Loperamide Availability Status
Yes, loperamide is available over-the-counter (OTC) and does not require a prescription for adults. 1
Evidence Supporting OTC Status
- Loperamide has an established FDA-labeled indication for treatment of mild traveler's diarrhea and is widely available without prescription 2
- The medication has been deemed safe and effective for self-medication in adults with appropriate usage guidelines 3
- Loperamide was released from prescription-only status to OTC based on its favorable safety profile, established efficacy, and minimal abuse potential when used as directed 3
Appropriate Use Guidelines
Recommended Dosing
- Initial dose is 4 mg (2 tablets) followed by 2 mg after each loose stool, with a maximum daily dose of 16 mg 2, 1
- For mild diarrhea, loperamide should be used as supportive treatment alongside proper hydration 2
- Therapeutic effect takes 1-2 hours to develop, so additional doses should be spaced accordingly to avoid rebound constipation 2
Clinical Applications
- Strongly recommended for treatment of mild traveler's diarrhea as monotherapy 2
- May be used as adjunctive therapy for moderate to severe traveler's diarrhea (with antibiotics) 2
- Effective for reducing stool volume in most non-cholera watery diarrhea syndromes 1
Safety Considerations and Warnings
Contraindications
- Should not be used in children under 18 years of age with acute diarrhea 1
- Should be avoided in cases of bloody diarrhea, high fever, or moderate to severe abdominal pain 2
- Not recommended for inflammatory diarrhea where toxic megacolon may result 1
Potential Adverse Effects
- Common side effects include abdominal cramps, nausea, constipation, and bloating 4
- At recommended doses, loperamide does not cross the blood-brain barrier and has minimal central nervous system effects 5
Risk of Misuse
- Abuse and misuse have been reported, especially at doses of 60 mg or greater 6
- Overdose can result in life-threatening cardiac adverse reactions including QT/QTc prolongation and ventricular arrhythmias 6
- Cases of abuse have been documented in individuals attempting to simulate opioid euphoria or prevent withdrawal symptoms 6
Advantages Over Other Antidiarrheals
- More effective than bismuth subsalicylate for controlling diarrhea 7
- Longer duration of action and better safety profile than diphenoxylate 8
- Unlike older opiates (morphine, codeine), loperamide is not sedative, addictive, or associated with fat malabsorption when used as directed 2
Key Clinical Pearls
- Rehydration should always be the first priority in managing diarrhea, with loperamide considered only after adequate hydration 1
- If diarrhea worsens or is accompanied by fever, severe abdominal pain, or bloody stools, antibiotics should be used instead of or in addition to loperamide 2
- Loperamide is metabolized by CYP3A4; concurrent administration with CYP3A4 inhibitors may elevate loperamide concentrations 5