DrugindexOnline^{2nd edition}

Pronouncation: (low-PEHR-uh-mide HIGH-droe-KLOR-ide)
Class: Antidiarrheal

Trade Names:
Diar-aid
- Tablets 2 mg

Trade Names:
Imodium
- Capsules 2 mg

Trade Names:
Imodium A-D
- Tablets 2 mg
- Liquid 1 mg/5 mL

Trade Names:
Kaopectate II Caplets
- Tablets 2 mg

Trade Names:
Neo-Diaral
- Capsules 2 mg

Trade Names:
Pepto Diarrhea Control
- Liquid 1 mg/ mL

Apo-Loperamide (Canada)
PMS-Loperamide Hydrochloride (Canada)
Rhoxal-loperamide (Canada)

Mechanism of Action

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 Diarrhea
Adults

PO 4 mg followed by 2 mg after each unformed stool, not to exceed 16 mg/24 h.

Children 8 to 12 yr of age (greater than 30 kg)

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 day

1 mg 3 times daily. May decrease to adjust for nutritional and hydration status after 24 h; usually 0.1 mg/kg after each loose stool but do not exceed total first day dosing recommendations on any day.

Chronic Diarrhea
Adults

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.