Reaction: Loperamide to 1 product

Reaction
Reaction type
N-demethylation
Direction
Major circulating metabolite?
Yes
Spontaneous?
No
Activity
inactive
References
  1. 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]
  2. 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]
  3. FDA Discontinued Drug Products: IMODIUM (loperamide) Oral Tablets [Link]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
Cytochrome P450 3A4Not AvailableNot Availableimplied
Cytochrome P450 2D6Not AvailableNot Availableimplied
Cytochrome P450 2C8Not AvailableNot Availableimplied
Cytochrome P450 2B6Not AvailableNot Availableimplied