loperamide oxide

Loperamide oxide is a prodrug of loperamide, an antidiarrheal agent. It is converted to the active drug, loperamide, in the gastrointestinal tract. Loperamide acts as a mu-opioid receptor agonist in the intestinal wall, inhibiting acetylcholine and prostaglandin release, which reduces peristalsis and increases absorption of fluids and electrolytes. This results in decreased gut motility and relief from diarrhea. Loperamide oxide has been shown to have similar antisecretory potency as loperamide itself in both the jejunum and colon. It has been used for treating acute diarrhea (notably under the brand name Arestal in the Netherlands) and has demonstrated efficacy for chronic diarrhea associated with Crohn's disease[1][6][8]. The drug was developed by Janssen Pharmaceutica.

Brand names

Arestal

Other names

loperamide N-oxide