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

The allosteric effect of fluconazole (effector) on the formation of 1’-hydroxymidazolam (1’-OH-MDZ) and 4-hydroxymidazolam (4-OH-MDZ) from the CYP3A4/5 substrate, midazolam (MDZ), was examined in healthy volunteers. Following pre-treatment of fluconazole, AUC(4-OH)/AUC(MDZ) increased 35–62%, while A...

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Autors principals: Yang, Jing, Atkins, William M., Isoherranen, Nina, Paine, Mary F., Thummel, Kenneth E.
Format: Artigo
Idioma:Inglês
Publicat: 2011
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Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC3830930/
https://ncbi.nlm.nih.gov/pubmed/22048224
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/clpt.2011.178
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