Tacrolimus metabolism

Tacrolimus [P] Decreased tacrolimus metabolism with diltiazem, nicardipine, verapamil. 

CALCIUM CHANNEL BLOCKERS TACROLIMUS Plasma concentrations of tacrolimus are t when given with diltiazem, felodipine or nifedipine however, they appear to protect renal function Uncertain, but presumed to be due to inhibition of CYP3A4-mediated tacrolimus metabolism Watch for side-effects of tacrolimus monitor ECG, blood count and renal and hepatic function... 

Sheikh AM, Wolf DC, Lebovics E, Goldberg R, Horowitz HW. Concomitant human immunodeficiency virus protease inhibitor therapy markedly reduces tacrolimus metabolism and increases blood levels. Transplantation 1999 68(2) 307-9. 

F i MP, Allen S. Vmconazole inhibiticn of tacrolimus metabolism. Clin Infect Dis (2003) 36,1089-91. 

The macrolides inhibit tacrolimus metabolism by the cytochrome P450 isoenzyme CYP3A. Azithromycin is less likely to interact with tacrolimus because it does not inhibit CYP3A. ... 

Another report describes the use of an intravenous phenytoin infusion to treat acute tacrolimus overdoses in 2 patients, with the aim of enhaneing tacrolimus metabolism. ... 

Levofloxacin modestly increased the bioavailability of tacrolimus in one study. In vitro, enoxacin had no effect on tacrolimus metabolism. 

Dai Y, Hebert MF, Isoherranen N, Davis CL, Marsh C, Shen DD and Thummel KE (2006) Effect of CYP3A5 pol5morphism on tacrolimus metabolic clearance in vitro. Drug Metab Dispos 34(5) 836-847. 

Chang HH, Lee NY, Ko WC, Lee HC, Yang YH, Wu CJ, Chang CM. Voriconazole inhibition of tacrolimus metabolism in a kidney transplant recipient with fluconazole-resistant cryptococcal meningitis. Int J Infect Dis 2010 14(4) e348-50. 

Tacrolimus The co-prescription of posaconazole with tacrolimus has been evaluated in 14 lung transplant recipients with cystic fibrosis. Posaconazole inhibited CYP3A4-mediated tacrolimus metabolism, resulting in a threefold reduction in tacrolimus dosage requirements f4T]. 

Both tacrolimus and estradiol are metabolized by CYP3A4 and tacrolimus is a potent inhibitor of 2-estradiol metabolism. Conversely, estradiol inhibits hepatic and intestinal CYP3A4 and reduces tacrolimus metabolism. Transdermal administration avoids hepatic first-pass metabolism, which explains why even small doses have a systemic effect. Co-administration of tacrolimus is possible, but close monitoring of tacrolimus trough concentrations and renal function is necessary. 

Drug-drug interactions Nicardipine has been reported to inhibit tacrolimus metabolism with consequent... 

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