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左西孟旦:当前数据、临床应用及未来发展

Levosimendan: current data, clinical use and future development.

作者信息

Nieminen M S, Fruhwald S, Heunks L M A, Suominen P K, Gordon A C, Kivikko M, Pollesello P

机构信息

Heart and Lung Center, University of Helsinki Central Hospital, Helsinki, Finland.

Medizinische Universität, Graz, Austria.

出版信息

Heart Lung Vessel. 2013;5(4):227-45.

Abstract

Levosimendan is an inodilator indicated for the short-term treatment of acutely decompensated severe chronic heart failure, and in situations where conventional therapy is not considered adequate. The principal pharmacological effects of levosimendan are (a) increased cardiac contractility by calcium sensitisation of troponin C, (b) vasodilation, and (c) cardioprotection. These last two effects are related to the opening of sarcolemmal and mitochondrial potassium-ATP channels, respectively. Data from clinical trials indicate that levosimendan improves haemodynamics with no attendant significant increase in cardiac oxygen consumption and relieves symptoms of acute heart failure; these effects are not impaired or attenuated by the concomitant use of beta-blockers. Levosimendan also has favourable effects on neurohormone levels in heart failure patients. Levosimendan is generally well tolerated in acute heart failure patients: the most common adverse events encountered in this setting are hypotension, headache, atrial fibrillation, hypokalaemia and tachycardia. Levosimendan has also been studied in other therapeutic applications, particularly cardiac surgery - in which it has shown a range of beneficial haemodynamic and cardioprotective effects, and a favourable influence on clinical outcomes - and has been evaluated in repetitive dosing protocols in patients with advanced chronic heart failure. Levosimendan has shown preliminary positive effects in a range of conditions requiring inotropic support, including right ventricular failure, cardiogenic shock, septic shock, and Takotsubo cardiomyopathy.

摘要

左西孟旦是一种强心扩血管药物,适用于急性失代偿性严重慢性心力衰竭的短期治疗,以及在传统治疗被认为不充分的情况下使用。左西孟旦的主要药理作用包括:(a)通过肌钙蛋白C的钙增敏作用增强心肌收缩力;(b)血管舒张;(c)心脏保护作用。后两种作用分别与肌膜和线粒体ATP敏感性钾通道的开放有关。临床试验数据表明,左西孟旦可改善血流动力学,且不会伴随心肌氧耗量显著增加,并能缓解急性心力衰竭症状;这些作用不会因同时使用β受体阻滞剂而受损或减弱。左西孟旦对心力衰竭患者的神经激素水平也有有利影响。左西孟旦在急性心力衰竭患者中一般耐受性良好:在此情况下最常见的不良事件是低血压、头痛、心房颤动、低钾血症和心动过速。左西孟旦还在其他治疗应用中进行了研究,特别是心脏手术——在心脏手术中它已显示出一系列有益的血流动力学和心脏保护作用,以及对临床结局的有利影响——并且已在晚期慢性心力衰竭患者的重复给药方案中进行了评估。左西孟旦在一系列需要使用正性肌力药物支持的病症中已显示出初步的积极效果,包括右心室衰竭、心源性休克、感染性休克和应激性心肌病。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/921d/3868185/7e3ad657336c/hlv-05-227-g001.jpg

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