Tacrolimus (FK-506)

Rescue of primary immunosuppressant Rx following liver, lung, heart, pancreas, and limb transplant.

Approximate number of candidates: 3000 awaiting liver transplant and 9000 awaiting kidney transplant in USA; 15,000 living liver transplant and 50,000 kidney transplant recipients are chronically receiving immunosuppressants.

Has been used to suppress the inflammation associated with ulcerative colitis.

Htn: CCBs may be effective in treating tacrolimus-associated Htn, but care is required. Interference with tacrolimus metabolism may necessitate a reduction in dose.

Nephrotoxicity: Do not administer concurrently with cyclosporine; administer cautiously with other potentially nephrotoxic drugs (e.g., aminoglycoside antibiotics).

Hypersensitivity may occur with IV formulation; pts should be monitored for 30 min after injection.

May result in opioid-induced hyperalgesia.

Drug is metabolized by cytochrome P450 (3A) enzyme system. Other medications that inhibit or induce this enzyme may affect tacrolimus drug levels.