Description

Simple

A medication used to treat diarrhea.

Clinical

A long acting antidiarrheal used to control nonspecific diarrhea and chronic diarrhea caused by inflammatory bowel disease, or gastroenteritis.

Overview

One of the long-acting synthetic antidiarrheals; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.

Pharmacology

Indication

For the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease or gastroenteritis. Also used for reducing the volume of discharge from ileostomies.

Pharmacodynamic

Loperamide is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide is also indicated for reducing the volume of discharge from ileostomies. In man, Loperamide prolongs... Read more

Mechanism of action

In vitro and animal studies show that Loperamide acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide inhibits peristaltic activity by a direct effect on the circular and longitudinal muscles of the intestinal wall. It is a non-sele... Read more

Absorption

Not significantly absorbed from the gut

Protein binding

97%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

9.1 to 14.4 hours (average 10.8 hours)

Route of elimination

Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces.

Toxicity

Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Abdominal pain without diarrhea
      • Drugbank Id: DBCOND0108046
  • Regions: US
  • Below Age:
    • Amount: 24
    • Unit: month
  • Regions: US
  • Patient Conditions:
      • Name: Use as primary therapy for acute ulcerative colitis
      • Drugbank Id: DBCOND0108048
  • Regions: US
  • Patient Conditions:
      • Name: Use as primary therapy for acute dysentery
      • Drugbank Id: DBCOND0108047
  • Regions: US
  • Patient Conditions:
      • Name: Use as primary therapy for pseudomembranous colitis
      • Drugbank Id: DBCOND0108050
  • Regions: US
  • Patient Conditions:
      • Name: Use as primary therapy for bacterial enterocolitis
      • Drugbank Id: DBCOND0108049

Food Interactions

  • Take without regard to meals. Increase liquid intake.

Interactions

Type in a drug name to check for interaction with Loperamide
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Loperamide.
(S)-Warfarin
The serum concentration of (S)-Warfarin can be increased when it is combined with Loperamide.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Loperamide can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Loperamide is combined with 2,4-thiazolidinedione.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Loperamide.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Loperamide.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Loperamide.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Loperamide.
Abafungin
The therapeutic efficacy of Abafungin can be increased when used in combination with Loperamide.
Abatacept
The metabolism of Loperamide can be increased when combined with Abatacept.
Abemaciclib
The metabolism of Abemaciclib can be decreased when combined with Loperamide.
Abexinostat
The risk or severity of QTc prolongation can be increased when Loperamide is combined with Abexinostat.
Abiraterone
The metabolism of Abiraterone can be decreased when combined with Loperamide.
Acarbose
The risk or severity of hypoglycemia can be increased when Loperamide is combined with Acarbose.
Acebutolol
The risk or severity of bradycardia can be increased when Loperamide is combined with Acebutolol.
Aceclofenac
The risk or severity of hyperkalemia can be increased when Loperamide is combined with Aceclofenac.
Acemetacin
The risk or severity of hyperkalemia can be increased when Loperamide is combined with Acemetacin.
Acenocoumarol
The serum concentration of Acenocoumarol can be increased when it is combined with Loperamide.
Acepromazine
The risk or severity of hypotension can be increased when Acepromazine is combined with Loperamide.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Loperamide is combined with Aceprometazine.