Loperamide

Indications
 Oral
Acute diarrhoea
Adult: As hydrochloride: Initially, 4 mg followed by 2 mg after each loose stool. Usual dose: 6-8 mg daily. As oxide: Initially, 2-4 mg followed by 1 mg after each loose stool. Max dose as hydrochloride: 16 mg daily; as oxide: 8 mg daily.
Child: As hydrochloride: 4-8 yr: 1 mg 3 or 4 times daily for up to 3 days; 9-12 yr: 2 mg 4 times daily for up to 5 days.
Oral
Chronic diarrhoea
Adult: As hydrochloride: Initially, 4-8 mg daily in divided doses, adjusted if necessary. Max: 16 mg daily; discontinue if no improvement at this dose after 10 days.
Child: Treatment in children is generally not recommended but the following doses have been suggested: 1 mth-1 yr: As hydrochloride, 100-200 mcg/kg bid given 30 min before feeds (Max: 2 mg/kg daily); 1-12 yr: As hydrochloride, 100-200 mcg/kg (Max: 2 mg/dose) 3 to 4 times daily (Max: 16 mg daily).
Contraindications
 Conditions when inhibition of peristalsis is undesirable (e.g. ileus or megacolon); antibiotic induced colitis; active inflammatory bowel disease; if abdominal distention develops during use; abdominal pain in the absence of diarrhoea.
Warnings / Precautions
 Concomitant specific therapy must be given in those with infectious diarrhoea; hepatic dysfunction; infants; pregnancy, lactation.
Adverse Reactions
 Abdominal pain, distention, and discomfort; paralytic ileus; constipation, dry mouth, drowsiness, dizziness, fatigue, rash.
Potentially Fatal: Toxic megacolon.
Overdose Reactions
 Urinary retention, paralytic ileus and CNS depression may occur. Perform gastric lavage (not necessary if spontaneous vomiting occurs) followed by administration of a slurry of 100 g activated charcoal. If symptoms of overdose occur, naloxone may be given as an antidote.
Drug Interactions
 Bioavailability increased by co-trimoxazole, ritonavir, saquinavir. Respiratory depression reported when administered with quinidine. Loperamide increases GI absorption of desmopressin and decreases exposure to saquinavir.
See Below for More loperamide Drug Interactions
Mechanism of Actions
 Loperamide inhibits peristalsis and prolongs transit time by acting directly on intestinal wall muscles. It also reduces faecal volume, increases viscosity and decreases fluid and electrolyte loss.
Onset: 0.5-1 hr.
Absorption: Absorbed from the GI tract. Peak plasma concentrations achieved after 2.5 hr (oral solution) or 4-5 hr (capsule).
Excretion: Excreted in the urine (<2%) and faeces (30% as unchanged drug). Elimination half life of around 10.8 hr.
Administration
 May be taken with or without food.
ATC Classification
 A07DA03 - loperamide ; Belongs to the class of antipropulsives. Used in the treatment of diarrhea.
Available As
  • Loperamide 1 mg
  • Loperamide 1.5 mg
  • Loperamide 2 mg
  • Loperamide 4 mg
  • Loperamide 5 mg
  • Loperamide 7.5 mg

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