Controlled Medicines for Diarrhea
Loperamide is the primary recommended controlled medicine for diarrhea, with an initial dose of 4 mg followed by 2 mg every 2-4 hours or after each unformed stool (maximum 16 mg/day). 1
First-Line Treatment: Loperamide
Loperamide is the opioid of choice for diarrhea management because it:
- Has local activity in the gut with minimal systemic absorption
- Reduces stool weight, frequency of bowel movements, urgency, and fecal incontinence
- Has minimal central nervous system effects due to its inability to cross the blood-brain barrier 2
Dosing Protocol:
- Initial dose: 4 mg (two capsules)
- Maintenance: 2 mg (one capsule) after each unformed stool or every 2-4 hours
- Maximum daily dose: 16 mg (eight capsules) 1
- For chronic diarrhea: Once controlled, dosage should be reduced to meet individual requirements (average maintenance 4-8 mg daily) 1
Second-Line Options (When Loperamide Fails)
If diarrhea persists for more than 48 hours on high-dose loperamide, consider:
Octreotide:
- Starting dose: 100-150 μg subcutaneously three times daily
- Can be titrated up to 500 μg three times daily
- For severe dehydration: IV administration (25-50 μg/hour) 3
Other Opioids:
Oral Budesonide:
- May be effective for chemotherapy-induced diarrhea refractory to loperamide
- Typical dose: 9 mg once daily 3
Special Considerations
For Immunotherapy-Induced Diarrhea:
- Grade 1: Loperamide with oral rehydration
- Grade 2: Add budesonide 9 mg daily (if no bloody diarrhea)
- Grade 3-4: Corticosteroids (1-2 mg/kg/day prednisone equivalent); avoid loperamide and opioids 3
For Chemotherapy-Induced Diarrhea:
- If mild to moderate diarrhea persists >24 hours: Increase loperamide to 2 mg every 2 hours and consider oral antibiotics 3
- For complicated cases: IV fluids, octreotide, and antibiotics (e.g., fluoroquinolone) 3
Precautions:
- Monitor for paralytic ileus with high-dose loperamide
- Use with caution in patients with hepatic impairment due to potentially increased systemic exposure 1
- Avoid in elderly patients taking medications that prolong QT interval 1
- Contraindicated in children under 2 years due to risk of respiratory depression 1
Adjunctive Measures
- Dietary modifications: Eliminate lactose-containing products, alcohol, and high-osmolar supplements
- Hydration: 8-10 large glasses of clear liquids daily
- Small, frequent meals (bananas, rice, applesauce, toast, plain pasta) 3
When treating infectious diarrhea, loperamide can be used safely in combination with appropriate antibiotics, which has been shown to further reduce gastrointestinal symptoms and duration of illness 4, 5.