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Pronunciation |
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(loe
PER a
mide) |
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U.S. Brand
Names |
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Diar-aid®[OTC]; Imodium®;
Imodium® A-D [OTC]; Kaopectate® II [OTC]; Pepto®
Diarrhea Control
[OTC] |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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PMS-Loperamine |
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Synonyms |
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Loperamide Hydrochloride |
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Pharmacological Index |
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Antidiarrheal |
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Use |
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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 |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Patients who must avoid constipation, diarrhea resulting from some
infections, or in patients with pseudomembranous colitis, hypersensitivity to
specific drug or component, bloody diarrhea |
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Warnings/Precautions |
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Large first-pass metabolism, use with caution in hepatic dysfunction; should
not be used if diarrhea accompanied by high fever, blood in
stool |
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Adverse
Reactions |
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Percentage unknown: Sedation, fatigue, dizziness, drowsiness, rash, nausea,
vomiting, constipation, abdominal cramping, xerostomia, abdominal
distention |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
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Increased toxicity: CNS depressants, phenothiazines, tricyclic
antidepressants may potentiate the adverse effects |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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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%) |
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Usual Dosage |
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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) |
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Mental Health: Effects
on Mental Status |
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May cause drowsiness or dizziness |
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Mental Health:
Effects on Psychiatric
Treatment |
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Concurrent use with psychotropics may produce additive sedation and dry
mouth |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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. |
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Nursing
Implications |
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Therapy for chronic diarrhea should not exceed 10 days |
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Dosage Forms |
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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 |
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References |
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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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