Trial reportBritish journal of clinical pharmacology2005
Effect of gemfibrozil on the pharmacokinetics and pharmacodynamics of racemic warfarin in healthy subjects.
Trial report in British journal of clinical pharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed, 45 citations in OpenAlex.
- A Phenotyping Tool for Seven Cytochrome P450 Enzymes and Two Transporters: Application to Examine the Effects of Clopidogrel and Gemfibrozil.Clinical pharmacology and therapeutics · 2025Trial
- CYP2C8 but not CYP3A4 is important in the pharmacokinetics of montelukast.British journal of clinical pharmacology · 2012Trial
- The CYP2C8 inhibitor gemfibrozil does not affect the pharmacokinetics of zafirlukast.European journal of clinical pharmacology · 2011Trial
- Stereoselective interaction between the CYP2C8 inhibitor gemfibrozil and racemic ibuprofen.European journal of clinical pharmacology · 2007Trial
- Coadministration of gemfibrozil and itraconazole has only a minor effect on the pharmacokinetics of the CYP2C9 and CYP3A4 substrate nateglinide.British journal of clinical pharmacology · 2005Trial
- Physiologically based pharmacokinetic modeling for optimal dosage prediction of statins and warfarin in patients with liver cirrhosis.European journal of clinical pharmacology · 2026Article
- Structural Analysis of Human Serum Albumin in Complex with the Fibrate Drug Gemfibrozil.International journal of molecular sciences · 2022Article
- Mechanisms of CYP450 Inhibition: Understanding Drug-Drug Interactions Due to Mechanism-Based Inhibition in Clinical Practice.Pharmaceutics · 2020Review
- Nutrient-sensing nuclear receptors PPARα and FXR control liver energy balance.The Journal of clinical investigation · 2017Review
- Article
- Validation of an LC/MS method for the determination of gemfibrozil in human plasma and its application to a pharmacokinetic study.Biomedical chromatography : BMC · 2010Article
- The role of metabolites in predicting drug-drug interactions: focus on irreversible cytochrome P450 inhibition.Current opinion in drug discovery & development · 2010Review
- Multiple inhibition mechanisms and prediction of drug-drug interactions: status of metabolism and transporter models as exemplified by gemfibrozil-drug interactions.Pharmaceutical research · 2008Article
- Effect of SLCO1B1 genetic polymorphism on the pharmacokinetics of nateglinide.British journal of clinical pharmacology · 2006Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsCase reports suggest that gemfobrozil can increase the anticoagulant effect of warfarin. Because gemfibrozil inhibits CYP2C9 in vitro, we studied its effects on the pharmacokinetics and pharmacodynamics of racemic warfarin.
methodsIn a randomized cross-over study, 10 healthy subjects ingested 600 mg gemfibrozil or placebo twice daily for 8 days. On day 3, they were administered a single dose of 10 mg racemic R-S-warfarin orally. The concentrations of R- and S-warfarin in plasma and thromboplastin time were monitored up to 168 h.
resultsGemfibrozil decreased the mean (+/-SD) area under the plasma concentration-time curve [AUC((0-infinity))] of S-warfarin by 11%, from 19.9 +/- 5.2 mg l(-1) h to 17.6 +/- 4.7 mg l(-1) h (95% CI on the difference -3.7, -0.78; P < 0.01) and that of R-warfarin by 6% from 31.3 +/- 7.5 mg l(-1) h during the gemfibrozil phase to 29.5 +/- 6.9 mg l(-1) h during the placebo phase (95% CI -3.3, -0.33; P < 0.05). There were no significant differences in the elimination half-lives of S- or R-warfarin between the phases. Gemfibrozil did not alter the anticoagulant effect of warfarin.
conclusionUnexpectedly, gemfibrozil slightly decreased the plasma concentrations of R- and S-warfarin. Displacement of warfarin from plasma albumin by gemfibrozil or its interference with the absorption of warfarin could explain the present findings. Usual therapeutic doses of gemfibrozil seem to have limited effects on the pharmacokinetics and pharmacodynamics of single dose warfarin in healthy subjects.
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