Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR004746)
Formula
UGT1A4 ...
SVG example
N-glucuronidation
Reactant Midazolam hydrochloride Product 4-hydroxymidazolam glucuronide
Reactant Info Product Info
Metabolic Enzyme UDP-glucuronosyltransferase 1A4 (UGT1A4) DME Info
UDP-glucuronosyltransferase 2B7 (UGT2B7) DME Info
Metabolic Type Conjugation - N-glucuronidation
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]
MR004744 Midazolam hydrochloride Alpha-hydroxymidazolam Oxidation - 1'-hydroxylation Midazolam hydrochloride [5], [4]
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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