Difenoxilato
Difenoxilato Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
Difenoxilato, an antidiarrheal, is effective as adjunctive therapy in the management of diarrhea. Difenoxilato 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.
Trade Name | Difenoxilato |
Generic | Diphenoxylate |
Diphenoxylate Other Names | Difenossilato, Difenoxilato, Diphenoxylate, Diphenoxylatum |
Type | |
Formula | C30H32N2O2 |
Weight | Average: 452.5873 Monoisotopic: 452.246378278 |
Protein binding | 74-95% |
Groups | Approved, Illicit |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Difenoxilato is an antidiarrheal medication used with atropine to manage diarrhea.
For as adjunctive therapy in the management of diarrhea
Difenoxilato is also used to associated treatment for these conditions: Diarrhoea
How Difenoxilato works
Difenoxilato is an opiate receptor agonists that stimulate mu receptors in GI to decrease the peristalsis and constrict the sphincters. Difenoxilato 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.
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
Food Interaction
- Avoid alcohol.
- Take with food.
Elimination Route
90%
Half Life
12-14 hours
Innovators Monograph
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