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伊伐布雷定对If电流的选择性和特异性抑制:心血管疾病治疗的新视角。

Selective and specific I(f) inhibition with ivabradine: new perspectives for the treatment of cardiovascular disease.

作者信息

Ferrari Roberto, Ceconi Claudio

机构信息

Department of Cardiology, University of Ferrara, Salvatore Maugeri Foundation, IRCCS, Lumezzane, Italy.

出版信息

Expert Rev Cardiovasc Ther. 2011 Aug;9(8):959-73. doi: 10.1586/erc.11.99.

Abstract

Heart rate is a major determinant of myocardial oxygen demand and supply, and increased heart rate adversely affects the pathophysiology of myocardial ischemia. High resting heart rate is a risk factor in cardiovascular disease. The development of the heart rate-lowering agent ivabradine showed that heart rate was also an important treatment target, notably in coronary artery disease and heart failure. Indeed, heart rate reduction with ivabradine, a selective and specific I(f) inhibitor, reduces myocardial oxygen demand, increases diastolic perfusion time and improves energetics in ischemic myocardium. Ivabradine protects the myocardium during ischemia, improves left ventricular function in heart failure and reduces remodeling following myocardial infarction. It improves prognosis in patients with coronary artery disease, left ventricular dysfunction and heart rate ≥70 beats per minute, as well as in patients with heart failure and left ventricular dysfunction. Ivabradine is safe, well tolerated and can be used in combination with the main drugs for cardiovascular disease.

摘要

心率是心肌氧需求和供应的主要决定因素,心率增加会对心肌缺血的病理生理学产生不利影响。静息心率升高是心血管疾病的一个危险因素。降低心率药物伊伐布雷定的研发表明,心率也是一个重要的治疗靶点,特别是在冠状动脉疾病和心力衰竭方面。事实上,使用选择性和特异性I(f)抑制剂伊伐布雷定降低心率可减少心肌氧需求,增加舒张期灌注时间,并改善缺血心肌的能量代谢。伊伐布雷定在缺血期间保护心肌,改善心力衰竭患者的左心室功能,并减少心肌梗死后的重塑。它改善了冠状动脉疾病、左心室功能障碍且心率≥70次/分钟的患者以及心力衰竭和左心室功能障碍患者的预后。伊伐布雷定安全、耐受性良好,可与心血管疾病的主要药物联合使用。

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