| Autor: |
Lammoglia BC; School of Medicine, Universidade Santo Amaro (UNISA), São Paulo 04829-300, SP, Brazil., Hasselmann G; School of Medicine, Universidade Santo Amaro (UNISA), São Paulo 04829-300, SP, Brazil., Pires-Oliveira M; School of Medicine, União Metropolitana de Educação e Cultura, Lauro de Freitas 42700-000, BA, Brazil., Duarte Nicolau LA; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (LAFIDG), Universidade Federal do Delta do Parnaíba (UFDPar), Parnaíba 64202-020, PI, Brazil., Rolim Medeiros JV; Laboratory of Pharmacology of Inflammation and Gastrointestinal Disorders (LAFIDG), Universidade Federal do Delta do Parnaíba (UFDPar), Parnaíba 64202-020, PI, Brazil., Sabia Tallo F; Department of Urgency and Emergency Care, Universidade Federal de São Paulo (UNIFESP), São Paulo 04023-062, SP, Brazil., Omar Taha M; Department of Surgery, Universidade Federal de São Paulo (UNIFESP), São Paulo 04023-062, SP, Brazil., Yamaguti Lima R; School of Medicine, Universidade Santo Amaro (UNISA), São Paulo 04829-300, SP, Brazil.; Postgraduate Program in Cardiology, Universidade Federal de São Paulo (UNIFESP), São Paulo 04023-062, SP, Brazil., Caricati-Neto A; Department of Pharmacology, Universidade Federal de São Paulo (UNIFESP), São Paulo 04023-062, SP, Brazil., Menezes-Rodrigues FS; School of Medicine, Universidade Santo Amaro (UNISA), São Paulo 04829-300, SP, Brazil.; Postgraduate Program in Cardiology, Universidade Federal de São Paulo (UNIFESP), São Paulo 04023-062, SP, Brazil. |
| Abstrakt: |
Loperamide is a synthetic opioid commonly used as an antidiarrheal due to its activation of u-opioid receptors in the myenteric plexus. In therapeutic doses, it inhibits peristalsis and has anti-secretory and anti-motility effects, until metabolized by intestinal and hepatic CYP3A4 and CYP2C8 into inactive metabolites. Furthermore, loperamide also inhibits L-type voltage-gated calcium (Ca 2+ ) channels, increases action potential duration, and can induce arrhythmias and even cardiotoxicity, particularly when taken in extremely high doses. Thus, the aim of this study was to perform an integrative review of the available evidence in the recent literature on the cardiac risks of acute and chronic use of loperamide. In electrocardiogram (ECG) analysis, the most common finding was QTc prolongation in 27 cases, followed by QRS prolongation, first-degree atrioventricular (AV) block, torsades de pointes, ventricular tachycardia, and right bundle branch block. As for the symptoms encountered, syncope, weakness, palpitations, lightheadedness, shortness of breath, nausea, vomiting, bradycardia, and cardiac arrest were the most common. Loperamide can inhibit hERG voltage-gated potassium (K + ) channels (Kv11.1), leading to the prolongation of repolarization, QTc interval prolongation, and increased risk of torsades de pointes. In addition, loperamide can inhibit voltage-gated sodium (Na + ) channels (Nav1.5), impairing electrical cardiac conduction and potentiating QRS interval widening. Therefore, QTc prolongation, torsades de pointes, and other ECG alterations are of particular concern regarding loperamide toxicity, particularly when overdosed. |
