Cardiology Unit, Department of Experimental, Diagnostic and Specialty Medicine, Alma Mater Studiorum - University of Bologna, Bologna, Italy.
Pharmacology Unit, Department of Medical and Surgical Sciences, Alma Mater Studiorum - University of Bologna, Bologna, Italy.
Drug Des Devel Ther. 2021 Aug 4;15:3391-3409. doi: 10.2147/DDDT.S295214. eCollection 2021.
Levosimendan is a distinctive inodilator combing calcium sensitization, phosphodiesterase inhibition and vasodilating properties through the opening of adenosine triphosphate-dependent potassium channels. It was first approved in Sweden in 2000 for the short-term treatment of acutely decompensated severe chronic heart failure when conventional therapy is not sufficient, and in cases where inotropic support is considered appropriate. After more than 20 years, clinical applications have considerably expanded across critical care and emergency medicine, and levosimendan is now under investigation in different cardiac settings (eg, septic shock, pulmonary hypertension) and for non-cardiac applications (eg, amyotrophic lateral sclerosis). This narrative review outlines key milestones in levosimendan history, by addressing regulatory issues, pharmacological peculiarities and clinical aspects (efficacy and safety) of a drug that did not receive great attention in the heart failure guidelines. A brief outlook to the ongoing clinical trials is also offered.
左西孟旦是一种独特的正性肌力药物,通过开放三磷酸腺苷(ATP)依赖性钾通道,具有增强心肌收缩力、抑制磷酸二酯酶和血管扩张的特性。该药于 2000 年在瑞典首次获批,用于常规疗法治疗效果不佳的急性失代偿性重度慢性心力衰竭的短期治疗,以及考虑使用正性肌力支持的情况下。20 多年来,该药在重症监护和急诊医学领域的临床应用得到了极大扩展,目前正在不同的心脏治疗环境(如感染性休克、肺动脉高压)和非心脏应用(如肌萎缩性侧索硬化症)中进行研究。本文通过讨论药物的监管问题、药理学特点和临床方面(疗效和安全性),概述了左西孟旦的重要历史里程碑,而该药在心力衰竭指南中并未受到广泛关注。本文还简要介绍了正在进行的临床试验。