Clinical pharmacokinetics of fexofenadine enantiomers

Expert Opinion on Drug Metabolism & Toxicology
Masatomo Miura, Tsukasa Uno

Abstract

Drug-transporters play an important role in the disposition of clinical medicines. Although there are plural studies that have reported on the stereoselective pharmacokinetics related to cytochrome P450s, previous reports of the stereoselective pharmacokinetics related to drug-transporters including P-glycoprotein have been lacking. This article reviews the pharmacokinetic differences between fexofenadine enantiomers in humans and summarizes the previous reports that co-administration of P-glycoprotein inhibitors has altered the stereoselective pharmacokinetics of fexofenadine enantiomers. Both in vitro and in vivo studies have demonstrated that both itraconazole and verapamil are potent P-glycoprotein inhibitors. Therefore, by comparing the stereoselective pharmacokinetics of (R)- and (S)-fexofenadine with or without itraconazole and verapamil, the contribution of P-glycoprotein-mediated transport to fexofenadine stereoselective pharmacokinetics could be estimated. In our studies, the plasma concentrations of (R)-fexofenadine were greater than those of the corresponding (S)-enantiomer. Co-administration of itraconazole and/or verapamil significantly increased the AUC(0 - 24) of both enantiomers; their influence on the P-glycop...Continue Reading

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Citations

Jun 1, 2013·Indian Journal of Dermatology·Martin K Church, Diana S Church
Jun 7, 2011·Expert Opinion on Drug Metabolism & Toxicology·Marta Ferrer
Dec 14, 2011·Current Medical Research and Opinion·Jean BousquetMartin K Church
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Jan 17, 2017·The Journal of Pharmacy and Pharmacology·Fei LiMichael J Myers
Apr 11, 2018·Expert Opinion on Drug Metabolism & Toxicology·Yumiko Akamine, Masatomo Miura
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Mar 1, 2011·The World Allergy Organization Journal·Diana S Church, Martin K Church

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