Article
Gemfibrozil is a strong inactivator of CYP2C8 in very small multiple doses.
Clinical pharmacology and therapeutics - 1 May 2012
Honkalammi J, Niemi M, Neuvonen P J, Backman J T
Abstract excerpt
Therapeutic doses of gemfibrozil cause mechanism-based inactivation of CYP2C8 via formation of gemfibrozil 1-O-β-glucuronide. We investigated the extent of CYP2C8 inactivation caused by three different doses of gemfibrozil twice dailyfor 5 days, using repaglinide as a probe drug, in 10 healthy volunteers. At the end of this 5-day regimen, there were dose-dependent increases in the area under the plasma...
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