超治疗性洛佩拉米德的毒性概况:系统性审查和剂量反应分析
Elias Bekka1, Adrian Martinez-De la Torre2,3, Manuel Haschke1
1Clinical Pharmacology and Toxicology, Department of General Internal Medicine, Inselspital, Bern University Hospital, University of Bern, Bern, Switzerland.
Clinical toxicology (Philadelphia, Pa.)
|March 12, 2026
概括
高剂量洛佩拉米德 (即每天超过16毫克) 可能导致危及生命的心脏毒性,即使剂量低于以前认为的. 本系统性审查强调了剂量依赖风险和相关死亡率,强调了暴露个体心脏监测的必要性.
科学领域:
- 心脏病学 心脏病学
- 毒理学 毒理学 毒理学
- 药理学 药理学是指药理学的学科.
背景情况:
- 超治疗性洛佩拉米德的使用越来越多地与心脏毒性有关.
- 对于洛佩拉米德的毒性概况和剂量反应关系的系统数据有限.
研究的目的:
- 系统地审查人类超治疗性洛佩拉米德暴露病例.
- 描述毒性概况,剂量反应关系和结果.
- 确定严重心脏毒性和死亡的危险因素.
主要方法:
- 对洛佩拉胺暴露 (>16毫克/天) 的病例报告和系列的系统审查.
- 提取有关剂量,度,临床过程和结果的数据.
- 回归分析以评估暴露毒性关系,调整混因素.
主要成果:
- 包括129例;中位数剂量为200毫克/天,中位数度为87微克/升.
- 在剂量低至20-40毫克/天时,发生严重的心脏毒性 (心室动脉冲动症).
- 死亡率与度相关 (LC50估计为210μg/L);胸与严重程度有关.
结论:
- 超治疗性洛佩拉米德与剂量依赖性心脏毒性有关,剂量低于以前认可的剂量存在显著风险.
- 对于超治疗性洛佩拉米德暴露的个人,应考虑心脏监测.
- 管理包括抗心律失常和支持性护理措施.
相关概念视频
Drugs Affecting GI Tract Motility: Opioids as Antidiarrheal Agents
1.0K
Diarrhea, a condition marked by frequent loose or watery bowel movements, can be triggered by multiple factors such as viral or bacterial infections, food intolerances, anxiety, medications, and digestive disorders. Symptoms may include abdominal pain, bloating, nausea, and cramping. Severe or prolonged diarrhea can lead to complications like electrolyte imbalances, malnutrition, and dehydration if left untreated.
Opioids, widely used antidiarrheal agents, mitigate diarrhea by slowing down...
Opioids, widely used antidiarrheal agents, mitigate diarrhea by slowing down...
1.0K
Drugs for Treatment of Constipation-Predominant IBS
1.4K
Pharmacological therapies for IBS-C are designed to alleviate abdominal discomfort and enhance bowel function. In patients with IBS-C, fiber supplements may help soften stools and decrease straining, but may also lead to increased gas production and bloating. Osmotic laxatives like milk of magnesia are frequently used to soften stools and increase stool frequency in IBS-C patients. In addition, two drugs approved for use in severe IBS-C adult cases are linaclotide (Linzess) and lubiprostone...
1.4K
Drug Toxicity: Overview
295
Drug toxicity quantifies the harm a compound causes to an organism, varying by dose and potentially impacting whole systems or specific organs like the liver. Toxic reactions may arise from venomous insect or spider bites, with effects ranging from mild symptoms to severe outcomes such as brain damage or death. Common forms of acute poisoning include ethanol intoxication and overdose of pain or fever medications, with substances like GHB and heroin being particularly lethal at doses close to...
295
Drug Toxicity: Dose-Dependent Reactions
229
Drug toxicities can be stratified into pharmacological, pathological, or genotoxic based on their mechanisms. The incidence and severity of these toxicities generally increase with the drug's concentration in the body and exposure time.Pharmacological toxicity is evident when the therapeutic effects of drugs overshoot into adverse reactions in a predictable, dose-dependent manner. Central nervous system (CNS) depression from barbiturates is a classic example, with effects escalating from...
229
Dose Response Curve: Conventional Versus Nonmonotonic
371
The correlation between a drug's dosage and its impact on a biological system is a cornerstone of pharmacology and toxicology. Conventional dose–response curves, which include graded and quantal relationships, are key to this understanding. Graded dose–response curves depict the spectrum of a biological reaction to different doses within an individual, indicating that as the drug dosage increases, so does the intensity of the response. On the other hand, quantal dose–response...
371
Toxicokinetics: Overview
314
Studies that assess how a drug is absorbed, distributed, metabolized, and excreted (ADME) at toxic doses are termed toxicokinetics. Understanding toxicokinetics helps predict adverse drug reactions (ADRs) and manage toxicity in humans.Toxicokinetics differs from pharmacokinetics mainly in the dose levels studied, with toxicokinetics focusing on higher toxic doses. The kinetics at these levels can be non-linear due to altered physiological processes. Toxicodynamics examines the relationship...
314


