Loperamide Hydrochloride
PronunciationClass: Antidiarrheal
Trade Names:
Diar-aid
- Tablets 2 mg
Trade Names:
Imodium
- Capsules 2ߙmg
Trade Names:
Imodium A-D
- Tablets 2 mg
- Liquid 1ߙmg/5 mL
Trade Names:
Kaopectate II Caplets
- Tablets 2ߙmg
Trade Names:
Neo-Diaral
- Capsules 2 mg
Trade Names:
Pepto Diarrhea Control
- Liquid 1 mg/ mL
PMS-Loperamide Hydrochloride (Canada)
Rhoxal-loperamide (Canada)
Pharmacology
Slows intestinal motility, affects water and electrolyte movement through intestine, inhibits peristalsis, reduces daily fecal volume, increases viscosity and bulk density of stool, diminishes loss of fluid and electrolytes.
Pharmacokinetics
Absorption
T max is 5 h (capsule) and 2.5 h (liquid). Bioavailability is 40%.
Elimination
Apparent t ½ is 10.8 h (9.1 to 14.4 h). 25% is excreted unchanged in the feces; 1.3% is excreted in the urine unchanged and conjugated.
Indications and Usage
Control and symptomatic relief of acute nonspecific or chronic diarrhea; reduction in volume of ileostomy output.
Contraindications
Pseudomembranous colitis caused by antibiotic use; acute diarrhea associated with organisms that penetrate intestinal wall (eg, toxigenic Escherichia coli , Salmonella , Shigella ); conditions in which constipation should be avoided; bloody diarrhea; fever; acute ulcerative colitis (potential for toxic megacolon).
Dosage and Administration
Acute DiarrheaAdults
PO 4 mg followed by 2 mg after each unformed stool, not to exceed 16 mg/24ߙh.
Children 8 to 12ߙyr of age (greater than 30ߙkg)2 mg 3 times daily.
Children 6 to 8 yr of age (20 to 30 kg)2 mg twice daily.
Children 2 to 5 yr of age (13 to 20 kg) First day1 mg 3 times daily. May decrease to adjust for nutritional and hydration status after 24 h; usually 0.1ߙmg/kg after each loose stool but do not exceed total first day dosing recommendations on any day.
Chronic DiarrheaAdults
PO 4 to 8 mg every day or twice daily.
Storage/Stability
Store at room temperature.
Drug Interactions
None well documented.
Laboratory Test Interactions
None well documented.
Adverse Reactions
CNS
Fatigue; drowsiness; dizziness.
Dermatologic
Rash.
GI
Abdominal pain; distention or discomfort; constipation; nausea; vomiting; dry mouth.
Precautions
Pregnancy
Category B .
Lactation
Undetermined.
Children
Not recommended for children less than 2 yr of age. Use with caution in young children.
Hepatic Function
Hepatic coma may be precipitated in patients with advanced hepatorenal disease or hepatic dysfunction.
Acute ulcerative colitis
Agents that inhibit intestinal motility or delay intestinal transit time may induce toxic megacolon. Discontinue if abdominal distention or other untoward symptoms occur.
Overdosage
Symptoms
Constipation, CNS depression, GI irritation.
Patient Information
- Instruct patient to record number and consistency of stools.
- Inform patient that medication may cause dry mouth. Encourage patient to drink plenty of clear fluids to help prevent dehydration that may accompany diarrhea.
- Advise patient to notify health care provider if diarrhea persists more than 48 h or if fever develops.
- Inform patient that drug may cause drowsiness or dizziness and to use caution while driving or performing other tasks requiring mental alertness.





