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

@article{Backman2009CYP2C8AR,
  title={CYP2C8 activity recovers within 96 hours after gemfibrozil dosing: estimation of CYP2C8 half-life using repaglinide as an in vivo probe.},
  author={Janne T. Backman and Johanna Honkalammi and Mikko Neuvonen and Kaisa J Kurkinen and Aleksi Tornio and Mikko T. Niemi and Pertti J Neuvonen},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2009},
  volume={37 12},
  pages={2359-66}
}
Gemfibrozil 1-O-beta-glucuronide is a mechanism-based inhibitor of cytochrome P450 2C8. We studied the recovery of CYP2C8 activity after discontinuation of gemfibrozil treatment using repaglinide as a probe drug, to estimate the in vivo turnover half-life of CYP2C8. In a randomized five-phase crossover study, nine healthy volunteers ingested 0.25 mg of repaglinide alone or after different time intervals after a 3-day treatment with 600 mg of gemfibrozil twice daily. The area under the plasma… CONTINUE READING

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Drug metabolism and disposition: the biological fate of chemicals • 2000
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