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Look Up > Drugs > Loperamide
Loperamide
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(loe PER a mide)

U.S. Brand Names
Diar-aid®[OTC]; Imodium®; Imodium® A-D [OTC]; Kaopectate® II [OTC]; Pepto® Diarrhea Control [OTC]

Generic Available

Yes


Canadian Brand Names
PMS-Loperamine

Synonyms
Loperamide Hydrochloride

Pharmacological Index

Antidiarrheal


Use

Treatment of acute diarrhea and chronic diarrhea associated with inflammatory bowel disease; chronic functional diarrhea (idiopathic), chronic diarrhea caused by bowel resection or organic lesions; to decrease the volume of ileostomy discharge


Pregnancy Risk Factor

B


Contraindications

Patients who must avoid constipation, diarrhea resulting from some infections, or in patients with pseudomembranous colitis, hypersensitivity to specific drug or component, bloody diarrhea


Warnings/Precautions

Large first-pass metabolism, use with caution in hepatic dysfunction; should not be used if diarrhea accompanied by high fever, blood in stool


Adverse Reactions

Percentage unknown: Sedation, fatigue, dizziness, drowsiness, rash, nausea, vomiting, constipation, abdominal cramping, xerostomia, abdominal distention


Overdosage/Toxicology

Symptoms of overdose include CNS and respiratory depression, gastrointestinal cramping, constipation, GI irritation, nausea, vomiting; overdosage is noted when daily doses approximate 60 mg of loperamide

Treatment of overdose: Gastric lavage followed by 100 g activated charcoal through a nasogastric tube. Monitor for signs of CNS depression; if they occur, administer naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as necessary up to a total of 10 mg.


Drug Interactions

Increased toxicity: CNS depressants, phenothiazines, tricyclic antidepressants may potentiate the adverse effects


Mechanism of Action

Acts directly on intestinal muscles to inhibit peristalsis and prolongs transit time enhancing fluid and electrolyte movement through intestinal mucosa; reduces fecal volume, increases viscosity, and diminishes fluid and electrolyte loss; demonstrates antisecretory activity; exhibits peripheral action


Pharmacodynamics/Kinetics

Onset of action: Oral: Within 0.5-1 hour

Absorption: Oral: <40%; levels in breast milk expected to be very low

Protein binding: 97%

Metabolism: Hepatic (>50%) to inactive compounds

Half-life: 7-14 hours

Elimination: Fecal and urinary (1%) excretion of metabolites and unchanged drug (30% to 40%)


Usual Dosage

Oral:

Acute diarrhea: Initial doses (in first 24 hours):

2-6 years: 1 mg 3 times/day

6-8 years: 2 mg twice daily

8-12 years: 2 mg 3 times/day

Maintenance: After initial dosing, 0.1 mg/kg doses after each loose stool, but not exceeding initial dosage

Chronic diarrhea: 0.08-0.24 mg/kg/day divided 2-3 times/day, maximum: 2 mg/dose

Adults: Initial: 4 mg (2 capsules), followed by 2 mg after each loose stool, up to 16 mg/day (8 capsules)


Mental Health: Effects on Mental Status

May cause drowsiness or dizziness


Mental Health: Effects on Psychiatric Treatment

Concurrent use with psychotropics may produce additive sedation and dry mouth


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Do not take more than 8 capsules or 80 mL in 24 hours. May cause drowsiness. If acute diarrhea lasts longer than 48 hours, consult prescriber. Do not take if diarrhea is bloody.


Nursing Implications

Therapy for chronic diarrhea should not exceed 10 days


Dosage Forms

Caplet, as hydrochloride: 2 mg

Capsule, as hydrochloride: 2 mg

Liquid, oral, as hydrochloride: 1 mg/5 mL (60 mL, 90 mL, 120 mL)

Tablet, as hydrochloride: 2 mg


References

Bhutta TI and Tahir KI, "Loperamide Poisoning in Children," Lancet, 1990, 335(8685):363.

Ericsson CD and Johnson PC, "Safety and Efficacy of Loperamide," Am J Med, 1990, 88(6A):10S-14S.

Friedli G and Haenggeli CA, "Loperamide Overdose Managed by Naloxone," Lancet, 1980, 1:1413.

Schwartz RH and Rodriguez WJ, "Toxic Delirium Possibly Caused by Loperamide," J Pediatr, 1991, 118(4 Pt 1):656-7.


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