Difenoxin

Difenoxin
Clinical data
Synonyms	Difenoxin, Motofen
Legal status
Legal status	US: Schedule I ;
Identifiers
	IUPAC name 1-[3-cyano-3,3-di(phenyl)propyl]-4-phenylpiperidine-4-carboxylic acid;
CAS Number	35607-36-4;
PubChem CID	34328;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C28H28N2O2
Molar mass	424.53 g/mol

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

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]

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References

↑ 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.
↑ 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.
↑ 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.

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[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.

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Difenoxin

References

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