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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Calcineurin inhibitors
tacrolimus
L04AD02
Forms & Strengths
- Capsules: 0.5mg, 1mg, 5mg
- Injection: 5mg/mL
- Ointment: 0.03%, 0.1%
- Tablets: 0.5mg, 1mg, 5mg
Adult Dosing
- Prevent organ rejection: 0.1-0.2mg/kg/day IV, 0.05-0.3mg/kg/day PO
- Transplant: initial 0.1-0.2mg/kg/day, target trough 5-20ng/mL
- Topical: apply ointment twice daily
Pediatric Dosing
- Prevent organ rejection: 0.1-0.2mg/kg/day IV, 0.05-0.3mg/kg/day PO, adjusted by trough levels
- Children > 16 years: same as adult dosing
- Children < 16 years: limited data, monitor closely
Indications
- Prevention of organ rejection in liver, kidney, heart transplant
- Treatment of moderate to severe atopic dermatitis
- Treatment of prevent graft-versus-host disease
Mechanism of Action
- Calcineurin inhibitor, suppresses T-cell activation
- Inhibits IL-2 transcription, reduces cytokine production
- Immunosuppressive effects, reduces graft rejection
Contraindications
- Hypersensitivity to tacrolimus
- Concomitant use with cyclosporine
- Concomitant use with sirolimus
Adverse Reactions
- Nephrotoxicity, neurotoxicity
- Hypertension, hyperkalemia, hypomagnesemia
- Diabetes mellitus, hyperglycemia
- Infections, malignancies
Drug Interactions
- Increased toxicity with concomitant nephrotoxic agents
- Metabolism induced by rifampicin, phenytoin, carbamazepine
- Metabolism inhibited by ketoconazole, erythromycin, diltiazem
- Concomitant use with grapefruit juice, avoid
Curated Content: Needs Vetting Before Put to Clinical Use