Loperamide: Uses, Dosage & Side Effects
A widely used antidiarrheal medicine that slows intestinal movement and reduces fluid loss
📊 Quick Facts About Loperamide
💡 Key Takeaways About Loperamide
- Effective for acute diarrhea: Loperamide slows intestinal movement, reduces fluid loss, and provides relief typically within one hour of the initial dose
- Do not use with bloody diarrhea or high fever: If diarrhea is accompanied by blood in the stool, high fever, or signs of bacterial infection, do not take loperamide – consult a doctor instead
- Limit self-treatment to 48 hours: For acute diarrhea, do not take loperamide for more than 2 days without medical advice; if symptoms persist, see a healthcare professional
- Fluid replacement is essential: Loperamide treats the symptom of diarrhea but does not address the cause; always ensure adequate fluid and electrolyte intake during diarrheal illness
- Not for children under 12: Over-the-counter loperamide should not be given to children under 12 years of age; oral rehydration therapy is the primary treatment for childhood diarrhea
What Is Loperamide and What Is It Used For?
Loperamide is a synthetic antidiarrheal medicine that works by slowing the movement of the intestines, reducing fluid and electrolyte secretion into the bowel, and increasing anal sphincter tone. It is the most widely used over-the-counter treatment for acute diarrhea in adults and adolescents aged 12 years and older. Under medical supervision, loperamide is also prescribed for chronic diarrhea and fecal incontinence.
Loperamide belongs to the class of antidiarrheal agents and is technically classified as a synthetic opioid, though it is fundamentally different from opioids used for pain relief. At standard therapeutic doses, loperamide acts almost exclusively on opioid receptors in the gut wall and does not cross the blood–brain barrier in significant amounts. This means it provides its intestinal effects without causing the pain-relieving, mood-altering, or respiratory-depressing effects associated with other opioid medicines. Loperamide was first developed in the 1960s by Janssen Pharmaceutica and received regulatory approval in the 1970s, initially as a prescription medicine before becoming available over the counter.
The drug exerts its therapeutic effects through binding to mu-opioid receptors in the myenteric plexus of the intestinal wall. This binding triggers several physiological responses: it slows peristalsis (the wave-like contractions that move food through the intestines), increases intestinal transit time, reduces secretion of fluids and electrolytes into the intestinal lumen, and enhances the reabsorption of water and electrolytes. Additionally, loperamide increases the tone of the anal sphincter, which helps reduce the urgency and incontinence often associated with diarrheal episodes.
Loperamide is approved and commonly used for the following indications:
- Acute (short-term) diarrhea – the primary over-the-counter use, providing rapid symptomatic relief from traveler's diarrhea, viral gastroenteritis, and non-specific acute diarrhea
- Chronic diarrhea – under medical supervision, for long-term management of conditions such as irritable bowel syndrome with diarrhea (IBS-D), inflammatory bowel disease, and other causes of persistent diarrhea
- High-output ileostomy – to reduce the volume of stool output in patients who have undergone certain gastrointestinal surgeries resulting in a stoma
- Fecal incontinence – loperamide increases anal sphincter tone and is used both on its own and as part of combination therapy for patients with bowel incontinence
It is important to understand that loperamide treats the symptom of diarrhea but does not address the underlying cause. Diarrhea serves a protective function in many cases, helping the body expel pathogens. For this reason, loperamide should not be used when diarrhea is caused by invasive bacterial infections (e.g., Salmonella, Shigella, Campylobacter) or by Clostridioides difficile colitis, as slowing gut motility in these conditions may worsen the illness.
Regardless of whether loperamide is used, adequate fluid and electrolyte replacement is the most critical aspect of managing any diarrheal illness. The World Health Organization (WHO) recommends oral rehydration solutions (ORS) as the cornerstone of diarrhea treatment, particularly in developing countries and in children. Loperamide can be used as an adjunct to rehydration therapy to provide symptomatic relief in appropriate patients.
Loperamide typically begins to provide relief within 1 hour after taking the initial dose of 2 tablets (4 mg). Most people notice a significant reduction in the frequency of bowel movements and urgency within 2–3 hours. For chronic diarrhea, it may take several days of regular dosing to find the optimal dose that provides consistent symptom control. The orodispersible (melt-in-mouth) tablet formulation dissolves on the tongue within seconds and can be taken without water, making it convenient for use when travelling.
What Should You Know Before Taking Loperamide?
Before taking loperamide, be aware that it must not be used if you have bloody diarrhea with high fever, active inflammatory bowel disease flare (such as ulcerative colitis or pseudomembranous colitis), constipation, or abdominal distension. Loperamide is not suitable for children under 12 years for self-treatment. People with liver impairment should consult a doctor before use.
While loperamide is widely available without a prescription and is considered safe for short-term use at recommended doses, it is not appropriate for all types of diarrhea or all patients. Understanding the situations in which loperamide should be avoided is essential for safe and effective use. The primary principle is that loperamide treats symptoms only – if the underlying cause of diarrhea requires specific treatment (such as antibiotics for a bacterial infection), addressing that cause must take priority.
Contraindications
You must not take loperamide if any of the following apply:
- Allergy to loperamide or any other ingredient in the product
- Blood in the stool or high fever – these may indicate a bacterial infection (e.g., Salmonella, Shigella, Campylobacter) where slowing gut motility could worsen the illness by preventing elimination of pathogens
- Active inflammatory bowel conditions – including acute flares of ulcerative colitis or pseudomembranous colitis (commonly caused by Clostridioides difficile after antibiotic use), as loperamide may increase the risk of toxic megacolon
- Constipation or abdominal distension – if intestinal transit is already slow or the abdomen is bloated, loperamide can make these conditions worse
- Children under 12 years – over-the-counter loperamide should not be given to children under 12; in younger children, diarrhea should be managed primarily with oral rehydration therapy under medical guidance
Warnings and Precautions
Speak to your doctor or pharmacist before taking loperamide in the following situations:
Symptom relief is not a cure: Loperamide alleviates the symptoms of diarrhea but does not treat the underlying cause. If you have chronic or recurrent diarrhea, see your doctor to investigate and treat the root cause before relying on long-term loperamide use.
Duration of self-treatment: If acute diarrhea has not resolved after 48 hours (2 days) of loperamide treatment, stop taking it and consult a doctor. Persistent diarrhea may indicate an underlying condition that requires specific diagnosis and treatment.
Watch for constipation: If you develop constipation or signs of reduced intestinal movement (such as bloating, abdominal discomfort, or inability to pass gas) while taking loperamide, stop the medication immediately and contact your healthcare provider.
Liver impairment: Loperamide is extensively metabolized by the liver through first-pass metabolism. People with impaired liver function may have higher blood levels of loperamide than expected, increasing the risk of central nervous system effects. Consult your doctor before using loperamide if you have liver disease.
Fluid replacement: Diarrhea causes significant loss of water and electrolytes (particularly sodium and potassium). It is essential to drink plenty of fluids during diarrheal illness, regardless of whether you are taking loperamide. Oral rehydration solutions are particularly recommended for vulnerable groups including elderly patients, young adults with dehydration signs, and travelers.
HIV/AIDS patients: If you have HIV/AIDS, stop loperamide treatment at the first sign of abdominal distension, as there is an increased risk of toxic megacolon in immunocompromised patients.
Do not take loperamide for any purpose other than its intended use, and never exceed the recommended dose. Serious and potentially life-threatening cardiac events (including rapid or irregular heartbeat, QT prolongation, torsades de pointes, and cardiac arrest) have been reported in people who have taken excessive doses of loperamide. At recommended doses, loperamide does not produce these effects. Seek immediate medical attention if you experience rapid heartbeat, palpitations, or fainting while taking loperamide.
Pregnancy and Breastfeeding
If you are pregnant, breastfeeding, think you may be pregnant, or are planning to have a baby, consult your doctor or pharmacist before taking loperamide.
Pregnancy: There is limited clinical data on the use of loperamide during pregnancy. Animal studies have not shown direct harmful effects on the fetus at therapeutic doses, but as with all medicines, loperamide should only be used during pregnancy if your doctor considers it clearly necessary and the potential benefit outweighs the potential risk. During pregnancy, the priority in managing diarrhea should be adequate fluid and electrolyte replacement.
Breastfeeding: Small amounts of loperamide may pass into breast milk. Loperamide is generally not recommended during breastfeeding as a precautionary measure. If you need an antidiarrheal medicine while breastfeeding, discuss the options with your doctor.
Driving and Operating Machinery
Fatigue, dizziness, and drowsiness may occur during treatment with loperamide. If you experience these effects, do not drive or operate machinery until they resolve. You are responsible for assessing whether you are fit to drive or perform tasks requiring alertness.
Loperamide orodispersible tablets may contain aspartam (a source of phenylalanine), which can be harmful for people with phenylketonuria (PKU). The mint flavoring may contain small amounts of sulfite, maltodextrin (containing glucose), and benzyl alcohol. If you have known intolerances or allergies to these substances, check the product information or consult your pharmacist. Most loperamide formulations are essentially sodium-free (less than 1 mmol per tablet).
How Does Loperamide Interact with Other Drugs?
Loperamide can interact with several medicines, including P-glycoprotein inhibitors and CYP enzyme inhibitors that may increase loperamide blood levels. Key interactions include quinidine, ritonavir, ciclosporin, verapamil, macrolide antibiotics, and azole antifungals. Cholestyramine may reduce loperamide absorption. Oral desmopressin levels may be increased when taken with loperamide.
Drug interactions with loperamide primarily involve medicines that inhibit P-glycoprotein (P-gp) or the CYP3A4 and CYP2C8 enzyme systems, which are responsible for metabolizing loperamide and limiting its absorption into the bloodstream. Normally, loperamide is rapidly metabolized and expelled from the body, with very little reaching the systemic circulation. When these pathways are inhibited by other medicines, loperamide blood levels can increase, potentially leading to enhanced effects or, in rare cases, adverse reactions including cardiac effects.
Clinically Significant Interactions
The following interactions require attention and may necessitate dose adjustment, monitoring, or avoidance of the combination:
| Drug / Drug Class | Effect of Interaction | Clinical Advice |
|---|---|---|
| Quinidine | Potent P-gp inhibitor that can significantly increase loperamide plasma concentrations by inhibiting its efflux from the brain and intestinal wall. | Avoid concurrent use. If combination is necessary, use the lowest effective loperamide dose and monitor closely. |
| Ritonavir | HIV protease inhibitor that inhibits both P-gp and CYP3A4, potentially increasing loperamide exposure and risk of cardiac effects. | Avoid concurrent use if possible. If needed, use with caution under medical supervision. |
| Ciclosporin | P-gp inhibitor that can increase loperamide absorption and systemic exposure by inhibiting intestinal efflux. | Monitor for increased loperamide effects. Use lowest effective dose. |
| Itraconazole, Ketoconazole | Potent CYP3A4 and P-gp inhibitors that can increase loperamide plasma levels 2–3 fold. | Avoid concurrent use if possible. If used together, reduce loperamide dose and monitor for adverse effects. |
| Erythromycin, Clarithromycin | Macrolide antibiotics that inhibit CYP3A4 and P-gp, increasing loperamide blood levels. | Use with caution. Consider alternative antidiarrheal if prolonged antibiotic course is needed. |
| Verapamil | Calcium channel blocker and P-gp inhibitor that can increase loperamide plasma concentrations. | Monitor for increased loperamide effects, particularly drowsiness and constipation. |
Other Important Interactions
The following interactions are also clinically relevant:
| Drug / Drug Class | Effect of Interaction | Clinical Advice |
|---|---|---|
| Cholestyramine | Bile acid sequestrant that can bind loperamide in the gut and reduce its absorption and effectiveness. | Separate administration by at least 2 hours. Take loperamide first if both are needed. |
| Gemfibrozil | Lipid-lowering agent and CYP2C8 inhibitor that can increase loperamide plasma levels by approximately 2-fold. | Use with caution. Monitor for increased side effects. |
| Oral desmopressin | Loperamide may increase the absorption and blood levels of oral desmopressin by up to 3-fold, increasing the risk of hyponatremia (low blood sodium). | Monitor for signs of water retention and hyponatremia. Dose adjustment of desmopressin may be needed. |
| Other opioids | Theoretical additive effect on gut motility when combined with other opioid analgesics, increasing constipation risk. | Use with caution. Monitor for severe constipation or ileus. |
Loperamide can be taken with or without food. Food does not significantly affect its absorption or effectiveness. Orodispersible tablets are placed on the tongue where they dissolve quickly and can be swallowed without water, making them particularly convenient for use when travelling or when access to water is limited. During diarrheal illness, focus on adequate fluid intake – preferably oral rehydration solutions, clear broths, or diluted fruit juices – rather than worrying about when to take loperamide relative to meals.
What Is the Correct Dosage of Loperamide?
For acute diarrhea in adults and adolescents aged 12 years and over, the initial dose is 2 tablets (4 mg), followed by 1 tablet (2 mg) after each subsequent loose stool. The maximum daily dose is 8 tablets (16 mg). Do not take loperamide for more than 2 days for self-treatment. For chronic diarrhea, dosing is individualized by your doctor, typically 1–8 tablets (2–16 mg) per day.
The correct dosage of loperamide depends on whether it is being used for acute or chronic diarrhea, and whether treatment is self-directed (OTC) or prescribed by a doctor. Always follow the instructions on the product packaging for self-treatment, or your doctor's specific instructions for prescribed use.
Adults and Adolescents Aged 12 Years and Over
Acute Diarrhea (Self-Treatment)
- Initial dose: 2 tablets (4 mg) at the onset of diarrhea
- Subsequent doses: 1 tablet (2 mg) after each loose stool
- Maximum daily dose: 8 tablets (16 mg)
- Maximum duration: 2 days (48 hours) for self-treatment; consult a doctor if diarrhea persists
- Wait between doses: Allow at least 2–3 hours between the initial dose and subsequent doses
Chronic Diarrhea (Medical Supervision)
- Dosing: Individually adjusted by your doctor based on symptoms
- Typical range: 1–8 tablets (2–16 mg) per day, divided into multiple doses
- Maximum daily dose: 8 tablets (16 mg)
- Monitoring: Regular review by your doctor is important to assess ongoing need and investigate the underlying cause of chronic diarrhea
Children
Over-the-counter loperamide should not be given to children under 12 years of age. Children are more sensitive to the effects of loperamide and are at greater risk of serious complications from dehydration. In childhood diarrhea, the primary treatment is oral rehydration therapy (ORT) to replace lost fluids and electrolytes. A doctor may prescribe loperamide for children in specific circumstances, but this always requires medical supervision and careful weight-based dosing.
Elderly Patients
No specific dose adjustment is required for elderly patients. However, older adults may be more susceptible to the fluid and electrolyte losses caused by diarrhea and should pay particular attention to adequate hydration. Elderly patients with liver impairment should consult their doctor before using loperamide.
How to Take Orodispersible Tablets
Loperamide orodispersible (melt-in-mouth) tablets are designed for convenient use without water:
- Fold back the foil edge on the blister pack
- Peel away the foil completely – do not push the tablet through the foil, as the tablet is fragile and may break
- Gently lift out the tablet
- Place the tablet on your tongue – it will dissolve within seconds
- Swallow with saliva; no water is needed
Handle the tablets carefully as they are delicate and can break easily.
Missed Dose
Since loperamide for acute diarrhea is taken as needed (after each loose stool), a missed dose is not usually a concern. Simply take the next dose after the next loose stool, without exceeding the maximum daily dose. If you are taking loperamide on a regular schedule for chronic diarrhea, take the missed dose as soon as you remember unless it is nearly time for your next dose. Do not take a double dose to make up for a missed one.
Overdose
If you or someone else has taken too much loperamide, seek immediate medical attention by contacting a poison control center or emergency department. This is especially urgent if a child has swallowed the medicine. Overdose symptoms may include:
- Cardiac symptoms: Increased heart rate, irregular heartbeat, and potentially life-threatening heart rhythm disturbances (QT prolongation, torsades de pointes)
- Neurological symptoms: Muscle stiffness, uncoordinated movements, drowsiness, small pupils (miosis), difficulty urinating
- Respiratory symptoms: Weak or slowed breathing, which can be life-threatening particularly in children
Children are significantly more sensitive to loperamide overdose than adults. If a child has swallowed loperamide, contact emergency medical services or a poison control center immediately, even if the child appears well. Symptoms of overdose in children can progress rapidly and may include CNS depression, respiratory depression, and cardiovascular effects.
What Are the Side Effects of Loperamide?
Common side effects of loperamide include constipation, nausea, flatulence (gas), headache, and dizziness. Serious but rare side effects include angioedema (severe allergic reaction with facial swelling), severe abdominal pain or distension (possible intestinal obstruction), toxic epidermal necrolysis, Stevens-Johnson syndrome, and acute pancreatitis. Stop taking loperamide and seek immediate medical attention if any serious symptoms occur.
Like all medicines, loperamide can cause side effects, although not everyone experiences them. Most side effects are mild and related to the drug's mechanism of action (slowing gut motility). The following frequency classification is based on clinical trial data and post-marketing surveillance.
Stop taking loperamide and seek emergency medical care immediately if you experience any of the following serious symptoms:
- Swelling of the face, tongue, or throat; difficulty swallowing; hives combined with breathing difficulties (signs of angioedema)
- Extreme tiredness, coordination problems, and loss of consciousness or reduced alertness
- Severe abdominal pain and/or a swollen abdomen, which may indicate intestinal obstruction or enlarged bowel
- Severe widespread skin reactions: skin peeling (toxic epidermal necrolysis), or blistering with sores in the mouth and eyes (Stevens-Johnson syndrome)
- Upper abdominal pain radiating to the back, tender abdomen, fever, rapid pulse, nausea, and vomiting (possible acute pancreatitis)
Common
- Constipation
- Nausea
- Flatulence (gas)
- Headache
- Dizziness
Uncommon
- Drowsiness
- Abdominal pain or discomfort
- Dry mouth
- Vomiting
- Indigestion (dyspepsia)
- Skin rash
Rare
- Hypersensitivity reactions (anaphylactic shock in very rare cases)
- Muscle rigidity or increased muscle tone
- Miosis (small pupils)
- Tongue pain
- Pruritus (itching)
- Urticaria (hives)
- Urinary retention (difficulty urinating)
Reported (Frequency Unknown)
- Acute pancreatitis (upper abdominal pain radiating to back, nausea, vomiting, fever)
- Toxic epidermal necrolysis (severe skin peeling)
- Stevens-Johnson syndrome (severe blistering skin reaction)
- Angioedema (swelling of face, tongue, or throat)
- Intestinal obstruction or ileus (severe constipation with abdominal distension)
If you experience any side effects while taking loperamide, particularly any serious or unexpected symptoms not listed above, report them to your healthcare provider. Reporting suspected adverse reactions after a medicine has been authorized helps ongoing monitoring of its benefit-risk balance. In many countries, patients and healthcare professionals can report side effects directly to the national pharmacovigilance authority.
Most side effects of loperamide are dose-related. Using the lowest effective dose for the shortest time necessary significantly reduces the risk of adverse effects. If you develop constipation, stop taking loperamide – this is a sign that the drug is working and the diarrhea has been controlled. Resume only if diarrhea returns. Ensure adequate fluid intake throughout treatment.
How Should You Store Loperamide?
Store loperamide at room temperature in its original packaging to protect from moisture. Keep all medicines out of sight and reach of children. Do not use loperamide after the expiration date on the packaging. Return unused or expired medicines to your local pharmacy for safe disposal.
Proper storage of loperamide ensures the medicine remains effective and safe throughout its shelf life. Follow these guidelines:
- Packaging: Store in the original packaging to protect from moisture, as loperamide tablets (particularly orodispersible formulations) are moisture-sensitive
- Temperature: Store at room temperature, typically below 25°C (77°F). Do not refrigerate or freeze.
- Children: Keep out of the sight and reach of children at all times. Loperamide overdose in children can be particularly dangerous.
- Expiration: Do not use after the expiration date (month/year) printed on the carton and blister. The expiration date refers to the last day of that month.
Disposal: Do not dispose of medicines via wastewater or household waste. Return unused or expired loperamide to your local pharmacy for safe disposal. These measures help protect the environment and prevent accidental ingestion.
What Does Loperamide Contain?
The active substance is loperamide hydrochloride 2 mg per tablet, capsule, or orodispersible tablet. Inactive ingredients vary by formulation and manufacturer. Orodispersible tablets typically contain gelatin, mannitol, aspartam (a source of phenylalanine), mint flavoring, and sodium bicarbonate.
Loperamide is available in several formulations to suit different patient preferences and situations:
| Formulation | Strength | Key Features |
|---|---|---|
| Orodispersible tablets | 2 mg | Dissolves on the tongue within seconds; no water needed; mint flavor; convenient for travel |
| Hard capsules | 2 mg | Standard oral formulation; swallowed whole with water |
| Film-coated tablets | 2 mg | Coated for easier swallowing; standard oral use |
| Standard tablets | 2 mg | Uncoated; widely available generic formulation |
Orodispersible tablet excipients typically include: gelatin, mannitol (E421), aspartam (E951), mint flavoring (which may contain glucose, benzyl alcohol, and traces of sulfite), and sodium bicarbonate. The tablets are white to off-white, round, and fragile – handle with care.
Capsule excipients vary by manufacturer but commonly include lactose monohydrate, maize starch, talc, and magnesium stearate. The capsule shell typically contains gelatin and colorants.
Most loperamide formulations contain less than 1 mmol (23 mg) sodium per tablet, meaning they are essentially sodium-free. Orodispersible tablets contain approximately 0.75 mg aspartam per tablet (a source of phenylalanine), which is relevant for patients with phenylketonuria (PKU).
Available pack sizes: Loperamide is commonly available in packs of 2, 3, 4, 6, 12, 18, or 24 tablets. Not all pack sizes may be marketed in all countries.
Frequently Asked Questions About Loperamide
Medical References
All medical information is based on peer-reviewed sources and international guidelines. Evidence level: 1A (systematic reviews and randomized controlled trials).
- World Health Organization (WHO). WHO Model List of Essential Medicines – 23rd List, 2023. Geneva: World Health Organization; 2023.
- European Medicines Agency (EMA). Loperamide – Summary of Product Characteristics. EMA assessment report, 2024.
- U.S. Food and Drug Administration (FDA). FDA Drug Safety Communication: FDA warns about serious heart problems with high doses of the antidiarrheal medicine loperamide (Imodium), including from abuse and misuse. FDA, June 2016 (updated 2020).
- British National Formulary (BNF). Loperamide hydrochloride. National Institute for Health and Care Excellence (NICE), 2025.
- Hanauer SB. The role of loperamide in gastrointestinal disorders. Rev Gastroenterol Disord. 2008;8(1):15–20.
- Ericsson CD. Nonantimicrobial agents in the prevention and treatment of traveler's diarrhea. Clin Infect Dis. 2005;41(Suppl 8):S557–S563.
- Riddle MS, Connor BA, Beeching NJ, et al. Guidelines for the prevention and treatment of travelers' diarrhea: a graded expert panel report. J Travel Med. 2017;24(Suppl 1):S57–S74.
- Baker DE. Loperamide: a pharmacological review. Rev Gastroenterol Disord. 2007;7(Suppl 3):S11–S18.
- Swank KA, Wu E, Kortepeter C, McAninch J, Levin RL. Adverse event detection using the FDA post-marketing drug safety surveillance system: cardiotoxicity associated with loperamide abuse and misuse. J Am Pharm Assoc. 2017;57(2S):S63–S67.
- World Health Organization (WHO). The Treatment of Diarrhoea: A Manual for Physicians and Other Senior Health Workers. 4th rev. Geneva: WHO; 2005.
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