Irreversible CYP3A inhibition accompanied by plasma protein-binding displacement: a comparative analysis in subjects with normal and impaired liver function.

@article{Orlando2009IrreversibleCI,
  title={Irreversible CYP3A inhibition accompanied by plasma protein-binding displacement: a comparative analysis in subjects with normal and impaired liver function.},
  author={Rocco Orlando and Sara De Martin and Paola Pegoraro and Luigi Quintieri and Pietro Palatini},
  journal={Clinical pharmacology and therapeutics},
  year={2009},
  volume={85 3},
  pages={319-26}
}
In this study, quinine was used as a probe substrate and erythromycin as a prototypical irreversible inhibitor of CYP3A to ascertain whether, like reversible CYP inhibition, the magnitude of irreversible inhibition is also strictly dependent on the status of liver function. The effect of erythromycin on oral quinine disposition was studied in 10 healthy subjects and in 20 patients with cirrhosis of the liver who had varying degrees of liver dysfunction. This effect was shown to be the result of… CONTINUE READING

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