Reaction: Midazolam to 1 product
- Reaction
- Reaction type
- N-glucuronidation
- Direction
- Major circulating metabolite?
- No
- Spontaneous?
- No
- Activity
- inactive
- References
- Klieber S, Hugla S, Ngo R, Arabeyre-Fabre C, Meunier V, Sadoun F, Fedeli O, Rival M, Bourrie M, Guillou F, Maurel P, Fabre G: Contribution of the N-glucuronidation pathway to the overall in vitro metabolic clearance of midazolam in humans. Drug Metab Dispos. 2008 May;36(5):851-62. doi: 10.1124/dmd.107.019539. Epub 2008 Feb 6. [Article]
- Swart EL, Slort PR, Plotz FB: Growing up with midazolam in the neonatal and pediatric intensive care. Curr Drug Metab. 2012 Jul;13(6):760-6. doi: 10.2174/138920012800840347. [Article]
- Tian DD, Leonowens C, Cox EJ, Gonzalez-Perez V, Frederick KS, Scarlett YV, Fisher MB, Paine MF: Indinavir Increases Midazolam N-Glucuronidation in Humans: Identification of an Alternate CYP3A Inhibitor Using an In Vitro to In Vivo Approach. Drug Metab Dispos. 2019 Jul;47(7):724-731. doi: 10.1124/dmd.119.087007. Epub 2019 Apr 26. [Article]
- Hyland R, Osborne T, Payne A, Kempshall S, Logan YR, Ezzeddine K, Jones B: In vitro and in vivo glucuronidation of midazolam in humans. Br J Clin Pharmacol. 2009 Apr;67(4):445-54. doi: 10.1111/j.1365-2125.2009.03386.x. [Article]
- Nguyen HQ, Kimoto E, Callegari E, Obach RS: Mechanistic Modeling to Predict Midazolam Metabolite Exposure from In Vitro Data. Drug Metab Dispos. 2016 May;44(5):781-91. doi: 10.1124/dmd.115.068601. Epub 2016 Mar 8. [Article]
- Wessels AMA, Bolhuis MS, Bult W, Nijsten MWN, Kneyber MCJ, Touw DJ: A fast and simple method for the simultaneous analysis of midazolam, 1-hydroxymidazolam, 4-hydroxymidazolam and 1-hydroxymidazolam glucuronide in human serum, plasma and urine. J Chromatogr B Analyt Technol Biomed Life Sci. 2021 Jan 1;1162:122476. doi: 10.1016/j.jchromb.2020.122476. Epub 2020 Dec 3. [Article]
- Comments
- Not Available
- Enzymes
Enzyme Km Vmax Role UDP-glucuronosyltransferase 2B7 Not Available Not Available confirmed
