Loperamide Hydrochloride

Generic Details

Generic Name

Loperamide-Hydrochloride

Other Names

  • Imodium

Drug Class

  • Antidiarrheal

Chemical Formula

C29H33ClN2O2

Molecular Weight

477.04 g/mol

Mechanism of Action

  • Acts on opioid receptors in the gut, decreasing gut motility and increasing transit time

Indications

  • Acute diarrhea
  • Chronic diarrhea
  • Traveler's diarrhea

Common Dosage Forms

  • Tablet
  • Capsule
  • Oral solution

Typical Dosage

  • 2 mg after the first loose stool, then 1 mg after each subsequent loose stool (not to exceed 16 mg/day)

Pediatric Dosage

  • Consult pediatrician for appropriate dosage based on weight and age

Geriatric Dosage

  • Lower initial and maintenance doses may be needed for the elderly

Side Effects

  • Constipation
  • Abdominal pain
  • Nausea
  • Vomiting
  • Dizziness

Contraindications

  • Hypersensitivity to loperamide
  • Acute dysentery
  • Abdominal pain without diarrhea

Pregnancy Category

  • C - Risk cannot be ruled out

Lactation Safety

  • Limited data available, caution advised

Drug Interactions

  • Avoid concomitant use with potent CYP3A4 inhibitors
  • Potential for interactions with other CNS depressants

Overdose Symptoms

  • Severe constipation
  • Paralytic ileus
  • Respiratory depression

Antidote for Overdose

  • No specific antidote, treatment is supportive

Storage Conditions

  • Store at room temperature between 20-25°C (68-77°F)
  • Protect from light and moisture

Pharmacokinetics

  • Absorption: Well absorbed from the GI tract
  • Distribution: Crosses the blood-brain barrier and placenta; found in breast milk
  • Metabolism: Primarily hepatic via CYP2C8
  • Excretion: Mainly in feces (40-50%), urine (1-13%)

Precautions

  • Monitor for signs of toxic megacolon in patients with inflammatory bowel disease

Warnings

  • Do not use in children under 2 years unless directed by a healthcare provider
  • Use with caution in hepatic impairment

Others

  • Avoid use in acute ulcerative colitis