৳ 50/unit
Pack: ৳ 1,000
৳ 50/unit
Pack: ৳ 1,000
At a glance
Tacrolimus is a calcineurin-inhibitor immunosuppressant used for the prophylaxis of organ rejection in allogeneic liver, kidney, heart, and lung transplants.
Indications
- Prophylaxis of organ rejection in allogeneic liver transplants
- Prophylaxis of organ rejection in allogeneic kidney transplants
- Prophylaxis of organ rejection in allogeneic heart transplants
- Prophylaxis of organ rejection in allogeneic lung transplants
Pharmacology
Tacrolimus binds to FKBP-12, inhibiting calcineurin phosphatase activity. This prevents dephosphorylation and translocation of NF-AT and NF-κB, inhibiting expression and production of cytokines including IL-1β, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8, IL-10, IFN-γ, TNF-α, and GM-CSF. It inhibits T-lymphocyte activation and proliferation.
Dosage
Adult Dose (Oral):
- Kidney (with azathioprine): 0.2 mg/kg/day; target trough 7-20 ng/mL (months 1-3)
- Kidney (with MMF/IL-2 antagonist): 0.1 mg/kg/day; target 4-11 ng/mL
- Liver: 0.10-0.15 mg/kg/day; target 5-20 ng/mL
- Heart: 0.075 mg/kg/day; target 10-20 ng/mL (months 1-3)
- Lung: 0.075 mg/kg/day; target 10-15 ng/mL (months 1-3)
Pediatric Dose (Oral):
- Kidney: 0.3 mg/kg/day; target 5-20 ng/mL
- Liver: 0.15-0.2 mg/kg/day; target 5-20 ng/mL
- Heart/Lung: 0.3 mg/kg/day; target 5-20 ng/mL
Side effects
Common Side Effects (≥15%):
- Abnormal renal function, hypertension
- Diabetes mellitus, fever, CMV infection
- Tremor, hyperglycemia, leukopenia
- Anemia, infection, bronchitis
- Constipation, diarrhea, headache
- Abdominal pain, insomnia, paresthesia
- Peripheral edema, nausea, hyperkalemia
Use in pregnancy
Use in Pregnancy: Can cause fetal harm; advise pregnant women of potential risk; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Precautions & warnings
- New-onset diabetes: Monitor blood glucose
- Nephrotoxicity: Reduce dose; caution with other nephrotoxic drugs
- Neurotoxicity (risk of PRES): Monitor neurologic abnormalities; reduce/discontinue
- Hyperkalemia: Monitor serum potassium
- Not recommended with sirolimus (liver/heart)
- Avoid live vaccines
Overdose effects
Acute overdosage (up to 30 times intended dose) may cause tremors, abnormal renal function, hypertension, peripheral edema; activated charcoal may be used; provide symptomatic treatment.
Storage conditions
Store below 30°C in a dry place, away from light and moisture; keep out of reach of children.