Loperamide 2mg Capsules
WARNING: Do not take more than the package label says or your doctor told you to take. Taking more than you were told can cause severe heart problems, including an abnormal heartbeat. Sometimes, these heart problems can lead to death. Taking this drug with certain other drugs may also raise the chance of heart problems. Call your doctor right away if you have chest pain or pressure, a fast or abnormal heartbeat, severe dizziness, or passing out.Do not give to a child younger than 2 years of age. @ COMMON USES: It is used to treat diarrhea.It is used to lower ostomy output.
Drug Class
Antidiarrheal
Pharmacologic Class
Opioid receptor agonist (peripheral)
Pregnancy Category
C
FDA Approved
Aug 1976
DEA Schedule
Not Controlled
Overview
What is this medicine?
Loperamide is a medication used to treat sudden (acute) diarrhea and ongoing (chronic) diarrhea. It works by slowing down the movement of the gut, which helps to reduce the number of bowel movements and make stools less watery.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. It's essential to drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake.
Important Usage Guidelines
Do not take this medication for a longer period than prescribed by your doctor. Adhere to the recommended dosage and treatment duration to ensure safe and effective use.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, avoiding bathrooms and areas where children and pets can access it. Keep all medications in a secure location, out of reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so by your doctor or pharmacist. Instead, check with your pharmacist for guidance on proper disposal methods, which may include drug take-back programs in your area.
Missing a Dose
If you take this medication regularly and miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you take this medication as needed, do not exceed the frequency recommended by your doctor.
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. It's essential to drink plenty of non-caffeinated liquids, unless your doctor advises you to limit your fluid intake.
Important Usage Guidelines
Do not take this medication for a longer period than prescribed by your doctor. Adhere to the recommended dosage and treatment duration to ensure safe and effective use.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, avoiding bathrooms and areas where children and pets can access it. Keep all medications in a secure location, out of reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so by your doctor or pharmacist. Instead, check with your pharmacist for guidance on proper disposal methods, which may include drug take-back programs in your area.
Missing a Dose
If you take this medication regularly and miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you take this medication as needed, do not exceed the frequency recommended by your doctor.
Lifestyle & Tips
- Drink plenty of clear fluids (water, broth, clear juices) to prevent dehydration caused by diarrhea.
- Avoid caffeine, alcohol, and sugary drinks, which can worsen diarrhea.
- Eat bland, easy-to-digest foods (e.g., bananas, rice, applesauce, toast) as tolerated.
- Do not take more than the recommended dose, as high doses can cause serious heart problems.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
4 mg initially, then 2 mg after each loose stool; max 8 mg/day (OTC) or 16 mg/day (Rx)
Dose Range:
2 - 16 mg
Condition-Specific Dosing:
acuteDiarrhea:
4 mg initially, then 2 mg after each loose stool; max 8 mg/day (OTC) or 16 mg/day (Rx)
chronicDiarrhea:
4-8 mg/day in divided doses, adjusted to patient response; max 16 mg/day
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established (contraindicated under 2 years)
Child:
6-8 years: 2 mg after first loose stool, then 1 mg after each subsequent loose stool; max 4 mg/day. 9-11 years: 2 mg after first loose stool, then 1 mg after each subsequent loose stool; max 6 mg/day.
Adolescent:
12 years and older: 4 mg initially, then 2 mg after each loose stool; max 8 mg/day (OTC) or 16 mg/day (Rx)
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed; not significantly removed by dialysis
Hepatic Impairment:
Mild:
Use with caution
Moderate:
Use with extreme caution; reduced metabolism may lead to increased systemic exposure and CNS effects
Severe:
Contraindicated or use with extreme caution; increased risk of CNS depression and toxic effects
Pharmacology
Mechanism of Action
Loperamide is a synthetic opioid agonist that acts on the Îŧ-opioid receptors in the myenteric plexus of the large intestine. It inhibits peristalsis by decreasing the activity of the longitudinal and circular smooth muscles, thereby prolonging transit time. It also increases the tone of the anal sphincter, reducing incontinence and urgency. Loperamide also reduces fluid and electrolyte secretion into the bowel.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 0.3% (due to extensive first-pass metabolism)
Tmax:
Approximately 5 hours (capsules), 2.5 hours (liquid)
FoodEffect:
Food may slightly increase absorption but is not clinically significant.
Distribution:
Vd:
Approximately 1.6 L/kg
ProteinBinding:
Approximately 97%
CnssPenetration:
Limited (due to P-glycoprotein efflux pump)
Elimination:
HalfLife:
Approximately 9.1 to 14.4 hours (mean 10.8 hours)
Clearance:
Not readily available, but primarily hepatic
ExcretionRoute:
Feces (primarily), small amount in urine
Unchanged:
<2% in urine
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Not precisely defined for antidiarrheal effect, but Tmax for plasma concentration is 2.5-5 hours.
DurationOfAction:
Up to 24 hours
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
Cases of Torsades de Pointes, cardiac arrest, and death have been reported with the use of higher than recommended doses of loperamide. Loperamide is contraindicated in pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions. Avoid doses higher than recommended in adults and children 2 years of age and older.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe stomach upset or vomiting
Abdominal pain
Constipation
Abdominal swelling
Bloating
Fever
Black, tarry, or bloody stools
Difficulty urinating or changes in urine output
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or persist, contact your doctor:
Feeling dizzy, sleepy, tired, or weak
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe stomach upset or vomiting
Abdominal pain
Constipation
Abdominal swelling
Bloating
Fever
Black, tarry, or bloody stools
Difficulty urinating or changes in urine output
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or persist, contact your doctor:
Feeling dizzy, sleepy, tired, or weak
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Diarrhea lasting more than 2 days (for OTC use)
- Fever
- Bloody or black stools
- Severe abdominal pain or bloating
- Signs of dehydration (e.g., extreme thirst, decreased urination, dry mouth, dizziness)
- Heart palpitations, dizziness, or fainting (seek immediate medical attention)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health issues, such as:
+ Gastrointestinal problems, including bloody or black stools, stomach pain without diarrhea, dysentery (characterized by blood in stools and fever), constipation, or a condition called colitis.
+ Abnormal heart rhythms, including a prolonged QT interval on an electrocardiogram (ECG) or other irregular heartbeats.
+ Pre-existing heart problems.
+ Low levels of potassium or magnesium in your blood.
Medications you are currently taking that may cause abnormal heart rhythms (prolonged QT interval). There are numerous medications that can have this effect, so consult your doctor or pharmacist if you are unsure.
If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine whether it is safe to take this medication in conjunction with your other treatments and health issues. Never start, stop, or modify the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health issues, such as:
+ Gastrointestinal problems, including bloody or black stools, stomach pain without diarrhea, dysentery (characterized by blood in stools and fever), constipation, or a condition called colitis.
+ Abnormal heart rhythms, including a prolonged QT interval on an electrocardiogram (ECG) or other irregular heartbeats.
+ Pre-existing heart problems.
+ Low levels of potassium or magnesium in your blood.
Medications you are currently taking that may cause abnormal heart rhythms (prolonged QT interval). There are numerous medications that can have this effect, so consult your doctor or pharmacist if you are unsure.
If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine whether it is safe to take this medication in conjunction with your other treatments and health issues. Never start, stop, or modify the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in any activity that requires your full attention, wait until you understand how this medication affects you. It is also crucial to discuss the use of alcohol, marijuana, or other cannabis products, as well as prescription or over-the-counter medications that may cause drowsiness, with your doctor beforehand.
If you experience diarrhea while taking this medication, be aware that dehydration and electrolyte imbalances can occur. Consult your doctor for guidance on preventing these complications.
When administering this medication to children, exercise caution, as they may be at a higher risk of experiencing certain side effects.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant or planning to become pregnant, inform your doctor, as it is necessary to discuss the potential benefits and risks associated with using this medication during pregnancy.
Before operating a vehicle or engaging in any activity that requires your full attention, wait until you understand how this medication affects you. It is also crucial to discuss the use of alcohol, marijuana, or other cannabis products, as well as prescription or over-the-counter medications that may cause drowsiness, with your doctor beforehand.
If you experience diarrhea while taking this medication, be aware that dehydration and electrolyte imbalances can occur. Consult your doctor for guidance on preventing these complications.
When administering this medication to children, exercise caution, as they may be at a higher risk of experiencing certain side effects.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant or planning to become pregnant, inform your doctor, as it is necessary to discuss the potential benefits and risks associated with using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Severe constipation
- Abdominal distension
- Nausea
- Vomiting
- Drowsiness
- Dizziness
- Pinpoint pupils
- Slow or shallow breathing
- Unresponsiveness
- Cardiac arrhythmias (e.g., QT prolongation, Torsades de Pointes, ventricular arrhythmias)
- Cardiac arrest
What to Do:
Call 911 or your local emergency number immediately. For poison control, call 1-800-222-1222. Naloxone may be used as an antidote for opioid effects, but cardiac monitoring is essential due to potential for prolonged QT interval and arrhythmias.
Drug Interactions
Major Interactions
- Saquinavir (reduced saquinavir levels)
- Ritonavir (increased loperamide levels)
- Quinidine (increased loperamide levels)
- Gemfibrozil (increased loperamide levels)
- Itraconazole (increased loperamide levels)
- Ketoconazole (increased loperamide levels)
- Desmopressin (increased desmopressin levels)
Moderate Interactions
- Co-administration with other CNS depressants (increased sedation)
- Drugs that prolong QT interval (increased risk of arrhythmias with high loperamide doses)
Monitoring
Routine Monitoring
Stool frequency and consistency
Frequency: Daily during treatment
Target: Reduction in loose stools
Action Threshold: If diarrhea persists for more than 2 days (OTC) or worsens, discontinue and seek medical attention.
Signs of CNS depression (drowsiness, dizziness)
Frequency: Daily during treatment
Target: Absence of significant CNS effects
Action Threshold: If significant CNS depression occurs, especially with concomitant medications or hepatic impairment, reduce dose or discontinue.
Symptom Monitoring
- Abdominal pain or distension
- Constipation
- Nausea
- Vomiting
- Drowsiness
- Dizziness
- Dry mouth
- Signs of paralytic ileus (severe constipation, absent bowel sounds)
- Signs of cardiac arrhythmias (palpitations, dizziness, syncope) - especially with high doses
Special Patient Groups
Pregnancy
Generally avoided unless clearly needed. Animal studies show some risk, but human data are limited. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Limited data, potential for increased risk of hypospadias reported in some studies, but not consistently confirmed.
Second Trimester:
Generally considered safer than first trimester, but still use with caution.
Third Trimester:
Potential for neonatal opioid withdrawal syndrome if used chronically or in high doses near term, though systemic absorption is low.
Lactation
Loperamide is excreted in breast milk in small amounts. While the amount is generally considered low, caution is advised, especially with prolonged use or in premature/neonatal infants. Monitor infant for drowsiness or constipation.
Infant Risk:
Low to moderate risk (L3); potential for constipation or CNS depression in infant, especially if mother takes high doses or infant is very young.
Pediatric Use
Contraindicated in children under 2 years of age due to risk of respiratory depression and serious cardiac adverse reactions. Use with caution and strict adherence to dosing guidelines in children 2 years and older. Risk of paralytic ileus in children with acute dysentery.
Geriatric Use
No specific dose adjustment needed based on age alone. However, elderly patients may be more susceptible to CNS effects or constipation. Use with caution in patients with underlying cardiac conditions due to the risk of QT prolongation at high doses.
Clinical Information
Clinical Pearls
- Loperamide is for symptomatic relief of diarrhea; it does not treat the underlying cause.
- Do not use in patients with bacterial enterocolitis (e.g., E. coli O157:H7, Salmonella, Shigella, C. difficile) as it may prolong fever, increase risk of toxic megacolon, or worsen disease.
- Discontinue if abdominal distension, constipation, or ileus occurs.
- High doses of loperamide, often used in attempts to self-treat opioid withdrawal or achieve euphoria, can lead to severe, life-threatening cardiac events including QT prolongation, Torsades de Pointes, and cardiac arrest.
- Patients should be advised to seek medical attention if diarrhea persists for more than 48 hours (OTC use) or if fever, bloody stools, or severe abdominal pain develop.
Alternative Therapies
- Bismuth subsalicylate (Pepto-Bismol)
- Diphenoxylate/atropine (Lomotil) - prescription only, controlled substance
- Racecadotril (acetorphan) - not available in US, but used elsewhere
- Oral rehydration solutions (primary treatment for dehydration)
Cost & Coverage
Average Cost:
$5 - $20 per 30 capsules (2mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.