心率降低由特定和选择性与ivabradine我当前抑制(f):一个新的心血管疾病治疗的视角。

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DiFrancesco D, Camm农协

心率降低由特定和选择性与ivabradine我当前抑制(f):一个新的心血管疾病治疗的视角。

药。2004;64 (16):1757 - 65。

PubMed ID

15301560 (在PubMed

]

文摘

静息心率与心血管和全因死亡率有关,和死亡率的好处似乎某些心血管药物相关部分他们的心rate-lowering效果。因为很难单独的心率降低的好处从其他行动与现有药物,“纯粹”的心rate-lowering药物将是极大的兴趣在建立心率降低本身的利益。心率是由自发电窦房结起搏点活动。心脏起搏器细胞自发生成缓慢舒张两极化的驱动膜电压从hyperpolarised水平转向发起后续动作电位阈值水平,产生有节奏的动作电位,通过心脏和传播引发心肌收缩。我(f)电流的离子电流确定舒张压两极化的斜率,进而控制心跳率。Ivabradine是第一个特定的心脏rate-lowering代理完成稳定心绞痛的临床开发。Ivabradine特别块心脏起搏器电池f-channels通过输入和绑定的网站频道孔隙从细胞内。Ivabradine是我选择性(f)电流和产生显著的抑制电流和心率降低浓度,不影响其他心脏离子电流。这个活动转化为特定的心率降低,从而降低心肌氧需同时改善氧气供应,以延长舒张,从而允许增加冠状动脉流量和心肌灌注。Ivabradine降低心率没有任何负性肌力或lusitropic效应,从而保护心室收缩性。 Ivabradine was shown to reduce resting heart rate without modifying any major electrophysiological parameters not related to heart rate. In patients with left ventricular dysfunction, ivabradine reduced resting heart rate without altering myocardial contractility. Thus, pure heart rate lowering can be achieved in the clinic as a result of specific and selective I(f) current inhibition. Two randomised clinical studies have shown that ivabradine is an effective anti-ischaemic agent that reduces heart rate and improves exercise capacity in patients with stable angina. Ivabradine was shown to be superior to placebo in improving exercise tolerance test (ETT) criteria (n = 360) and, in a 4-month, double-blind, controlled study (n = 939), ivabradine 5 and 7.5mg twice daily were shown to be at least as effective as atenolol 50 and 100mg once daily, respectively, in improving total exercise duration and other ETT criteria, and reducing the number of angina attacks. Experimental data indicate a potential role of pure heart rate lowering in other cardiovascular conditions, such as heart failure.

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药物

Ivabradine