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QuickView for Diphenoxylate (compound)
PubChem
| Name: | Diphenoxylate |
|---|---|
| PubChem Compound ID: | 13505 |
| Description: | 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. |
| Molecular formula: | C30H32N2O2 |
| Molecular weight: | 452.587 g/mol |
| Synonyms: |
5-22-02-00487 (Beilstein Handbook Reference); R-1132; 4-Piperidinecarboxylic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester (9CI); 1-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-isonipecotic acid ethyl ester; Difenoxilato [Spanish]; 1-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylic acid ethyl ester; 915-30-0; Diphenoxylatum [Latin]; Isonipecotic acid, 1-(3-cyano-3,3-diphenylpropyl)-4-phenyl-, ethyl ester; 2,2-Diphenyl-4-(4-carbethoxy-4-phenylpiperidino)butyronitrile.
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DrugBank
Identification
| Name: | Diphenoxylate |
|---|---|
| Name (isomeric): | DB01081 |
| Drug Type: | small molecule |
| Description: | 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. |
| Synonyms: |
Diphenoxylatum [INN-Latin]; Diphenoxylate Hydrochloride; Diphenoxalate; Difenossilato [Dcit]; Dea No. 9170; Difenoxilato [INN-Spanish]
|
| Brand: | Lomotil |
| Brand name mixture: | Lomotil(Atropine Sulfate + Diphenoxylate Hcl) |
| Category: | Antiperistaltic, Narcotics, Analgesics, Opioid, Antidiarrheals |
| CAS number: | 915-30-0 |
Pharmacology
| 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 diphenoxyl...
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| Absorption: | 90% |
| Protein binding: | 74-95% |
| Biotransformation: | Hepatic |
| Half Life: | 12-14 hours |
| 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 |
| Affected organisms: | Humans and other mammals |
Interactions
| Food interaction: |
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Targets
