Evidence of CYP3A Allosterism In Vivo: Analysis of Interaction Between Fluconazole and Midazolam

@article{Yang2012EvidenceOC,
  title={Evidence of CYP3A Allosterism In Vivo: Analysis of Interaction Between Fluconazole and Midazolam},
  author={J. Yang and W. Atkins and N. Isoherranen and M. Paine and K. Thummel},
  journal={Clinical Pharmacology & Therapeutics},
  year={2012},
  volume={91}
}
  • J. Yang, W. Atkins, +2 authors K. Thummel
  • Published 2012
  • Biology, Medicine
  • Clinical Pharmacology & Therapeutics
  • The allosteric effect of fluconazole (effector) on the formation of 1′–hydroxymidazolam (1′–OH–MDZ) and 4–hydroxymidazolam (4–OH–MDZ) from midazolam (MDZ), a substrate of CYP3A4/5—members of the cytochrome P450 superfamily of enzymes—was examined in healthy volunteers. Following pretreatment with fluconazole, the ratio of the areas under the curve (AUCs) for 4–OH–MDZ and MDZ (AUC4–OH/AUCMDZ) increased by 35–62%, whereas the ratio AUC1′–OH/AUCMDZ decreased by 5–37%; the ratio AUC1′–OH/AUC4–OH… CONTINUE READING
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