NCIt definition : A phenylpiperidine with antidiarrheal activity and an active metabolite of diphenoxylate.
Difenoxin is chemically related to the narcotic opioid meperidine. Difenoxin acts
primarily on the gastrointestinal wall by binding to opioid receptors on acetylcholine-containing
nerves and inhibiting the release of acetylcholine from presynaptic nerve terminals.
This leads to a reduction in intestinal motility. Difenoxin hydrochloride also mimics
the action of endogenous opioid peptides at the CNS opioid receptors, (primarily mu-receptors),
thereby inducing CNS effects.;