Why the study?
Does gemfibrozil alter the pharmacokinetics and pharmacodynamics of glimepiride in healthy volunteers?
Does gemfibrozil alter the pharmacokinetics and pharmacodynamics of glimepiride in healthy volunteers?
Gemfibrozil modestly increases plasma concentrations of glimepiride, likely through CYP2C9 inhibition, though without significant acute changes in blood glucose or insulin.
Gemfibrozil may modestly increase glimepiride exposure in patients; extends CYP2C9 interaction data without altering short-term glycemic response.
OBJECTIVE: Our objective was to study the effects of gemfibrozil on the pharmacokinetics and pharmacodynamics of glimepiride, a new sulfonylurea antidiabetic drug and a substrate of cytochrome P4502C9 (CYP2C9). METHODS: In a randomized, 2-phase crossover study, 10 healthy volunteers were treated for 2 days with 600 mg oral gemfibrozil or placebo twice daily. On day 3, they received a single dose of 600 mg gemfibrozil or placebo and 1 hour later a single dose of 0.5 mg glimepiride orally. Plasma glimepiride, serum insulin, and blood glucose concentrations were measured up to 12 hours. RESULTS: Gemfibrozil increased the mean total area under the plasma concentration-time curve of glimepiride by 23% (range, 6%-56%; P <.005). The mean elimination half-life of glimepiride was prolonged from 2.1 to 2.3 hours (P <.05) by gemfibrozil. No statistically significant differences were found in the serum insulin or blood glucose variables between the two phases. CONCLUSIONS: Gemfibrozil modestly increases the plasma concentrations of glimepiride. This may be caused by inhibition of CYP2C9.
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Niemi et al. (2001) studied this question.
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