior chamber and if bacteria are actually present there, the blood ocular barrier is lost and systemically administered antibiotics can achieve therapeutic levels. Because of the potential toxicity associated with chlorampheni-col to humans, chloramphenicol's use in veterinary ophthalmology is becoming less widespread. It may be useful, however, in treating cats with suspected Mycoplasma or chlamydial conjunctivitis. Suggested Dosages/Precautions/Adverse Effects For prophylaxis following surgery or for cats with Mycoplasma or chlamydial conjunctivitis: One drop (or 1/4 inch strip if us-ing ointment) four times daily. For established corneal infection: Application may be very frequent (up to hourly). Chloramphenicol exposure in humans has resulted in fatal aplastic anemia. For this reason, this drug should be used with cau-tion in veterinary patients and some ophthalmologists avoid its use entirely. Clients should be cautioned to use appropriate safeguards when applying the drug and avoiding contact with drops or solu-tions after application. Labels state to not use longer than 7 days in cats, but tid applica-tion of ointment for 21 days to cats did not cause toxicity. Must not be used in any food producing animal. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Chloramphenicol 1% Ophthalmic Ointment in 3. 5 gm tubes; Chlo-romycetin® (Parke Davis); Chloroptic® (Allergan); generic (Rx) Chloramphenicol 0. 5% Ophthalmic Drops in 7. 5 m L; Chloroptic® (Allergan); generic; (Rx). Refrigerate until dispensed. These products are sporadically available commercially and may need to be com-pounded by an appropriately trained compounding pharmacist. ci Pro Flox Acin (OPHTHALm IC) GATi Flox Acin (OPHTHALm IC) levo Flox Acin (OPHTHALm IC) moxi Flox Acin (OPHTHALm IC) nor Flox Acin (OPHTHALm IC) o Flox Acin (OPHTHALm IC) Indications/Pharmacology These fluroquinolone ophthalmic antibiotics are primarily useful for established gram negative corneal infections. They are not rec-ommended for prophylactic use prior to or after surgery. See the main enrofloxacin/ciprofloxacin monograph for additional phar-macologic information. Clinicians are strongly cautioned regarding the development of retinal neurotoxicity at or above the formerly recommended sys-temic enrofloxacin dosage in cats. There are no reports at the time of writing of retinal toxicity in cats administered topical fluroqui-nolone ophthalmic products. Precautions/Adverse Effects Ciprofloxacin may cause crusting or crystalline precipitates in the superficial portion of corneal defects. Other potential adverse ef-fects with quinolones include: conjunctival hyperemia, bad taste in mouth, itching foreign body sensation, photophobia, lid edema, tearing keratitis and nausea. Allergic reactions have been reported with quinolone eye preps. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Ciprofloxacin 3 mg/m L drops in 2. 5 & 5 m L btls; Ciloxan® (Alcon); (Rx) Ciprofloxacin:Dexamethasone 0. 3%:0. 1% drops in 7. 5 m L btls; Ciprodex® (Alcon); (Rx) Gatifloxacin 0. 3% drops in 5 m L btls; Zymar® (Allergan); (Rx) Levofloxacin 0. 5% drops in 5 m L btls, Quixin® (JOM Pharmaceuti-cals); 1. 5% drops, 5 m L btls; Iquix® (JOM Pharmaceuticals); (Rx) Moxifloxacin 5 mg/m L drops: 3 m L & 6 m L btls; Vigamox® (Alcon); (Rx) Norfloxacin 3 mg/m L drops in 5 m L btls; Chibroxin® (Merck); (Rx) Ofloxacin 3 mg/m L drops in 5 m L btls; Ocuflox® (Allergan); (Rx) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 961 Gen TAmicin (OPHTHALm IC) To Br Amycin (OPHTHALm IC) (jen-ta-mye-sin; toe-bra-mye-sin) Indications/Pharmacology The aminoglycosides are excellent drugs for gram negative or staphylococcal corneal infections. With frequent application, clini-cians can establish corneal drug levels far in excess of MIC for most organisms without exceeding toxic systemic levels. Therefore, MIC reports may not be meaningful. Because of the high levels attain-able, gentamicin usually exhibits similar efficacy to tobramycin, ex-cept in certain resistant gram-negative infections (e. g., Pseudomonas aeruginosa). For serious gram negative or staphylococcal corneal ulcer infec-tions, some ophthalmologists use cefazolin eye drops (compounded preparation 33 mg/m L - 50 mg/m L in artificial tears) in combina-tion with gentamicin or tobramycin. Synergism may result. Precautions/Adverse Effects Hypersensitivity, and localized ocular toxicity (lid itching, swelling and conjunctival erythema) have been reported rarely. Mydriasis and conjunctival paresthesias may also occur. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Gentamicin Ophthalmic Ointment: 3 mg/g in 3. 5 gm tubes; Gento-cin® (Schering); (Rx). Approved for use in dogs and cats. Gentamicin Ophthalmic Drops: 3 mg/m L in 5 m L btls; Gentocin® (Schering); (Rx). Approved for use in dogs and cats. Hum AN-LAb ELED PRODu CTS: Gentamicin Ophthalmic Ointment: 3 mg/g in 3. 5 gm tubes; Ga-ramycin® (Schering); Genoptic® (Allergan); generic; (Rx)Gentamicin Ophthalmic Drops: 3 mg/m L in 5 m L btls Garamycin® (Schering); Genoptic® (Allergan); generic; (Rx) T obramycin Ophthalmic Ointment: 3 mg/g in 3. 5 gm tubes; To-brex® (Alcon); (Rx) T obramycin Ophthalmic Drops: 3 mg/m L in 5 m L btls; Tobrex ® (Alcon); (Rx) sul FAce TAmide (sul-fa-see-ta-mide) Indications/Pharmacology For the treatment of conjunctivitis and other superficial ocular infections due to susceptible microorganisms, and as an adjunc-tive in systemic sulfonamide therapy of trachoma, Escherichia coli, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus (viridans group), Haemophilus Muenzae, Klebsiella species and Enterobacter species. T opically applied sulfonamides do not provide adequate coverage against Neisseria species, Serratia marcescens and Pseudomonas aeruginosa. A significant percentage of staphylococcal isolates are completely resistant to sulfa drugs. Precautions/Adverse Effects For conjunctivitis and other superficial ocular infections: Instill one or two drops into the conjunctival sac(s) of the affected eye(s) every two to three hours initially. Dosages may be tapered by increasing the time interval between doses as the patient responds. The usual duration of treatment is seven to ten days. Owners with sulfa aller-gies should be cautioned to avoid all contact with this medication. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Sulfacetamide Ophthalmic Solution 10%: 15 m L bts; Sulf-10®, AK-10® (Akorn); Bleph-10® (Allergan); (Rx) Sulfacetamide Ophthalmic Ointment 10%: Bleph-10® (Allergan); (Rx) Te Tr Acycline/ oxy Te Tr Acycline (OPHTHALm IC) (tet-ra-sye-kleen)/(ox-ee-tet-ra-sye-kleen) Indications/Pharmacology The tetracyclines are most useful in cats for the treatment of Chlamydial and Mycoplasma conjunctivitis as well as nonspecific or symptomatic therapy for undiagnosed (causative organism not determined) conjunctivitis in cats. While its use in dogs and horses is questionable, it may be useful in goats for Chlamydial/ Mycoplasma keratoconjunctivitis. At the time of publication, there are no commercially available ophthalmic dosage forms of tetracy-cline. There are, however, Veterinary-Labeled forms of oxytetracy-cline and Polymyxin B ophthalmic ointments (Terramycin ®). It is again, important to note, that severe anaphylaxis, sometimes fatal, has been associated with topical Polymyxin and neomycin in cats and caution is recommended when using this product in cats. Suggested Dosages/Precautions/Adverse Effects For Chlamydial/Mycoplasma keratoconjunctivitis: Apply 4 times daily. Dramatic improvement should be noted in 3-4 days, but treatment should continue for 3-4 weeks for Chlamydia to break the reproductive cycle of this organism. Expect potential recurrence after discontinuation of topical treatment from organisms dormant in the nasal passage. As oral doxycycline has been documented to eliminate the carrier state of Chlamydia in cats; better treatment is oral doxycycline 25 mg PO twice daily for three weeks. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Oxytetracycline HCl 5 mg/Polymyxin B Sulfate 10,000 U/gm: 3. 5 gm tubes; Terramycin® Ophthalmic Ointment (Pfizer); (Rx) Hum AN-LAb ELED PRODu CTS: T etracycline HCl Ointment: 10 mg/g in 3. 75 g tubes; Achromycin® (Storz/Lederle); (Rx) T etracycline HCl Suspension: 10 mg/m L in 4 m L btls; Achromycin® (Storz/Lederle); (Rx) Other available ophthalmic antibiotics: Chlortetracycline: Aureomycin® (Storz Lederle); Bacitracin (alone); Erythromycin Ointment; Polymyxin B powder for solution; Sodium Sulfacetamide. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
962 OPHTHALm IC PRODu CTS An Ti Bio Tic com Bin ATions (OPHTHALm IC) Indications/Pharmacology These combination products exhibit a broad-spectrum of activity and are considered the first choice for symptomatic treatment of conjunctivitis in dogs and for prophylactic treatment of small ani-mals prior to or after eye surgery. These agents are also used pro-phylactically for corneal injuries/wounds. Suggested Dosages/Precautions/Adverse Effects Usually applied 4 times daily to prevent infection and up to every 30 minutes in established corneal infections. See individual product label information and the information noted previously. Neomycin has been reported to cause allergic reactions in dogs and cats, particularly after prolonged usage. As noted above, avoid neomycin treatment in cats unless absolutely necessary. Interestingly, anaphylactic reactions in cats have only been associated with neo-mycin products in ointment form in the absence of cortisone, but not with antibiotic-steroid combination preparations. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Bacitracin zinc 400 units/Neomycin 3. 5 mg/Polymyxin B Sulfate 10,000 Units per gram Ophthalmic Ointment: 3. 5 gm tubes; My-citracin® (Upjohn) (Note : contains 500 mg bacitracin/gm); Neoba-cimyx® (Schering); Trioptic-P® (Pfizer); Vet ropolyc in ® (Pitman-Moore); generic; (Rx). Approved for dogs and cats. Oxytetracycline HCl 5 mg/Polymyxin B Sulfate 10,000 U/gm Oph-thalmic Ointment: 3. 5 gm tubes; Terramycin® Ophthalmic Oint-ment (Pfizer); (OTC). Approved for use in dogs, cats, sheep, cattle, and horses. Neomycin 3. 5 mg/Polymyxin B Sulfate 10,000 Units per m L Oph-thalmic Solution: Optiprime® (Syntex); (Rx). Approved for use in dogs. Hum AN-LAb ELED PRODu CTS: There are a wide variety of human-labeled ophthalmic combination products available. Most are a combination of bacitracin/neomy-cin/polymyxin B. However, there are variations of this theme (e. g., gramicidin in place of bacitracin in topical solutions-Neosporin® Ophthalmic Solution). All these products require a prescription. An Ti Bio Tic And cor Tico s Teroid com Bin ATions (OPHTHALm IC) Indications/Pharmacology There are three basic categories of these products that are routinely used in veterinary medicine; antibiotic combinations with hydro-cortisone, antibiotic combinations with dexamethasone, and in-dividual antibiotics (e. g., gentamicin or chloramphenicol) with a steroid. Antibiotic combinations with hydrocortisone (ointment or so-lution) are used in dogs and horses for conjunctivitis as nonspecific therapy after ruling out other causes for red painful eyes, including glaucoma and anterior uveitis. They generally are applied 4 times daily and then on a tapering schedule based on the response to therapy. The hydrocortisone is relatively weak as an antiinflamma-tory agent and is not effective for intraocular inflammatory disease such as anterior uveitis. The relative penetration and potency of hydrocortisone in these preparations makes them relatively inef-fective for immune mediated extraocular disease including scleri-tis, episcleritis and or nodular granulomatous episclerokeratitis. Anterior uveitis is statistically more common in horses than simple conjunctivitis and the steroid in these agents would not be helpful in improving the clinical signs of immune mediated uveitis. Antibiotic combinations with dexamethasone are valuable for use in cases of more severe canine or equine conjunctivitis, nonul-cerative keratitis and for immune-mediated scleral or corneal con-ditions such as chronic superficial keratitis (German shepherd pan-nus), feline eosinophilic keratitis, scleritis, episcleritis and nodular granulomatous episclerokeratitis. For these conditions the antibi-otic agent is not necessary but dexamethasone-only products are not always available. These medications are also used in the equine species with equine uveitis because the ointment forms persist on the cornea longer than drops. Single agent antibiotic (gentamicin) and potent steroid (be-tamethasone) combination products (e. g., Gentocin Durafilm®) are commonly used in veterinary medicine. However, there are few instances in veterinary ophthalmology in which a very potent cor-ticosteroid agent and an aminoglycoside antibiotic are necessary in combination. Simple conjunctivitis in dogs and horses is adequate-ly treated with antibiotic combinations with hydrocortisone. Avoid use of this agent in cats with conjunctivitis for the reasons noted below. Suggested Dosages/Precautions/Adverse Effects See individual product label information and the information not-ed above. Avoid use of antibiotic/steroid combination agents in cats with conjunctivitis as the most common cause of conjunctivitis in the cat is primary or recurring infection with exposure to, or reacti-vation of, latent feline herpes virus. Recent research indicates that topical steroids increase the length of the typical course of feline herpes virus related conjunctivitis and/or keratitis and can induce corneal involvement in cases that might otherwise have remained confined to conjunctiva. Corneal sequestration has been noted to occur in cats with herpes virus conjunctivitis after treatment with topical steroids. Recommended treatment for feline herpes virus conjunctivitis is tetracycline ointment QID during active disease, as this drug is effective against Mycoplasma and Chlamydia (Note: concurrent systemic treatment with doxycycline will likely be nec-essary to clear Chlamydia organisms from the nasal and/or GI pas-sages in cats as discussed above). Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Triple Antibiotic Ointments with Hydrocortisone: Bacitracin zinc 400 units/Neomycin 3. 5 mg/Polymyxin B Sulfate 10,000 Units & Hydrocortisone acetate 1% per gram in 3. 5 gm tubes; Neobacimyx H® (Schering); Trioptic-S® (Pfizer); Vetropolycin HC® (Pitman-Moore); generic; (Rx). Approved for dogs and cats. Other Antibiotic/Steroid Ointments: Neomycin Sulfate 5 mg & Prednisolone 2 mg (0. 2%) per gram in 3. 5 gram tubes; Optisone® (Evsco); (Rx). Approved for use in dogs and cats. Neomycin Sulfate 5 mg & Isoflupredone acetate 1 mg (0. 1%) per gram in 3. 5 & 5 gram tubes; Neo-Predef® Sterile Ointment (Up-john); (Rx). Approved for use in horses, cattle, dogs and cats. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 963 Chloramphenicol 1% and Prednisolone acetate 2. 5 mg (0. 25%) in 3. 5 gm tubes; Chlorasone® (Evsco) (Rx). Approved for use dogs and cats. Drops: Gentamicin Ophthalmic Drops 3 mg/m L & Betamethasone acetate 1 m/m L in 5 m L btls; Gentocin Durafilm® (Schering); (Rx). Ap-proved for use in dogs. Hum AN-LAb ELED PRODu CTS: There are a wide variety of human-labeled ophthalmic antibiotic/steroid combination products available. Some of the more com-monly used combinations include: Ointments: Bacitracin/Neomycin/Polymyxin B and Hydrocortisone; Cor-tisporin® (BW); (Rx) Neomycin/Polymyxin B & Dexamethasone; Maxitrol® (Alcon); (Rx)Neomycin and Dexamethasone; Neo Decadron® (Merck); (Rx)Drops: Neomycin/Polymyxin B and Hydrocortisone; Cortisporin® (BW, etc. ); (Rx) Neomycin/Polymyxin B & Dexamethasone; Maxitrol® (Alcon); (Rx)Neomycin and Dexamethasone; Neo Decadron® (Merck); (Rx) Antifungals Fungal keratitis is a serious corneal disease, most commonly re-ported in the horse. The species selectivity of this disease is related to the environment of this animal, which is often contaminated with fungal elements. An increased incidence of fungal keratitis in people was directly related to the development of multiple topical steroid agents for treatment of eye diseases. In the horse, many cases of fungal keratitis are noted in association with prior treatment of conjunctival and/or corneal diseases with topical steroid agents. Aspergillus is the most common cause of fungal keratitis in the horse, although there is a great deal of variation in fungal isolates from the cornea depending upon geographical location. Studies in people and anecdotal reports from veterinarians suggest that fungal keratitis due to fusarium organisms are more resistant to therapy than are those caused by aspergillus. Most studies in the equine sug-gest that about 50% of cases of fungal keratitis in the horse result in perforation of the corneal and enucleation of the eye. Medical and surgical therapy (keratectomy, corneal debridement, and conjunc-tival grafting) are used to treat such cases with the goals of therapy including arresting infection, mechanical removal of organisms from the cornea, and support of the cornea. All antifungal agents available for use in the equine suffer from poor penetration into the corneal stroma. Conjunctival grafting may further hinder drug penetration as a trade off to improving vascular availability to the cornea and mechanical support. Pathologic specimens from horses with fungal keratitis indicate that fungal organisms, unlike bacterial organisms, have a propensity to multiply deep in the stroma, di-rectly adjacent to Descemet's membrane, making corneal penetra-tion an important issue. Because the prognosis for return of vision and saving the globe in cases of fungal keratitis cases is guarded and because treatment is labor intensive, referral to teaching or other hospitals for 24 hour care and observation is recommended. Am Pho Tericin B (OPHTHALm IC) (am-foe-ter-i-sin B) Indications/Pharmacology Amphotericin B has been used topically and subconjunctivally to treat cases of equine fungal keratitis. Amphotericin B is fungistatic or fungicidal depending on the concentration obtained in body flu-ids and the susceptibility of the fungus. The drug acts by binding to sterols in the cell membrane of susceptible fungi with a resultant change in membrane permeability allowing leakage of intracellular components. Mammalian cell membranes also contain sterols and it has been suggested that the damage to human cells and fungal cells may share common mechanisms. Amphotericin B has been shown to be effective against the following fungi: Histoplasma cap-sulatum, Coccidioides immitis, Candida species, Blastomyces derma-titidis, Rhodotorula, Cryptococcus neoformans, Sporothrix schenckii, Mucor mucedo, and Aspergillus fumigatus. While Candida albicans is generally quite susceptible to amphotericin B, non-albicans species may be less susceptible. Pseudallescheria boydii and Fusarium spp. are often resistant to amphotericin B. The major action of ampho-tericin B is to bind ergosterol in the fungal plasma cell membrane, making the membrane more permeable and resulting in leakage of cell electrolytes and cell death. At high concentrations, amphoteri-cin B is thought to cause oxidative damage to the fungal cell or dis-ruption of fungal cell enzymes. Suggested Dosages/Precautions/Adverse Effects Instill 0. 2 m L of a 0. 15% solution in the eye or the palpebral lavage catheter every 2-6 hours, or 0. 25 m L of a 0. 5 mg/m L solution sub-conjunctivally every 48 hours. There are no commercially available amphotericin B ophthalmic products, but the non-liposomal in-jectable formulation can be reconstituted with sterile water to make sterile solutions suitable for topical or subconjunctival adminis-tration. Amphotericin B should not be reconstituted with sodium chloride containing solutions as this encourages degradation of the drug. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None. Sterile solutions for topical ophthalmic administration or subcon-junctival injection may be prepared by reconstituting commercially available amphotericin B injection lyophilized powder and dilut-ing to appropriate concentrations with sterile water for injection. Chemical stability is concentration dependent, but most resulting solutions may be stored for at least 7 days under refrigeration and protected from light. Povidone iodine (OPHTHALm IC) Indications/Pharmacology Dilute solutions of povidone iodine (1%-5%) have been utilized for chemical debridement of loose epithelium in canine indolent ulcers. 5% povidone iodine has also been used as an antifungal for fungal keratitis, but must be lavaged from the eye within 5 minutes to prevent damage to corneal epithelium. Generally, povidone io- | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
964 OPHTHALm IC PRODu CTS dine is only used once daily and then rinsed off when used in the eye as an anti-fungal. There has also been a renewed interest in utiliz-ing povidone iodine in treating feline herpes keratitis. Solutions of commercially available 10% povidone iodine are diluted in physi-ologic saline to concentrations of 0. 5-1% and applied 1 drop twice to four times daily for treatment of chronic feline herpes keratitis and may also be used prophylactically for feline herpes-virus (FHV) cats with a history of recurring ulcer. Suggested Dosages/Precautions/Adverse Effects Solutions of 1% are applied twice to four times daily for treat-ment and prophylaxis of feline herpes-virus (FHV) keratitis and for chemical debridement of epithelium for canine indolent ulcers. Solutions of concentration greater than 1% should be lavaged from the eye after no more than 5 minutes to prevent corneal epithelial damage. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None Products must be compounded and diluted from the commercially available povidone iodine 10% solutions and diluted to final con-centrations of 0. 5-1% for antiviral indications and no more than 5% for use as an ophthalmic irrigant. n ATAmycin (na-ta-mye-sin) Indications/Pharmacology Natamycin is a semisynthetic polyene antibiotic. Natamycin is poorly water-soluble and will not penetrate the intact corneal epi-thelium. Natamycin is the only antifungal agent approved for use on the eye and the only commercially available eye drug for treat-ment of fungal keratitis. Suggested Dosages/Precautions/Adverse Effects The product comes as a thick white suspension that complicates the use of subpalpebral lavage apparatus for frequent treatment of the cornea of the horse. This drug will obstruct catheter systems used for medication. It will cause dramatic swelling and pain in the up-per eyelid if it leaks out of the tubing into the subcutaneous tissues of the eyelid. Corneal penetration is poor and the medication is very expensive. Fungal keratitis cases are treated aggressively with hourly or bi-hourly treatment the first 1-3 days and gradual reduction in treatment frequency with signs of clinical improvement. Cytology and repeated cultures of the cornea are used to indicate treatment effectiveness. Worsening of the corneal edema and cellular infiltra-tion can be a sign of treatment response. This is thought to be due to antigenic release associated with killing of fungal organisms (like the pulmonary response noted in dogs with institution of antifun-gal therapy for blastomycosis, etc. ). Four to six weeks of treatment is not uncommon for fungal keratitis cases. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Natamycin Ophthalmic Suspension 5%: 15 m L btls; Natacyn® (Al-con); (Rx)micon Azole (OPHTHALm IC) (mi-kon-a-zole) Indications/Pharmacology Miconazole is a broad spectrum imidazole antifungal agent with some antibacterial activity. Miconazole will penetrate the intact corneal epithelium. T opical miconazole therapy has been a favor-ite first choice agent for treatment of fungal keratitis in the horse by veterinary ophthalmologists for several years. Miconazole may be delivered by subconjunctival route, but with some local irrita-tion, and topical use is the most commonly employed treatment method. Suggested Dosages/Precautions/Adverse Effects Miconazole was formerly available as a 10 mg/m L injectable solu-tion for IV use in humans. It can now only be obtained through s. It is a clear solution readily delivered through subpalpebral la-vage apparatus systems. The medication is significantly less expen-sive compared with natamycin and its corneal penetration is more favorable, although still less than optimal. Treatment is generally delivered hourly or bi-hourly during the first several days of treat-ment. Once clinical improvement is noted and cytology specimens and repeated cultures indicate eradication of fungal organisms, the treatment frequency is gradually reduced. Most fungal keratitis cas-es are treated 4-6 weeks. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None suitable for the eye. All commercially available miconazole topical preparations contain alcohols or other agents that cause corneal damage. It is imperative that a 1% miconazole solution be compounded without alcohols for use on the cornea. silver sul FAdi Azine (OPHTHALm IC) (sil-ver sul-fa-dye-a-zeen) Indications/Pharmacology Silver sulfadiazine cream is a broad spectrum agent which covers bacteria (gram positive and negative) and fungal agents. It has been used extensively in people suffering from skin burns. It is nontoxic to the skin, conjunctiva and cornea and has been used in the last several years for cases of fungal keratitis. Particularly good results have been noted in cases of superficial keratitis prior to develop-ment of advanced disease. Clinical response is better when used early in the course of the disease. Treatment with silver sulfadiazine is considered non-conventional in people. It is gaining in popular-ity in the treatment of equine fungal keratitis by veterinary oph-thalmologists. For medico-legal reasons, in very expensive horses in which litigation may be an issue, treatment with more conventional therapy (natamycin) may be indicated first, or consideration can be given to signed consent regarding treatment with silver sulfadiaz-ine. The initial response to this drug has been promising, however. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 965 Suggested Dosages/Precautions/Adverse Effects The commercially available product is a cream, but can be delivered into the conjunctival sac using a tuberculin syringe, without the needle. A typical treatment dose is 0. 2 m L drawn into a syringe. It will not pass through standard sized subpalpebral lavage catheters, although it may be administered through large medication admin-istration systems using red rubber feeding tubes passed through the lid, with variable results getting the medication to pass through the tube. It is probably best applied manually. The cream sticks well to the cornea that probably improves effectiveness, similar to na-tamycin, as compared to miconazole. Treatment regimes are simi-lar to the other antifungal agents with very frequent applications necessary during the early phases of the treatment and reduction in therapy based upon clinical response. Daily debridement of the necrotic corneal stroma and epithelium will improve penetration of the drug and the clinical response. The medication is inexpensive and is available from any phar-macy, but it is not labeled for use in eyes. The label (package insert) specifically states “not to be used in eyes” so liability for use in eyes rests solely with the prescribing veterinarian and some pharmacists may be unwilling to dispense this medication for ophthalmic use. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Silver Sulfadiazine T opical (not an ophthalmic product ): 10 mg per gram in a water miscible cream base; 20, 50, 400, and 1000 g con-tainers; Silvadene® (Marion); Flint SSD® (Flint); (Rx). Preferably dispensed aseptically in single use sterile tuberculin syringes for ap-plication to the conjunctival sac. i Tr Acon Azole (OPHTHALm IC) (i-tra-koe-na-zole) Indications/Pharmacology Itraconazole is a broad spectrum synthetic antifungal agent effec-tive against a wide range of filamentous fungi, dimorphic fungi, and yeasts. It is the most popular systemic antifungal agent for treatment of blastomycosis related and other systemic fungal in-fections in dogs and people. Itraconazole specifically targets oxida-tive enzymes of fungal organisms thereby increasing efficacy while lowering toxicity. Itraconazole prepared as a 1% ointment in 30% dimethylsulfoxide (DMSO) is well tolerated in horses with kerato-mycosis with reported good results. Itraconazole is relatively in-soluble in water and must be diluted in DMSO to achieve solution. Itraconazole 1% suspensions in a vehicle of 30% DMSO and 70% artificial tears have also been used successfully to treat fungal kera-titis in horses. It is important to note that the DMSO may be topi-cally irritating to many horses. The fungal species most commonly isolated from cases of equine keratomycosis and their particular sensitivity to specific antifungal agents varies greatly by geography in the United States. In vitro sensitivity testing can be done at select laboratories on fungal isolates from the equine eye but this infor-mation generally takes several weeks to become available. Because of these considerations, the selection of a particular antifungal drug for an individual case is largely based on local clinical experience and impressions. Suggested Doses/Precautions/Adverse Effects Compounded itraconazole/DMSO preparation is applied to the cornea frequently in horses with confirmed keratomycosis. Treatment every 2-3 hours would not be uncommon initially with tapering of the treatment based on clinical response. Individuals treating horses need to use routine precautions (gloves) while han-dling this medication to minimize any skin uptake enhanced by the DMSO solvent. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Compounded product. Must be obtained from a compounding pharmacy as a 1% suspension or ointment. voricon Azole (vor-i-kon-a-zole) Indications/Pharmacology Voriconazole has been used clinically for the treatment of equine fungal keratitis. Voriconazole is a triazole antifungal agent. The primary mode of action of voriconazole is the inhibition of fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylation, an essential step in fungal ergosterol biosynthesis. The accumulation of 14 alpha-methyl sterols correlates with the subsequent loss of er-gosterol in the fungal cell wall and may be responsible for the anti-fungal activity of voriconazole. Voriconazole has been shown to be more selective for fungal cytochrome P-450 enzymes than for vari-ous mammalian cytochrome P-450 enzyme systems. Voriconazole has demonstrated in vitro activity against Aspergillus ( A. fumigatus, A. flavus, A. niger and A. terreus), Candida ( C. albicans, C. glabrata, C. krusei, C. parapsilosis and C. tropicalis), Scedosporium apiosper-mum and Fusarium spp., including Fusarium solani. Voriconazole drug resistance development has not been adequately studied in vitro against Candida, Aspergillus, Scedosporium and Fusarium spe-cies. The frequency of drug resistance development for the various fungi for which this drug is indicated is not known. Fungal isolates exhibiting reduced susceptibility to fluconazole or itraconazole may also show reduced susceptibility to voriconazole, suggesting cross-resistance can occur among these azoles. The relevance of cross-resistance and clinical outcome has not been fully character-ized. Clinical cases where azole cross-resistance is demonstrated may require alternative antifungal therapy. There are no approved ophthalmic formulations of voriconazole, however, a suitable solu-tion for ophthalmic administration can be prepared by utilizing the approved voriconazole injectable product. Suggested Dosages/Precautions/Adverse Effects 0. 2 m L in the eye or palpebral lavage catheter every 2-4 hours. Voriconazole is contraindicated in patients with known hyper-sensitivity to voriconazole or its excipients. There is no informa-tion regarding cross-sensitivity between voriconazole and other azole antifungal agents. Caution should be used when prescrib-ing voriconazole to patients with hypersensitivity to other azoles. Voriconazole treatment-related visual disturbances are common in humans. In therapeutic trials, approximately 21% of patients ex-perienced abnormal vision, color vision change and/or photopho-bia. The visual disturbances were generally mild and rarely resulted in discontinuation. Visual disturbances may be associated with higher plasma concentrations and/or doses. Since topical admin-istration of voriconazole has not been evaluated in humans, it is | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
966 OPHTHALm IC PRODu CTS not known if this adverse event occurs with topical administration. The mechanism of action of the visual disturbance is unknown, although the site of action is most likely to be within the retina. In a study in healthy volunteers investigating the effect of 28-day treat-ment with voriconazole on retinal function, voriconazole caused a decrease in the electroretinogram (ERG) waveform amplitude, a decrease in the visual field, and an alteration in color perception. The ERG measures electrical currents in the retina. The effects were noted early in administration of voriconazole and continued through the course of study drug dosing. Fourteen days after end of dosing, ERG, visual fields and color perception returned to nor-mal. Dermatological reactions are also common in human patients treated with voriconazole. The mechanism underlying these der-matologic adverse events remains unknown. In clinical trials, rashes considered related to therapy were reported by 7% (110/1655) of voriconazole-treated patients. The majority of rashes were of mild to moderate severity. Cases of photosensitivity reactions appear to be more likely to occur with long-term treatment. Human pa-tients have rarely developed serious cutaneous reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythe-ma multiforme during treatment with VFEND. If patients develop a rash, they should be monitored closely and consideration given to discontinuation of VFEND. It is recommended that patients avoid strong, direct sunlight during VFEND therapy. The extent of these adverse drug reactions in animals is unknown at this time. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None There are no commercially available ophthalmic dosage forms of voriconazole. A suitable solution for ophthalmic administration may be prepared by aseptically adding 19 m L of sterile water for injection to a 200 mg vial of VFend® injection to result in a sterile 1% solution. Resulting solution should be stored under refrigera-tion and discarded 28 days after reconstitution. Antivirals (Ophthalmic) Antiviral drugs are used most commonly in clinical practice for the treatment of feline ocular herpes virus infections. Simple acute conjunctivitis is best managed with symptomatic antibiotic thera-py alone (i. e., tetracycline treatment or systemic doxycycline treat-ment). The development of concurrent corneal disease, however, indicates that consideration should be given to the use of antiviral drugs. Persistent cases of conjunctivitis in the cat due to feline her-pes virus infection may also benefit from treatment with topical antiviral drugs. Although in vitro studies indicate that trifluridine is the most effective agent against feline herpes virus, idoxuridine is a less irritating, more economical alternative. In general, all antivirals are virustatic (not cidal) and require application every 2 hours for the first 24 hours followed by 5-6 times daily treatment thereafter. While this appendix focuses mostly on topical ophthalmic thera-pies, it is important to note that studies support use of l-lysine at 500 mg orally twice daily in cats to prevent or reduce the severity of feline herpes virus ocular infections through disruption of viral replication. Tri Fluridine (Tri Fluoro Thymidine) (trye-flure-i-deen) Indications/Pharmacology Trifluridine (trifluorothymidine; Viroptic®) is a pyrimidine nucleo-side analog. It is structurally related to 2-deoxythymidine, the natu-ral precursor of DNA synthesis. Trifluridine is poorly absorbed by the cornea and is virostatic. Viroptic® interrupts viral replication by substituting “nonsense” pyrimidine analogues. For this reason, a competent surface immunity is necessary to resolve ocular disease, with or without antiviral therapy. A recent in vitro study in which several strains of feline herpes virus were collected from the United States and were used to infect kidney epithelial cells showed that tri-fluridine was more effective at lower concentrations compared with several other agents. For this reason, trifluridine was the first choice drug employed in the treatment of feline herpes virus ocular dis-ease for many years. Because of the topical toxicity associated with use of trifluridine in cats, its popularity has diminished greatly. In many milder cases, the irritation associated with topical trifluridine is more intense then the inflammation induced by viral infection. Antiviral agents have also been used in the treatment of superficial punctate keratitis in the horse, thought to be associated with equine herpes virus-2 (EHV-2) infection of the cornea. Suggested Dosages/Precautions/Adverse Effects Trifluridine must be applied very frequently. Many veterinary oph-thalmologists recommend treatment every 2 hours (waking hours) during the first 2 days of therapy to establish effective corneal drug levels. After this time, treatment 4-6 times daily is indicated. Because trifluridine is virostatic and not viricidal, treatment 1 week beyond the resolution of clinical signs is recommended, to prevent a rebound effect associated with poor surface immunity in com-bination with residual active viral agents. However, a maximum supply of 3 weeks medication should initially be dispensed as tri-fluridine is a corneal toxin and can retard corneal epithelial healing. Additionally, if cats do not respond favorably to trifluridine therapy within three weeks, they are not likely to respond with longer dura-tions of therapy. If no improvement is noted in three weeks, trifluri-dine (or any antiviral) should be discontinued for a rest period and then a different antiviral initiated. Anecdotally, improvement with antiviral agents is noted in about 50% of cats in which the treatment is employed. In some cats the ocular disease persists despite treatment with antiviral agents. It is not certain if these are truly cases of feline herpes virus infection or other disease as the confirmation of feline herpes virus infection is exceedingly difficult in practice, (except in the acute disease with respiratory and ocular involvement, because of the logistics of viral isolation tests for doctors in clinical practice (usually only available at major institutions or referral centers) and because of the high degree of false negatives with herpes virus FA tests and with avail-able polymerase chain reaction (DNA amplification) technology). Chronic conjunctivitis in the cat seems to be the most resistant to treatment with antiviral agents. Conjunctival and lid margin irrita-tion are commonly reported with trifluridine use. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Trifluridine Ophthalmic Solution: 1% in 7. 5 m L btls; Viroptic® (Monarch); (Rx) | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 967 idoxuridine (eye-dox-yoor-i-deen) Indications/Pharmacology Idoxuridine (IDU) is chemically similar to thymidine and its sub-stitution into viral DNA causes misreading of the viral genetic code thereby inhibiting viral replication. Like trifluridine, IDU is consid-ered virostatic rather than viricidal. IDU was found to be second to trifluridine in efficacy in vitro against common strains of feline herpes virus growing in kidney epithelial cells. IDU is extremely well tolerated in cats and this feature alone makes it the most popu-lar antiviral currently available for use in cats with presumed or established feline herpes virus infection. Although trifluridine was shown to be more effective in vitro, the topical irritation it induces in cats frequently negates any beneficial effect that might be noted clinically. Stinging upon application is a rare feature with IDU/ar-tificial tear preparations. Suggested Doses/Precautions/Adverse Effects IDU, like trifluridine, penetrates poorly into the cornea (except in instances of ulceration) and conjunctiva and therefore must ini-tially be applied frequently. Most treatment protocols involve ap-plication every two to three hours during waking hours the first two days of acute infection, followed by four to five times daily treat-ment continued a week beyond resolution of clinical signs. IDU has been particularly useful in the management of cats with chronic feline herpes virus conjunctivitis. These cats maintain low-grade viral activity in the cornea, occasionally showing accelerated viral growth with secondary corneal involvement (ulceration/seques-trum). With chronic treatment, the conjunctivitis component is rarely suppressed in total, but usually the corneal disease, which is the most problematic from a vision and comfort standpoint, can be controlled. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None. Formerly approved as Stoxil® and Herplex®; must be obtained from compounding pharmacies as a 0. 1% ophthalmic solution or a 0. 5% ophthalmic ointment. in Ter Feron Al Ph A (TOPICAL) (in-ter-feer-on al-fa) Indications/Pharmacology Interferon alpha-2B is thought to stimulate local immunity against viral infection and has been advocated as an adjunct therapy for treatment of feline herpes keratitis. A German study has also re-cently reported that topical interferon alpha may speed the resolu-tion of corneal sequestrum without surgery. Suggested Dosages/Precautions/Adverse Effects It has been used both systemically (30 IU PO q24h) and/or topically (30 - 50 IU/m L in artificial tears in both eyes 3-5 times daily) for refractory cases of feline herpes keratitis. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None. The human interferon alpha-2B injection (Intron-A®—Schering) is diluted to a final concentration of 30 - 50 IU/m L in saline or artifi-cial tears and administered orally or topically respectively. Acyclovir v Al Acyclovir FAmciclovir GAnciclovircido Fovir Penciclovir Indications/Pharmacology Ophthalmic acyclovir is not yet available in the US, but is avail-able in other countries. It is being compounded for use in the US. Systemic anti-retroviral agents have been tried in cats with persis-tent herpes keratitis, but myelosuppression and nephrotoxicity fol-lowing systemic use is a serious risk with acyclovir and valacyclovir. Acyclovir should only be used systemically as a last resort and CBC should be monitored weekly in cats receiving this drug. Valacyclovir apparently has no effect on feline herpes replication and should be avoided completely due to fatal myeloid dysplasia. Anecdotal re-sponse to famciclovir (metabolized to penciclovir in cats) has been discussed, but no scientific evidence is available to substantiate its effectiveness against FHV or its safety in cats. As other agents in this drug class are myelosuppressive, extreme caution is recommended regarding famciclovir therapy in cats. T opically administered cido-fovir 0. 5% solutions have recently been shown to reduce the sever-ity and duration of FHV-1 infections. The in vitro efficacy of com-monly available antiviral agents for FHV-1 has been studied and is as follows: trifluridine > ganciclovir = idoxuridine = cidofovir = penciclovir = vidarabine > acyclovir >> foscarnet. Suggested Doses/Precautions/Adverse Effects Cidofovir 0. 5% topical solution, 1 drop in each eye twice daily. Until further data is available, systemic use of these agents is not recommended in cats. Myelosuppression, often fatal, and neph-rotoxicity are likely when using these agents systemically in cats. Doses of acyclovir at 100 - 200 mg per cat orally BID-TID have been used with anecdotal reports of success but weekly monitoring of CBC is imperative with use of these agents systemically. T opical acyclovir ophthalmic ointment should be used with caution in cats as they are likely to groom off medication and experience systemic adverse effects. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None. Sterile solutions of cidofovir suitable for ophthalmic administra-tion may be prepared by diluting the commercially available injec-tion to a final concentration of 5 mg/m L using 1% carboxymeth-ylcellulose solutions. Acyclovir 3% ophthalmic ointment may be obtained from compounding pharmacies. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
968 OPHTHALm IC PRODu CTS Keratoconjunctivitis Sicca Keratoconjunctivitis sicca (KCS) is a common ocular disorder in dogs. Recent research efforts indicate that KCS in dogs is an im-mune mediated disease. It is similar to Sjogren's Syndrome in hu-mans except we do not recognize a connective tissue disorder in the dog compared to this disease in people (man-dry eye, dry mouth, and connective tissue disorder like rheumatoid arthritis; dogs just dry eye). Immune mediated lacrimal adenitis can result in com-plete destruction of tear producing glands in dogs. Glandular fi-brosis produces absolute sicca and these cases may be better man-aged with a parotid duct transposition surgery because there may be little remaining gland tissue to treat. cyclos Porine (OPHTHALm IC) (sye-kloe-spor-een) Indications/Pharmacology Cyclosporine is a polypeptide agent first isolated from a fungus. The agent interferes with interleukin synthesis by T lymphocytes and in so doing has been employed extensively in people follow-ing major organ transplantation to prevent immune rejection. Cyclosporine is extremely hydrophobic and was originally com-pounded by pharmacists in virgin olive oil or purified corn oil for the topical application to dogs with keratoconjunctivitis sicca. T opical cyclosporine is now commercially available as a 0. 2% oint-ment (Optimmune®-Schering). The mechanism of action of cy-closporine in the treatment of keratoconjunctivitis sicca is still not fully understood, although it has been employed in the treatment of KCS in dogs for several years. It stimulates increased tear pro-duction in normal dogs and for this reason it is thought to have a direct stimulatory effect on the tear gland. It may do this acting as a prolactin analog, fitting onto lacrimal prolactin receptors. Its interleukin blocking effects likely are the major mechanism of ac-tion. Halting local inflammatory mediator production appears to arrest self perpetuating lacrimal adenitis resulting in resumption of normal or improved tear production after several weeks of therapy, however, cessation of therapy results in return of symptoms in a matter of days. Cyclosporine in the cornea appears to have the abil-ity to lessen granulation and pigment development. This property appears to be unrelated to its tear producing ability. The reported success rate of alleviating the signs of KCS in dogs with treatment with cyclosporine is 75-85%. Some studies indi-cate that the higher the Schirmer value prior to starting therapy, the more likely that the dog will be well managed with cyclosporine alone. Absolute sicca may be associated with extensive fibrosis of the tear glands, leaving little tissue for stimulation or repair. Cyclosporine is effective in the management of German Shepherd Pannus or chronic superficial keratitis in the dog. This condition is an immune disease of the cornea and likely is interleukin mediated. Cyclosporine may be preferred for the treatment of pannus because of the lack of systemic side effects noted in dogs with chronic topi-cal administration of cyclosporine. Chronic topical corticosteroid treatment is associated with biochemical changes in the blood of large and small dogs. Cyclosporine has been tried in the management of the rare case of keratoconjunctivitis sicca in the cat. Dry eye in cats is usually associated with herpes virus destruction of lacrimal epithelial cells and or stenosis of the ductules or openings of the ductules due to chronic viral conjunctivitis. Preliminary results have not been promising. T opical cyclosporine often aggravates ophthalmic her-pes virus infections in people. Cyclosporine has not shown prom-ising effects in the management of feline eosinophilic keratitis, a condition now thought to be related to chronic stromal herpes vi-rus infection in cats. Suggested Dosages/Precautions/Adverse Effects Cyclosporine is initiated generally as the first course of therapy for confirmed dry eye cases in the dog. The topical half-life of cy-closporine is about 8 hours and most canine cases of KCS are man-aged with twice daily therapy with 0. 2% ointment (Optimmune®). Three times a day therapy has been employed during the initial phases of treatment in more difficult or slow responding cases. For unknown reasons (reversal of lacrimal adenitis > reorganization of lacrimal epithelial cell function > formation of secretory granules > tear production) 3-8 weeks of therapy are necessary before a dra-matic increase in the Schirmer tear test becomes evident. Patients are generally maintained for life on cyclosporine ophthalmic once or twice daily depending on the response. Discontinuation of therapy is usually associated with the return of clinical signs of KCS within a few days. Reinstitution of therapy, at this time, is usually associ-ated with an almost immediate return of tear production (versus the initial lag phase noted). This likely is related to the degree of inflammatory disease noted with short discontinuation of therapy versus that present initially, prior to the diagnosis of KCS. If tear production is very low, cyclosporine is often used in com-bination with artificial tears during the initial phases of therapy. Once tear production is improved, artificial tears can generally be removed completely or their frequency reduced in the treatment plan. After treatment is initiated, reevaluation of tear production in one month is recommended. If ulcerative keratitis complicates keratoconjunctivitis sicca in the dog, more frequent evaluation is necessary. Cyclosporine, although an immunomodulating agent, is considered safe in the face of ulcerative keratitis, with concurrent antibiotic therapy. Caution is advised, however. When cyclosporine is delivered topically, no systemic toxicity has been noted in dogs given this drug chronically. This is prob-ably associated with the poor absorption of this drug across the GI tract and because it is delivered to the eye at very low concentra-tions which even if 100% absorbed, when divided over the body weight of the dog is well below even the therapeutic dose. Advanced detection methods have made it possible to measure trace levels of cyclosporine in the blood of dogs being topically treated for dry eye. The clinical implication of this finding is uncertain at this time. Dosage Forms/Regulatory Status Optimmune® ointment is the approved formulation of topical cy-closporine for the management of dry eye in dogs. Compounding of topical cyclosporine drops was popular before the introduction, approval, and marketing of Optimmune® ointment. Clinicians persistently using compounded formulations of cyclosporine eye drops may be outside of expected ethical and legal standards of practice except under very specific situations. The use of commer-cially available ophthalmic products instead of compounded medi-cations is highly recommended. Optimmune® is first applied 2 or 3 times daily and frequency of daily application is adjusted based on clinical response. VETERINAR y-LAb ELED PRODu CTS: Cyclosporine Ophthalmic Ointment 0. 2%; Optimmune® (Scher-ing-Plough); (Rx) Hum AN-LAb ELED PRODu CTS: Cyclosporine 0. 05% Ophthalmic Emulsion; Restasis® (Allergan). Note : the concentration of this product has not been shown to in- | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 969 crease tear production in dogs. Patients failing to respond to the veterinary approved ophthalmic ointment may respond to com-pounded cyclosporine 1% ophthalmic solution or tacrolimus 0. 03% ophthalmic solution. TAcrolimus (OPHTHALm IC) (ta-kroe-li-mus) Indications/Pharmacology Tacrolimus has recently been studied at the University of T ennessee College of Veterinary Medicine where investigators found it equally effective as cyclosporine and effective for cyclosporine-resistant cases of KCS. It exerts its effects through a mechanism similar to that of cyclosporine, however exact mechanisms of action in caus-ing tear production are still being determined. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None appropriate for the eye. At the time of publication, Fujisawa, Inc. has granted exclusive rights to Sucampo, Inc. to study, develop, and market an ophthalmic tacrolimus formulation for use in KCS. Note : Protopic ® topical ointment is a topical tacrolimus formulated with propylene carbonate that is known to deplete cholinesterase and to be an ophthalmic irritant and should not be used in the eye. Tacrolimus 0. 01-0. 03% solutions and ointments should be pre-scribed through a compounding pharmacy until a suitable com-mercially available product are available. Artificial Tear Products/ Ocular Lubricants Ar Ti Fici Al Te Ars/ ocul Ar lu Bric An Ts Indications/Pharmacology Artificial tear solutions are aqueous isotonic, p H buffered viscous solutions that serve as a lubricant for dry eyes and associated eye ir-ritation due to dry eye syndromes. They are often useful adjuncts in keratoconjunctivitis sicca in dogs early in cyclosporine therapy. Ocular lubricants are white petrolatum-based products that serve to lubricate and protect eyes. They are particularly useful dur-ing anesthetic procedures where animals' eyes may remain open and during which time tear production is dramatically reduced. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: There are a plethora of products available with a variety of formula-tions and trade names. All are OTC. Some commonly known prod-ucts include: Artificial T ear Products (Methylcellulose-based): Adsorbotear® (Al-con); Comfort Tears® (Pilkington Barnes Hind); Gen Teal® (Ciba Vision); Isopto-Tears® (Alcon); Tears Naturale® (Alcon); Lacril® (Allergan)Artificial T ear Products (Polyvinyl Alcohol-based): Hypotears® (Io-lab); Liquifilm Tears® (Allergan); Tears Plus® (Allergan)Artificial T ear Products (Glycerin-based): Dry Eye Therapy® (Bausch & Lomb); Eye Lube A® (Optopics) Ocular Lubricants (Petrolatum-based): Lacri-Lube® S. O. P. (Aller-gan); Akwa Tears® (Akorn) o Ph Th Almic irri GAn Ts Indications/Pharmacology Sterile isotonic solutions are used for flushing the nasolacrimal sys-tem and for removing debris from the eye. They are also used to remove excess stain after diagnostic staining of the cornea. Sterile lactated Ringer's solution (LRS) is well tolerated by the surface of the eye as is a balanced salt solution (BSS). Extraocular irrigating solutions may contain preservatives. Intraocular irrigating solu-tions (used during surgical procedures) do not contain preserva-tives and also contain electrolytes that are required for normal cell function. Suggested Dosages/Precautions/Adverse Effects Extraocular: Use to flush eye as necessary; control rate of flow by exerting pressure on bottle. Intraocular: Refer to both established practices for each surgical procedure as well as the specific manu-facturers' recommendations. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Eye Rinse® (Butler); (OTC): Contains: water, boric acid, zinc sulfate, glycerin, camphor. Note: This product is not labeled for use as an irrigant per se, but as an aid in cleaning the eye and removing eye stains. Hum AN-LAb ELED PRODu CTS: Common trade name products for extraocular irrigation: AK-Rinse® (Akorn), Blinx® (Pilkington Barnes Hind), Collyrium for Fresh Eyes Eye Wash® (Wyeth-Ayerst), Dacriose® (Iolab), Eye Irri-gating Solution® (Rugby), Eye-Stream® (Alcon), Eye Wash® (sev-eral manufacturers), Eye Irrigating Wash® (Roberts Hauck), Irrigate Eye Wash® (Optopics), Optigene® (Pfeiffer), Star-Optic Eye Wash® (Stellar), Visual-Eyes® (Optopics). All are OTC. Common trade name products for intraocular irrigation: Note : Most of these products contain Balanced Salt Solution (BSS) = Na Cl 0. 64%, KCl 0. 075%, Ca Cl 22H20 0. 048%, Mg Cl 26H20 0. 03%, Na acetate trihydrate 0. 39%, sodium citrate dihydrate 0. 17%, sodium hydroxide and/or hydrochloric acid to adjust p H, and water: Bal-anced Salt Solution (various manufacturers), BSS® (Alcon), Iocare Balanced Salt Solution® (Iolab); All are Rx. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
970 OPHTHALm IC PRODu CTS BSS + solutions that also contain dextrose, glutathione, bicarbon-ate, phosphate are also available as: BSS Plus® (Alcon) and AMO Endosol Extra® (Allergan); All are Rx. Topical Hyperosmotic Agents Polysul Fon ATed Glycos Amino Glyc An (OPHTHALm IC) Indications/Pharmacology Polysulfated glycosaminoglycan (PSGAG) Adequan® (Luitpold) in-hibits a number of enzymes (lysozyme, hyaluronidase, and serine proteases), decreases prostaglandin E2 synthesis, reduces produc-tion of toxic superoxide radicals, and increases synthesis of collagen proteoglycans and hyaluronic acid. Thus polysulfated glycosamino-glycan, originally developed for use in degenerative osteoarthritis cases, has intriguing properties suggesting usefulness in corneal ulcer management. It has anecdotally been effective in promoting healing of indolent corneal ulcers in dogs but no studies in dogs have been published to date. A Brazilian study reported that when using a 5% PSGAG formulation was applied to indolent ulcers of horses, that 86% of eyes treated were considered healed within 3 weeks of initiation of therapy. Fibronectin and epidermal growth factors have also been applied in treating indolent ulcers but scientific studies remain to be pub-lished regarding efficacy. At the time of publication, surgical kerate-ctomy remains the most reliable treatment for indolent ulcers. Suggested Dosages/Precautions/Adverse Effects 1 drop of a 5% PSGAG solution in artificial tears applied to the af-fected eye(s) three times daily. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None, however the veterinary ap-proved Adequan® injection may be diluted 1:1 with sterile artificial tears to produce a 5% PSGAG solution. Hum AN-LAb ELED PRODu CTS: None. hy Per Tonic sodium chloride (OPHTHALm IC) Indications/Pharmacology The stroma of the cornea is the middle layer located between the outer epithelial layer on the surface of the eye and the inner single epithelial layer lining the cornea, called the corneal endothelium. The stroma consists of highly organized collagen bundles and a few keratocytes (fibroblasts). The spacing of the collagen bundles is critical to absolute clarity of the cornea. The spacing of these bundles is disturbed when fluid enters the stroma. Surrounded by water to the exterior (tears) and on the interior (aqueous humor) the relative dehydration of the stroma is maintained by an active ATP-dependent pump mechanism in the corneal endothelial cells. Degeneration of the corneal endothelium is a relatively common eye problem in older dogs and is a known genetic condition in Boston T errier and Chihuahua dogs. Fluid continuously seeps into the corneal stroma via the tear film and through aqueous humor passing between corneal endothelial cells. When the endothelial pumping capacity deteriorates, fluid retention in the stroma causes two problems. Visual impairment can eventually develop. The other common complication is the development of corneal ulcers. Edema fluid retained in the cornea pools into pockets called bullae which progressively migrate to the surface of the cornea, eventually draining through and disrupting the surface epithelium. This re-sults in very slow healing and painful corneal erosions in dogs (type II refractory ulcers). Hyperosmotic agents applied 2-3 times daily help to prevent recurrence of bullae and subsequent corneal ulcers after the erosions have healed. Because osmotic agents require an intact epithelial barrier in which to induce a pressure gradient (5% Na Cl commercial preparation versus 0. 9% Na Cl body fluids), they are not effective with respect to healing of stubborn corneal ulcers when present. They simply help to prevent re-ulceration once an intact epithelial barrier has been established. It may be said that these agents simply aggravate irritation already present when used in the face of ulcerative keratitis. Suggested Dosages/Precautions/Adverse Effects Muro 128 (5% Na Cl) eye drops or ointment are applied two to three times daily on an indefinite basis to the surface of eyes with corneal endothelial degeneration to prevent corneal ulceration. In the event of corneal ulceration, treatment is discontinued and sub-stituted for antibiotic and mydriatic treatment in addition to pro-cedures to promote healing of refractory type corneal ulcers. Muro 128 eye drops are available at a 2% and 5% concentration. The Muro 128 ointment is available at a 5% concentration. Because of limited contact time with eye drops, the 2% solution would not be considered for use in animals. Because of prolonged contact time associated with ointments, the 5% Muro 128 ointment is probably the best of the available products for use in animals. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: Sodium Chloride 2% Ophthalmic Solution in 15 m L btls; Adsorbo-nac® (Alcon), Muro 128® (Bausch & Lomb); (OTC) Sodium Chloride 5% Ophthalmic Solution in 15 m L btls; Adsorbo-nac® (Alcon), Muro 128® (Bausch & Lomb), AK-Na Cl® (Akorn), Muroptic-5® (Optopics); (OTC)Sodium Chloride 5% Ophthalmic Ointment in 15 m L btls; Muro 128® (Bausch & Lomb), AK-Na Cl® (Akorn); (OTC) Viscoelastic Substances Viscoelastic substances are vital to ocular surgery, minimizing loss of fluid from the anterior chamber while maintaining intraocu-lar space during surgical procedures. The purity and integrity of viscoelastics ensure tissue protection during and after surgery. Viscoelastics generally fall into two categories — cohesives‚ that tend to stick together‚ and dispersives‚ which are more likely to diffuse out into the anterior chamber. Cohesives‚ in general‚ cre-ate and maintain space very well in the anterior chamber and help stabilize tissue. Such viscoelastics are easily washed away at the end of the case‚ but are also‚ unfortunately‚ all too easily removed dur-ing phacoemulsification. Dispersives‚ that have lower viscosity‚ remain in the eye more readily‚ making them well-suited for dif-ficult cases. They are also excellent for various maneuvers‚ such as retrieving a lost lens fragment‚ attempting to viscoelevate cortex‚ or partitioning away a small piece that continues to get caught on the phacoemulsifier tip. Ophthalmic surgeons should be familiar with the advantages and disadvantages of several viscoelastics and real- | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
OPHTHALm IC PRODu CTS 971 ize the limitations encountered if the surgeon chooses to rely on a single viscoelastic. Veterinary ophthalmologist loyalty to brands of viscoelastics is well-earned as newcomer products to this field have frequently resulted in surgical disasters. Viscoelastics are also vital to tear replacement. hy Aluronic Acid (hye-a-loo-ron-ik as-id) Indications/Pharmacology Hyaluronic acid is a natural complex sugar of the glycosaminogly-can family and is a long-chain polymer containing repeating disac-charide units of Na-glucuronate-N-acetylglucosamine. Hyaluronic acid is indicated for use as a surgical aid in cataract extraction (intra-and extracapsular), IOL implantation, corneal transplant, glaucoma filtration and retinal attachment surgery. In surgical procedures in the anterior segment of the eye, instillation of hy-aluronic acid serves to maintain a deep anterior chamber within corneal endothelium and other surrounding tissues. Furthermore, its viscoelasticity helps to push back the vitreous face and prevent formation of a postoperative flat chamber. In posterior segment surgery hyaluronic acid serves as a surgical aid to gently separate, maneuver and hold tissues. Hyaluronic acid creates a clear field of vision thereby facilitating intra-and post-operative inspection of the retina and photocoagulation. Suggested Dosages/Precautions/Adverse Effects A sufficient amount of hyaluronic acid (generally 10% concentra-tion) is slowly, and carefully introduced (using a cannula or needle into the anterior chamber. Injection of hyaluronic acid can be per-formed either before or after delivery of the lens. Injection prior to lens delivery will, however, have the additional advantage of pro-tecting the corneal endothelium from possible damage arising from the removal of the cataractous lens. Hyaluronic acid may also be used to coat surgical instruments and the IOL prior to insertion. Additional hyaluronic acid can be injected during surgery to re-place any hyaluronic acid lost during surgical manipulation. T opical solutions of hyaluronic acid are also used to provide a viscoelastic shield to the cornea and provide prolonged relief from ocular sur-face discomfort. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: Hyaluronic acid 10% Solution: 2 m L pre-filled syringe; Hylartin-V® (Pfizer Pharmacia); I-Drop Med® 0. 3% solution, 20 x 1 m L preser-vative-free unit dose containers; (Rx) Hum AN-LAb ELED PRODu CTS: Hyaluronic acid 10%-23%: Healon® products (Pfizer); (Rx) Cytotoxic Ophthalmic Agents cis Pl ATin Be Ads (sis-pla-tin) Indications/Pharmacology Cisplatin 1. 6 mg biodegradable beads are used for intralesional che-motherapy in various cutaneous neoplasia including squamous cell carcinoma and sarcoids in equine patients. A recent retrospective case series study demonstrated that implantation of cisplatin beads into cutaneous neoplasia was an effective method of treatment for these tumors. Implantation of commercially available beads is less time consuming and safer than intralesional injection of cytotoxic agents suspended in fixed oils. Dosage Forms/Regulatory Status VETERINAR y APPROVED PRODu CTS: Matrix III Cisplatin Beads: 1. 6 mg per 3 mm bead; 3 beads per packet; (Royer Biomedical, Inc. ), (Rx) Hum AN APPROVED PRODu CTS: None 5Fluorour Acil (flure-oh-yoor-a-sil) Indications/Pharmacology/Suggested Dosage 5-fluorouracil is a potent cytotoxic chemotherapeutic agent used for the topical therapy of equine limbal and eyelid squamous cell carcinoma. It is also used as an antimetabolite to limit fibrosis over the body of gonioimplant devices used to artificially shunt aqueous humor out of the eye in glaucoma as well as improve long-term filtering performance of the implant. 1% solution applied to the affected eye three times daily. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None. Must be compounded from the injectable product by an appropri-ately trained compounding pharmacist in a biological safety cabi-net approved for preparation of cytotoxic agents mi Tomycinc (mye-toe-mye-sin) Indications/Pharmacology Mitomycin C is a potent cytotoxic chemotherapeutic agent used for topical therapy of equine limbal and eyelid squamous cell car-cinoma. It is also used as an antimetabolite to limit fibrosis over the body of gonioimplant devices used to artificially shunt aqueous humor out of the eye in glaucoma as well as improve long-term filtering performance of the implant. Suggested Doses/Precautions 0. 4% solution applied initially followed by 0. 04% solution applied topically three times daily for 21 days. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None Must be compounded from the injectable product by an appropri-ately trained compounding pharmacist in a biological safety cabi-net approved for preparation of cytotoxic agents. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
972 OPHTHALm IC PRODu CTS Sympathomimetics hydroxy Am Phe TAmine (hye-drox-ee-am-fe-ta-meen) Indications/Pharmacology Hydroxyamphetamine is an indirectly acting sympathomimetic which is used to diagnose Cranial Nerve III denervation syndromes such as Horner's Syndrome. Hydroxyamphetamine stimulates re-lease of norepinephrine from postganglionic neurons and there-fore amplifies pupil dilation response in hypersensitive, denerved neurons. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None Must be compounded by an appropriately trained compounding pharmacist. coc Aine (OPHTHALm IC) (koe-kane) Indications/Pharmacology Cocaine is an indirectly acting sympathomimetic which is used to diagnose Cranial Nerve III denervation syndromes such as Horner's Syndrome. Cocaine prevents reuptake of norepinephrine into post-ganglionic neurons and therefore amplifies pupil dilation response in hypersensitive, denerved neurons. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None Must be compounded by an appropriately trained compounding pharmacist. Anticollagenase Agents Ace Tylcys Teine (a-se-teel-sis-teen) Indications/Pharmacology Acetylcysteine is a mucolytic agent which is also used to stop the melting effect of collagenases and proteases on the cornea. Acetylcysteine is useful in halting melting through inhibition of metalloproteinases, but is not felt to be useful for melting caused by infectious agents. Suggested Dosages/Precautions/Adverse Effects Acetylcysteine 5% solution is dosed 1 drop in the affected eye ev-ery 1-2 hours for the first 24 hours and then 3-4 times daily for the next 7-10 days. Acetylcysteine solutions are diluted with artifi-cial tears to a final concentration of 5% prior to administration as commercially available solutions of 10% and 20% are topically ir-ritating. Acetylcysteine possesses a foul, sulfur-like smell and own-ers should be informed that this foul odor does not indicate drug deterioration. Acetylcysteine is unstable at room temperature and solutions should be refrigerated. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None; Mucomyst® 10% and 20% solution for inhalation may be used to compound a 5% solution in artificial tears. ede TATe disodium (ed-a-tayt) Indications/Pharmacology Edetate Disodium (Sodium EDTA) is a chelating agent that is also used to stop the melting effect of collagenases and proteases on the cornea. EDTA is useful in halting melting through inhibition of matrix metalloproteinases, but is not felt to be useful for melting caused by infectious agents. As the effect of EDTA on metallopro-teinases is reversible, it must be administered several times daily to be effective. Suggested Dosages/Precautions/Adverse Effects 0. 05%-1% Solution applied as 1 drop in the affected eye several times daily. Dosage Forms/Regulatory Status VETERINAR y-LAb ELED PRODu CTS: None Hum AN-LAb ELED PRODu CTS: None EDTA solutions must be compounded by an appropriately trained compounding pharmacist. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
COm POu NDING OPHTHALm IC PRODu CTS 973 Principles of Compounding Ophthalmic Products GIGI DAVIDSON, DICVP Physiochemical Considerations for Compounding Ophthalmic Preparations The availability of suitable commercially available products for ev-ery veterinary ophthalmic indication is highly unlikely. Many agents used in veterinary ophthalmology are no longer or never were com-mercially available. Examples of agents that are commonly used by veterinarians but are no longer commercially available currently include oxytetracycline ophthalmic ointment, idoxuridine oph-thalmic solution and ointment, miconazole solution, vidarabine ophthalmic solution, trifluridine ophthalmic solution, tetracycline ophthalmic solution, rose bengal solution, and chloramphenicol ophthalmic ointment. Even if commercially available, products may be of inappropriate concentration to achieve a therapeutic effect in a given patient (e. g., cyclosporine A) or may have agents and ex-cipients that have adverse effects in animal patients (e. g., neomycin sulfate in cats). In other cases, no product is commercially available and must be compounded from other non-ophthalmic drugs or from bulk chemicals (e. g., acetylcysteine ophthalmic solution and disodium edetate ophthalmic solution). For these reasons, pharma-cists are frequently called upon to compound products to be used in the animal eye. These products may be administered topically in the form of solutions, suspensions or ointments, by periocular or intraocular injection, by drug-implanted collagen shields, or by drug-impregnated disposable contact lens delivery systems. The quality and sterility of these products is critical. T o ensure adequate stability, uniformity, and sterility, both the American Society of Health-Systems Pharmacists and the United States Pharmacopoeial (USP) Convention have published guidelines for pharmacy-pre-pared ophthalmic products (See Appendix 1). These guidelines ad-dress the following areas of concern. Validation of Formulation Before compounding any product for ophthalmic use, the pharma-cist should obtain documentation that substantiates the stability, safety and benefit of the requested formulation. Pharmacists may call the manufacturer of the drug, refer to primary literature, call re-gional eye centers, or call professional compounding organizations to obtain such information. If no such documentation is available, the pharmacist must employ professional judgment in determin-ing a suitable formulation for ophthalmic administration. Factors to consider when making this judgment include: sterility, tonicity, p H and buffering, toxicity of the drug, need for preservatives, solu-bility, stability in the chosen vehicle, viscosity, packaging, and any precautions necessary to keep drug residues from occurring in any food-producing animals. Documentation A written procedure for each ophthalmic product compounded should be recorded and kept in a readily retrievable place. This mas-ter formulation sheet should indicate the name of the product, the dosage form, the specifications and source of each ingredient used, the weights and measures of each ingredient used, the equipment required, a complete description of each step in the compound-ing process with special notation of aseptic techniques utilized and which method of terminal sterilization is appropriate, beyond-use dating, storage requirements, specific packaging requirements, sample label and auxiliary labeling, quality control testing per-formed, and references for formula. Production records for each batch should include the date of compounding, lot or batch num-ber assigned, the manufacturer and lot number and expiration date of each ingredient used, a sign-off provision for compounder and checker, the amount compounded, and the projected beyond-use date for the batch compounded. Sterility Ophthalmic dosage forms must be compounded in aseptic condi-tions. Sterility is the most important consideration for ophthalmic products. Contaminated ophthalmic products can result in eye in-fections leading to blindness or even loss of the eye, especially if pathogens such as Pseudomonas are present. Eye infections from contamination can also lead to systemic infections requiring hos-pitalization and may even result in death. All ophthalmics should be compounded in a laminar flow hood that has undergone annual checkups and certification of acceptable performance. It is also im-portant to note that the laminar flow hood does not guarantee steril-ity. The compounding pharmacist must also use impeccable aseptic technique when handling products intended for use in the eye. (See Appendix 2 for standard operating procedures in a laminar airflow hood. ) All products must be rendered sterile after formulation in the laminar flow hood. Sterilization of the final product is most easily achieved through filtration through 0. 2µ filters, which also remove particulate matter. This method is obviously only suitable for ophthalmic solutions. Ophthalmic suspensions and ointments must be sterilized by other means to avoid filtering out active drug. Other methods of sterilization available to the pharmacist include dry heat, autoclaving, and ethylene oxide gas sterilization. Gamma radiation is also commercially available for bulk sterilization, but is very expensive. Preservatives may also be added to prevent bacte-rial growth, especially if the container is intended for multiple use. The preservative selected must be compatible with the active drug and excipients as well as non-toxic to the eye or to the patient. A description of commonly used ophthalmic preservatives and maxi-mal concentrations in provided in Table 1. Table 1. Agents used for preserving ophthalmic products. Agent maximum concentration (%)* Benzalkonium chloride 0. 01 Benzethonium chloride 0. 01 Phenylmercuric acetate 0. 004 Phenylmercuric nitrate 0. 004 Methylparaben 0. 2 Propylparaben 0. 04 Thiomersol 0. 01 Chlorobutanol 0. 5 *As recommended by FDA Advisory Review Panel on OTC Ophthalmic Drug Products Clarity Drugs prepared as ophthalmic solutions should be free from for-eign particles. This can be accomplished through filtration with a 0. 45µ filter needle attached to a sterile syringe, or through the use of clarifying agents such as polysorbate 20 (maximum of 1%) and polysorbate 80 (maximum of 1%). Drugs prepared as ophthalmic suspensions, obviously cannot be filtered, but must be of a particle size that does not irritate or scratch the cornea. A micronized form | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
974 COm POu NDING OPHTHALm IC PRODu CTS of the drug is required. The use of an ointment mill is highly rec-ommended to decrease particle size for ophthalmic ointments. Tonicity Ophthalmic products do not need to be isotonic if the contact time with the cornea is only for a few minutes. The eye can tolerate a range of 200 - 600m Osm/L for short periods of time. For oint-ments, irrigations and products that will remain in contact with the eye longer than a few minutes, isotonic products should be used. Hypotonic agents may cause corneal edema and hypertonic agents may dehydrate the cornea and cause pain. T ear fluid and normal sa-line have identical osmotic pressures making 0. 9% sodium chloride an excellent vehicle for ophthalmic products. For products that are hypotonic, sodium chloride equivalencies can be used to determine how much sodium chloride to render the product isotonic. (Fig. 1) buffering and p H Ophthalmic preparations are generally buffered in a range from 4. 5 - 11. 5. Buffering is necessary to provide maximal stability of the drug or for comfort and safety of the patient. Alkaloids such as atropine and pilocarpine are usually buffered. If the activity and stability of the drug are not p H dependent, and the p H of the product is not irritating, then buffers may be omitted from the for-mulation. Commonly used buffers for ophthalmic preparations include Palitzsch buffer, boric acid buffer, boric acid/sodium bo-rate buffer, sodium acetate/boric acid buffer, Sorensen's modified phosphate buffer, Atkins and Pantin buffer solution, Feldman buf-fer, and Gilford ophthalmic buffer. Formulations for these solutions and ratios required to achieve a desired p H are referenced in the International Journal of Pharmaceutical Compounding, Vol. 2, No. 3 May/June 1998. Viscosity Enhancers Because tears and blinking reflexes reduce the total amount of drug available for penetration, an increase in residence time in the eye will increase drug absorption. Increasing the viscosity of the drug is the most common way to prolong contact time. Methylcellulose is the most commonly used agent and is generally formulated at a concentration of 0. 25%. Hydroxypropylmethylcellulose is used in concentrations of 0. 5 - 1%. Polyvinyl alcohol has also been used in concentrations of 0. 5 - 1% w/v. Agents used to increase the viscos-ity of ophthalmic products are shown in Table 2. Table 2. Agents used to increase viscosity of ophthalmic solutions and suspensions. Agent maximum Concentration (%) Hydroxyethylcellulose 0. 8 Hydroxypropylmethylcellulose 1. 0 Methylcellulose 2. 0 Polyvinyl alcohol 1. 5 Polyvinylpyrrolidone 1. 7 Quality Control Finished products should be thoroughly inspected visually for clarity and uniformity of suspension. The p H of the final product should always be checked and the value recorded on the master formula record for that batch. Most compounded products should have a p H of 5-7 unless otherwise indicated for stability or penetra-tion of ocular tissue. Practitioners compounding large volumes of ophthalmic products should periodically perform testing to ensure sterility. Various agencies provide this service. The nearest college of pharmacy can be consulted for a list of providers of this service. Packaging Ophthalmic preparations should be packaged in sterile dropper bottles (glass or plastic), or individual doses can be placed in ster-ile syringes with sterile tip caps. Ointments should be packaged in sterile ointment tubes and heat-sealed. beyond use Dating The USP/NF standards for preparation of ophthalmic medications indicate that, unless otherwise documented, the beyond-use date for water containing formulations is 14 days. For non-aqueous liquids, the recommendation is not more than 25% of the time remain-ing until the expiration date of the starting product or six months, whichever is earlier. For all other products, the expiration dating should be the duration of therapy or 30 days whichever is shorter. These beyond-use recommendations can be extended in the face of supporting, valid, scientifically conducted stability information. Considerations for use of ophthalmics in veterinary patients Veterinary patients experience many of the same ophthalmic dis-eases and conditions as humans, and treatments are often based on human therapy. Animals, however, have a variety of species-related characteristics that might cause human-designed therapies to fail or be toxic. Behavioral characteristics such as grooming may sig-nificantly reduce the contact time of ophthalmic agents with the eye, and increase systemic exposure through ingestion. Anatomical differences such as size must be considered. Horses and other large animals may simply elevate their eyes out of a caregiver's reach if ophthalmic treatments are objectionable. Specialized delivery de-vices have been created to treat these patients. Subcutaneous palpe-bral lavage systems are tunneled under the skin over the animal's brow and allow for passage of medication through long catheters that are easily reachable by caregivers. Food-producing animals require special consideration. Systemic absorption of ophthalmic agents in food-producing animals could result in violative drug residues in food intended for human consumption. General Principles of Ocular Penetration Corneal penetration Drugs must generally be administered topically to treat corneal and intraocular conditions. While the eye would appear to be an easy target for topical administration, the eye has several anatomical bar-riers to prevent penetration by foreign substances. Instantaneous tear production, strong blinking reflexes, and alternating layers of lipophilic and hydrophilic tissue all work in conjunction to prevent entry of foreign substances. The clear tissue known as the cornea covers the visible outer surface of the eye between the lids. The cor-nea must be clear in order to allow for vision, and nature has ac-complished this by omitting blood vessels in the cornea. Because of this lack of vascular tissue, systemically administered drugs do not penetrate into the cornea. The cornea is composed of several layers of lipophilic (outer layers) and hydrophilic (inner layer) tis-sue. For a topically administered drug to fully penetrate the cornea, the drug must be able to exist in ready equilibrium between both ionized and non-ionized forms (e. g., chloramphenicol, atropine, and pilocarpine). Most antibiotics are water-soluble and will not penetrate the lipophilic outer layer of the cornea unless ulcers are present. Small molecular weight (<350) and high local concentra- | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
COm POu NDING OPHTHALm IC PRODu CTS 975 tion of drugs will also increase penetration even if the drugs are ionized and hydrophilic. T opical administration is ideal as it allows for very high local concentrations of drug on the cornea. For a topi-cally administered drug to reach the anterior chamber and bind to intraocular structures (e. g., ciliary body, iris, aqueous humor), the drug must pass through the cornea. Drugs may also reach the an-terior chamber to some extent by passive absorption through the conjunctiva. Key points for corneal penetration of drugs: lipophilic !! equilibrium between ionized and non-ionized forms!! small molecular weight (<350)!! high local concentrations!! Intravitreal Penetration: T opically administered drugs reach the vitreous only in very small concentrations. T o treat severe conditions of the anterior chamber (uveitis) as well as intravitreal conditions, drugs must be adminis-tered by periocular or intraocular injection. The periocular routes include subconjunctival injection and sub-T enon's membrane in-jection while the intraocular routes are intracameral injection (di-rectly into the aqueous humor) or intravitreal injection (directly into the vitreous humor). Periocular injections can be adminis-tered under sedation and topical anesthesia. Intraocular injections are usually only performed in the operating room while the pa-tient is completely anesthetized. These routes bypass the outermost chemical and physical ocular defenses and allow for better con-centration of drug in the vitreous. The volume of administration for these routes is relatively small. Periocular injections should not exceed 0. 5 - 1. 0 m L in small animals and 2 m L in large animals. Intraocular injections should not exceed 0. 1 m L in small animals and 0. 25 m L in large animals due to the risk in increasing intraocu-lar pressure. Drugs injected into the eye should be free of preserva-tives and buffers. Route of Therapy for Given Ocular Target: Tissue Routes of Administration Eyelids Topical, systemic Corneal surface Topical Anterior segment Topical if good penetration or mild disease Systemic if poor penetration or severe disease Posterior segment Systemic or intraocular injection (rarely) Any site where multiple dosing is impractical Subconjunctival depot injection Questions to Ponder Prior to Compounding Ophthalmic Products Where is the target of therapy? (eyelids, corneal surface, cornea, 1. anterior segment, posterior segment) What is the character of the drug?2. Lipophilic? Hydrophilic?!! What is the molecular weight?!! What is the inherent toxicity of the drug to the eye (gentami-!! cin)? T o the caregiver (chloramphenicol); to the patient (neo-mycin sulfate in cats)?Is there data to support what concentration is necessary for !! corneal penetration?Is the drug soluble in a vehicle that is not toxic to the eye? !! If not soluble, will the particle size of the suspension or the !! ointment scratch the corneal or conjunctiva?What is the p H of the final product? Is this in an acceptable !! range to avoid irritation (4. 5-11. 5)? What is the tonicity of the final product? Hypertonic? Hy-!! potonic? How long will the product be in contact with the cornea if not isotonic?Will the viscosity need to be enhanced in order to prolong !! contact with the eye? Which agent is compatible?What is the duration of therapy? Will the product require !! preservation if long term multiple use? Which preservative is compatible? | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
976 DERm ATOLOGICAL PRODu CTS Dermatological Agents, Topical The following section lists many of the active ingredients and corresponding preparations used topically for their local action in vet-erinary medicine. It includes both veterinary-labeled dermatological products and some potentially useful human-labeled products. Active ingredients are listed by therapeutic class. Products that are applied topically, but are absorbed systemically and used primarily for their systemic effects are found in the general monograph section. For veterinary products, refer to the complete label for additional information. Reviewed and Contributions By: Sandra Koch, DVM, MS, DACVD College of Veterinary Medicine, University of Minnesota St. Paul, MN Andrea G. Cannon, DVM, DACVD Animal Dermatology & Allergy Rocklin, CA; Modesto, CA; Boise, ID Veterinary-Labeled Aluminum Acetate Solution Topical Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Cort/Astrin Solution® (Vedco) Solution: all products contain: Hydrocortisone 1%; Burow's Solution 2%OTC (Vet) 1 oz. dropper btl, 16 oz. Corti-Derm Solution® Solution OTC (Vet) 1 oz. Hydro-Plus® (Phoenix) Solution OTC (Vet) 1, 2, 16 oz. Bur-O-Cort 2:1® (Q. A. Labs) Solution OTC (Vet) 1, 16 oz. Hydro-B 1020® (Butler) Solution OTC (Vet) 1, 2, 16 oz. Human-Labeled Aluminum Acetate Topical Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s) Bluboro Powder® (Allergan Herbert)Powder Packets: Aluminum sul fate and Calcium acetate 1. 8 g OTC (Human) Packets of 12 or 100/box. One packet dissolved in 16 oz (480 m L) of water makes a 1:40 (2. 5%) modified Burow's sol. Domeboro Powder® (Miles) Powder Packets: Aluminum sulfate and Calcium acetate OTC (Human) Packets of 12 or 100/box. One packet dissolved in 16 oz (480 m L) of water makes a 1:40 (2. 5%) modified Burow's sol. Pedi-Boro Soak Paks® (Pedinol)Powder Packets: Aluminum sul fate and Calcium acetate 2. 7 g OTC (Human) Packets of 12 or 100/box. One packet dissolved in 16 oz (480 m L) of water makes a 1:40 (2. 5%) modified Burow's sol. Buro-Sol® (Doak) Powder Packets: Aluminum acetate 0. 23%OTC (Human) 12 packets/box Non-Corticosteroid Antipruritics, Topical Aluminum Ace TATe solu Tion (Burow's solu Tion or modi Fied Burow's solu Tion) (ah-loo-mi-num ass-ih-tate) For otic use, refer to the Otic appendix Indications/Actions An astringent antipruritic agent, Burow's solution can be useful for adjunctive treatment of moist dermatitis conditions. Burow's solution also has acidifying qualities and is mildly antiseptic. Suggested Dosages/Precautions/Adverse Effects T opical use of Burow's solution (alone) is usually as a wet compress or dressing. Application for 15-30 minutes is generally recommended and the affected area is air-dried between applications. Use can be as often as necessary, but every 4-6 hours is often employed. The veterinary-labeled products containing hydrocortisone may be directly applied. As Burow's solution products come in various dosage forms (powder or tablets for dissolving, liquid); refer to package directions for proper dilutions. Dilutions of 1:40, 1:20, or 1:10 are com-monly used. Do not use plastic or any occlusive dressing material to prevent evaporation. Use room temperature water for dissolving and applica-tion. Avoid contact with eyes. Clients should wash hands after application or wear gloves when applying. May cause skin irritation on some patients. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
DERm ATOLOGICAL PRODu CTS 977 Product (Company) Form: Concentration Label Status Other Ingredients; Size(s) Domeboro Tablets® (Miles) Effervescent Tablets: Aluminum sulfate and Calcium acetate OTC (Human) Tablets of 12 or 100/box. One tablet dissolved in 16 oz (480 m L) of water makes a 1:40 (2. 5%) modified Burow's sol Burow's Solution (various) Solution: Aluminum acetate (Burow's)OTC (Human) 480 m L bottles di Phenhydr Amine hcl, To Pic Al (dye-fen-hye-dra-meen) Benadryl® For systemic use, see the monograph found in the main section Indications/Actions A first generation antihistamine, diphenhydramine has some local anesthetic activity that probably is its main antipruritic mechanism of action. Diphenhydramine may be absorbed in small amounts transdermally, but should not cause systemic side effects. Precautions/Adverse Effects Avoid contact with eyes or mucous membranes. Do not apply to blistered or oozing areas of skin. Clients should wash hands after ap-plication or wear gloves when applying. Prolonged use could potentially cause local irritation and/or hypersensitization. Veterinary-Labeled Diphenhydramine HCl Topical Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Hista-Calm® Spray (Virbac) Spray: 2% Rx (Vet) In an aqueous vehicle. Also contains Omega3 & 6 essential fatty acids. 59 m L. Shake well before use; labeled for use on dogs or cats 2-3 times a day Resihist® Leave-On Conditioner (Virbac)Conditioner: 2% Rx (Vet) Water, cetyl alcohol base. 8, 16 oz. Labeled for use on dogs and cats Histacalm® Shampoo (Virbac) Shampoo: 2% Rx (Vet) Colloidal oatmeal base; also contains Omega6 fatty Acids. 8, 16 oz; 1 gal. Labeled for use on dogs and cats Human-Labeled Diphenhydramine HCl Topical Products Product (Company) Forms: Concentration Label Status Other Ingredients; Size(s); Comments Products include: Benadryl®, Dermamycin®, Ziradryl®, Caladryl® (various manufacturers and additional trade name modifiers such as Maximum Strength, etc may be found)Spray: 2%Lotion: 1%Gel: 1%, 2% Cream: 1%, 2%OTC (Human) These products may also contain astringents (calamine, zinc acetate), other antihistamines (pyrilamine), and /or counter irritants (menthol, camphor) Pr Amoxine hcl, To Pic Al (pra-moks-een) Indications/Actions A surface and local anesthetic to peripheral nerves not related structurally to procaine-type anesthetics, pramoxine is often added to other topicals to reduce pain and/or itching. Suggested Dosages/Precautions/Adverse Effects Depending on the product labeling, pramoxine 1% may be applied every 3-4 hours. Peak local anesthetic effects occur within 3-5 min-utes of application. It provides only temporary effects. Avoid contact with eyes; pramoxine is too irritating for ophthalmic use. Depending on product labeling, clients should wash hands after application or wear gloves when applying. Adverse effects are unlikely, but localized dermatitis is possible. Veterinary-Labeled Pramoxine Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Micro-Pearls Advantage Dermal-Soothe® Anti-Itch Spray (Evsco) Spray: 1% OTC (Vet) Lactamide monoethanolamine and Novasome® microvesicles. 12 oz. Shake well and repeat as necessary. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
978 DERm ATOLOGICAL PRODu CTS colloid Al o ATme Al (ko-loyd-al ote-meel) Indications/Actions Colloidal oatmeal is used topically as an antiinflammatory and antipruritic, but an exact mechanism for this effect is not known. It is thought that as the concentration of oatmeal increases, both its drying and antipruritic effects increase; it has been suggested that it may inhibit prostaglandin synthesis. Precautions/Adverse Effects Other than the potential for increased drying of already dry skin, colloidal oatmeal is very safe. In humans, there are some reports of contact dermatitis associated with its use. Veterinary-Labeled Colloidal Oatmeal Products Note: Products listed are those containing only colloidal oatmeal as the principle active ingredient. For other products that contain col-loidal oatmeal, see Diphenhydramine, Pramoxine, Hydrocortisone, Permethrin, or Pyrethrins listings. Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Relief® Spray (DVM) Spray: 1% OTC (Vet) Colloidal oatmeal. 8 oz. For dogs or cats. Labeled for daily use or as directed by DVM Pramoxine Anti-Itch® Spray (Davis)Spray: 1% OTC (Vet) 8 oz. For dogs or cats. Labeled for daily use or as directed by DVM Resiprox® Leave-On Lotion (Virbac) Lotion: 1. 5% Rx (Vet) Water, cetyl alcohol, stearyl alcohol base. 8 oz. Shake well. Use daily or as directed by DVM Micro-Pearls Advantage Dermal-Soothe® Anti-Itch Shampoo (Evsco) Shampoo: 1% OTC (Vet) Colloidal Oatmeal, Novasome® microvesicles, Skin respiratory fac tor. 12 oz, 1 gal. Labeled for dogs, cats, horses. Pramoxine Anti-Itch® Shampoo (Davis) Shampoo: 1% OTC (Vet) Colloidal oatmeal, emollients. 12 oz, 1 gal. Labeled for dogs, cats, puppies, kittens Relief® Shampoo (DVm) Shampoo: 1% OTC (Vet) Colloidal oatmeal, Omega6 FA's. 8, 12 oz, 1 gal. Micro-Pearls Advantage Dermal-Soothe® Anti-Itch Cream Rinse (Evsco)Rinse: 1% OTC (Vet) Colloidal Oatmeal, Novasome® microvesicles, Skin respiratory fac tor. 12 oz, 1 gal. Labeled for dogs, cats, horses. Pramoxine Anti-Itch® Creme Rinse (Davis)Rinse: 1% OTC (Vet) Colloidal oatmeal, emollients, Omega6 FA's. 12 oz, 1 gal. Labeled for dogs, cats, puppies, kittens Relief® Creme Rinse (DVM) Rinse: 1% OTC (Vet) Colloidal oatmeal, emollients, Omega6 FA's. 8, 12 oz, 1 gal. Human-Labeled Pramoxine Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Am Lactin® AP (Upsher Smith) Cream: 1% OTC (Human) Usually used for extremely dry, painful or itchy skin in humans. Prax® (Ferndale) Lotion: 1% OTC (Human) Usually used for extremely dry, painful or itchy skin in humans. Tronothane® (Abbott) Lotion: 1% OTC (Human) Usually used for extremely dry, painful or itchy skin in humans. Itch-X® (Ascher) Spray: 1% OTC (Human) Benzyl alcohol 10%, aloe vera gel. 60 m L. Itch-X® (Ascher) Gel: 1% OTC (Human) Benzyl alcohol 10%, aloe vera gel. 35. 4 g. Prame Gel® (Gen Derm) Gel: 1% OTC (Human) 0. 5% menthol, emollient base, benzyl alcohol. 118 g. Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Dermapet Dermallay® Conditioner (Derma Pet)Conditioner: 0. 75% OTC (Vet) 8 oz; 1 gal Epi-Soothe® Cream Rinse and Conditioner (Virbac) Conditioner: % not listed 8, 16 oz; 1 gal Resisoothe® Leave-On Conditioner (Virbac) Conditioner: % not listed 8, 16 oz; 1 gal. Shake well. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
DERm ATOLOGICAL PRODu CTS 979 Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Aloe & Oatmeal Skin and Coat Conditioner® (Vet Solutions, RXV, Vedco)Conditioner: % not listed OTC (Vet Aloe vera gel, vitamins A, D & E, chamomile. 16 oz; 1 gal. Dermapet Dermallay® Shampoo (Derma Pet)Shampoo: 2% OTC (Vet) 8 oz; 1 gal Epi-Soothe® Shampoo (Virbac) Shampoo: 2% OTC (Vet) Chitosanide, glycerin. Ingredients in free form and in Spherulites®. 8, 16 oz; 1 gal Cortisoothe Shampoo® (Virbac) Shampoo: Colloidal Oatmeal % not listed; Hydrocortisone 1%Rx (Vet) 8, 16 oz. Labeled for dogs and cats. Pearlyt® Shampoo (DVM) Shampoo: % not listed OTC (Vet) 12 oz; 1 gal. Hartz Living Groomer's Best Oatmeal Shampoo® (Hartz Mountain)Shampoo: % not listed Rx (Vet) 18 oz Aloe & Oatmeal Shampoo® (Vet Solutions, RXV, Vedco) Shampoo: % not listed Rx (Vet) Aloe vera. 16 oz; 1 gal. Foaming Silk Bath® (AAH) Shampoo: % not listed Rx (Vet) Aloe vera, vitamins A & E. 16 oz. Human-Labeled Colloidal Oatmeal Products Note: There are several human products available containing colloidal oatmeal, including creams, lotions and products to be added to the bath. Common trade names include: Aveeno®, Geri SS®, and Actibath®. Phenol/men Thol/c Am Phor (fee-nol; men-thol; kam-for) Indications/Actions When used in low concentrations, these agents can be used as counterirritants and may be added to proprietary or compounded products primarily as antipruritics. Camphor and phenol may also have some antiseptic properties. Precautions/Adverse Effects These compounds may cause local irritation and should not be used around or in eyes. Products containing phenol should not be used on cats. Veterinary-Labeled Phenol, menthol, or Camphor Products Note: There are also several over the counter products not listed containing menthol, phenol or camphor used primarily on equine pa-tients for overexertion, soreness, or stiffness. These include a variety of liniments (e. g., white liniment, Choate's liniment) or gels (e. g., Cool Gel®, Ice-O-Gel®, Shin-O-Gel®, etc. ). Product (Company) Form: Active Ingredients/Concentrations Label Status Other Ingredients; Size(s) Scarlet Oil Pump Spray (Dominion)Spray: Menthol, Phenol, Oil of Camphor, Oil of Eucalyptus & Oil of Pine each at 7. 5mg/m L; Oil of Thyme 2. 8mg/m L; Peru Balsam 1. 5mg/m L; Biebrich Scarlet Red 100 ppm. OTC (Vet) 500 m L. Labeled for superficial cuts, wounds, burns, etc for horses and mules. Shake well. lidoc Aine, To Pic Al lidoc Aine/Priloc Aine (eml A cre Am) (lye-doe-kane; prye-loe-kane) For systemic use of lidocaine, see the monograph found in the main section Indications/Actions Lidocaine is used topically as a dermal anesthetic or antipruritic and is included in several “hot spot” (acute moist dermatitis, pruritic lesions) products. When combined with prilocaine (commonly called EMLA cream), it may be useful for dermal anesthesia prior to in-vasive procedures (e. g., catheter placement, etc). | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
980 DERm ATOLOGICAL PRODu CTS Lidocaine exerts its anesthetic properties via alteration of cell membrane ion permeability, thereby inhibiting conduction from sensory nerves. Precautions/Adverse Effects T opical lidocaine may be absorbed systemically, but systemic toxicity is unlikely to occur unless used on a significant percentage of body area, for prolonged times or at high concentrations. Be extra vigilant in patients also receiving Class I antiarrhythmics (lidocaine, mexi-letine, or tocainide). Avoid contact with eyes and do not use in ears, unless specifically labeled for such. Clients should wash hands after application or wear gloves when applying. Hypersensitivity or skin irritation (burning, tenderness, etc) are possible, but apparently occur uncommonly. Products containing prilocaine (EMLA), may be more prone to causing (rarely) methemoglobinemia or systemic toxicity. Veterinary-Labeled Lidocaine Topical Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Allercaine® (Tomlyn) Spray: 2. 4% OTC (Vet) Denatonium benzoate (bittering agent), Benzalkonium Chloride 0. 1%. 4, 12 oz. Do not apply to entire body or to large areas of broken skin. Allerspray® (Evsco) Spray: 2. 4% OTC (Vet) Denatonium benzoate (bittering agent), Benzalkonium Chloride 0. 1%, aloe vera gel, allantoin, PEG75 lanolin. 4 oz. Dermacool w/ Lidocaine Spray® (Virbac)Spray: Concentration not listed OTC (Vet) Hamamelis extract, menthol. 4 oz Hexa-Caine® (PRN Pharmacal) Spray: 2. 4% OTC (Vet) Denatonium benzoate (bittering agent), Benzalkonium Chloride 0. 1%, aloe vera gel, allantoin, lanolin. 4, 8, 16 oz. Biocain® (Tomlyn) Lotion: 2% OTC (Vet) Bittran® II (bittering agent), Benzalkonium Chloride 0. 1%. 2, 4 oz. Human-Labeled Lidocaine Topical Products There are also several topical OTC products listed for human use, including sprays (2-2. 5%), liquids (2-4%), creams (0. 5-2%), gels (0. 5-2. 5%) and topical patches. Product (Company) Form: Concentration Label Status Other Ingredients; Size(s) EMLA® (Astra) Lidocaine/Prilocaine Cream (Generic various)Cream: Lidocaine 2. 5%; Prilocaine 2. 5%Rx (Human) Depending on manufacturer: 5, 15, 30 g. Antiinflammatory Agents, Topical Corticosteroids, Topical Note: There are at least 20 chemical entities (plus a variety of salts) used in humans for topical corticosteroid therapy. The following sec-tion includes many veterinary topical products and some human products that may be of use in veterinary medicine. Also, see the Otic section for more products. hydrocor Tisone (TOPICAL) (hye-droe-kor-ti-zone) Indications/Actions Considered a low potency topical corticosteroid, hydrocortisone may useful for adjunctive treatment of pruritic conditions. Because risks associated with hydrocortisone are significantly less when compared to higher potency corticosteroids, hydrocortisone is a reasonable first choice, particularly when treating large areas, or when used on smaller patients. Some products also contain the astringent Burow's solution, which may have additional antipruritic effects. Corticosteroids are non-specific anti-inflammatory agents. They probably act by inducing phospholipase A2 inhibitory proteins (lipo-cortins) in cells, thereby reducing the formation, activity, and release of endogenous inflammatory mediators (e. g., histamine, prostaglan-dins, kinins, etc). Corticosteroids also reduce DNA synthesis via an anti-mitotic effect on epidermal cells. T opically applied corticosteroids also inhibit the migration of leukocytes and macrophages to the area reducing erythema, pruritus and edema. Dosages/Precautions/Adverse Effects Initially, topical corticosteroids are usually used sparingly 2-4 times per day. Refer to individual product labeling for actual dosing rec-ommendations for veterinary products. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
DERm ATOLOGICAL PRODu CTS 981 Several veterinary topical products list tuberculosis of the skin or pregnancy as contraindications. Clients should wash hands after ap-plication or wear gloves when applying. Local skin reactions are possible, but unlikely to occur. Atrophy associated with skin fragility and comedones may be seen with long term, frequent use. Although systemic absorption is rare with hydrocortisone, long term use may lead to HPA axis suppression. Veterinary-Labeled Hydrocortisone Topical Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Corticalm Lotion® (DVM) Sulfodene HC AntiItch Lotion® (Farnam)Lotion: 1% Lotion: 0. 5%Rx (Vet)OTC (Vet)3, 6 oz. 1. 5 oz. Cortispray® (DVM) Spray: 1% Rx (Vet) 60 m L. Labeled for use on dogs, cats, horses. Dermacool HC Spray® (Virbac) Spray: 1% Rx (Vet) Hamamelis extract, lactic acid, menthol, propylene glycol. 2, 4 oz. Hartz Advanced Care Hydrocortisone Spray w/Aloe® (Hartz Mountain)Spray: 0. 5% OTC (Vet) Aloe. 5 oz. Hartz Advanced Care Extra Strength Hydrocortisone Spray w/Bitrex® (Hartz Mountain)Spray: 0. 75% OTC (Vet) Bitrex (bittering agent), aloe. 5 oz. Cort/Astrin Solution® (Vedco) Solution: all products contain: Hydrocortisone 1%Burow's Solution 2%OTC (Vet) 1 oz dropper btl, 16 oz. Corti-Derm Solution® (First Priority) OTC (Vet) 1 oz. Hydro-Plus® (Phoenix) OTC (Vet) 1, 2, 16 oz. Bur-O-Cort 2:1® (Q. A. Labs) OTC (Vet) 1, 16 oz. Hydro-B 1020® (Butler) OTC (Vet) 1, 2, 16 oz. Cortisoothe Shampoo® (Virbac) Hartz Advanced Care Hydrocortisone Shampoo w/Aloe® (Hartz Mountain)Shampoo: 1% Shampoo: 0. 5%Rx (Vet) OTC (Vet)Colloidal oatmeal base. 8, 16 oz. Labeled for use on dogs and cats. Aloe. 8 oz. Resicort Leave-On Conditioner® (Virbac)Conditioner: 1% Rx (Vet) 8, 16 oz. Hartz Advanced Care Hydrocortisone Spot® Liquid Spot: 0. 5% OTC (Vet) 3 x 3 m L tubes. For dogs and cats Human-Labeled Hydrocortisone Topical Products Note: Partial listing. There are many branded products available with hydrocortisone; these will be listed only when they have relatively unique formulations and concentrations. For more information on human-labeled hydrocortisone products, refer to a comprehensive human drug reference (e. g., Facts and Comparisons) or contact a pharmacist. Product (Company) Form: Concentration Label Status Size(s) Hydrocortisone Ointment Ointment: 0. 5, 1% OTC/Rx (Human). Status deter mined by labeling15, 20, 28. 4, 30 60, 120, 454 g. Hydrocortisone Ointment Ointment: 2. 5% Rx (Human) 20, 30 g Hydrocortisone Cream Cream: 0. 5, 1% OTC/Rx (Human). Status determined by labeling1 g pkts, 15, 20, 28. 4, 30, 60, 120, 454 g. Hydrocortisone Cream Cream: 2. 5% Rx (Human) 15, 20, 30, 60, 240, 454 g Hydrocortisone Lotion Lotion: 0. 5, 1% OTC/Rx (Human). Status determined by labeling30, 60, 120 m L. Hydrocortisone Lotion Lotion: 2. 5% Rx (Human) 60, 120m L Extra-Strength Corta Gel® (Norstar) Gel: 1% OTC (Human) 15, 30 g Alcortin® (Primus) Gel: 2% Rx (Human) 2 g Texacort® (Gen Derm) Solution: 1%, 2. 5% Rx (Human) 30 m L Penecort® (Allergan) Solution: 1% Rx (Human) 30, 60 m L Scalpicin® (Combe) Liquid: 1% OTC (Human) Menthol. 45, 75, 120 m L T/Scalp® (Neutrogena) Liquid: 1% OTC (Human) 60, 600 m L. Procort® (Roberts) Spray: 1% OTC (Human) 45 m L. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
982 DERm ATOLOGICAL PRODu CTS Product (Company) Form: Concentration Label Status Size(s) Cortizone-10 Quickshot® (Pfizer) Spray: 1% OTC (Human) 44 m L. Maximum Strength Cortaid® (Pharmacia Upjohn)Pump Spray: 1% OTC (Human) 45 m L. Tri Amcinolone Ace Tonide (TOPICAL) (trye-am-sin-ohe-lone ass-si-toe-nide) For systemic use, see the monograph found in the main section. Indications/Actions Considered a medium potency topical corticosteroid when used at concentrations less than 0. 5% (high potency), triamcinolone ac-etonide may useful for adjunctive treatment of pruritic conditions. Because risks associated with triamcinolone (HPA axis suppression, skin atrophy) are greater than with hydrocortisone, triamcinolone acetonide products are generally reserved for more serious pruritic conditions or when hydrocortisone is not effective. Triamcinolone can be found in a veterinary-labeled sole agent cream (Medalone®) or spray (Genesis®). It is also an ingredient in combination with antibiotics and anti-yeast ingredients in several veterinary products (e. g., Panalog®). Corticosteroids are non-specific anti-inflammatory agents. They probably act by inducing phospholipase A2 inhibitory proteins (lipo-cortins) in cells, thereby reducing the formation, activity, and release of endogenous inflammatory mediators (e. g., histamine, prostaglan-dins, kinins, etc). Corticosteroids also reduce DNA synthesis via an anti-mitotic effect on epidermal cells. T opically applied corticosteroids also inhibit the migration of leukocytes and macrophages to the area reducing erythema, pruritus and edema. Dosages/Precautions/Adverse Effects Initially, topical corticosteroids are usually used sparingly 2-4 times per day. Refer to individual product labeling for actual dosing rec-ommendations for veterinary products. Several veterinary topical products list tuberculosis of the skin or pregnancy as a contraindication. Systemic corticosteroids can be teratogenic or induce parturition during the third trimester of pregnancy in animals. If considering use during pregnancy, weigh the respective risks with treating versus potential benefits. Clients should wash hands after application or wear gloves when applying. Use care when treating large areas, or when used on smaller patients. Risks can be reduced by treating for only as long as necessary on as small an area as possible. Increased risks of HPA axis suppression, systemic corticosteroid effects (polydipsia/polyuria, Cushing's, gastrointestinal effects) and skin atrophy (skin fragility, due to atrophy, alopecia, localized pyoderma and comedones are other possible complications) occur as product concentration and duration of use increases. Local skin reactions (burning, itching, redness) are pos-sible, but unlikely to occur. Veterinary-Labeled Triamcinolone Acetonide Topical Products Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Medalone Cream® (MedPharmex)Cream: 0. 1% Rx (Vet) 7. 5, 15 g. Approved for dogs. Indications include allergic dermatitis and summer eczema. Genesis Topical Spray® (Virbac) Spray: 0. 015% Rx (Vet) 16 oz spray bottle. Approved for dogs. Indication is for control of pruritus associated with allergic dermatitis. Bacterial skin infection needs to be resolved prior to use. Strongly recommend referring to the package insert information for maximum allowable dosages, treatment durations, etc. Panolog Cream® (Fort Dodge) Cortalone Cream® (Vedco)Derma-Vet Cream® (MedPharmex)Cream: Nystatin 100,000 units/g Triamcinolone Acet. 1 mg Neomycin Sulf. 2. 5 mg Thiostrepton 2,500 units Rx (Vet) Aqueous vanishing cream. 7. 5, 15 g. Panalog and DermaVet labeled for use in dogs or cats. Cortalone labeled for dogs only. Panalog Ointment® (Fort Dodge)Animax Ointment® (Pharmaderm) Quadratop Ointment® (Butler) Derma-Vet Ointment® (MedPharmex)Dermalog Ointment® (RXV)Dermalone Ointment® (Vedco)Ointment: Nystatin 100,000 units/g Triamcinolone Acet. 1 mg Neomycin Sulf. 2. 5 mg Thiostrepton 2,500 units Rx (Vet) 7. 5, 15, 30, 240 m L. Labeled for use in dogs or cats. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
DERm ATOLOGICAL PRODu CTS 983 Human-Labeled Triamcinolone Acetonide Topical Products: Note: Partial listing. There are several topical branded products (two common trade names are Aristocort® and Kenalog®) available with triamcinolone. For more information on human-labeled triamcinolone products, refer to a comprehensive human drug reference (e. g., Facts and Comparisons) or contact a pharmacist. Product (Company) Form: Concentration Label Status Size(s); Comments Triamcinolone Acetonide Ointment Ointment: 0. 025, 0. 1, 0. 5% Rx (Human) 15, 20, 28. 4, 30, 60, 120, 454 g. Triamcinolone Acetonide Cream Cream: 0. 025, 0. 1, 0. 5% Rx (Human) 15, 20, 30, 60, 120, 240 454 g. Triamcinolone Acetonide Lotion Lotion: 0. 025, 0. 1% Rx (Human) 15, 60 m L. Kenalog® (Westwood Squibb) Aerosol Spray: 0. 1% Rx (Human) 23, 63 g. 10. 3% alcohol Nystatin-Triamcinolone Acetonide (various)Mycogen II® (Goldline) Mycolog-II® (Bristol Meyers Squibb) Myco-Triacet II® (Lemmon)Myconel® (Marnel)Cream: Nystatin 100,000 units/g Triamcinolone Acet. 0. 1%Rx (Human) Depending on product: 1. 5 g. pkts, 15, 30, 60, 120 g. Myco-Biotic II® (Moore) Cream: Nystatin 100,000 units/g Triamcinolone Acet. 0. 1%Neomycin Sulf. 0. 5%Rx (Human) Aqueous vanishing cream w/ white petrolatum. 15, 30, 60, 454 g. Be TAme Th Asone (TOPICAL) (bet-ah-meth-ah-zone) For systemic use, see the monograph found in the main section Indications/Actions Considered a high potency topical corticosteroid, betamethasone may useful for adjunctive treatment of localized pruritic or inflamma-tory conditions. Because risks associated with betamethasone (HPA axis suppression, systemic corticosteroid effects, skin atrophy) are greater than with hydrocortisone, betamethasone products are generally reserved for more serious localized pruritic conditions or when hydrocortisone is not effective. All veterinary-labeled products are in combination with gentamicin and labeled indications are for treat-ment of infected superficial lesions caused by bacteria sensitive to gentamicin. Sole ingredient betamethasone topical forms are available with human labeling. Corticosteroids are non-specific anti-inflammatory agents. They probably act by inducing phospholipase A2 inhibitory proteins (lipo-cortins) in cells, thereby reducing the formation, activity, and release of endogenous inflammatory mediators (e. g., histamine, prostaglan-dins, kinins, etc). Corticosteroids also reduce DNA synthesis via an anti-mitotic effect on epidermal cells. T opically applied corticosteroids also inhibit the migration of leukocytes and macrophages to the area reducing erythema, pruritus and edema. Dosages/Precautions/Adverse Effects Initially, topical corticosteroids are usually used sparingly 2-4 times per day. Refer to individual product labeling for actual dosing rec-ommendations for veterinary products. Several veterinary topical products list tuberculosis of the skin or pregnancy as a contraindication. Systemic corticosteroids can be teratogenic or induce parturition during the third trimester of pregnancy in animals. If considering use during pregnancy, weigh the respective risks with treating versus potential benefits. Clients should wash hands after application or wear gloves when applying. Use care when treating large areas, or when used on smaller patients. Risks can be reduced by treating for only as long as necessary on as small an area as possible. Increased risks of HPA axis suppression, systemic corticosteroid effects (polydipsia/polyuria, Cushing's, gastrointestinal effects) and skin atrophy occur as product concentration and duration of use increases. Local skin reactions (burning, itching, redness) are possible, but unlikely to occur. Betamethasone may delay wound healing particularly if used longer than 7 days in duration. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |
984 DERm ATOLOGICAL PRODu CTS Veterinary-Labeled betamethasone Topical Products Note: At time of writing there are no veterinary-labeled sole active ingredient betamethasone products in the USA. Product (Company) Form: Concentration Label Status Other Ingredients; Size(s); Comments Gentocin Topical Spray® (Schering) Gentaspray® (Butler) Betagen Topical Spray® (MedPharmex)Gentamicin Topical Spray® (RXV)Gentaved Topical Spray® (Vedco)Spray (all products listed): Gentamicin 0. 57 mg/m L;Betamethasone (as valerate) 0. 284 mg/m LRx (Vet) Rx (Vet) Rx (Vet) Rx (Vet)Rx (Vet) Rx (Vet)72 m L. 60 m L. 60, 120, 240 m L. 60, 120 m L. 60, 120, 240 m L. 15 g, 30 g. Extra label use on localized lesions on the skin, e. g., bacterial Otomax® Ointment (Schering) Ointment (otic): Gentamicin 3 mg/g; Betamethasone (as valerate) 1 mg/g; Clotrimazole 10 mg/g Rx (Vet) Approved for otic use in dogs; used in extralabel manner for bacterial skin lesions or Malassezia dermatitis; 7. 5 & 15 g tubes DVMAX® Ointment (IVX) Ointment (otic): Gentamicin 3 mg/g; Betamethasone (as valerate) 1 mg/g; Clotrimazole 10 mg/g Rx (Vet) Approved for otic use in dogs; used in extralabel manner for bacterial skin lesions or Malassezia dermatitis; 10, 20 & 215 g bottles Human-Labeled betamethasone Topical Products Note: Partial listing. There are also topical branded products (two common trade names are Diprosone® and Maxivate®) available with betamethasone dipropionate. Do not confuse products containing augmented betamethasone dipropionate (Diprolene®, etc) with be-tamethasone dipropionate. Augmented betamethasone dipropionate is not equivalent with betamethasone dipropionate as it is more potent. For more information on human-labeled betamethasone products, refer to a comprehensive human drug reference (e. g., Facts and Comparisons) or contact a pharmacist. Product (Company) Form: Concentration Label Status Size(s); Comments betamethasone Dipropionate Ointment Ointment: 0. 05% Rx (Human) 15, 45 g. betamethasone Dipropionate Cream Cream: 0. 05% Rx (Human) 15, 45 g. betamethasone Dipropionate Lotion Lotion: 0. 05% Rx (Human) 20, 30, 60 m L. Diprosone® (Westwood Squibb) Aerosol Spray: 0. 1% Rx (Human) 85 g. 10% isopropyl alcohol, mineral oil Clotrimazole & betamethasone Diprop. (Fougera)Lotrisone® (Schering)Lotion: Clotrimazole 1%Betamethasone dip. 0. 05%Rx (Human) 30 m L. Clotrimazole & betamethasone Diprop. (Fougera)Lotrisone® (Schering)Cream: Clotrimazole 1%Betamethasone dip. 0. 05%Rx (Human) 15, 45 g. iso Flu Predone Ace TATe (TOPICAL) (eye-soe-flue-pre-done ass-i-tate) Indications/Actions Considered a high potency topical corticosteroid, isoflupredone in combination with neomycin and tetracaine may be useful for adjunc-tive treatment of otic or topical localized pruritic or inflammatory conditions. Because risks associated with isoflupredone (HPA axis suppression, systemic corticosteroid effects, skin atrophy) are greater than with hydrocortisone, these products are generally reserved for more serious localized pruritic conditions or when hydrocortisone is not effective. All veterinary-labeled products (Tritop ® Ointment and Neo-Predef w/Tetracaine Powder®) have labeled indications for conditions associated with neomycin-susceptible organisms and/or allergy, or as a superficial dressing applied to minor cuts, wounds, lacerations, abrasions and for post-surgical pain application where reduction in pain and inflammatory response is deemed desirable. Corticosteroids are non-specific anti-inflammatory agents. They probably act by inducing phospholipase A2 inhibitory proteins (lipo-cortins) in cells, thereby reducing the formation, activity, and release of endogenous inflammatory mediators (e. g., histamine, prostaglan-dins, kinins, etc). Corticosteroids also reduce DNA synthesis via an anti-mitotic effect on epidermal cells. T opically applied corticosteroids also inhibit the migration of leukocytes and macrophages to the area reducing erythema, pruritus and edema. | ctl5q-Veterinary_drug_hand_book_Plumbs.pdf |