Tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a ubiquitous mammalian intracellular enzyme) is then formed, after which the phosphatase activity of calcineurin is inhibited. Such inhibition prevents the dephosphorylation and translocation of various factors such as the nuclear factor of activated T-cells (NF-AT), and nuclear factor kappa-light-chain enhancer of activated B-cells (NF-κB). See package insert for complete information.

PROGRAF is a calcineurin-inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in adult and pediatric patients receiving allogeneic liver, kidney or heart transplants, in combination with other immunosuppressants.

See package insert for complete information.

The most common adverse reactions (≥ 15%) were abnormal renal function, hypertension, diabetes mellitus, fever, CMV infection, tremor, hyperglycemia, leukopenia, infection, anemia, bronchitis, pericardial effusion, urinary tract infection, constipation, diarrhea, headache, abdominal pain, insomnia, paresthesia, peripheral edema, nausea, hyperkalemia, hypomagnesemia, and hyperlipemia.

• Hypersensitivity to tacrolimus or HCO-60 (polyoxyl 60 hydrogenated castor oil).

• Not Interchangeable with Extended-Release Tacrolimus Products ­ Medication Errors: Instruct patients or caregivers to recognize the appearance of PROGRAF capsules.
• New Onset Diabetes After Transplant: Monitor blood glucose.
• Nephrotoxicity (acute and/or chronic): Reduce the dose; use caution with other nephrotoxic drugs.
• Neurotoxicity: Including risk of Posterior Reversible Encephalopathy Syndrome (PRES); monitor for neurologic abnormalities; reduce or discontinue PROGRAF.
• Hyperkalemia: Monitor serum potassium levels. Consider careful before using with other agents also associated with hyperkalemia.
• Hypertension: May require antihypertensive therapy. Monitor relevant drug-drug interactions. See package insert for complete information.