Rapid stimulating effect of the antiarrhythmic agent amiodarone on absorption of organic anion compounds

Masahiro Segawa, Jiro Ogura, Satoru Seki, Shirou Itagaki, Natsuko Takahashi, Masaki Kobayashi, Takeshi Hirano, Hiroaki Yamaguchi, Ken Iseki

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)


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

Original languageEnglish
Pages (from-to)178-186
Number of pages9
JournalDrug metabolism and pharmacokinetics
Issue number3
Publication statusPublished - 2013


  • Absorption
  • Amiodarone
  • Drug-drug interaction
  • OATP2B1
  • Organic anion transport

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science
  • Pharmacology (medical)


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