|
| Pronunciation |
|
(loe
PER a
mide) |

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

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| Generic
Available |
|
|
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 |
|
|
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 |
|
|
B |

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|
| 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 |

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| 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 |

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| 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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