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Loperamide – Uses, Dosage and Side Effects

Loperamide is an antidiarrheal medication that slows intestinal movement and normalizes stool consistency. It is widely available over the counter and commonly used for acute diarrhea.

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Things worth knowing about "Loperamide"

Loperamide is an antidiarrheal medication that slows intestinal movement and normalizes stool consistency. It is widely available over the counter and commonly used for acute diarrhea.

What is Loperamide?

Loperamide is an antidiarrheal agent used to treat acute and chronic diarrhea. It belongs to the class of opioid receptor agonists but acts primarily within the gut and barely crosses the blood-brain barrier, meaning it does not produce the central nervous system effects typical of opioids such as pain relief or euphoria. Loperamide is available over the counter in most countries and is one of the most widely used treatments for diarrhea.

Indications

Loperamide is indicated for:

Acute diarrhea (e.g., travelers diarrhea, infectious gastroenteritis)
Chronic diarrhea associated with inflammatory bowel diseases such as Crohn disease or ulcerative colitis (under medical supervision)
Increased stool frequency following ileostomy or colostomy procedures

Mechanism of Action

Loperamide binds to mu-opioid receptors located in the gut wall. This produces the following effects:

Slowing of intestinal motility (peristalsis), reducing the speed at which gut contents move through the intestine
Increased reabsorption of water and electrolytes from the intestinal lumen
Increased anal sphincter tone, which reduces the urge to defecate

Because loperamide does not significantly cross the blood-brain barrier, its action is almost entirely localized to the gastrointestinal tract.

Dosage

The standard adult dosage for acute diarrhea is:

Initial dose: 4 mg (two 2 mg capsules or tablets)
Subsequent dose: 2 mg after each loose stool
Maximum daily dose: 16 mg

In children under 12 years of age, loperamide should only be used under medical guidance. For acute diarrhea, treatment should generally not exceed 2 days without consulting a healthcare professional.

Side Effects

Loperamide is generally well tolerated. Possible side effects include:

Constipation - the most common side effect
Abdominal cramps and bloating
Nausea and dizziness
Rarely: allergic reactions (rash, itching)
In cases of overdose: serious cardiac arrhythmias (QT interval prolongation)

Contraindications and Warnings

Loperamide should not be used in cases of:

Bloody or mucous diarrhea accompanied by fever (suspected bacterial infection, e.g., Salmonella or Shigella)
Acute flare of ulcerative colitis (risk of toxic megacolon)
Children under 2 years of age
Concurrent use of medications that may affect heart rhythm

If diarrhea persists for more than 2 days, medical attention should always be sought.

Drug Interactions

Loperamide may interact with the following substances:

Quinidine and other P-glycoprotein inhibitors: increase loperamide plasma levels and the risk of cardiac arrhythmias
Other antidiarrheal agents: may enhance the constipating effect
Certain antibiotics and antifungals: may increase loperamide concentrations in the bloodstream

References

European Medicines Agency (EMA) - Product Monograph: Loperamide (2023). Retrieved from: www.ema.europa.eu
Lacy BE et al. - ACG Clinical Guideline: Management of Irritable Bowel Syndrome. American Journal of Gastroenterology, 2021.
World Health Organization (WHO) - Model Formulary: Antidiarrhoeal Medicines. Retrieved from: www.who.int

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