P4503a4

• Grapefruit and grapefruit juice can increase tacrolimus levels.

Drugs that Decrease Tacrolimus Levels

• Rifampin • Carbamazepine

• Rifabutin • Phenobarbitol

• Drugs that induce cytochrome P450 3A4 Other

• Vaccinations—live vaccinations should be avoided

Formulations

• 1 mg capsules supplied in 100 count bottles

• 5 mg capsules supplied in 100 count bottles

• 1 mL ampules containing the equivalent of 5 mg of anhydrous tacrolimus per mL—supplied in boxes of 10 ampules

Dosage and Administration

IV Infusion

• 0.03 to 0.05 mg/kg/d to 0.10 mg/kg/d as a continuous infusion

• Patients should be converted to oral therapy as soon as can be tolerated

Capsules

• First dose should be given 8 to 12 hours after discontinuing IV infusion

Editors' Notes:

Tacrolimus appears to be a more effective drug than cyclosporine for liver transplantation. Rescue for refractory liver and kidney rejection has also been shown to be an important use for the drug. A double-blind study comparing Sandimmune and FK506 in cadaveric renal transplantation demonstrated superior efficacy of FK506 for rejection prophylaxis. A higher incidence of PTDM was noted, but was reversible in 50% of patients at 2 years. The 5-year data from this study was recently published. Treatment failure was significantly less frequent in tacrolimus-treated recipients (43.8% vs. 56.8%; p=0.008). With cross-over due to rejection counted as graft failure, graft survival was significantly better with tacrolimus (63.8% vs. 53.8%; p=0.014). Hypertension and hyperlipidemia were less with tacrolimus. Nearly 50% of patients who required insulin with tacrolimus were able to discontinue insulin. (Vincenti F, Jensik SC, Filo RS et al. A long-term comparison of tacrolimus (FK-506) and cyclosporine in kidney transplantation: evidence for improved allograft survival at five years. ©2002 Transplantation. Lippincott, Williams and Wilkins) Avoid taking with meals, antacids and divalent cation supplements.

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