difenoxin

Difenoxin is a synthetic opioid antidiarrheal agent and the principal active metabolite of diphenoxylate. It is used primarily as an adjunct for the management of acute nonspecific diarrhea and acute exacerbations of chronic functional diarrhea. Difenoxin acts mainly in the periphery by activating opioid receptors in the intestine, thereby inhibiting peristalsis and slowing intestinal transit time. This results in decreased frequency and liquidity of bowel movements. While structurally related to meperidine, difenoxin has minimal central nervous system effects at therapeutic doses but can cross the blood-brain barrier at higher doses to produce weak sedative or analgesic effects. To deter abuse, it is commonly formulated with atropine (as in Motofen), which induces unpleasant side effects if taken in excess[1][2][4][5]. Difenoxin alone is classified as a Schedule I controlled substance in the US; when combined with atropine, it is Schedule IV.

Brand names

Motofen

Other names

difenoxindiphenoxylic acid