Diphenoxylate: profile and news

Fired campus bus driver had history of auto accidents Nov 16, 2005
...oxicated and possession of a controlled substance -- diphenoxylate with atropine, said Bloomington Police Department Capt. Joe Qualters. ... - Indiana Daily Student

HEALTH WARNINGS FOR TRAVELERS' Sep 13, 2005
Anti-motility agents such as loperamide and diphenoxylate and/or bismuth subsalicylate (Pepto-Bismol) can reduce bowel movement frequency. ... - One Bakersfield Online,

Four Local Dentists Disciplined By Licensing Board Aug 4, 2005
A dental board investigator also examined four prescriptions for diphenoxylate with atropine, an anti-diarrhea medication, that Jaynes wrote for himself. ... - RedNova.com

Bonds' doc on probation, was disciplined twice May 5, 2005
...to the documents, issued prescriptions for hydrocodone (a narcotic analgesic), zolpidem (sold as the sleeping aid Ambien) and diphenoxylate/atropine (usually ... - San Francisco Chronicle,

Other information

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
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