Medications for Alleviating Diarrhea
Loperamide is the first-line medication for alleviating acute diarrhea in adults due to its proven efficacy in reducing stool frequency and improving consistency, with a recommended initial dose of 4 mg followed by 2 mg after each loose stool (maximum 16 mg daily). 1, 2
First-Line Medications
Loperamide
- Mechanism: Opioid receptor agonist that decreases intestinal motility and increases water absorption 3
- Dosing:
- Best for: Acute watery diarrhea in adults, traveler's diarrhea, chronic diarrhea 2
- Contraindications:
- Children under 12 years
- Bloody diarrhea or high fever (>38.5°C)
- Inflammatory diarrhea or suspected toxic megacolon 2
Bismuth Subsalicylate
- Mildly effective for acute diarrhea 2
- Less effective than loperamide but can be used as an alternative
Second-Line Medications
Antimotility Agents
- Diphenoxylate: Less effective than loperamide and has more central nervous system effects 4
- Codeine/Morphine: Can be used when loperamide is ineffective, but have more side effects 2
Antisecretory Agents
- Racecadotril: Reduces stool volume but not available in North America 2
- Octreotide: For severe cases, especially chemotherapy-induced diarrhea
- Dosing: 100-150 μg subcutaneously/IV three times daily 2
Special Populations and Conditions
Irritable Bowel Syndrome with Diarrhea (IBS-D)
- Loperamide is suggested for IBS-D patients (conditional recommendation) 2
- Benefits: Improves stool consistency and abdominal pain
- Limitations: Limited effect on urgency symptoms and global improvement 2
Travelers' Diarrhea
- Loperamide can be used as monotherapy for mild cases 2
- For moderate to severe cases, combination with antibiotics (fluoroquinolones or azithromycin) is more effective 2
- Reduces duration of illness from 59 hours to approximately 27 hours when combined with antibiotics 2
Cancer Treatment-Related Diarrhea
- Loperamide: First-line treatment (4 mg initially, then 2 mg every 2-4 hours) 2
- For chemotherapy-induced diarrhea refractory to loperamide:
- Octreotide: 100-150 μg subcutaneously/IV three times daily
- Oral budesonide may be considered 2
Important Precautions
Avoid antimotility agents in:
- Children under 12 years
- Bloody diarrhea or high fever
- Suspected bacterial enterocolitis or C. difficile infection 2
Seek medical attention if:
- No improvement after 48 hours
- Symptoms worsen
- Warning signs develop (severe vomiting, dehydration, persistent fever, blood in stool) 2
Fluid replacement:
- Maintain adequate fluid intake guided by thirst
- Consider drinks containing glucose and electrolytes 2
Effectiveness Comparison
- Loperamide is more effective than diphenoxylate and bismuth subsalicylate preparations 5
- When combined with antibiotics for travelers' diarrhea, loperamide reduces duration of illness to less than half a day compared to approximately 1.5 days with antibiotics alone 2
- Loperamide has minimal central nervous system effects due to low oral absorption and inability to cross the blood-brain barrier 3
For most cases of acute diarrhea in adults, loperamide provides the best balance of efficacy, safety, and accessibility as an over-the-counter medication, making it the first choice for symptomatic treatment.