Prophylaxis of organ rejection in patients receiving a liver, kidney or heart transplant.
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Tacrolimus, a macolide antibiotic with immunosuppressant properties, has a mechanism of action similar to that of cyclosporine. Tacrolimus inhibits T-cell activation after intracellular protein binding and suppression of IL-2 and other cytokines production.

Oral bioavailability : about 25%; time to peak: 2 hr (0.5-6); food reduces the rate and extent (30% decrease)of absorption. Primarily metabolized by CYP450 3A4 enzymes in the liver to at least 15 metabolites; protein binding 77%; elimination half-life 12 hr.

Hypersensitivity to Tacrolimus

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Tacrolimus is distributed into milk. Because of the potential for serious adverse reactions to tacrolimus in nursing infants, nursing should be avoided in women receiving the drug.

Febrile neutropenia, optic neuropathy <20201110>, nephrotoxicity, hyperkalemia, new onset diabetes mellitus, hypertension, tremor, headache, diarrhea, abdominal pain, nausea, insomnia, infection, and alopecia.

Liver transplant: initial 0.1-0.15 mg/kg/day PO divided into Q12H; kidney transplant: 0.2 mg/kg/day PO divided into Q12H. Children liver transplant: initial 0.15-0.2 mg/kg/day PO.
Shift from cyclosporin: stop cyclosporine 24 to 48 hours before starting tacrolimus.