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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.
==Actions and use==
Diphenoxylate works by decreasing the speed and amplitude of wave-like movements of the intestines (peristalsis) therefore allowing the body time to remove moisture from the intestinal contents and consolidate waste product into a dense solid form rather than loose and watery as is diarrhea.
Similar to loperamide and difenoxin preparations, the usual protocol is to take a loading dose (usually two tablets or the quantity of liquid containing 5 mg of diphenoxylate) and then the standard dose of one tablet every 3 to 4 hours ''prn'' over a time period not to exceed 48 hours unless so ordered by the physician. Long-term intermittent ''prn'' users should contact their physician if the need for it arises more than was usual at the outset of therapy as tolerance to diphenoxylate can occur. Those taking it in large quantities or continuously over an extended period should taper down the dose on a schedule devised by the physician and/or pharmacist.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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