Loperamide cardiotoxicity: "A Brief Review"

Ann Noninvasive Electrocardiol. 2018 Mar;23(2):e12505. doi: 10.1111/anec.12505. Epub 2017 Nov 10.

Abstract

Loperamide is a popular antidiarrheal medication that has been used for many years. It is currently gaining more attention among healthcare professionals due to its increasing potential for side effects. At present, it is considered safe enough to be sold over the counter. In contrast with other opioid agonists, loperamide is a peripherally acting μ-receptor agonist exerting its effects mainly on the myenteric plexus of the gastrointestinal longitudinal muscle layer. It decreases peristalsis and fluid secretion resulting in longer gastrointestinal transit time. The bioavailability of the drug is extremely low. Moreover, it is actively excluded from the central nervous system; hence, it lacks the central effects of euphoria and analgesia at the recommended dosages. Loperamide abuse has been steadily increasing in the United States. Abusers typically ingest high doses in desire to achieve a satisfactory central nervous system drug penetration. This has made it a potential over the counter substitute for self-treating opioid withdrawal symptoms and achieving euphoric effects.

Keywords: Clinical electrophysiology-cardiac arrest/sudden death; Clinical electrophysiology-ventricular tachycardia; Clinical ion channels and membrane transporters; Electrophsiology-long QT syndrome.

Publication types

  • Review

MeSH terms

  • Antidiarrheals / adverse effects*
  • Antidiarrheals / therapeutic use
  • Cardiotoxicity / etiology*
  • Cardiotoxicity / physiopathology
  • Diarrhea / drug therapy
  • Diarrhea / physiopathology
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Female
  • Humans
  • Loperamide / pharmacology
  • Loperamide / therapeutic use
  • Loperamide / toxicity*
  • Male
  • Patient Safety*
  • Risk Assessment

Substances

  • Antidiarrheals
  • Loperamide