Nonlinear pharmacokinetics of oral quinidine and verapamil in healthy subjects: a clinical microdosing study.

@article{Maeda2011NonlinearPO,
  title={Nonlinear pharmacokinetics of oral quinidine and verapamil in healthy subjects: a clinical microdosing study.},
  author={Kazuya Maeda and Junichi Takano and Yasuhiko Ikeda and Tomoe Fujita and Yujiro Oyama and Kohei Nozawa and Yuji Kumagai and Yuichi Sugiyama},
  journal={Clinical pharmacology and therapeutics},
  year={2011},
  volume={90 2},
  pages={263-70}
}
Microdosing studies are effective in enabling the early identification of the pharmacokinetic properties of compounds administered to humans. However, the nonlinearity of the pharmacokinetics between microdose and therapeutic dose, attributable to the saturation of metabolic enzymes and transporters, is a major concern. Verapamil and quinidine are good substrates of both the multidrug resistance 1 transporter (MDR1) and the cytochrome P450 (CYP) 3A4 enzyme (CYP3A4). We investigated their dose… CONTINUE READING

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