Rapid Stimulating Effect of the Antiarrhythmic Agent Amiodarone on Absorption of Organic Anion Compounds

摘要: Summary: In a clinical setting, changes in pharmacokinetics due to drug-drug interactions can often directly affect the therapeutic safety and efficacy of drugs. Recently, interest has been shown intestine. It is now recognized that functions drug transporters substantially influence absorption administered drugs from Amiodarone (AMD) potent used treatment serious supraventricular ventricular tachyarrhythmias. Despite its pharmacological effects, wide use precluded by interactions. this study, we characterized transporter function between AMD various compounds human intestinal model Caco-2 cells. significantly rapidly increased uptake [ 3 H]estrone-3-sulfate (E-3-S) for 5 min. The apical-to-basal transport H]E-3-S was AMD. AMD-stimulated inhibited organic anion transporting polypeptide (OATP) substrates. cells treated with showed OATP2B1 expression on cell surface. also sulfobromophthalein (BSP), which typical compound, level Oatp2b1 at membrane vivo experiments. results indicate induces OATP2B1/Oatp2b1 intestine enhances compounds.