natgillin/translations-raw huggingface dataset:
ileus paralytic, peritonitis, acute and chronic pancreatitis, blood amylase increased, gastrooesophageal reflux disease, impaired gastric emptying
paralitični ileus, peritonitis, akutni in kronični pankreatitis, zvišanje amilaze v krvi, gastroezofagealna refluksna bolezen, okvarjeno praznjenje želodca
rare:
redki:
subileus, pancreatic pseudocyst
subileus, psevdocista pankreasa
Renal and urinary disorders very common: common:
Bolezni sečil zelo pogosti: pogosti:
renal impairment renal failure, renal failure acute, oliguria, renal tubular necrosis, nephropathy toxic, urinary abnormalities, bladder and urethral symptoms
okvara ledvic odpoved ledvic, akutna odpoved ledvic, oligurija, nekroza ledvičnih tubulov, toksična nefropatija, motnje v sečilih, motnje v mehurju in sečnici
uncommon: very rare:
občasni: zelo redki:
anuria, haemolytic uraemic syndrome nephropathy, cystitis haemorrhagic
anurija, hemolitično- uremični sindrom nefropatija, hemoragični cistitis
Skin and subcutaneous tissue disorders common: uncommon: rare: very rare:
9 srbenje, izpuščaj, alopecija, akne, močnejše znojenje pogosti: občasni: redki:
pruritus, rash, alopecias, acne, sweating increased dermatitis, photosensitivity toxic epidermal necrolysis (Lyell’ s syndrome) Stevens Johnson syndrome
dermatitis, fotosenzibilnost toksična epidermalna nekroliza (Lyellova bolezen)
Musculoskeletal and connective tissue disorders common: uncommon:
Stevens- Johnsonov sindrom
arthralgia, muscle cramps, pain in limb, back pain joint disorders
Bolezni mišično- skeletnega sistema in vezivnega tkiva artralgija, mišični krči, bolečine v okončini, bolečine v hrbtu pogosti: občasni:
Endocrine disorders rare: hirsutism
sklepne motnje
Metabolism and nutrition disorders very common: common:
Bolezni endokrinega sistema redki:
hyperglycaemic conditions, diabetes mellitus, hyperkalaemia hypomagnesaemia, hypophosphataemia, hypokalaemia, hypocalcaemia, hyponatraemia, fluid overload, hyperuricaemia, appetite decreased, anorexia,
Presnovne in prehranske motnje hiperglikemična stanja, diabetes mellitus, hiperkaliemija zelo pogosti: pogosti:
9 metabolic acidoses, hyperlipidaemia, hypercholesterolaemia, hypertriglyceridaemia, other electrolyte abnormalities
hipomagneziemija, hipofosfatemija, hipokaliemija, hipokalciemija, hiponatriemija, preobremenitev s tekočino, hiperurikemija, zmanjšanje apetita, anoreksija, metabolična acidoza, hiperlipidemija, hiperholesterolemija, hipertrigliceridemija, druge nepravilnosti elektrolitov
dehydration, hypoproteinaemia, hyperphosphataemia, hypoglycaemia
dehidracija, hipoproteinemija, hiperfosfatemija, hipoglikemija
Infections and infestations As is well known for other potent immunosuppressive agents, patients receiving tacrolimus are frequently at increased risk for infections (viral, bacterial, fungal, protozoal).
Infekcijske in parazitske bolezni Tako kot med zdravljenjem z drugimi močnimi imunosupresivi bolnike tudi med zdravljenjem s takrolimusom pogosto bolj ogrožajo okužbe (virusne, bakterijske, glivične, protozojske).
Injury, poisoning and procedural complications common:
Poškodbe, zastrupitve in zapleti pri posegih pogosti:
Neoplasms benign, malignant and unspecified (incl cysts and polyps)
Benigne, maligne in neopredeljene novotvorbe (vključno s cistami in polipi) Bolnike, ki prejemajo imunosupresive, bolj ogroža pojav malignomov.
Vascular disorders very common: common:
Žilne bolezni zelo pogosti: pogosti:
hypertension haemorrhage, thromboembolic and ischaemic events, peripheral vascular disorders, vascular hypotensive disorders
hipertenzija krvavitev, trombembolični in ishemični dogodki, bolezen perifernih žil, žilna hipotenzija
infarction, venous thrombosis deep limb, shock
infarkt, globoka venska tromboza v udih, šok
asthenic conditions, febrile disorders, oedema, pain and discomfort, blood alkaline phosphatase increased, weight increased, body temperature perception disturbed
Splošne težave in spremembe na mestu aplikacije astenična stanja, vročinska stanja, edemi, bolečine in nelagodje, zvišanje alkalne pogosti: fosfataze v krvi, povečanje telesne mase, moteno zaznavanje telesne temperature občasni: redki: zelo redki:
multi-organ failure, influenza like illness, temperature intolerance, chest pressure sensation, feeling jittery, feeling abnormal, blood lactate dehydrogenase increased, weight decreased
odpoved več organov, gripi podobna bolezen, intoleranca vročine, občutek tiščanja v prsih, občutek živčnosti, nenormalno počutje, zvišanje laktat- dehidrogenaze v krvi, hujšanje žeja, padec, tiščanje v prsih, zmanjšanje gibljivosti, razjeda povečanje maščobnega tkiva
rare: very rare:
Bolezni imunskega sistema
Immune system disorders Allergic and anaphylactoid reactions have been observed in patients receiving tacrolimus (see section 4.4).
10 Pri bolnikih, ki so dobivali takrolimus, so opisane alergijske in anafilaktoidne reakcije (glejte poglavje 4. 4).
Hepatobiliary disorders common:
Bolezni jeter, žolčnika in žolčevodov pogosti:
hepatic enzymes and function abnormalities, cholestasis and jaundice, hepatocellular damage and hepatitis, cholangitis
nenormalnosti jetrnih encimov in delovanja jeter, holestaza in zlatenica, okvara jetrnih celic in hepatitis, holangitis
hepatitic artery thrombosis, venoocclusive liver disease hepatic failure, bile duct stenosis
tromboza jetrne arterije, venookluzivna bolezen jeter odpoved jeter, stenoza žolčevoda
Reproductive system and breast disorders uncommon:
Motnje reprodukcije
dysmenorrhoea and uterine bleeding
dismenoreja in krvavitev iz maternice
Psychiatric disorders very common: common:
Psihiatrične motnje nespečnost zelo pogosti: pogosti:
insomnia anxiety symptoms, confusion and disorientation, depression, depressed mood, mood disorders and disturbances, nightmare, hallucination, mental disorders
simptomi anksioznosti, zmedenost in dezorientiranost, depresija, potrtost, motnje razpoloženja, nočne more, halucinacije, duševne motnje
4.9 Overdose
psihotična motnja
psychotic disorder 10
4. 9 Preveliko odmerjanje
Several cases of accidental overdose have been reported with tacrolimus; symptoms have included tremor, headache, nausea and vomiting, infections, urticaria, lethargy, increased blood urea nitrogen and elevated serum creatinine concentrations, and increase in alanine aminotransferase levels.
Med simptomi so bili tremor, glavobol, navzea in bruhanje, okužbe, urtikarija, letargija, zvišanje sečnine v krvi, povišanje koncentracije kreatinina v serumu in zvišanje ravni alanin- aminotransferaze.
In cases of oral intoxication, gastric lavage and/ or the use of adsorbents (such as activated charcoal) may be helpful, if used shortly after intake.
Pri peroralni intoksikaciji lahko pomaga izpiranje želodca in/ ali uporaba adsorbensov (npr. aktivnega oglja), če so uporabljeni kmalu po zaužitju.
5.1 Pharmacodynamic properties
Farmakodinamične lastnosti 5. 1
Calcineurin inhibitors, ATC code:
Zaviralci kalcinevrina, oznaka ATC:
Mechanism of action and pharmacodynamic effects At the molecular level, the effects of tacrolimus appear to be mediated by binding to a cytosolic protein (FKBP12) which is responsible for the intracellular accumulation of the compound.
Mehanizem delovanja in farmakodinamični učinki Kaže, da učinek takrolimusa na molekulski ravni posreduje vezava na citosolno beljakovino (FKBP12), ki je odgovorna za njegovo znotrajcelično kopičenje.
The FKBP12-tacrolimus complex specifically and competitively binds to and inhibits calcineurin, leading to a calcium-dependent inhibition of T-cell signal transduction pathways, thereby preventing transcription of a discrete set of lymphokine genes.
To povzroči od kalcija odvisno zavrtje poti prenosa signalov v celicah T in tako prepreči transkripcijo posebne skupine limfokinskih genov.
Tacrolimus suppresses T-cell activation and T-helper-cell dependent B-cell proliferation, as well as the formation of lymphokines (such as interleukins-2, -3, and γ -interferon) and the expression of the interleukin-2 receptor.
Takrolimus zavira aktivacijo celic T in od celic T pomagalk odvisno proliferacijo celic B, pa tudi nastajanje limfokinov (npr. interlevkina- 2, - 3 in γ- interferona) ter izražanje receptorja za interlevkin- 2.
Results from clinical trials performed with once-daily tacrolimus Advagraf Liver transplantation The efficacy and safety of Advagraf and Prograf, both in combination with corticosteroids, was compared in 471 de novo liver transplant recipients.
Rezultati iz kliničnih preskušanj izvedenih z enkrat dnevno obliko takrolimusa (Advagraf) Presaditev jeter Učinkovitost in varnost uporabe zdravil Advagraf in Prograf, obe zdravili v kombinaciji s kortikosteroidi, so primerjali pri 471 bolnikih z na novo presajenimi jetri.
The event rate of biopsy confirmed acute rejection within the first 24 weeks after transplantation was 32.6% in the Advagraf group (N=237) and 29.3% in the Prograf group (N=234).
V skupini, ki je prejemala zdravilo Advagraf (n = 237), je bil delež z biopsijo potrjene akutne zavrnitve v prvih 24 tednih po presaditvi 32, 6- odstoten, v skupini, ki je prejemala zdravilo Prograf (n = 234), pa 29, 3- odstoten.
The treatment difference (Advagraf – Prograf) was 3.3% (95% confidence interval [-5.7%, 12.3%]). The 12-month patient survival rates were 89.2% for Advagraf and 90.8% for Prograf; in the Advagraf arm 25 patients died (14 female, 11 male) and in the Prograf arm 24 patients died (5 female, 19 male).
V skupini, ki je prejemala zdravilo Advagraf, je umrlo 25 bolnikov (14 žensk, 11 moških), v skupini, ki je prejemala zdravilo Prograf pa 24 bolnikov (5 žensk, 19 moških).
12-month graft survival was 85.3% for Advagraf and 85.6% for Prograf.
Pri uporabi zdravila Advagraf je bilo 12- mesečno preživetje presadka 85, 3 - odstotno, pri uporabi zdravila Prograf pa 85, 6- odstotno.
Kidney transplantation The efficacy and safety of Advagraf and Prograf, both in combination with mycophenolate mofetil (MMF) and corticosteroids, was compared in 667 de novo kidney transplant recipients.
Presaditev ledvic Učinkovitost in varnost uporabe zdravil Advagraf in Prograf, obe zdravili v kombinaciji z mikofenolat mofetilom (MMF) in s kortikosteroidi, so primerjali pri 667 bolnikih z na novo presajenimi ledvicami.
The event rate for biopsy-confirmed acute rejection within the first 24 weeks after transplantation was 18.6% in the Advagraf group (N=331) and 14.9% in the Prograf group (N=336).
V skupini, ki je prejemala zdravilo Advagraf (n = 331), je bil delež z biopsijo potrjene akutne zavrnitve v prvih 24 tednih po presaditvi 18, 6- odstoten, v skupini, ki je prejemala zdravilo Prograf (n = 336), pa 14, 9- odstoten.
The treatment difference (Advagraf-Prograf) was 3.8% (95% confidence interval [-2.1%, 9.6%]).
Razlika med zdravljenjem (Advagraf – Prograf) je bila 3, 8% (95% interval zaupanja [- 2, 1%, 9, 6%]).
The 12-month patient survival rates were 96.9% for Advagraf and 97.5% for Prograf; in the Advagraf arm 10 patients died (3 female, 7 male) and in the Prograf arm 8 patients died (3 female, 5 male).
V skupini, ki je prejemala zdravilo Advagraf, je umrlo 10 bolnikov (3 ženske, 7 moških), v skupini, ki je prejemala zdravilo Prograf pa 8 bolnikov (3 ženske, 5 moških).
12-month graft survival was 91.5% for Advagraf and 92.8% for Prograf.
Pri uporabi zdravila Advagraf je bilo 12- mesečno preživetje presadka 91, 5- odstotno, pri uporabi zdravila Prograf pa 92, 8- odstotno.
11 The efficacy and safety of Prograf, ciclosporin and Advagraf, all in combination with basiliximab antibody induction, MMF and corticosteroids, was compared in 638 de novo kidney transplant recipients.
Učinkovitost in varnost uporabe zdravila Advagraf, ciklosporina in zdravila Prograf, vsa v kombinaciji z indukcijo protiteles z baziliksimabom, mikofenolat mofetilom (MMF) in s kortikosteroidi, so primerjali pri 638 bolnikih z na novo presajenimi ledvicami.
The incidence of efficacy failure at 12 months (defined as death, graft loss, biopsy- confirmed acute rejection, or lost to follow-up) was 14.0% in the Advagraf group (N=214), 15.1% in the Prograf group (N=212) and 17.0% in the ciclosporin group (N=212).
V skupini, ki je prejemala zdravilo Advagraf (n = 214), je bila izguba učinkovitosti po 12 mesecih (definirana kot smrt, odmrtje presadka, z biopsijo potrjena akutna zavrnitev ali izguba podatkov o spremljanju bolnika) 14, 0- odstotna, v skupini, ki je prejemala zdravilo Prograf (n = 212), 15, 1- odstotna, v skupini, ki je prejemala ciklosporin (n = 212), pa 17, 0- odstotna.
The treatment difference was -3.0% (Advagraf-ciclosporin) (95.2% confidence interval [-9.9%, 4.0%]) for Advagraf vs. ciclosporin and -1.9% (Prograf-ciclosporin) (95.2% confidence interval [-8.9%, 5.2%]) for Prograf vs. ciclosporin.
Razlika med zdravljenjem z zdravilom Advagraf in zdravljenjem s ciklosporinom (Advagraf – ciklosporin) je bila - 3, 0% (95, 2% interval zaupanja [- 9, 9%, 4, 0%]), razlika med zdravljenjem z zdravilom Prograf in zdravljenjem s ciklosporinom (Prograf – ciklosporin) pa - 1, 9% (95, 2% interval zaupanja [- 8, 9%, 5, 2%]).
12-month graft survival was 96.7% for Advagraf, 92.9% for Prograf and 95.7% for ciclosporin.
Pri uporabi zdravila Advagraf je bilo 12- mesečno preživetje presadka 96, 7- odstotno, pri uporabi zdravila Prograf 92, 9- odstotno, pri uporabi ciklosporina pa 95, 7- odstotno.
Results from published data of tacrolimus administered twice daily as Prograf capsules in other primary organ transplantation Prograf has evolved into an accepted treatment as primary immunosuppressive medicinal product following pancreas, lung and intestinal transplantation.
Rezultati iz objavljenih podatkov o uporabi takrolimusa v obliki Prograf kapsul dvakrat na dan pri drugih primarnih presaditvah organov Zdravilo Prograf se je uveljavilo kot primarna imunosupresivna terapija po presaditvi pankreasa, pljuč in črevesa.
In prospective published studies oral Prograf was investigated as primary immunosuppressant in approximately 175 patients following lung, 475 patients following pancreas and 630 patients following intestinal transplantation.
V prospektivnih objavljenih študijah so zdravilo Prograf v peroralni obliki raziskovali kot primarni imunosupresiv pri približno 175 bolnikih po presaditvi pljuč, 475 bolnikih po presaditvi pankreasa in 630 bolnikih po presaditvi črevesa.
Lung transplantation The interim analysis of a recent multicentre study using oral Prograf discussed 110 patients who underwent 1:1 randomisation to either tacrolimus or ciclosporin.
Presaditev pljuč Vmesna analiza novejše multicentrične študije obravnava uporabe peroralne oblike zdravila Prograf 110 bolnikov, ki so bili v razmerju 1: 1 randomizirani na takrolimus ali ciklosporin.
Tacrolimus was started as continuous intravenous infusion at a dose of 0.01 to 0.03 mg/ kg/ day and oral tacrolimus was administered at a dose of 0.05 to 0.3 mg/ kg/ day.
Takrolimus je bil uveden kot stalna intravenska infuzija v odmerku od 0, 01 do 0, 03 mg/ kg/ dan, peroralni takrolimus pa je bil uporabljen v odmerku od 0, 05 do 0, 3 mg/ kg/ dan.
A lower incidence of acute rejection episodes for tacrolimus- versus ciclosporin-treated patients (11.5% versus 22.6%) and a lower incidence of chronic rejection, the bronchiolitis obliterans syndrome (2.86% versus 8.57%), was reported within the first year after transplantation.
8, 57%.
The 1-year patient survival rate was 80.8% in the tacrolimus and 83% in the ciclosporin group (Treede et al., 3rd ICI San Diego, US, 2004; Abstract 22).
Enoletno preživetje bolnikov je bilo v skupini s takrolimusom 80, 8% in v skupini s ciklosporinom 83% (Treede et al., 3rd ICI San Diego, ZDA, 2004; Izvleček 22).
Tacrolimus was started as continuous intravenous infusion at a dose of 0.025 mg/ kg/ day and oral tacrolimus was administered at a dose of 0.15 mg/ kg/ day with subsequent dose adjustments to target trough levels of 10 to 20 ng/ ml.
12 takrolimus pa je bil uporabljen v odmerku 0, 15 mg/ kg/ dan z nadaljnjimi prilagoditvami odrka, da je bila dosežena ciljna najnižja koncentracija od 10 do 20 ng/ ml.
The 1-year patient survival was 83% in the tacrolimus and 71% in the ciclosporin group, the 2-year survival rates were 76% and 66%, respectively.
Enoletno preživetje v skupini s takrolimusom je bilo 83% in v skupini s ciklosporinom 71%, dveletno pa v prvi 76% in v drugi 66%.
Acute rejection episodes per 100 patient-days were numerically fewer in the tacrolimus (0.85 episodes) than in the ciclosporin group (1.09 episodes).
Številčno je bilo akutnih zavrnitvenih epizod na 100 bolnikovih dni v skupini s takrolimusom manj (0, 85 epizode) kot v skupini s ciklosporinom (1, 09 epizode).
Obliterative bronchiolitis developed in 21.7% of patients in the tacrolimus group compared with 38.0% of patients in the ciclosporin group (p = 0.025).
Obliteracijski bronhiolitis se je pojavil pri 21, 7% bolnikov v skupini s takrolimusom in pri 38, 0% bolnikov v skupini s ciklosporinom (p = 0, 025).
Significantly more ciclosporin-treated patients (n = 13) required a switch to tacrolimus than tacrolimus-treated patients to ciclosporin (n = 2) (p = 0.02) (Keenan et al., Ann Thoracic Surg 1995; 60:580).
S ciklosporina na takrolimus je moralo preiti statistično značilno več bolnikov (n = 13) kot s takrolimusa na ciklosporin (n = 2) (p = 0, 02) (Keenan et al., Ann Thoracic Surg 1995; 60: 580).
Tacrolimus was started as continuous intravenous infusion at a dose of 0.05 mg/ kg/ day and oral tacrolimus was administered at a dose of 0.1 to 0.3 mg/ kg/ day with subsequent dose adjustments to target trough levels of 12 to 15 ng/ ml.
Takrolimus je bil uveden kot stalna intravenska infuzija v odmerku 0, 05 mg/ kg/ dan, peroralni takrolimus pa je bil uporabljen v odmerku od 0, 1 do 0, 3 mg/ kg/ dan z nadaljnjimi prilagoditvami odmerka, da je bila dosežena ciljna najnižja koncentracija od 12 do 15 ng/ ml.
The 1-year survival rates were 73.1% in the tacrolimus versus 79.2% in the ciclosporin group.
Enoletno preživetje v skupini s takrolimusom je bilo 73, 1% in v skupini s ciklosporinom 79, 2%.
Freedom from acute rejection was higher in the tacrolimus group at 6 months (57.7% versus 45.8%) and at 1 year after lung transplantation (50% versus 33.3%) (Treede et al., J Heart Lung Transplant 2001; 20:511).
Delež bolnikov brez akutne zavrnitve je bil v skupini s takrolimusom večji po 6 mesecih (57,% v prim. s 45, 8%) in po 1 letu po presaditvi pljuč (50% v primerjavi s 33, 3%) (Treede et al., J Heart Lung Transplant 2001; 20: 511).
Pancreas transplantation A multicentre study using oral Prograf included 205 patients undergoing simultaneous pancreas- kidney transplantation who were randomised to tacrolimus (n = 103) or to ciclosporin (n = 102).
Presaditev pankreasa Multicentrična študija uporabe peroralne oblike zdravila Prograf je zajela 205 bolnikov, pri katerih je bila hkrati narejena presaditev pankreasa in ledvice; bolnike so randomizirali na takrolimus (n = 103) ali na ciklosporin (n = 102).
The initial oral per protocol dose of tacrolimus was 0.2 mg/ kg/ day with subsequent dose adjustments to target trough levels of 8 to 15 ng/ ml by Day 5 and 5 to 10 ng/ mL after Month 6.
Uvodni peroralni odmerek takrolimusa po protokolu je bil 0, 2 mg/ kg/ dan z nadaljnjimi prilagoditvami odmerka tako, da je bila do 5. dne dosežena ciljna najnižja koncentracija od 8 do 15 ng/ ml in po 6. mesecu od 5 do 10 ng/ ml.
Pancreas survival at 1 year was significantly superior with tacrolimus:
Preživetje pankreasa je bilo po 1 letu značilno boljše s takrolimusom:
In total 34 patients switched treatment from
91, 3% v primerjavi s 74, 5% pri ciklosporinu (p < 0, 0005); preživetje ledvičnega presadka je bilo v obeh skupinah podobno.
12 ciclosporin to tacrolimus, whereas only 6 tacrolimus patients required alternative therapy (Bechstein et al., Transplantation 2004; 77:1221).
V celoti je 34 bolnikov prešlo s ciklosporina na takrolimus, le 6 bolnikov na takrolimusu pa je potrebovalo drugo terapijo (Bechstein et al., Transplantation 2004; 77: 1221).
Intestinal transplantation Published clinical experience from a single centre on the use of oral Prograf for primary treatment following intestinal transplantation showed that the actuarial survival rate of 155 patients (65 intestine alone, 75 liver and intestine, and 25 multivisceral) receiving tacrolimus and prednisone was 75% at 1 year, 54% at 5 years, and 42% at 10 years.
Presaditev črevesa Objavljene klinične izkušnje enega samega centra o uporabi peroralne oblike zdravila Prograf pri primarnem zdravljenju po presaditvi črevesa kažejo, da je bilo aktuarsko preživetje 155 bolnikov (65 samo črevo, 75 jetra in črevo, 25 multivisceralno), ki so dobivali takrolimus in prednizon, po 1 letu 75%, po 5 letih 54% in po 10 letih 42%.
In the early years the initial oral dose of tacrolimus was 0.3 mg/ kg/ day.
V zgodnjih letih je bil začetni peroralni odmerek takrolimusa 0, 3 mg/ kg/ dan.
A variety of innovations, such as techniques for early detection of Epstein-Barr (EBV) and CMV infections, bone marrow augmentation, the adjunct use of the interleukin-2 antagonist daclizumab, lower initial tacrolimus doses with target trough levels of 10 to 15 ng/ ml, and most recently allograft irradiation were considered to have contributed to improved results in this indication over time (Abu- Elmagd et al., Ann Surg 2001; 234:404).
Domnevno so k izboljšanju rezultatov skozi čas pri tej indikaciji pripomogle različne inovacije, npr. postopki za zgodnje odkrivanje okužb z virusom Epstein- Barr (EBV) in CMV, prirast kostnega mozga, dodatna uporaba antagonista interlevkina- 2 daklizumaba, manjši začetni odmerki takrolimusa s ciljno najnižjo koncentracijo od 10 do 15 ng/ ml in, v najnovejšem času, obsevanje alotransplantata (Abu- Elmagd et al., Ann Surg 2001; 234: 404).
5.2 Pharmacokinetic properties
Farmakokinetične lastnosti 5. 2
Absorption In man tacrolimus has been shown to be able to be absorbed throughout the gastrointestinal tract.
Absorpcija Pri človeku je dokazano, da se takrolimus absorbira skozi celotna prebavila.
Advagraf is a prolonged-release formulation of tacrolimus resulting in an extended oral absorption profile with an average time to Cmax of approximately 2 hours.
Cmax je v povprečju dosežena po približno 2 urah.
Absorption is variable and the mean oral bioavailability of tacrolimus (investigated with the Prograf formulation) is in the range of 20% - 25% (individual range in adult patients 6% - 43%).
Povprečna biološka uporabnost peroralno uporabljenega takrolimusa (raziskave so bile izvedene s farmacevtsko obliko Prograf) je od 20 do 25% (individualni razpon pri odraslih bolnikih 6% do 43%).
Bile flow does not influence the absorption of tacrolimus and therefore treatment with Advagraf may commence orally.
Tok žolča ne vpliva na absorpcijo takrolimusa in zato se zdravljenje z zdravilom Advagraf lahko začne peroralno.
A strong correlation exists between AUC and whole blood trough levels at steady-state for Advagraf.
13 Obstaja močna korelacija med AUC in najnižjo koncentracijo v polni krvi v stanju ravnotežja za zdravilo Advagraf.
Distribution and elimination In man, the disposition of tacrolimus after intravenous infusion may be described as biphasic.
Porazdelitev in izločanje Porazdelitev takrolimusa po intravenski infuziji pri človeku je mogoče opisati kot dvofazno.
In the systemic circulation, tacrolimus binds strongly to erythrocytes resulting in an approximate 20:1 distribution ratio of whole blood/ plasma concentrations.
V sistemskem obtoku se takrolimus močno veže na eritrocite, zato je porazdelitveno razmerje med koncentracijo v polni krvi in plazmi približno 20: 1.
In plasma, tacrolimus is highly bound (> 98.8%) to plasma proteins, mainly to serum albumin and α -1-acid glycoprotein.
V plazmi je takrolimus v veliki meri (> 98, 8%) vezano na plazemske beljakovine, predvsem na serumski albumin in α- 1- kisli glikoprotein.
The steady-state volume of distribution based on plasma concentrations is approximately 1300 l (healthy subjects).
Volumen porazdelitve v stanju dinamičnega ravnovesja je glede na koncentracijo v plazmi približno 1. 300 litrov (zdravi preiskovanci).
Corresponding data based on whole blood averaged 47.6 l.
Ustrezni podatek na podlagi polne krvi je povprečno 47, 6 l.