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洛哌丁胺代谢物诱导的心肌病和QTc间期延长。

Loperamide metabolite-induced cardiomyopathy and QTc prolongation.

作者信息

Bhatti Zabeer, Norsworthy Jessica, Szombathy Tamas

机构信息

a Department of Medicine , State University of New York , Syracuse , NY , USA.

出版信息

Clin Toxicol (Phila). 2017 Aug;55(7):659-661. doi: 10.1080/15563650.2017.1304555. Epub 2017 Mar 28.

DOI:10.1080/15563650.2017.1304555
PMID:28349724
Abstract

Loperamide is an over-the-counter, peripherally acting, μ-opioid receptor agonist used for the treatment of diarrhea. In recent times users have found that at higher doses, loperamide crosses the blood-brain barrier and reaches central μ-receptors in the brain, leading to central opiate effects including euphoria and respiratory depression. We report a case of a 37-year-old female who attempted suicide with over 200 loperamide tablets. During her overdose, her QTc was significantly prolonged at >600 ms. Our case aims to add to the growing body of literature describing life-threatening ventricular arrhythmias associated with loperamide toxicity and further suggests that a metabolite of loperamide, desmethylloperamide, may play a role in the pathogenesis.

摘要

洛哌丁胺是一种非处方的外周作用μ-阿片受体激动剂,用于治疗腹泻。近来,使用者发现,高剂量的洛哌丁胺会穿过血脑屏障,到达大脑中的中枢μ-受体,从而产生包括欣快感和呼吸抑制在内的中枢阿片类效应。我们报告了一例37岁女性试图服用200多片洛哌丁胺自杀的病例。在她过量服药期间,其QTc显著延长,超过600毫秒。我们的病例旨在补充越来越多描述与洛哌丁胺毒性相关的危及生命的室性心律失常的文献,并进一步表明洛哌丁胺的代谢产物去甲基洛哌丁胺可能在发病机制中起作用。

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Loperamide metabolite-induced cardiomyopathy and QTc prolongation.洛哌丁胺代谢物诱导的心肌病和QTc间期延长。
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The long QT teaser: loperamide abuse.长QT综合征的诱因:洛哌丁胺滥用
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引用本文的文献

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Evaluation of the Effect of Loperamide on the Cardiac Repolarization Interval Using Exposure-Response Analysis.使用暴露-反应分析评估洛哌丁胺对心脏复极间期的影响。
Clin Transl Sci. 2025 Feb;18(2):e70114. doi: 10.1111/cts.70114.
2
Left Ventricular Regional Wall Motion Abnormality in the Setting of Acute Loperamide Overdose.急性洛哌丁胺过量情况下的左心室局部壁运动异常
Clin Pract Cases Emerg Med. 2019 Jul 1;3(3):262-266. doi: 10.5811/cpcem.2019.4.42510. eCollection 2019 Aug.
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Pharmacologic Treatment of Opioid Use Disorder: a Review of Pharmacotherapy, Adjuncts, and Toxicity.
阿片类物质使用障碍的药物治疗:药物疗法、辅助治疗及毒性综述
J Med Toxicol. 2018 Dec;14(4):306-322. doi: 10.1007/s13181-018-0685-1. Epub 2018 Oct 30.
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Is there such a thing as a 'lope' dope? Analysis of loperamide-related European Medicines Agency (EMA) pharmacovigilance database reports.是否存在“洛哌丁胺”类药物?对欧洲药品管理局(EMA)药物警戒数据库中与洛哌丁胺相关报告的分析。
PLoS One. 2018 Oct 4;13(10):e0204443. doi: 10.1371/journal.pone.0204443. eCollection 2018.
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Abuse of Prescription Drugs in the Context of Novel Psychoactive Substances (NPS): A Systematic Review.新型精神活性物质(NPS)背景下的处方药滥用:一项系统综述
Brain Sci. 2018 Apr 22;8(4):73. doi: 10.3390/brainsci8040073.
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Loperamide cardiotoxicity: "A Brief Review".洛哌丁胺的心脏毒性:“简要综述”
Ann Noninvasive Electrocardiol. 2018 Mar;23(2):e12505. doi: 10.1111/anec.12505. Epub 2017 Nov 10.