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St John's Wort induces intestinal P-glycoprotein/MDR1 and intestinal and hepatic CYP3A4

Clinical Pharmacology & Therapeutics · 2000 · Vol. 68(6) · pp. 598–604

Daniel Dürr✉(University of Zurich)

Abstract

These results indicate direct inducing effects of St John's Wort on intestinal P-glycoprotein/MDR1 (in rats and humans), hepatic CYP3A2 (in rats), and intestinal and hepatic CYP3A4 (in humans). Therefore the results provide a mechanistic explanation for the previously observed drug interactions in patients and support the importance of intestinal P-glycoprotein/MDR1 in addition to intestinal and hepatic CYP3A4 for overall drug absorption and disposition in humans.

Pharmacogenetics and Drug Metabolism Drug Transport and Resistance Mechanisms Pharmaceutical studies and practicesP-glycoproteinDigoxinHypericum perforatumPharmacologyCYP3A4PharmacokineticsMedicinePharmacokinetic interactionOrganic anion-transporting polypeptideChemistry

MeSH terms

AdultAnimalsBiological AvailabilityCardiotonic AgentsCytochrome P-450 Enzyme SystemDigoxinDrug InteractionsDuodenumEnzyme InductionHumansMixed Function OxygenasesIntestine, SmallLiverMalePlant Extracts

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586

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32.85

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Herb-Drug Interactions