Cardiotoxicity in Loperamide Misuse and Abuse - Insights into Clinical Evidence, Underlying Mechanisms, and Clinical...

Loperamide is a commonly available over-the-counter (OTC) antidiarrheal medication that emerged as a drug of abuse due to its opioid-receptor agonist activity at higher doses. Although loperamide has been found safer at recommended dosages, a growing number of reports have connected its misuse and abuse to serious cardiotoxicity. This review focuses on available clinical data, underlying mechanisms, clinical presentation, diagnostic challenges, and management strategies regarding loperamide-induced cardiotoxicity.

To find articles pertinent to cardiotoxicity associated with the abuse and misuse of loperamide, the online databases such as Medline/PubMed/PMC, Scopus, Web of Science, Google Scholar, and reference lists were searched.

Higher doses of loperamide have been linked to QT prolongation, Torsades de Pointes (TdP), ventricular arrhythmias, and sudden cardiac death, according to several clinical trials.

People with opioid use disorder misuse higher dosages of loperamide to self-treat the symptoms of opiate withdrawal or abuse it to achieve euphoric effects. Supratherapeutic doses of loperamide may induce cardiotoxicity via a number of possible mechanisms, including potassium channel blockade, sodium channel blockade, calcium channel blockade, P-gp inhibition, QT prolongation, opioid receptor-mediated effects, and electrolyte imbalances.

In order to promote safer prescribing practices and better patient outcomes, this review aims to increase awareness among physicians, researchers, and the general public regarding the possible risks associated with loperamide misuse and abuse by compiling existing knowledge.