Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR004744)
Formula
SVG example
1'-hydroxylation
Reactant Midazolam hydrochloride Product Alpha-hydroxymidazolam
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A4 (CYP3A4) DME Info
Metabolic Type Oxidation - 1'-hydroxylation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR004747 Midazolam hydrochloride 1',4'-dihydroxymidazolam Unclear Midazolam hydrochloride [1]
MR004745 Midazolam hydrochloride 1-hydroxymidazolam glucuronide Conjugation - N-glucuronidation Midazolam hydrochloride [2], [3], [4]
MR004742 Midazolam hydrochloride 4-hydroxymidazolam Oxidation - 4-hydroxylation Midazolam hydrochloride [5]
MR004746 Midazolam hydrochloride 4-hydroxymidazolam glucuronide Conjugation - N-glucuronidation Midazolam hydrochloride [2], [3]
References
1 Pharmacokinetics and metabolism of midazolam in chimeric mice with humanised livers
2 The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors
3 Contribution of the N-glucuronidation pathway to the overall in vitro metabolic clearance of midazolam in humans
4 The Oral Bioavailability and Metabolism of Midazolam in Stable Critically Ill Children: A Pharmacokinetic Microtracing Study
5 Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions

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