IMODIUM 2/MG CAP 6/CAP

Indications

Approved Uses

Symptomatic treatment of acute nonspecific diarrhea; symptomatic treatment of chronic diarrhea (including that associated with inflammatory bowel disease) under medical supervision; reduction of volume of discharge from ileostomies.

Off-Label Uses

Adjunct for traveler’s diarrhea (symptomatic relief when no dysentery/fever) and management of chemotherapy-induced diarrhea (often as adjunct and per oncology protocols).

Dosage & Administration

Dosing by Condition

Acute diarrhea (adults): 4 mg initially (2 capsules), then 2 mg after each loose stool; maximum OTC 8 mg/day unless directed by a clinician (maximum 16 mg/day under medical supervision). Chronic diarrhea (adults, medical supervision): 4 mg/day initially, then titrate to the lowest effective dose (commonly 4-8 mg/day in divided doses), maximum 16 mg/day. Ileostomy (medical supervision): individualized; typical total daily dose 4-16 mg/day in divided doses.

Initial Dose

4mg (2 capsules) as a single initial dose

Maintenance Dose

2mg after each subsequent loose stool. For chronic diarrhea, typical maintenance is 4-8mg daily.

Maximum Dose

OTC maximum: 8 mg/day; prescription maximum: 16 mg/day.

Children's Dosage

Not for use in children under 2 years. 2-5 years (13-20 kg): 1mg three times a day on day 1. 6-8 years (20-30 kg): 2mg twice a day on day 1. 9-12 years (>30 kg): 2mg three times a day on day 1. Subsequent doses are 0.1mg/kg after each loose stool, not to exceed the total daily dose of day 1.

Dose Adjustment Notes

No dose adjustment required for renal or mild-to-moderate hepatic impairment; use with caution in severe hepatic impairment due to reduced first-pass metabolism

How to Take

Swallow the 2 mg capsule whole with water; may be taken with or without food. Maintain adequate fluid and electrolyte intake (oral rehydration) to prevent dehydration.

Side Effects

Common Side Effects

Constipation, abdominal cramps/pain, nausea, flatulence; dizziness may occur.

Side Effect Frequency

Common (≥1%): constipation, nausea, flatulence, abdominal pain/cramps, dizziness, headache. Uncommon (0.1-1%): vomiting, abdominal distension/discomfort, dry mouth, dyspepsia, rash/urticaria, drowsiness. Rare (<0.1%): ileus (including paralytic ileus), megacolon/toxic megacolon, urinary retention, severe hypersensitivity reactions; serious cardiac arrhythmias mainly with overdose/misuse.

Safety & Warnings

Contraindications

Hypersensitivity to loperamide; children <2 years; acute dysentery (blood in stool and high fever); acute ulcerative colitis; bacterial enterocolitis due to invasive organisms (e.g., Salmonella, Shigella, Campylobacter); pseudomembranous colitis associated with antibiotics; and any condition where inhibition of peristalsis should be avoided (e.g., ileus/abdominal distension/constipation).

Warnings & Precautions

Do not use with blood in stool or high fever (possible invasive/inflammatory diarrhea); not a substitute for rehydration; stop and seek care if no improvement within 48 hours; stop if constipation/abdominal distension/ileus occurs; use caution in hepatic impairment; do not exceed recommended dose due to risk of life-threatening cardiac arrhythmias (QT prolongation/Torsades/cardiac arrest).

Age Restriction

Contraindicated/not recommended in children <2 years; for OTC use, adults and children 12 years and older unless directed by a doctor; children 2-12 years per dosing schedule.

Driving Warning

May Cause Drowsiness

Drug Interactions

Drug Interactions

Clinically important: inhibitors of P-gp and/or CYP3A4/CYP2C8 (e.g., quinidine, ritonavir, ketoconazole/itraconazole, gemfibrozil) can increase loperamide exposure and cardiac/CNS toxicity risk; additive risk with other QT-prolonging drugs; additive constipation/ileus risk with other antimotility/anticholinergic/opioid agents.

Interaction Severity

MAJOR: Strong CYP3A4/CYP2C8 and/or P-gp inhibitors (e.g., itraconazole/ketoconazole, gemfibrozil, ritonavir, quinidine) and other QT-prolonging risk factors/drugs-can increase loperamide exposure and raise risk of serious cardiac arrhythmias, especially with supratherapeutic dosing. MODERATE: Other QT-prolonging drugs (e.g., amiodarone, macrolides, fluoroquinolones, SSRIs) and additional P-gp/CYP inhibitors-use caution and avoid exceeding recommended doses. MINOR: Oral rehydration solutions-no pharmacokinetic interaction; co-administration is recommended.

Food Interaction

No restriction.

Special Populations

Pregnancy

Pregnancy Category C

Breastfeeding

Consult Doctor

Children

Not for use in children under 2 years. 2-5 years (13-20 kg): 1mg three times a day on day 1. 6-8 years (20-30 kg): 2mg twice a day on day 1. 9-12 years (>30 kg): 2mg three times a day on day 1. Subsequent doses are 0.1mg/kg after each loose stool, not to exceed the total daily dose of day 1.

Elderly

Standard adult dosing; ensure adequate hydration

Kidney Impairment

No adjustment needed.

Liver Impairment

No specific dose adjustment provided; use with caution in hepatic impairment (especially severe) due to reduced first-pass metabolism and increased risk of CNS/cardiac toxicity.

Storage & Patient Advice

Stopping the Medicine

Stop if constipation, abdominal distension, or ileus develops; and for acute diarrhea stop and seek medical advice if not improved within 48 hours (no taper required).

Overdose

Overdose may cause CNS depression (somnolence/stupor), miosis, respiratory depression, urinary retention, ileus, and serious cardiac toxicity (QT prolongation, Torsades, ventricular arrhythmias/cardiac arrest); management includes urgent medical care, cardiac monitoring, activated charcoal if appropriate, supportive care, and naloxone (may require repeated dosing).

Patient Counseling

Adults: take 4 mg (2 capsules) once, then 2 mg (1 capsule) after each loose stool; do not exceed 8 mg (4 capsules) in 24 hours unless a clinician directs otherwise. Stop and seek medical advice if symptoms persist >48 hours, or if fever, blood/mucus in stool, severe abdominal pain/distension, or signs of dehydration occur. Drink plenty of fluids/ORS. Do not use in children <2 years; use caution with liver disease. Do not exceed recommended dose due to risk of serious heart rhythm problems; may cause dizziness-use caution driving.

Monitoring Requirements

No routine laboratory monitoring for short-term OTC use; monitor clinical response and hydration/electrolyte status. For prolonged/chronic use or hepatic impairment, monitor for constipation/ileus, CNS effects, and cardiac symptoms (palpitations/syncope) especially if interacting drugs are present or doses approach the maximum.

Pharmacology

Mechanism of Action

Peripherally acting μ-opioid receptor agonist in the intestinal wall (myenteric plexus) that decreases propulsive peristalsis and intestinal secretion, increases transit time and anal sphincter tone, with minimal CNS opioid effects at therapeutic doses due to P-gp efflux and first-pass metabolism.

Onset of Action

Approximately 1 hour

Half-Life

Approximately 10-11 hours (reported range about 9-14 hours).

Bioavailability

<1% systemic bioavailability (often cited around ~0.3%) due to extensive first-pass metabolism and P-gp efflux.

Metabolism

Extensive hepatic first-pass metabolism, primarily via CYP3A4 and CYP2C8 (oxidative metabolism including N-demethylation).

Excretion

Primarily fecal excretion via bile (major route); renal excretion is minimal (typically <2%).

Product Information

Available Dosage Forms

For this SFDA-registered product: Capsule (oral).

Composition per Dose

Each capsule: 2mg loperamide hydrochloride

Generic Availability

Yes

Gi Condition

Diarrhea

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