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伊伐布雷定:If 电流抑制在稳定型心绞痛及其他心血管疾病治疗中的应用

Ivabradine: I(f) inhibition in the management of stable angina pectoris and other cardiovascular diseases.

作者信息

Tardif Jean-Claude

机构信息

Montreal Heart Institute, University of Montreal, Montreal, QC, Canada.

出版信息

Drugs Today (Barc). 2008 Mar;44(3):171-81. doi: 10.1358/dot.2008.44.1193864.

Abstract

Elevated heart rate plays a major role in coronary artery disease, not only as a trigger of most ischemic episodes but also as a significant predictor of cardiovascular morbidity and mortality. Heart rate is an important target in the management of stable angina pectoris. Against this background, a new class of antianginal drugs has recently become available: the selective and specific I(f) inhibitors. The mode of action of this novel class involves selective and specific inhibition of the major pacemaker current in the sinoatrial node, the mixed sodium/potassium current (I(f)), which results in pure heart rate reduction. The first member of this class available for clinical use is ivabradine (available under the brandnames of Procoralan, Coralan, Corlentor, Coraxan, Servier, France). Building on solid preclinical studies, ivabradine was shown to have anti-ischemic and antianginal efficacy in patients with stable angina pectoris in clinical trials versus placebo, beta-blockers and calcium channel blockers. Ongoing studies will determine the potential of pure heart rate reduction with ivabradine to improve morbidity and mortality.

摘要

心率升高在冠状动脉疾病中起主要作用,不仅是大多数缺血发作的触发因素,也是心血管疾病发病率和死亡率的重要预测指标。心率是稳定型心绞痛治疗的重要靶点。在此背景下,一类新型抗心绞痛药物最近问世:选择性和特异性I(f)抑制剂。这类新型药物的作用方式包括选择性和特异性抑制窦房结中的主要起搏电流,即混合钠/钾电流(I(f)),从而导致单纯心率降低。这类药物中首个可用于临床的是伊伐布雷定(以法国施维雅公司的商品名Procoralan、Coralan、Corlentor、Coraxan销售)。基于扎实的临床前研究,在临床试验中,与安慰剂、β受体阻滞剂和钙通道阻滞剂相比,伊伐布雷定在稳定型心绞痛患者中显示出抗缺血和抗心绞痛疗效。正在进行的研究将确定伊伐布雷定单纯降低心率改善发病率和死亡率的潜力。

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