Reaction: Loperamide to 1 product
- Reaction
- Reaction type
- N-demethylation
- Direction
- Major circulating metabolite?
- Yes
- Spontaneous?
- No
- Activity
- inactive
- References
- Kalgutkar AS, Nguyen HT: Identification of an N-methyl-4-phenylpyridinium-like metabolite of the antidiarrheal agent loperamide in human liver microsomes: underlying reason(s) for the lack of neurotoxicity despite the bioactivation event. Drug Metab Dispos. 2004 Sep;32(9):943-52. [Article]
- Lin QM, Li YH, Liu Q, Pang NH, Xu RA, Cai JP, Hu GX: Functional characteristics of CYP3A4 allelic variants on the metabolism of loperamide in vitro. Infect Drug Resist. 2019 Sep 10;12:2809-2817. doi: 10.2147/IDR.S215129. eCollection 2019. [Article]
- FDA Discontinued Drug Products: IMODIUM (loperamide) Oral Tablets [Link]
- Comments
- Not Available
- Enzymes
Enzyme Km Vmax Role Cytochrome P450 3A4 Not Available Not Available implied Cytochrome P450 2D6 Not Available Not Available implied Cytochrome P450 2C8 Not Available Not Available implied Cytochrome P450 2B6 Not Available Not Available implied