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Animal studies have shown that difenoxin hydrochloride manifests its antidiarrheal effect by slowing intestinal motility. The mechanism of action is by a local effect on the gastrointestinal wall.

Difenoxin is the principal active metabolite of diphenoxylate.

Following oral administration of MOTOFEN (difenoxin and atropine) ®, difenoxin is rapidly and extensively absorbed. Mean peak plasma levels of approximately 160 ng/mL occurred within 40 to 60 minutes in most patients following an oral dose of 2 mg. Plasma levels decline to less than 10% of their peak values within 24 hours and to less than 1% of their peak values within 72 hours. This decline parallels the appearance of difenoxin and its metabolites in the urine. Difenoxin is metabolized to an inactive hydroxylated metabolite. Both the drug and its metabolites are excreted, mainly as conjugates, in urine and feces.

Last reviewed on RxList: 5/12/2009
This monograph has been modified to include the generic and brand name in many instances.

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