Tacrolimus (FK-506)


Uses

  • 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.

Perioperative Risks

  • 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.

Worry About

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

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