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Pronunciation
(loe PER a mide)
Generic Available (U.S.)
Yes
Index Terms
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Treatment of chronic diarrhea associated with inflammatory bowel disease; acute nonspecific diarrhea; increased volume of ileostomy discharge
OTC labeling: Control of symptoms of diarrhea, including Traveler's diarrhea
Use: Unlabeled/Investigational
Cancer treatment-induced diarrhea (eg, irinotecan induced); chronic diarrhea caused by bowel resection
Pregnancy Risk Factor
C
Pregnancy Considerations
Teratogenic effects were not observed in animal studies.
Lactation
Enters breast milk/not recommended.
Contraindications
Hypersensitivity to loperamide or any component of the formulation; abdominal pain without diarrhea; children <2 years
Avoid use as primary therapy in acute dysentery, acute ulcerative colitis, bacterial enterocolitis, pseudomembranous colitis
Warnings/Precautions
Concerns related to adverse effects:
• Allergic reactions: Rare cases of anaphylaxis and anaphylactic shock have been reported.
• GI effects: Discontinue if constipation, abdominal pain, or ileus develop.
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment because of reduced first-pass metabolism; monitor for signs of CNS toxicity.
Special populations:
• AIDS patients: Use with caution in treatment of AIDS patients; stop therapy at the sign of abdominal distention. Cases of toxic megacolon have occurred in AIDS patients with infectious colitis.
• Pediatrics: Use with caution in young children as response may be variable because of dehydration.
Other warnings/precautions:
• Appropriate use: Loperamide is a symptom-directed treatment; if an underlying diagnosis is made, other disease-specific treatment may be indicated. Should not be used if diarrhea is accompanied by high fever or blood in stool. Should not be used when inhibition of peristalsis is undesirable or dangerous. Concurrent fluid and electrolyte replacement is often necessary in all age groups depending upon severity of diarrhea.
• OTC labeling: If diarrhea lasts longer than 2 days, patient should stop taking loperamide and consult healthcare provider.
Adverse Reactions
1% to 10%:
Central nervous system: Dizziness (1%)
Gastrointestinal: Constipation (2% to 5%), abdominal cramping (<1% to 3%), nausea (<1% to 3%)
Postmarketing and/or case reports: Abdominal distention, abdominal pain, allergic reactions, anaphylactic shock, anaphylactoid reactions, angioedema, bullous eruption (rare), drowsiness, dry mouth, dyspepsia, erythema multiforme (rare), fatigue, flatulence, paralytic ileus, megacolon, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, toxic megacolon, urinary retention, urticaria, vomiting
Metabolism/Transport Effects
Substrate of CYP2B6 (minor), P-glycoprotein
Drug Interactions
P-Glycoprotein Inducers: May decrease the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-Glycoprotein Inhibitors: May increase the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Storage
Store at 15°C to 25°C (59°F to 77°F).
Mechanism of Action
Acts directly on circular and longitudinal intestinal muscles, through the opioid receptor, to inhibit peristalsis and prolong transit time; reduces fecal volume, increases viscosity, and diminishes fluid and electrolyte loss; demonstrates antisecretory activity. Loperamide increases tone on the anal sphincter
Pharmacodynamics/Kinetics
Absorption: Poor
Distribution: Poor penetration into brain; low amounts enter breast milk
Metabolism: Hepatic via oxidative N-demethylation
Half-life elimination: 7-14 hours
Time to peak, plasma: Liquid: 2.5 hours; Capsule: 5 hours
Excretion: Urine and feces (1% as metabolites, 30% to 40% as unchanged drug)
Dosage
Oral:
Children:
Acute diarrhea: Initial doses (in first 24 hours):
2-5 years (13-20 kg): 1 mg 3 times/day
6-8 years (20-30 kg): 2 mg twice daily
8-12 years (>30 kg): 2 mg 3 times/day
Maintenance: After initial dosing, 0.1 mg/kg doses after each loose stool, but not exceeding initial dosage
Traveler's diarrhea:
6-8 years: 2 mg after first loose stool, followed by 1 mg after each subsequent stool (maximum dose: 4 mg/day)
9-11 years: 2 mg after first loose stool, followed by 1 mg after each subsequent stool (maximum dose: 6 mg/day)
≥12 years: See adult dosing.
Adults:
Acute diarrhea: Initial: 4 mg, followed by 2 mg after each loose stool, up to 16 mg/day
Chronic diarrhea: Initial: Follow acute diarrhea; maintenance dose should be slowly titrated downward to minimum required to control symptoms (typically, 4-8 mg/day in divided doses)
Traveler's diarrhea: Initial: 4 mg after first loose stool, followed by 2 mg after each subsequent stool (maximum dose: 8 mg/day)
Irinotecan-induced diarrhea (unlabeled use): 4 mg after first loose or frequent bowel movement, then 2 mg every 2 hours until 12 hours have passed without a bowel movement. If diarrhea recurs, then repeat administration
Dosage adjustment in hepatic impairment: No specific guidelines available.
Dietary Considerations
Some products may contain sodium.
Patient Education
May cause drowsiness. If acute diarrhea lasts longer than 48 hours, consult prescriber. Do not take if diarrhea is bloody.
Geriatric Considerations
Elderly are particularly sensitive to fluid and electrolyte loss. This generally results in lethargy, weakness, and confusion. Repletion and maintenance of electrolytes and water are essential in the treatment of diarrhea. Drug therapy must be limited in order to avoid toxicity with this agent.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
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
Nursing: Physical Assessment/Monitoring
Assess for cause of diarrhea before administering first dose.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet, oral, as hydrochloride: 2 mg
Anti-Diarrheal: 2 mg
Diamode: 2 mg
Imodium® A-D: 2 mg [scored]
Capsule, oral, as hydrochloride: 2 mg
Liquid, oral, as hydrochloride: 1 mg/5 mL (120 mL)
Anti-Diarrheal: 1 mg/5 mL (120 mL)
Imodium® A-D: 1 mg/5 mL (60 mL, 120 mL) [contains benzoic acid, ethanol 0.5%, sodium benzoate; cherry-mint flavor]
Imodium® A-D: 1 mg/7.5 mL (120 mL) [contains sodium 10 mg/30 mL, sodium benzoate; creamy-mint flavor]
Imodium® A-D for children: 1 mg/7.5 mL (120 mL) [contains sodium 16 mg/30 mL, sodium benzoate; creamy-mint flavor]
Solution, oral, as hydrochloride: 1 mg/5 mL (5 mL, 10 mL)
Pricing: U.S. (www.drugstore.com)
Capsules (Loperamide HCl)
2 mg (30): $12.99
References
Benson AB 3rd, Ajani JA, Catalano RB, et al, "Recommended Guidelines for the Treatment of Cancer Treatment-Induced Diarrhea," J Clin Oncol, 2004, 22(14):2918-26.
Bhutta TI and Tahir KI, “Loperamide Poisoning in Children,” Lancet, 1990, 335(8685):363.
Ericsson CD, "Nonantimicrobial Agents in the Prevention and Treatment of Traveler's Diarrhea," Clin Infect Dis, 2005, 41(Suppl 8):557-63.
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.
Rothenberg ML, Eckardt JR, Kuhn JG, et al, "Phase II Trial of Irinotecan in Patients With Progressive or Rapidly Recurrent Colorectal Cancer," J Clin Oncol, 1996, 14(4):1128-35.
Schwartz RH and Rodriguez WJ, “Toxic Delirium Possibly Caused by Loperamide,” J Pediatr, 1991, 118(4 Pt 1):656-7.
International Brand Names
Lexi-Comp.com
Last full review/revision June 2011
Content last modified June 2011
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