Diphenoxylate

Products

Diphenoxylate is not commercially available in many countries. Combination products with atropine sulfate are commercially available in the United States.

Structure and properties

Diphenoxylate (C30H32N2O2, Mr = 452.6 g/mol) is present in drugs as diphenoxylate hydrochloride, a white crystalline powder that is very sparingly soluble in water. It is a derivative of pethidine and structurally related to loperamide.

Effects

Diphenoxylate (ATC A07DA01) is antidiarrheal. It is a prodrug that is biotransformed in the organism by ester hydrolysis to the active acid difenoxin. Its effects are based on inhibition of intestinal motility, resulting in a longer contact time of intestinal contents with the mucosa.

Indications

For the treatment of diarrheal diseases.