Loperamide: Effects, Dosage & Side Effects
Loperamide is an active ingredient used to treat diarrhea. It slows intestinal movement and helps firm up stools. It is widely available without a prescription.
Wissenswertes über "Loperamide"
Loperamide is an active ingredient used to treat diarrhea. It slows intestinal movement and helps firm up stools. It is widely available without a prescription.
What is Loperamide?
Loperamide is a synthetic drug belonging to the class of opioid receptor agonists, used to treat both acute and chronic diarrhea. Unlike most other opioids, loperamide acts almost exclusively within the gastrointestinal tract and does not readily cross the blood-brain barrier at therapeutic doses, meaning it has minimal abuse potential when used as directed. It is available over the counter in pharmacies in many countries.
Mechanism of Action
Loperamide binds to mu-opioid receptors located in the wall of the intestine. This binding produces several key effects:
- It slows intestinal motility (gut movement), allowing stool to remain in the intestine longer.
- It increases the absorption of water and electrolytes from the intestinal contents back into the bloodstream, resulting in firmer stools.
- It increases the tone of the anal sphincter, which reduces the urgency to defecate.
This combination of slowed passage and improved water absorption makes loperamide an effective antidiarrheal agent.
Indications
Loperamide is used for:
- Acute diarrhea, such as traveler's diarrhea or infectious diarrhea (as symptomatic relief)
- Chronic diarrhea associated with conditions such as irritable bowel syndrome or inflammatory bowel disease (under medical supervision)
- Patients with a stoma (artificial bowel opening) to help regulate stool output
Dosage
The standard dosage for adults with acute diarrhea is:
- Initial dose: 4 mg (two 2 mg capsules or tablets)
- Subsequent doses: 2 mg after each loose stool
- Maximum daily dose: 16 mg (8 mg per day for self-medication without medical supervision)
In children under 12 years, loperamide should only be used under medical supervision. It is contraindicated in children under 2 years of age.
Side Effects
Loperamide is generally well tolerated. Possible side effects include:
- Constipation if taken for too long or at too high a dose
- Abdominal cramps or bloating
- Nausea and dizziness
- Rarely: allergic reactions or skin rash
At very high doses (overdose), loperamide can cause dangerous cardiac arrhythmias, as it may then cross the blood-brain barrier and affect the central nervous system.
Contraindications and Warnings
Loperamide should not be used in cases of:
- Bloody or purulent diarrhea or high fever (suspected invasive bacterial infection)
- Children under 2 years of age
- Known hypersensitivity to the active ingredient
- Acute ulcerative colitis or pseudomembranous colitis
If diarrhea persists for more than 2 days, or if symptoms such as high fever occur, medical advice should be sought promptly.
References
- World Health Organization (WHO): Model Formulary 2023 - Loperamide hydrochloride.
- Brunton L, Knollmann B (eds.): Goodman & Gilman's The Pharmacological Basis of Therapeutics, 13th edition, McGraw-Hill, 2018.
- European Medicines Agency (EMA): Loperamide - Product Information and Assessment Report, 2022.
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Related search terms: Loperamide + Loperamid + Loperamidum