Tacrolimus, Oral

Immunomodulator · Immunomodulator

Indications

Prophylaxis of organ rejection in liver, kidney and heart allograft recipients and allograft rejection resistant to conventional immunosuppressive regimens.

Dosage

Primary immunosuppression in liver & kidney allograft recipients: Adults: Oral liver transplantation: 0.1-0.2 mg/kg/day in 2 divided doses, start approx 6 hr after completion of surgery. Kidney transplantation: 0.15-0.3 mg/kg/day in 2 divided doses, start within 24 hr of surgery. Children: Oral liver transplantation: 0.3 mg/kg/day in 2 divided doses. Allograft rejection resistant to conventional immunosuppressive regimens: Begin with initial dose for primary immunosuppression in that particular allograft.

Adverse Effects

Gastro-intestinal disturbances including dyspepsia and inflammatory and ulcerative disorders; hepatic dysfunction, jaundice, bile-duct and gallbladder abnormalities; hypertension (less frequently hypotension), tachycardia, angina, arrhythmias, thromboembolic and ischaemic events, rarely myocardial hypertrophy, cardiomyopathy; dyspnoea, pleural effusion; tremor, headache, insomnia, paraesthesia, confusion, depression, dizziness, anxiety, convulsions, incoordination, encephalopathy, psychosis; visual and hearing abnormalities; haematological effects including anaemia, leukocytosis, leucopenia, thrombocytopenia, Coagulation disorders; altered acid-base balance and glucose metabolism, electrolyte disturbances including hyperkalaemia (less frequently hypokalaemia); altered renal function including increased serum creatinine; hypophosphataemia, hypercalcaemia, hyperuricaemia; muscle cramps,…

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Hypersensitivity to macrolides. Precautions: Cardiomyopathy has been reported in children given tacrolimus after transplantation. Patients should be monitored carefully by echocardiography for hypertrophic changes; dose reduction or discontinuation should be considered if these occur. Monitor visual status, blood glucose, haematological and neurological parameters and whole blood 'trough' concentrations of tacrolimus (especially during episodes of diarrhoea). May affect performance of skilled tasks (e.g. driving).

Pharmacokinetics

Absorption: Incomplete and variable. Metabolism: Hepatic. Bioavailability: 25%. Half-life elimination: Healthy adult: 35 hrs. Renal transplant patient: 19 hrs. Hepatic transplant patient: 12 hrs. Cardiac transplant patient: 24 hrs. Paediatric hepatic transplant patient: 11.5 ± 3.8 hrs. Paediatric renal transplant patient: 10.2 ± 5.0 hrs. Time to peak, plasma: 0.5-6 hrs. Excretion: Faeces (primarily). Urine (minor).

Brands with this active ingredient

• Aerograf
• Arilio
• Crolimus
• Cyonse
• Inograf
• Medigraf
• Mirograf
• Neutacroli
• Prograf
• Romlus
• Tacgraf
• Taclekin
• Tacmus
• Tacogen
• Tacrobell

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.