Difenoxin

Difenoxin (Motofen) is a 4-phenylpiperidine derivative that is related to the opioid analgesic drug pethidine (meperidine).

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Difenoxin is an active metabolite of the anti-diarrhea drug diphenoxylate.^[1] It is not used by itself and is a Schedule I drug in the USA, however in some countries a combination product containing difenoxin and atropine is used to treat diarrhea, in a similar way to how diphenoxylate itself is used.^[2]

Difenoxin also has some sedative and analgesic effects as with other opioids, but diphenoxylate itself is a relatively weak analgesic, and difenoxin has similarly limited analgesic effects, although it is a potent anti-diarrhoreal drug. Research suggests that additional non-opioid mechanisms may also be involved in the action of difenoxin, explaining its strong anti-diarrhoreal effects despite only limited opioid action.^[3]

References

1. ^ Jackson LS, Stafford JE. The evaluation and application of a radioimmunoassay for the measurement of diphenoxylic acid, the major metabolite of diphenoxylate hydrochloride (Lomotil), in human plasma. Journal of Pharmacological Methods. 1987 Nov;18(3):189-97.
2. ^ Innocenti P, Rossi L, Bombardieri G. Clinical effectiveness of difenoxine in patients with acute and chronic diarrhea. (Italian). Bollettino Chimico Farmaceutico. 1983 Dec;122(12):64S-68S.
3. ^ De Luca A, Coupar IM. Difenoxin and loperamide: studies on possible mechanisms of intestinal antisecretory action. Naunyn Schmiedebergs Archives of Pharmacology. 1993 Feb;347(2):231-7.