Astellas Pharma


Concise Prescribing Info
Primary immunosuppression in liver & kidney allograft recipients & liver & kidney allograft rejection resistant to conventional immunosuppressive agents.
Dosage/Direction for Use
Primary immunosuppression in liver & kidney transplantation Adult Liver Oral 0.1-0.2 mg/kg/day in 2 divided doses, start approx 6 hr after the completion of liver transplant surgery. IV Initially 0.01-0.05 mg/kg as continuous 24-hr infusion. Kidney Oral 0.15-0.3 mg/kg/day in 2 divided doses. Start w/in 24 hr after completion of kidney transplant surgery. IV Initially 0.05-0.1 mg/kg as continuous 24-hr infusion. Paed Liver & kidney Initially 0.3 mg/kg/day in 2 divided doses. IV Liver 0.05 mg/kg/day as a continuous 24-hr infusion. Kidney 0.1 mg/kg/day as a continuous 24-hr infusion. Liver & kidney allograft rejection resistant to conventional immunosuppressive regimens Begin treatment w/ initial dose recommended for primary immunosuppression in that particular allograft. Patients should be converted from IV to oral medication as soon as individual circumstances permit. Do not continue IV therapy for >7 days.
Should be taken on an empty stomach: Take at least 1 hr before or 2-3 hr after meals.
Hypersensitivity to tacrolimus or other macrolides; polyoxyethylated castor oil or structurally related compd (infusion conc).
Special Precautions
Observe medication errors including inadvertent, unintentional or unsupervised substitution of immediate- or prolonged-release tacrolimus formulations. Monitor BP, ECG, neurological & visual status, fasting blood glucose levels, electrolytes (particularly K), liver & renal function tests, haematology parameters, coagulation values & plasma protein determinations during the initial post-transplant period. Monitor tacrolimus blood levels in combination w/ strong CYP3A4 inhibitors (eg, telaprevir, boceprevir, ritonavir, ketoconazole, voriconazole, itraconazole, telithromycin or clarithromycin) or CYP3A4 inducers (eg, rifampicin, rifabutin). Avoid herbal prep containing St. John's wort or other herbal prep, combination w/ ciclosporin; high K intake or K-sparing diuretics; drug w/ nephrotoxic or neurotoxic effects; live attenuated vaccines. GI perforation. Monitor tacrolimus conc during episodes of diarrhoea. Monitor high-risk patients, particularly childn, receiving substantial immunosuppression, using procedures eg, echocardiography or ECG pre- & post-transplant; consider dose reduction if abnormalities develop. Patients w/ risk factor for QT prolongation, including w/ a personal or family history of QT prolongation, CHF, bradyarrhythmias & electrolyte abnormalities. Patients diagnosed or suspected to have congenital long QT syndrome or acquired QT prolongation; concomitantly using known QT prolonging-medications; induce electrolyte abnormalities; increase tacrolimus exposure. Epstein-Barr virus (EBV)-associated lymphoproliferative disorders; increased risk of developing lymphoproliferative disorders in childn (<2 yr), EBV-VCA-negative; carefully monitor EBV-PCR during treatment. Limit exposure to sunlight & UV light. Perform radiological procedure (MRI) if posterior reversible encephalopathy syndrome symptoms is present, eg, headache, altered mental status, seizure & visual disturbances occur. Increased risk for opportunistic infections eg, BK virus-associated nephropathy & JC virus-associated progressive multifocal leukoencephalopathy; consider in patients w/ deteriorating hepatic or renal function or neurological symptoms. Pure Red Cell Aplasia. Patients w/ rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Hypersensitivity to peanut or soya; polyoxyethylene hydrogenated castor oil (infusion conc). May cause visual & neurological disturbances & may be enhanced w/ alcohol. Pregnancy & lactation.
Adverse Reactions
Hyperglycaemic conditions, DM, hyperkalaemia; insomnia; tremor, headache; HTN; diarrhoea, nausea; renal impairment. Anaemia, leukopenia, thrombocytopenia, leukocytosis, abnormal RBC analyses; hypomagnesaemia, hypophosphataemia, hypokalaemia, hypocalcaemia, hyponatraemia, fluid overload, hyperuricaemia, decreased appetite, metabolic acidoses, hyperlipidaemia, hypercholesterolaemia, hypertriglyceridaemia, other electrolyte abnormalities; anxiety symptoms, confusion & disorientation, depression, depressed mood, mood disorders & disturbances, nightmare, hallucination, mental disorders; seizures, disturbances in consciousness, paraesthesias & dysaesthesias, peripheral neuropathies, dizziness, impaired writing, nervous system disorders; blurred vision, photophobia, eye disorders; tinnitus; ischaemic CAD, tachycardia; haemorrhage, thromboembolic & ischaemic events, peripheral vascular disorders, vascular hypotensive disorders; dyspnoea, parenchymal lung disorders, pleural effusion, pharyngitis, cough, nasal congestion & inflammations; GI inflammatory conditions, ulceration & perforation, GI haemorrhages, stomatitis & ulceration, ascites, vomiting, GI & abdominal pains, dyspeptic signs & symptoms, constipation, flatulence, bloating & distension, loose stools, GI signs & symptoms; hepatic enzymes & function abnormalities, cholestasis & jaundice, hepatocellular damage & hepatitis, cholangitis; pruritus, rash, alopecia, acne, increased sweating; arthralgia, muscle spasms, pain in extremity, back pain; renal failure, acute renal failure, oliguria, renal tubular necrosis, toxic nephropathy, urinary abnormalities, bladder & urethral symptoms; asthenic conditions, febrile disorders, oedema, pain & discomfort, increased blood alkaline phosphatase, increased wt, disturbed body temp perception; primary graft dysfunction.
Drug Interactions
Increased tacrolimus blood levels w/ antifungals (eg, ketoconazole, fluconazole, itraconazole & voriconazole), macrolide antibiotics (eg, erythromycin), HIV PIs (eg, ritonavir, nelfinavir, saquinavir) or HCV PIs (eg, telaprevir, boceprevir) & letermovir; clotrimazole, clarithromycin, josamycin, nifedipine, nicardipine, diltiazem, verapamil, amiodarone, danazol, ethinylestradiol, omeprazole, nefazodone, & herbal remedies containing Schisandra sphenanthera extr; naringenine (flavonoid in grapefruit juice); NSAIDs, oral anticoagulants, oral antidiabetics. May potentially inhibit metabolism w/ bromocriptine, cortisone, dapsone, ergotamine, gestodene, lidocaine, mephenytoin, miconazole, midazolam, nilvadipine, norethisterone, quinidine, tamoxifen, troleandomycin; lansoprazole & ciclosporin. May increase systemic exposure w/ prokinetic agent metoclopramide, cimetidine & Mg-Al-hydroxide. Decreased blood levels w/ rifampicin, phenytoin, or St. John's wort; phenobarb. Potential increase or decrease blood levels w/ high dose prednisolone or methylprednisolone. Potential decrease conc w/ carbamazepine, metamizole, INH. Prolonged t½ of ciclosporin. Increased blood level of phenytoin. May reduce the clearance of steroid-based contraceptives. Decreased clearance & increased t½ of phenobarb & phenazone. May increase nephrotoxic or neurotoxic effects w/ aminoglycosides, gyrase inhibitors, vancomycin, sulfamethoxazole + trimethoprim, NSAIDs, ganciclovir or aciclovir. Enhanced nephrotoxicity w/ amphotericin B & ibuprofen. Avoid high K intake or K-sparing diuretics (eg, amiloride, triamterene or spironolactone); live attenuated vaccines.
MIMS Class
ATC Classification
L04AD02 - tacrolimus ; Belongs to the class of calcineurin inhibitors. Used as immunosuppressants.
Prograf cap 5 mg
Prograf infusion conc 5 mg/mL
(amp) 1 mL x 10 × 1's
Prograf cap 0.5 mg
Prograf cap 1 mg
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