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Effects of Cyclosporine A and Itraconazole on Permeability, Biliary Excretion and Pharmacokinetics of Amlidipine

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Cyclosporin A (CsA) is a P-glycoprotein (P-gp) inhibitor clinically used as an immunosuppressant. Itraconazole (ITZ) functions as an inhibitor of both the P-gp and CYP3A and is used as afungistatic/fungicidal agent in human and veterinary medicine. The present studies were designed to investigate the effects of CsA and ITZ on 1 intestinal permeability of amlodipine (a calcium channel blocker used as a cardiovascular agent) in isolated rat everted gut sac modle, and 2) biliary excretion and pharmacokinetics of amlodipine in rats. The concentrations of amlodipine in biosamples were measured by the liquid chromatograph mass spectrometer (LC/MS). Both CsA ITZ significantly increased permeability of amlodipine in the ileum and jejunum of the rat everted gut sac modle,and ITZ showed more potent than CsA IN this modle. Pretreatment pf rats with ITZ increased plasma levels and biliary excretion of amlodipine and made no changes in its plasma levels. In conclusion, ITZ inreased in vitro permeability of amlodipine and bile in vivo. Whereas, CsA showed no significant efects on the levels of amlodipine in rat plasma and bile in vivo. Whereas, CsA showed no significant effects on the levels of amlodipine in rat plasma and bile probably due to the potent inhibition of ITZ against both CYP3A and P-gp.

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Keywords: Amlodipine; CYP3A; P-glycoprotein; biliary exretion; cyclosporin A; itraconazole; permeability; pharmacokinerics

Document Type: Research Article

Publication date: August 1, 2008

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  • Drug Metabolism Letters publishes short papers on major advances in all areas of drug metabolism and disposition. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of the Internet technology for both the submission and review of manuscripts. The journal covers the following areas:

    In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites, reactive intermediate and glutathione conjugates.
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