Loperamide 1mg/7.5ml Suspension
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.
Drug Class
Antidiarrheal
Pharmacologic Class
Peripherally acting opioid receptor agonist
Pregnancy Category
Category C
FDA Approved
Aug 1976
DEA Schedule
Not Controlled
Overview
What is this medicine?
Loperamide is a medicine used to treat sudden (acute) 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. It can also be used for chronic diarrhea under a doctor's supervision.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food. Unless your doctor advises you to limit your fluid intake, drink plenty of non-caffeinated liquids. Do not take this medication for a longer period than prescribed by your doctor.
To measure liquid doses accurately, use the measuring device that comes with the medication. If one is not provided, ask your pharmacist for a suitable measuring device. Some medications require shaking before use, so make sure you know if this applies to your product.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, consult your pharmacist, who may be aware of drug take-back programs in your area.
Missing a Dose
If you take this medication on a regular schedule, take a missed dose as soon as you remember. However, if it's close to the time for your next 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 take it more frequently than advised by your doctor.
To ensure you get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food. Unless your doctor advises you to limit your fluid intake, drink plenty of non-caffeinated liquids. Do not take this medication for a longer period than prescribed by your doctor.
To measure liquid doses accurately, use the measuring device that comes with the medication. If one is not provided, ask your pharmacist for a suitable measuring device. Some medications require shaking before use, so make sure you know if this applies to your product.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, consult your pharmacist, who may be aware of drug take-back programs in your area.
Missing a Dose
If you take this medication on a regular schedule, take a missed dose as soon as you remember. However, if it's close to the time for your next 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 take it more frequently than advised by your doctor.
Lifestyle & Tips
- Drink plenty of fluids (water, clear broths, electrolyte solutions) to prevent dehydration caused by diarrhea.
- Avoid caffeine, alcohol, and sugary drinks, which can worsen diarrhea.
- Eat bland foods (e.g., bananas, rice, applesauce, toast) and avoid fatty, spicy, or high-fiber foods until diarrhea subsides.
- Do not take more than the recommended dose, as this can lead to serious heart problems or other severe side effects.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Acute Diarrhea: 4 mg (30 ml) initially, then 2 mg (15 ml) after each loose stool, not to exceed 8 mg (60 ml) per day for OTC use or 16 mg (120 ml) per day for prescription use.
Dose Range:
2 - 16 mg
Condition-Specific Dosing:
Acute Diarrhea (OTC):
4 mg (30 ml) initially, then 2 mg (15 ml) after each loose stool, max 8 mg (60 ml)/day.
Acute Diarrhea (Rx):
4 mg (30 ml) initially, then 2 mg (15 ml) after each loose stool, max 16 mg (120 ml)/day.
Chronic Diarrhea (Rx):
Initially 4-8 mg (30-60 ml) daily in divided doses, adjusted to control symptoms, typically 4-8 mg (30-60 ml) daily.
Pediatric Dosing
Neonatal:
Not established (Contraindicated in infants <2 years due to risk of paralytic ileus and CNS depression).
Infant:
Not established (Contraindicated in infants <2 years due to risk of paralytic ileus and CNS depression).
Child:
2-5 years (13-20 kg): 1 mg (7.5 ml) three times daily on day 1, then 1 mg (7.5 ml) after each loose stool, max 3 mg (22.5 ml)/day.
6-8 years (20-30 kg): 2 mg (15 ml) two times daily on day 1, then 2 mg (15 ml) after each loose stool, max 4 mg (30 ml)/day.
9-11 years (30-43 kg): 2 mg (15 ml) three times daily on day 1, then 2 mg (15 ml) after each loose stool, max 6 mg (45 ml)/day.
Adolescent:
12 years and older: Same as adult dosing for acute diarrhea (4 mg (30 ml) initially, then 2 mg (15 ml) after each loose stool, max 8 mg (60 ml)/day for OTC use).
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed.
Moderate:
No adjustment needed.
Severe:
No adjustment needed.
Dialysis:
Not significantly dialyzable. No specific adjustment, but monitor for adverse effects.
Hepatic Impairment:
Mild:
Use with caution.
Moderate:
Use with extreme caution; reduced dosage may be required due to decreased first-pass metabolism and increased risk of CNS effects. Monitor closely for signs of CNS toxicity.
Severe:
Contraindicated due to risk of CNS depression and precipitation of hepatic encephalopathy.
Pharmacology
Mechanism of Action
Loperamide is a synthetic opioid derivative that acts directly on the mu-opioid receptors in the intestinal wall. It inhibits peristalsis by decreasing the activity of the longitudinal and circular muscles, thereby increasing intestinal transit time. It also increases the tone of the anal sphincter, reducing incontinence and urgency. Loperamide reduces fluid and electrolyte loss by decreasing secretion and increasing absorption in the gut.
Pharmacokinetics
Absorption:
Bioavailability:
Less than 1% (due to extensive first-pass metabolism)
Tmax:
Approximately 4-5 hours
FoodEffect:
Food may slightly increase absorption, but not clinically significant.
Distribution:
Vd:
Not available (highly lipophilic, extensively distributed)
ProteinBinding:
Approximately 95% (primarily to albumin)
CnssPenetration:
Limited (due to high affinity for P-glycoprotein efflux pump), but can occur at high doses, in overdose, or in individuals with impaired P-gp function.
Elimination:
HalfLife:
Approximately 9-14 hours (range 7-15 hours)
Clearance:
Not available
ExcretionRoute:
Primarily fecal (as unchanged drug and metabolites); less than 2% excreted renally.
Unchanged:
Less than 1% (in urine)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Not precisely defined for antidiarrheal effect, but Tmax for plasma concentration is 4-5 hours.
DurationOfAction:
Approximately 8-12 hours
Confidence:
High
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 paralytic ileus. Avoid use in patients with acute dysentery, bacterial enterocolitis, and pseudomembranous colitis.
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
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. While 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 for guidance:
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 about side effects, 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.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:
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. While 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 for guidance:
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 about side effects, 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:
- Severe constipation or abdominal bloating
- Severe stomach pain
- Bloody or black, tarry stools
- Fever
- Dizziness or fainting
- Fast or irregular heartbeat
- Difficulty breathing
- Rash or itching
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 problems, such as:
+ Gastrointestinal issues, including bloody or black stools, stomach pain without diarrhea, dysentery (characterized by blood in stools and fever), constipation, or colitis (a specific bowel condition).
+ Abnormal heart rhythms, including a prolonged QT interval on an electrocardiogram (ECG) or other irregular heartbeats.
+ Heart block, a condition where the electrical impulses that control the heartbeat are delayed or blocked.
+ Low levels of potassium or magnesium in the blood.
Medications you are taking that may cause abnormal heart rhythms, specifically a prolonged QT interval. There are many medications that can have this effect, so it is crucial to 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 vital to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose 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 problems, such as:
+ Gastrointestinal issues, including bloody or black stools, stomach pain without diarrhea, dysentery (characterized by blood in stools and fever), constipation, or colitis (a specific bowel condition).
+ Abnormal heart rhythms, including a prolonged QT interval on an electrocardiogram (ECG) or other irregular heartbeats.
+ Heart block, a condition where the electrical impulses that control the heartbeat are delayed or blocked.
+ Low levels of potassium or magnesium in the blood.
Medications you are taking that may cause abnormal heart rhythms, specifically a prolonged QT interval. There are many medications that can have this effect, so it is crucial to 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 vital to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose 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 forms of cannabis, as well as prescription or over-the-counter (OTC) medications that may cause drowsiness, with your doctor beforehand.
Be aware that dehydration and electrolyte imbalances can occur, particularly in individuals experiencing diarrhea. 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 for 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. It is necessary to discuss the potential benefits and risks associated with using this medication during pregnancy to make an informed decision.
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 forms of cannabis, as well as prescription or over-the-counter (OTC) medications that may cause drowsiness, with your doctor beforehand.
Be aware that dehydration and electrolyte imbalances can occur, particularly in individuals experiencing diarrhea. 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 for 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. It is necessary to discuss the potential benefits and risks associated with using this medication during pregnancy to make an informed decision.
Overdose Information
Overdose Symptoms:
- Severe constipation
- Abdominal distension
- Nausea and vomiting
- Drowsiness
- Dizziness
- Pinpoint pupils
- Slow or shallow breathing (respiratory depression)
- Loss of consciousness
- Cardiac arrhythmias (e.g., QT prolongation, Torsades de Pointes)
- Urinary retention
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Naloxone may be used to reverse opioid effects, but cardiac monitoring is crucial due to potential for prolonged QT interval.
Drug Interactions
Contraindicated Interactions
- Not applicable (no absolute contraindications based on drug-drug interactions, but severe hepatic impairment is a contraindication for the drug itself).
Major Interactions
- QT-prolonging drugs (e.g., Class IA and III antiarrhythmics, antipsychotics, macrolide antibiotics, tricyclic antidepressants) - increased risk of cardiac arrhythmias (QT prolongation, Torsades de Pointes) with high doses of loperamide.
- P-glycoprotein (P-gp) inhibitors (e.g., quinidine, ritonavir, gemfibrozil, itraconazole, ketoconazole, clarithromycin) - can significantly increase loperamide plasma concentrations, leading to increased risk of CNS and cardiac toxicity, especially at higher loperamide doses.
Moderate Interactions
- CYP3A4 inhibitors (e.g., erythromycin, cimetidine, grapefruit juice) - may increase loperamide levels.
- CYP2C8 inhibitors (e.g., trimethoprim) - may increase loperamide levels.
- Opioid analgesics - increased risk of severe constipation and CNS depression.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Fluid and Electrolyte Status
Rationale: To assess dehydration and electrolyte imbalance due to diarrhea before initiating treatment.
Timing: Prior to initiation, especially in severe diarrhea or vulnerable populations.
Routine Monitoring
Stool frequency and consistency
Frequency: Daily
Target: Reduction in loose stools, return to normal consistency
Action Threshold: If diarrhea persists for more than 2 days (48 hours) or worsens, discontinue and seek medical attention.
Signs of CNS depression (drowsiness, dizziness, respiratory depression)
Frequency: Daily, especially with higher doses or in patients with hepatic impairment or P-gp dysfunction.
Target: Absence of CNS depression
Action Threshold: If CNS depression occurs, reduce dose or discontinue.
Signs of abdominal distension, constipation, or ileus
Frequency: Daily
Target: Absence of these symptoms
Action Threshold: If severe constipation, abdominal distension, or signs of ileus develop, discontinue immediately.
Cardiac rhythm (ECG)
Frequency: Not routinely for therapeutic doses; consider if high doses are used or in patients with cardiac risk factors or on interacting medications.
Target: Normal QT interval
Action Threshold: If QT prolongation or arrhythmias occur, discontinue immediately.
Symptom Monitoring
- Abdominal pain or cramping
- Bloating
- Nausea/Vomiting
- Drowsiness or dizziness
- Dry mouth
- Fatigue
- Signs of dehydration (decreased urination, dry mouth, excessive thirst)
Special Patient Groups
Pregnancy
Loperamide is classified as Pregnancy Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Limited human data suggest low risk, but animal studies show some adverse effects at high doses.
Trimester-Specific Risks:
First Trimester:
Limited data, generally considered low risk for major malformations, but caution advised.
Second Trimester:
Generally considered safer than first trimester, but use only if clearly needed.
Third Trimester:
Use with caution, as there is a theoretical risk of neonatal opioid withdrawal symptoms or respiratory depression if used close to delivery, though systemic absorption is low.
Lactation
Loperamide is excreted in breast milk in very small amounts. It is generally considered compatible with breastfeeding (Lactation Risk Category L2). Monitor the infant for signs of constipation or CNS depression.
Infant Risk:
Low risk. Monitor for constipation, drowsiness, or respiratory depression, especially in premature or very young infants.
Pediatric Use
Contraindicated in children less than 2 years of age due to the risk of respiratory depression and paralytic ileus. Use with caution and strict adherence to weight-based dosing in children 2-12 years. Overdose can be particularly dangerous in this population.
Geriatric Use
No specific dose adjustment is typically needed, but use with caution. Elderly patients may be more sensitive to the CNS effects of loperamide and may have underlying conditions (e.g., hepatic impairment, cardiac issues) that increase risk of adverse effects. Monitor closely for constipation and CNS depression.
Clinical Information
Clinical Pearls
- Loperamide treats symptoms of diarrhea, not the underlying cause. It should not be used in cases of infectious diarrhea where retention of toxins might be harmful (e.g., C. difficile, E. coli O157:H7).
- Always ensure adequate hydration and electrolyte replacement, especially in children and the elderly.
- Discontinue loperamide if abdominal distension, constipation, or ileus occurs.
- Warn patients about the serious cardiac risks associated with taking higher than recommended doses, often seen in abuse/misuse for opioid withdrawal symptoms.
- The 1mg/7.5ml suspension concentration is important for accurate pediatric dosing to avoid errors.
Alternative Therapies
- Bismuth subsalicylate (e.g., Pepto-Bismol, Kaopectate)
- Diphenoxylate/Atropine (e.g., Lomotil - prescription only, controlled substance)
- Racecadotril (not available in US, but used in other countries for acute diarrhea)
- Oral Rehydration Solutions (ORS) - primary treatment for dehydration, not an antidiarrheal but crucial supportive care.
Cost & Coverage
Average Cost:
Varies widely, typically $10-$30 per 120 ml bottle of 1mg/7.5ml suspension
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, 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 your 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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.