Midazolam hydroxylation by human liver microsomes in vitro: inhibition by fluoxetine, norfluoxetine, and by azole antifungal agents.

L von Moltke, L; J Greenblatt, D; Schmider, J; X Duan, S; E Wright, C; S Harmatz, J; I Shader, R

doi:10.1002/j.1552-4604.1996.tb04251.x

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Midazolam hydroxylation by human liver microsomes in vitro: inhibition by fluoxetine, norfluoxetine, and by azole antifungal agents.

Shared by NobleBlocks on Sep 1, 1996 • 12:00 AM UTC

Authors:

L L von Moltke

D J Greenblatt

J Schmider

Abstract

Biotransformation of the imidazobenzodiazepine midazolam to its alpha-hydroxy and 4-hydroxy metabolites was studied in vitro using human liver microsomal preparations. Formation of alpha-hydroxy-midazolam was a high-affinity (Km = 3.3 mumol/L) Michaelis-Menten process coupled with substrate inhibiti...

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