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diphenoxylate

n. (context pharmaceutical drug English) A particular narcotic used in the treatment of diarrhea.

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Diphenoxylate

Diphenoxylate ( INN, BAN) (brand name Diocalm), or diphenoxylate hydrochloride ( USAN), is a centrally-active opioid drug of the phenylpiperidine series that is used for the treatment of diarrhea. It acts by slowing intestinal contractions and peristalsis allowing the body to consolidate intestinal contents and prolong transit time, thus allowing the intestines to draw moisture out of them at a normal or higher rate and therefore stop the formation of loose and liquid stools. It is the main active ingredient in the anti- peristaltic medication Lomotil, which also contains atropine.

Diphenoxylate is the prototype of a small subfamily of opioids (the phenylpiperidines) including difenoxin (diphenoxylic acid), an active metabolite of diphenoxylate produced in the human body, and loperamide, which unlike the former two works exclusively in the intestines because it only crosses the blood–brain barrier in very small amounts. It was discovered at Janssen Pharmaceutica in 1956. It is a congener to the narcotic pethidine. Other somewhat more distant relatives include alphaprodine and piritramide.