Related Compounds
Loperamide (Imodium) is also closely related to difenoxin in chemical structure but does not cross the blood–brain barrier as does difenoxin, and the combination drug diphenoxylate hydrochloride with atropine sulfate (Lomotil) is the prototype of this four-member subfamily of the synthetic opioid receptor agonists and sub-category of opioid anti-diarrhoeals. Pethidine was serendipitously discovered in research during the 1930s on gastrointestinal drugs to serve as alternatives to belladonna and opium derivatives, but the anti-diarrhoeal effects of pethidine are less than those of this subclass and equivalent constipating doses of pethidine have prominent central actions. Therefore, with difenoxin and related drugs, the ratio of GI effects to central narcotic effects is particularly high, which makes it an attractive alternative in the minds of many to the other opioids used for diarrhoea, viz. codeine, morphine, dihydrocodeine, paregoric, laudanum and opium . The parent of the three above-mentioned pethidine-related anti-diarrhoeals is diphenoxylic acid, which can also be manufactured and used pharmaceutically.
Read more about this topic: Difenoxin
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