Loperamide cardiotoxicity: “A Brief Review”

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 opi...

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Bibliographic Details
Published in:Annals of noninvasive electrocardiology 2018-03, Vol.23 (2), p.e12505-n/a
Main Authors: Akel, Tamer, Bekheit, Soad
Format: Article
Language:English
Subjects:
Abuse
Analgesia
Antidiarrheals - adverse effects
Antidiarrheals - therapeutic use
Bioavailability
Cardiac arrest
Cardiotoxicity
Cardiotoxicity - etiology
Cardiotoxicity - physiopathology
Central nervous system
Clinical electrophysiology‐cardiac arrest/sudden death
Clinical electrophysiology‐ventricular tachycardia
Clinical ion channels and membrane transporters
Diarrhea - drug therapy
Diarrhea - physiopathology
Dose-Response Relationship, Drug
Drug Administration Schedule
Electrophsiology‐long QT syndrome
Enteric nervous system
Female
Health care
Humans
Loperamide - pharmacology
Loperamide - therapeutic use
Loperamide - toxicity
Male
Medical personnel
Muscles
Myenteric plexus
Narcotics
Nervous system
Opioid receptors
Pain perception
Patient Safety
Peristalsis
Review
Risk Assessment
Secretion
Side effects
Transit time
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Summary: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.
ISSN:1082-720X
1542-474X
DOI:10.1111/anec.12505