Generic
Loperamide
5 brands available in the market
At a glance
Loperamide is used in the treatment of diarrhea. It slows down intestinal contractions, decreasing the speed at which contents pass through, allowing more time for reabsorption of fluids and nutrients, making stools more solid and less frequent.
Description
Loperamide binds to opioid receptors in the gut wall, reducing propulsive peristalsis, increasing intestinal transit time, increasing anal sphincter tone, and inhibiting electrolyte and fluid secretion in the intestine.
Indications
- Acute diarrhea
- Chronic diarrhea
- Abdominal cramps associated with diarrhea
- Crohn's disease
- Post-gastric surgery
- Ulcerative colitis
Therapeutic class
Anti-diarrheal & Anti-motility Drugs
Pharmacological class
Opioid Receptor Agonist
Pharmacology
Loperamide binds to opioid receptors in the gut wall, reducing peristalsis, increasing intestinal transit time, and inhibiting electrolyte and fluid secretion.
Mechanism of action
Slows intestinal contractions to make stools more solid and less frequent, relieving diarrhea.
Dosage
Acute Diarrhea (Adults):
- Initial: 4 mg, then 2 mg after each loose stool; max 16 mg/day
- Discontinue if no improvement within 48 hours
Children (2-6 years): 1 mg q8hr; (6-8 years): 2 mg q12hr; (8-12 years): 2 mg q8hr
Chronic Diarrhea: 4 mg initially, then 2 mg after each loose stool; maintenance 4-8 mg/day
Administration
- Swallow tablet whole; do not chew, crush or break
- May be taken with or without food, but at a fixed time is preferable
Missed dose
If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed dose and go back to your regular schedule. Do not double the dose.
Side effects
Common Side Effects:
- Constipation
- Nausea
- Headache
- Abdominal pain
- Dry mouth
- Dizziness
- Fatigue
- Skin rash
Precautions & warnings
- Do not use if blood in stool or severe constipation
- Consult doctor if diarrhea lasts more than 48 hours
- Drink plenty of fluids to prevent dehydration and electrolyte imbalance
- Caution when driving or doing activities requiring concentration (may cause dizziness and sleepiness)
Contraindications
- Conditions where inhibition of peristalsis is undesirable (e.g., ileus, megacolon)
- Antibiotic-induced colitis
- Active inflammatory bowel disease
- Abdominal pain without diarrhea
Drug interactions
- Increased bioavailability with co-trimoxazole, ritonavir, saquinavir
- Respiratory depression reported with quinidine
- Increases GI absorption of desmopressin
Food interactions
Loperamide may cause excessive drowsiness with alcohol.
Use in pregnancy
Use in Pregnancy: Loperamide may be unsafe during pregnancy; animal studies have shown harmful effects on the fetus. Consult your doctor.
Use in lactation
Use in Lactation: Loperamide is safe during breastfeeding; does not pass into breastmilk in significant amounts.
Pediatric use
Pediatric doses are established (age and weight-based).
Geriatric use
No dose adjustment needed in elderly.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; no dose adjustment needed.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed (caution in severe hepatic disturbance).
Overdose effects
Overdose may cause constipation, CNS depression, and nausea.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Loperamide