1999
DOI: 10.1177/00912709922007499
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Effects of Rifampin on Tacrolimus Pharmacokinetics in Healthy Volunteers

Abstract: Tacrolimus is a marketed immunosuppressant used in liver and kidney transplantation. It is subject to extensive metabolism by CYP3A4 and is a substrate for P-glycoprotein-mediated transport. A pharmacokinetic interaction with rifampin, an antituberculosis agent and potent inducer of CYP3A4 and P-glycoprotein, and tacrolimus was evaluated in six healthy male volunteers. Tacrolimus was administered at doses of 0.1 mg/kg orally and 0.025 mg/kg/4 hours intravenously. The pharmacokinetics of tacrolimus were obtaine… Show more

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Cited by 129 publications
(72 citation statements)
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“…The variation in morbidity of anti-tuberculosis therapy depends in part on the immunosuppressive regimens. Patients on cyclosporine A (CsA) (23,(25)(26)(27) and tacrolimus (28,29) seem to be at higher risk of graft loss when these medications are combined with an antituberculosis drug such as rifampin. This is in part due to the cytochrome P450 induction of the metabolism of CsA by rifampin and the need for increased dosing of CsA.…”
Section: Discussionmentioning
confidence: 99%
“…The variation in morbidity of anti-tuberculosis therapy depends in part on the immunosuppressive regimens. Patients on cyclosporine A (CsA) (23,(25)(26)(27) and tacrolimus (28,29) seem to be at higher risk of graft loss when these medications are combined with an antituberculosis drug such as rifampin. This is in part due to the cytochrome P450 induction of the metabolism of CsA by rifampin and the need for increased dosing of CsA.…”
Section: Discussionmentioning
confidence: 99%
“…Other examples for which individual estimates of F G were available in the literature include tacrolimus (Floren et al, 1997;Hebert et al, 1999) and terfenadine (Clifford et al, 1997). The interindividual variabilities of in vivo F G estimates for tacrolimus and terfenadine were 36 and 54%, respectively.…”
Section: F G Predictions Using Individual Jejunal Microsomal Samplesmentioning
confidence: 99%
“…4 Hebert et al 40 evaluated the pharmacokinetics of tacrolimus in 6 healthy volunteers. Subjects were treated with either a single oral dose (0.1 mg/kg) or an IV dose (0.025 mg/kg) of tacrolimus, before and after 18 days of rifampin, 600 mg/d.…”
Section: Immunosuppressantsmentioning
confidence: 99%