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艾司洛尔对心肌缺血疗效的实验与临床观察

Experimental and clinical observations on the efficacy of esmolol in myocardial ischemia.

作者信息

Kloner R A, Kirshenbaum J, Lange R, Antman E M, Braunwald E

出版信息

Am J Cardiol. 1985 Oct 23;56(11):40F-48F. doi: 10.1016/0002-9149(85)90915-4.

Abstract

Beta blockers reduce myocardial oxygen demand and are therefore useful in ischemic states. They reduce angina pectoris and reduce the risk of death when administered long-term after acute myocardial infarction. Some studies suggest that when administered early after coronary occlusion they can reduce myocardial infarct size. Relative contraindications to beta blockers, such as a history of congestive heart failure, chronic obstructive lung disease, atrioventricular conduction defects and low blood pressure, limit their use. Conventional beta blockers have a relatively long duration of action and are either contraindicated or must be used with particular caution in patients with these contraindications. Esmolol is an ultrashort-acting beta blocker with a biologic half-life of 9 minutes. Therefore, such an agent may be useful in patients with ischemic heart disease in whom reducing heart rate would be beneficial but in whom there is concern that beta blockers might not be tolerated. Esmolol reduced myocardial infarct size in 2 experimental studies of coronary occlusion followed by reperfusion, and improved the recovery of the stunned myocardium when administered during experimental myocardial ischemia. Esmolol's brief duration of action may make it safer than conventional beta blockers for the management of patients with unstable angina or myocardial infarction.

摘要

β受体阻滞剂可降低心肌需氧量,因此对缺血状态有效。它们可减轻心绞痛,并在急性心肌梗死后长期使用时降低死亡风险。一些研究表明,在冠状动脉闭塞后早期使用,它们可减小心肌梗死面积。β受体阻滞剂的相对禁忌证,如充血性心力衰竭病史、慢性阻塞性肺疾病、房室传导缺陷和低血压,限制了它们的使用。传统的β受体阻滞剂作用持续时间相对较长,在有这些禁忌证的患者中要么禁忌使用,要么必须特别谨慎使用。艾司洛尔是一种超短效β受体阻滞剂,生物半衰期为9分钟。因此,这种药物可能对缺血性心脏病患者有用,在这类患者中降低心率有益,但担心β受体阻滞剂可能无法耐受。在两项冠状动脉闭塞后再灌注的实验研究中,艾司洛尔减小了心肌梗死面积,并在实验性心肌缺血期间使用时改善了顿抑心肌的恢复。艾司洛尔作用持续时间短暂,这可能使其在治疗不稳定型心绞痛或心肌梗死患者时比传统β受体阻滞剂更安全。

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