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Animal Health Anthelmintic Review - Approved Drugs | Unnamed: 1 | Unnamed: 2 | Unnamed: 3 | Unnamed: 4 | Unnamed: 5 | Unnamed: 6 | Unnamed: 7 | Unnamed: 8 | Unnamed: 9 | Unnamed: 10 | Unnamed: 11
Compound General Information |  |  |  |  |  | Parasite and Animal Coverage
Compound Class | Generic Name | Structure | Current Supplier | US Patent Approval | US Approval | MOA | Animal Species covered                       Parasite Claims | Efficacy/Resistance | Dose Rate  (mg/kg) | Safety and Toxicity Issues | Summary use in AH
Avermectins | Ivermectin |  | Merck / Merial | 1980                      generic | 1984 | Glutamate and GABA gated Cl- channel agonist | All livestock and companion animals                               *BS GI nematodes - adults and 4th stage larvae    - persistant activiity                                                                               *lungworm                                                                       *cattle grubs, sucking live, mites                                                                                *prevention of heartworm disease caused by Dirofilaria immitis (canine heartworm) | *excellent BS nematocide                             *no activity vs flukes or tapeworms          *reported resistance in sheep stomach parasites and Cooperia resistance in cattle | 200 ug/kg | *potent compounds but wide safety margins above use levels                                 *no reproductive safety issues | *still a most effective anthelmintic in a wide variety of animals and parasites with little resistance except in sheep
Milbemycins | [NAME] |  | Fort Dodge  (Pfizer) | 1987                          generic | 1997 | Glutamate and GABA gated Cl- channel agonist | Beef and non-lactating dairy cattle, horses, dogs                                                                                    *BS GI nematodes - adult and immature - persistant activity                                    *Lungworm  (Dictyocaulus viviparus) - adult and immature                                                         *Eyeworm - Thelazia spp.                                     *Sucking lice, fly grugs, mange mites | excellent but reported resistance with parasites resistant to other MLs | 200 ug/kg | *potent compounds but wide safety margins above use levels                                 *no reproductive safety issues | *good market but has not replaced ivermectin as the primary ML anthelmintic
Benzimidazoles | Albendazole |  | GSK | 1975           generic | 1989 | Tubulin formation inhibitor | Beef and dairy cattle, sheep                                    *Fasciola hepatica                                               *Tapeworms                                                   *BS GI tract nematodes, including inhibited larvae                                                            *Dictyocaulus viviparus | good but widespread resistance issues amongst sheep parasites, particularly Haemonchus contortus | 10 mg/kg | BZ class are teratogens, particularly in first trimester | *old but still usuable anthelmintic particularly in combination with MLs
Depsipeptides | Emodepside |  | Bayer | 1996 | 2007 | *binds to GCPR lactophilins                                   *inhibits pharyngeal pumping and paralysis | Cats                                                                                      *Hookworm ([NAME] tubaeforme)                                                *Ascarid (Toxacara cati)                               *Tapeworm (Dipylidium caninum and Taenia taeniaformis) - praziquantel | *excellent BS Intestinal nematocide in dogs (not approved)                                                     *known to have excellent antifilarial activity (Dirofilaria immitis and Onchocerca spp.)   *no resistance reported | 3 mg/kg | emodepside safe in dogs; aniline  analogs is quite toxic | *novel anthelmintic of high interest in AH but very limited use due to cost and formulation issues
[NAME]quamides | Derquantel |  | Pfizer | tbd | not approved | *nicotinic antagonist inducing flaccid paralysis | Sheep                                                                                               *Most GI tract nematodes in sheep, including ones resistant to approved anthelmintics                                                           *not very effective vs Oesophagostomum, Ostertagia, Trichuris and Dictycaulus (lungworm) so product is combined with abamectin | *excellent vs fairly limited spectrum vs sheep parasites                                                                       *requires combination with an avermectin *effective vs strains resistant to other anthelmintics | 2 mg/kg | *meets "safety targets" in rat, dog, sheep, cattle                                                            *not safe in horses | *meets a great need as active against multiply resistant parasites
Hexahydroxy-                                     pyrazines | DEC |  | Generic | 1949                   generic | 1974 | *inhibitor of arachidonic acid metabolism in MF                                                                *MF more susceptible to immune attack | Dogs                                                                                   *prevention of heartworm disease caused by Dirofilaria immitis (canine hearworm) | *good efficacy but requirement for daily treatment led to use of ivermectin (30 day preventative)                                                                       *no reported resistance | 6 mg/kg | contra-indicated for use in dogs infected with heartworm | *still used in AH but mostly supplanted by the AVMS and [NAME] for canine heartworm disease prevention
 | Piperazine |  | Dow | 1959                   generic | 1955 | GABA agonist | Chickens, turkeys, pigs                                                                   *Ascarids (Ascaridia spp and [NAME] suum)  in birds and swine                                         *Oesophagostomum spp) in swine | *good but very limited                                                  *resistance issues and usually used in combination | ~100 mg/kg | Acute oral Rat LD50:    1900 mg/kg | *limited use in AH; largely replacead by more broad spectrum anthelmintics
 | Praziquantel |  | Bayer | 1975                        generic | 1981 | voltage dependent Ca++ channels | Dog, cat, horse                                                                           Canine tapeworms:  Dipylidium caninum and Echinococcus multilocularis | *excellent                                                                 *no reported resistance | ~7.5 mg/kg | safe for use in pregnant dogs | primary therapy for tapeworms in animals
Tetrahydro-                       pyrimidines | Pyrantel                 pamoate |  | Pfizer | 1968                                   generic | 1976 | *depolarizing neuromuscular blocking agent, producing spastic paralysis | Horse, dog                                                                 *Ascarids and hookworms in dogs                                     *GI parasites in horses except tapeworms | *good to excellent                                                          *no resistance reported in approved animal species | 5 to 10 mg/kg | high safety margin | limited spectrum so used in combination
Imidazo-                    thiazoles | Levamisole |  | [NAME] | 1966                                      generic | 1988 | *inhibits succinic dehydrogenase in parasite muscle, decreasing muscle activity | Cattle, sheep                                                                           *BS GI nematodes and lungworm | *Excellent                                                                       *widespread resistance particularly amongst Haemonchus contortus | ~4 mg/kg | Acute oral Rat LD50:  180 mg/kg | *used in AH but much parasite resistance, particularly in sheep
Amino-acetonitriles | Monepantel |  | Novartis | 2009 | not approved | *novel helminth nicotinic acetylcholine receptor agonist                    *causes hypercontraction of body and spasmodic contraction of pharynx                                      *effective vs parasites resistant to known anthelmintics | Sheep                                                                           *BS GI nematodes | *excellent; active vs AVM, BZ and LEV resistance parasites                                                                         *no field resistance reported (launched 2009) | 2.5 mg/kg | *no contraindications                                                         *no adverse effects reported                                      *no effects on reproduction in rats or rabbits                                                             *non-mutagenic | *not effective vs ascarids
Salicylanilides | Closantel |  | [NAME] | 1976               generic | not approved | uncoupler | [NAME] Fluke                                                              *Fasciola hepatica                                                                    *Fascioloides magna                                                             *Stomach helminths:  Haemonchus contortus | *highly effective vs adults and 6-8 week old immatures                                                                   *not effective vs earlier stages | 7.5 mg/kg | only for use in male sheep | *limited product use in AH                  *not approved in the US
 | Rafoxanide |  | Merck | 1969               generic | not approved | uncoupler | Cattle, sheep                                                                                   *Adult liver fluke; some efficacy vs immatures                                                                   *GI nematodes                                                           *Bot fly | mediocre vs liver fluke | 7.5 mg/kg | *defects can be observed in teratogenicity studies in rats and rabbits but NOELs have been set. | *limited product use in AH                  *not approved in the US
Phenyl-sulfonamide | Clorsulon |  | Merck | 1976                               generic | 1985 | inhibition of glycolysis | Cattle                                                                             *Adult and immature liver fluke (Fasciola hepatica) | good | 7 mg/kg | very safe drug | still a useful product in AH
Biphenyl-                    sulfides | Bithionol |  | Monsanto | 1958                    generic | not approved | anthelmintic in sulfoxide form | Ruminants                                                                             *Rumen flukes ([NAME] spp.)                            *Liver flukes (Fasciola and Fascioloides spp.)                                                                                       *Tapeworm ([NAME]) |  | 40 mg/kg | *sulfoxide form toxic at 280 mg/kg BW                                                                                    *contraindicated in animals with renal disease | *limited product use in AH                  *not approved in the US
 | Febantel |  | Bayer | 1975                         generic | 1978 | pro-benzimidazole | Horse, dog, cat                                                         *Canine Intestinal tract nematodes including whipworm (Trichuris vulpis) | excellent vs limited spectrum in dogs | ~30 mg/kg | teratogenicity in first trimester as is a pro-benzimidazole | *BZ type compound with limited spectrum                                                                       *must be combined with other anthelmintics for complete spectrum in dogs
Misc | Nitroscanate |  | Novartis | 1972                    generic | not approved | decreases parasite cellular energy production | Dog: BS intestinal parasites |  | 50 mg/kg | safe to give to pregnant animals | *limited use in veterinary medicine
 | Nitroxynil |  | generic | 1966           generic | not approved | uncoupler | Cattle, sheep                                                                 *Flukes - adult and immatures                                   *GI parasites in Cattle and Sheep (Haemonchus spp.; Oesophagostomum spp., Bunostomum phlebotomum) |  | 10 mg/kg | no safety issues reported | *limited use in veterinary medicine