Clopidogrel Markedly Increases Plasma Concentrations of CYP2C8 Substrate Pioglitazone.

  title={Clopidogrel Markedly Increases Plasma Concentrations of CYP2C8 Substrate Pioglitazone.},
  author={Matti K. Itkonen and Aleksi Tornio and Mikko Neuvonen and Pertti J Neuvonen and Mikko T. Niemi and Janne T. Backman},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  volume={44 8},
The glucose-lowering drug pioglitazone undergoes hepatic CYP2C8-mediated biotransformation to its main metabolites. The antiplatelet drug clopidogrel is metabolized to clopidogrel acyl-β-d-glucuronide, which was recently found to be a strong time-dependent inhibitor of CYP2C8 in humans. Therefore, we studied the effect of clopidogrel on the pharmacokinetics of pioglitazone. In a randomized crossover study, 10 healthy volunteers ingested either 300 mg of clopidogrel on day 1, and 75 mg on days 2… CONTINUE READING
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