Loperamide cardiotoxicity: "A Brief Review".

Area of Science:

• Pharmacology
• Gastroenterology

Background:

• Loperamide is a widely used over-the-counter antidiarrheal.
• It acts as a peripherally acting μ-receptor agonist, primarily affecting the gastrointestinal tract.
• Despite low bioavailability and exclusion from the CNS at recommended doses, its abuse is rising.

Purpose of the Study:

• To review the pharmacological profile of loperamide.
• To discuss the increasing trend of loperamide abuse.
• To highlight the potential side effects and risks associated with high-dose loperamide ingestion.

Main Methods:

• Literature review of pharmacological studies on loperamide.
• Analysis of trends in loperamide abuse from available data.
• Examination of reported side effects and adverse events.

Main Results:

• Loperamide reduces peristalsis and fluid secretion, increasing gastrointestinal transit time.
• At recommended doses, it lacks central nervous system effects like euphoria.
• High-dose ingestion leads to central nervous system penetration, causing euphoria and opioid withdrawal symptom relief.

Conclusions:

• Loperamide abuse is a growing concern, with individuals using high doses for psychoactive effects.
• The accessibility of loperamide as an over-the-counter medication contributes to its abuse potential.
• Healthcare professionals should be aware of the risks associated with loperamide misuse.