Diphenoxylate

Diphenoxylate 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.

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.

Trade Name Diphenoxylate
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
Diphenoxylate
Diphenoxylate

Uses

Diphenoxylate is an antidiarrheal medication used with atropine to manage diarrhea.

For as adjunctive therapy in the management of diarrhea

Diphenoxylate is also used to associated treatment for these conditions: Diarrhoea

How Diphenoxylate works

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.

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

You find simplified version here Diphenoxylate

*** Taking medicines without doctor's advice can cause long-term problems.
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