Lomotil - General Information:

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.

Pharmacology:

Lomotil, an antidiarrheal, is effective as adjunctive therapy in the management of diarrhea. Lomotil 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.

Lomotil for patients

INFORM THE PATIENT (PARENT OR GUARDIAN) NOT TO EXCEED THE RECOMMENDED DOSAGE AND TO KEEP DIPHEN-OXYLATE HCL AND ATROPINE SULFATE OUT OF THE REACH OF CHILDREN AND IN A CHILD-RESISTANT CONTAINER, INFORM THE PATIENT OF THE CONSEQUENCES OF OVERDOSAGE, INCLUDING SEVERE RESPIRATORY DEPRESSION AND COMA, POSSIBLY LEADING TO PERMANENT BRAIN DAMAGE OR DEATH.

Diphenoxylate HCl and atropine sulfate may produce drowsiness or dizziness. The patient should be cautioned regarding activities requiring mental alertness, such as driving or operati ng dangerous machinery. Potentiation of the action of alcohol, barbiturates and tranquilizers with concomitant use of diphenoxylate HCl and atropine sulfate should be explained to the patient. The physician should also provide the patient with other information in this labeling, as appropriate.

Lomotil Interactions

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.

Lomotil Contraindications

Diphenoxylate HCl and atropine sulfate is contraindicated in patients with:

1. Known hypersensitivity to diphenoxylate or atropine.

2. Obstructive jaundice.

3. Diarrhea associated with pseudomembranous enterocolitis or enterotoxin-* producing bacteria.

Additional information about Lomotil

Lomotil Indication: For as adjunctive therapy in the management of diarrhea
Mechanism Of Action: Lomotil is an opiate receptor agonists that stimulate mu receptors in GI to decrease the peristalsis and constrict the sphincters. Lomotil 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 Interactions: Not Available
Food Interactions: Avoid alcohol.
Take with food.
Generic Name: Diphenoxylate
Synonyms: Dea No. 9170; Difenossilato [Dcit]; Difenoxilato [Inn-Spanish]; Diphenoxalate; Diphenoxylate Hydrochloride; Diphenoxylatum [Inn-Latin]
Drug Category: Narcotics; Antidiarrheals; Antiperistaltic
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Diphenoxylate: Lomotil;
Absorption: 90%
Toxicity (Overdose): 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
Protein Binding: 74-95%
Biotransformation: Hepatic
Half Life: 12-14 hours
Dosage Forms of Lomotil: Tablet Oral
Solution Oral
Chemical IUPAC Name: ethyl 1-[3-cyano-3,3-di(phenyl)propyl]-4-phenylpiperidine-4-carboxylate
Chemical Formula: C30H32N2O2
Diphenoxylate on Wikipedia: http://en.wikipedia.org/wiki/Diphenoxylate
Organisms Affected: Humans and other mammals

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