Diphenoxylate resources


DRUG INFO
Diphenoxylate

Drug Name: Diphenoxylate

Indication: For as adjunctive therapy in the management of diarrhea



Pharmacology: 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.

Drug Category: Narcotics; Antidiarrheals; Antiperistaltic; ATC:A07DA01

Brand Names/Synonyms: Dea No. 9170; Difenossilato [Dcit]; Difenoxilato [Inn-Spanish]; Difenoxilato [Spanish]; Diphenoxalate; Diphenoxylate; Diphenoxylate Hydrochloride; Diphenoxylate-Atropine; Diphenoxylatum [Inn-Latin]; Diphenoxylatum [Latin]; HSDB 3067; Lomotil; R 1132; R-1132

Dosage Forms: Oral Solution; Tablet

Absorption: 90%

Interactions: DrugBank: Interactions for Diphenoxylate

Interactions for Diphenoxylate:


Known drug interactions include barbiturates, tranquilizers, and alcohol. Diphenoxylate HCl and atropine sulfate may interact with MAO inhibitors

In studies with male rats, diphenoxylate hydrochloride was found to inhibit the hepatic microsomal enzyme system at a dose of 2 mg/kg/day.

Therefore, diphenoxylate has the potential to prolong the biological half-lives of drugs for which the rate of elimination is dependent on the microsomal drug metabolizing enzyme system.





Chemical IUPAC Name: ethyl 1-(3-cyano-3,3-diphenyl-propyl)-4-phenyl-piperidine-4-carboxylate

Chemical Formula: C30H32N2O2

Half Life: 12-14 hours

Drug Type: Approved Drug

# Accession No: APRD00366

CAS Registry Number: 915-30-0



Diphenoxylate News
(When available)


Health Recommendations for Relief Workers Responding to Disasters  Dec 22, 2005
Community Dispatch (press release) Anti-motility agents, such as loperamide and diphenoxylate and/or bismuth subsalicylate (Pepto-Bismol), can reduce bowel movement frequency. ...

Prescribed drug addiction on rise  Jan 1, 2006
Ludhiana Newsline, Many people are into high addiction of lomotil, a medicine administered while someone suffers from diarrhoea. ‘‘We have been ...

Wortham: Club sicker than dogs  Dec 21, 2005
Bryan College Station Eagle, ...door. "Get some Peptol Bismol or Lomotil!" Doc shouted just before the door closed behind him. "Upset stomach," Doc answered. "We ...


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