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RISS 인기검색어
- 검색키워드
- 저자 : Lemler, S.M. (검색결과 1 건)
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Rifampin enhances cytochrome P450 (CYP) 2B6-mediated efavirenz 8-hydroxylation in healthy volunteers
Cho, D.Y.,Shen, J.H.Q.,Lemler, S.M.,Skaar, T.C.,Li, L.,Blievernicht, J.,Zanger, U.M.,Kim, K.B.,Shin, J.G.,Flockhart, D.A.,Desta, Z. 日本藥物動態學會 2016 DRUG METABOLISM AND PHARMACOKINETICS Vol.31 No.2
The effect of rifampin on the in vivo metabolism of the antiretroviral drug efavirenz was evaluated in healthy volunteers. In a cross-over placebo control trial, healthy subjects (n = 20) were administered a single 600 mg oral dose of efavirenz after pretreatment with placebo or rifampin (600 mg/day for 10 days). Plasma and urine concentrations of efavirenz, 8-hydroxyefavirenz and 8,14-dihydroxyefavirenz were measured by LC-MS/MS. Compared to placebo treatment, rifampin increased the oral clearance (by ~2.5-fold) and decreased maximum plasma concentration (C<SUB>max</SUB>) and area under the plasma concentration-time curve (AUC<SUB>0-~</SUB>) of efavirenz (by ~1.6- and ~2.5-fold respectively) (p < 0.001). Rifampin treatment substantially increased the C<SUB>max</SUB> and AUC<SUB>0-12h</SUB> of 8-hydroxyefavirenz and 8,14-dihydroxyefavirenz, metabolic ratio (AUC<SUB>0-72h</SUB> of metabolites to AUC<SUB>0-72h</SUB> efavirenz) and the amount of metabolites excreted in urine (Ae<SUB>0-12hr</SUB>) (all, p < 0.01). Female subjects had longer elimination half-life (1.6-2.2-fold) and larger weight-adjusted distribution volume (1.6-1.9-fold) of efavirenz than male subjects (p < 0.05) in placebo and rifampin treated groups respectively. In conclusion, rifampin enhances CYP2B6-mediated efavirenz 8-hydroxylation in vivo. The metabolism of a single oral dose of efavirenz may be a suitable in vivo marker of CYP2B6 activity to evaluate induction drug interactions involving this enzyme.
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