Diphenoxylate drug data and news

Diphenoxylate drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Diphenoxylate
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
Indication For as adjunctive therapy in the management of diarrhea
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Description Not Available
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.
Diphenoxylate News
(When available)

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,

Dosage Forms Oral Solution; Tablet
Drug_Category Narcotics; Antidiarrheals; Antiperistaltic; ATC:A07DA01
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.

Toxicity 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
Organisms Affected Humans and other mammals
Chemical IUPAC Name ethyl 1-(3-cyano-3,3-diphenyl-propyl)-4-phenyl-piperidine-4-carboxylate
Chemical Formula C30H32N2O2
Molecular Weight 452.587 g/mol
Smiles String CCOC(=O)C1(CCN(CC1)CCC(C#N)(C2=CC=CC=C2)C3=CC=CC=C3)C4=CC=CC=C4
Melting Point 221 °C
Water Solubility 0.8 mg/ml
State Solid
LogP/Hphobicity 7.385
Isoelectric Point Not Available
Biotransformation Hepatic
Half Life 12-14 hours
Protein Binding [%] 74-95%
RxList Link RXlist
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Drug Reference http://www.rxlist.com/cgi/generic3/diphenoxylate.htm
Drug Type Approved Drug
Accession No APRD00366
CAS Registry Number 915-30-0
KEGG Compound ID D00301
PubChem ID SID:10074
PharmGKB ID Not Available
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

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