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Article

Dose-dependent interaction between gemfibrozil and repaglinide in humans: strong inhibition of CYP2C8 with subtherapeutic gemfibrozil doses.

Drug metabolism and disposition: the biological fate of chemicals - 1 Oct 2011

Honkalammi Johanna, Niemi Mikko, Neuvonen Pertti J, Backman Janne T

Abstract excerpt

Gemfibrozil 1-O-β-glucuronide inactivates CYP2C8 irreversibly. We investigated the effect of gemfibrozil dose on CYP2C8 activity in humans using repaglinide as a probe drug. In a randomized, five-phase crossover study, 10 healthy volunteers ingested 0.25 mg of repaglinide 1 h after different doses of gemfibrozil or placebo. Concentrations of plasma repaglinide, gemfibrozil, their metabolites, and blood glucose...

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PMID: 21778352
DOI: 10.1124/dmd.111.040931

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Dose-dependent interaction between gemfibrozil and repaglinide in humans: strong inhibition of CYP2C8 with subtherapeutic gemfibrozil doses.PMID 21778352Read ↗

Gemfibrozil is a strong inactivator of CYP2C8 in very small multiple doses.Semantic proximity Read ↗

CYP2C8 activity recovers within 96 hours after gemfibrozil dosing: estimation of CYP2C8 half-life using repaglinide as an in vivo probe.Semantic proximity Read ↗

Effect of the CYP2C8 genotype on the pharmacokinetics and pharmacodynamics of repaglinide.Semantic proximity Read ↗

Effects of gemfibrozil and atorvastatin on the pharmacokinetics of repaglinide in relation to SLCO1B1 polymorphism.Semantic proximity Read ↗

Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics.Semantic proximity Read ↗

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Cyclosporine markedly raises the plasma concentrations of repaglinide.Semantic proximity Read ↗

The effect of SLCO1B1 polymorphism on repaglinide pharmacokinetics persists over a wide dose range.Semantic proximity Read ↗

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A Phenotyping Tool for Seven Cytochrome P450 Enzymes and Two Transporters: Application to Examine the Effects of Clopidogrel and Gemfibrozil.Semantic proximity Read ↗

Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers.Semantic proximity Read ↗

Different effects of SLCO1B1 polymorphism on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide.Semantic proximity Read ↗

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