Hydroxyitraconazole, formed during intestinal first-pass metabolism of itraconazole, controls the time course of hepatic CYP3A inhibition and the bioavailability of itraconazole in rats.

@article{Quinney2008HydroxyitraconazoleFD,
  title={Hydroxyitraconazole, formed during intestinal first-pass metabolism of itraconazole, controls the time course of hepatic CYP3A inhibition and the bioavailability of itraconazole in rats.},
  author={Sara K. Quinney and Raymond E. Galinsky and Vanida A Jiyamapa-Serna and Y Chen and Mitchell A. Hamman and Stephen D. Hall and Robert E. Kimura},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2008},
  volume={36 6},
  pages={1097-101}
}
Itraconazole (ITZ) is a substrate of CYP3A and both ITZ and hydroxyitraconazole (OH-ITZ), a major metabolite formed by CYP3A, are potent inhibitors of CYP3A. The concentration- and time-dependent changes in the hepatic availability (F(H)) of ITZ were evaluated in rats after oral doses of 5 and 40 mg/kg. Simultaneous blood samples were obtained from the aorta, portal vein, and hepatic vein for 24 h following duodenal ITZ administration, and concentrations of ITZ and OH-ITZ determined by LC/MS… CONTINUE READING