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Home / Drugs / Starting with D / Diphenoxylate

A meperidine congener used as an antidiarrheal, usually in combination with atropine. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. This medication is classified as a Schedule V under the Controlled Substances Act by the Food and Drug Administration (FDA) and the DEA in the United States when used in preparations. When diphenoxylate is used alone, it is classified as a Schedule II.
Analgesics, Opioid
PackagersAmerisource Health Services Corp.
Amneal Pharmaceuticals
A-S Medication Solutions LLC
Bryant Ranch Prepack
Cardinal Health
Caremark LLC
Comprehensive Consultant Services Inc.
Direct Dispensing Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Eon Labs
GD Searle LLC
Group Health Cooperative
H.J. Harkins Co. Inc.
Heartland Repack Services LLC
Ivax Pharmaceuticals
Kaiser Foundation Hospital
Keltman Pharmaceuticals Inc.
Lake Erie Medical and Surgical Supply
Lannett Co. Inc.
Murfreesboro Pharmaceutical Nursing Supply
Nucare Pharmaceuticals Inc.
Palmetto Pharmaceuticals Inc.
Patient First Corp.
PD-Rx Pharmaceuticals Inc.
Pharmacia Inc.
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Prepackage Specialists
Prepak Systems Inc.
Rebel Distributors Corp.
Redpharm Drug
Remedy Repack
Roxane Labs
Sandhills Packaging Inc.
St Mary's Medical Park Pharmacy
UDL Laboratories
Va Cmop Dallas
SynonymsDea No. 9170
Difenossilato [Dcit]
Difenoxilato [INN-Spanish]
Diphenoxylate Hydrochloride
Diphenoxylatum [INN-Latin]


For as adjunctive therapy in the management of diarrhea


Diphenoxylate, an antidiarrheal, is effective as adjunctive therapy in the management of diarrhea. Diphenoxylate is rapidly and extensively metabolized in man by ester hydrolysis to diphenoxylic acid (difenoxine), which is biologically active and the major metabolite in the blood.

mechanism of action

Diphenoxylate is an opiate receptor agonists that stimulate mu receptors in GI to decrease the peristalsis and constrict the sphincters. Diphenoxylate has a direct effect on circular smooth muscle of the bowel, that conceivably results in segmentation and prolongation of gastrointestinal transit time. The clinical antidiarrheal action of diphenoxylate may thus be a consequence of enhanced segmentation that allows increased contact of the intraluminal contents with the intestinal mucosa.


Coma, dry skin and mucous membranes, enlarged pupils of the eyes, extremely high body temperature, flushing, involuntary eyeball movement, lower than normal muscle tone, pinpoint pupils, rapid heartbeat, restlessness, sluggishness, suppressed breathing





half life

12-14 hours

drug interactions

Donepezil: Possible antagonism of action

Galantamine: Possible antagonism of action