What is Loperamide?

Loperamide is over the counter (OTC) medication used to treat diarrhea. It relieves frequent loose motions and associated discomfort.

How it works?

Loperamide is oral antidiarrheal agent. It increases intestinal transit time. Loperamide has antisecretory activity against toxins of cholera and some forms of E.coli toxins, by acting on G1-linked receptors to inhibit adenylyl cyclase activity.

Uses:

Diarrhea

Dosage:

• Adults: usual dose of loperamide for both adult and chronic diarrhoea is 4 mg taken orally after first loose stool then 2 mg after each liquid stool. You should not take 16 mg per day.

Side effects:

• Constipation
• Drowsiness
• Headache
• Nausea
• Stomach cramps
• Allergic reactions (skin rash, difficulty in breathing, swelling of face)

Quick tips from experts:

• Diarrhea can cause more fluid loss and electrolyte imbalance. Drink plenty of water, juices to avoid dehydration.
• Do not use loperamide tablet if you have blood in your stools, it can be sign of infectious diarrhea.
• Consult your doctor if your diarrhea last for more than 48 hours.
• Stop taking loperamide as soon as your symptoms are relieved.

Safety precautions:

• Alcohol: It is not safe to consume alcohol while taking loperamide. It can cause excessive drowsiness and increase side effects.
• Pregnancy: Loperamide may be unsafe to use in pregnancy. It can be prescribed by your doctor under certain circumstances. Consult your doctor before use.
• Breastfeeding: Loperamide is generally considered safe to use while breastfeeding. Consult your doctor before use.
• Driving: Loperamide can cause sleepiness and reduced alertness. Avoid driving or operating machinery if you feel drowsy after taking loperamide.
• Kidney: Loperamide is safe to use in kidney disease. No dose adjustment is usually needed.
• Liver: Loperamide should be used with caution in liver disease. Dose adjustment may be needed. Consult your doctor before use.

Drug interactions:

• QT-prolonging drugs: includes certain antibiotics (e.g., clarithromycin, azithromycin, ciprofloxacin), antidepressants (e.g., citalopram, fluoxetine, escitalopram), antiarrhythmic drugs (e.g., amiodarone, sotalol, quinidine), antipsychotics (e.g., thioridazine, ziprasidone, clozapine), and some antifungals (e.g., itraconazole, ketoconazole).
  Both loperamide and these interacting drugs can affect the heart's electrical activity, specifically by inhibiting certain ion channels that are crucial for normal heart rhythm.
• CYP3A4 and CYP2C8 Inhibitors: drugs like Itraconazole, Gemfibrozil, Ritonavir, Clarithromycin inhibits CYP3A4 and CYP2C8. Loperamide is primarily metabolized in the liver by certain enzymes, notably CYP3A4 and CYP2C8. Drugs that inhibit these enzymes can slow down the breakdown of loperamide, leading to increased levels of loperamide in the body.
• P-glycoprotein Inhibitors (e.g., Quinidine, Ritonavir, Itraconazole): P-glycoprotein acts as a "pump" that limits the systemic exposure and brain penetration of loperamide. When this pump is inhibited, more loperamide can enter the bloodstream and potentially cross the blood-brain barrier.
• Other Antidiarrheal or Constipating Drugs: includes opioids, anticholinergic medications, and certain antipsychotics. Both loperamide and these other drugs work to reduce intestinal movement. Combining them can lead to additive effects, significantly increasing the risk and severity of constipation.
• Drugs for Inflammatory Bowel Conditions (e.g., Eluxadoline): While loperamide is used for diarrhea, some medications for irritable bowel syndrome (IBS) or other inflammatory bowel conditions that also cause constipation should be used with caution. For instance, eluxadoline (used to treat IBS with diarrhea) can cause constipation and pancreatic issues.

📦 Storage

• Store at room temperature (68-77°F or 20-25°C)
• Keep in original container, tightly closed
• Protect from moisture and light