Antidiarrheals

Loperamide

Indications Listed in Dosage.

Dosage Adult: PO Acute diarrhoea As HCl: Inital: 4mg, then 2 mg after each loose stool. Usual dose: 6-8 mg/day. As oxide: Inital: 2-4 mg, then 1 mg after each loose stool. Max: 16 mg/day (as HCl) or 8 mg/day (as oxide). Chronic diarrhoea As HCl: Initial: 4-8 mg/day in divided doses. Max: 16 mg/day.

Administration May be taken with or without food.

Overdosage For action to be taken in the event of accidental overdose

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.

Special Precautions Concomitant specific therapy must be given in those with infectious diarrhoea; hepatic dysfunction; infants; pregnancy, lactation.

Adverse Drug Reactions Abdominal pain, distention, and discomfort; paralytic ileus; constipation, dry mouth, drowsiness, dizziness, fatigue, rash.

Potentially Fatal: Toxic megacolon.

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.

Pregnancy Category (US FDA)

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Mechanism of Action

Class Antidiarrheals

ATC Classification A07DA03 - loperamide ; Belongs to the class of antipropulsives. Used in the treatment of diarrhea.

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