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急性β受体阻滞剂的心脏安全性:内在拟交感活性优于β1选择性。

Cardiac safety of acute beta blockade: intrinsic sympathomimetic activity is superior to beta-1 selectivity.

作者信息

Heikkilä J, Nieminen M S

出版信息

Am Heart J. 1982 Aug;104(2 Pt 2):464-72. doi: 10.1016/0002-8703(82)90141-7.

Abstract

Regional myocardial function was assessed by multidirectional echocardiography from eight standardized segments around the left ventricle. Thirty-six subjects (healthy, severe angina pectoris, or acute myocardial infarction) were studied 15 minutes either after the beta 1-selective beta-blocking drug metoprolol had been administered in total doses of 2 and 10 mg intravenously or after pindolol, a beta blocker with intrinsic sympathomimetic activity (ISA), in total doses of 0.2 and 1.0 mg intravenously had been given. Metoprolol and pindolol reduced rate-pressure product (p less than 0.001 each), heart rate (p less than 0.001), and systolic blood pressure (p less than 0.05 to 0.001) in almost the same way. In patients with acute myocardial infarction, 0.2 mg pindolol improved ST segments by 33% and 2 mg metoprolol by 18%. Left ventricular diameter increased (p less than 0.001) and ejection fraction decreased (p less than 0.05) after metoprolol but not after pindolol. Pindolol did not reduce wall motion amplitudes of healthy myocardial segments, while metoprolol did ( p less than 0.01). The overall contractile function of the left ventricle is characterized by composite segmental amplitudes from both ischemic and healthy ventricular regions. In ischemic hearts this function remained unchanged after metoprolol but improved markedly after pindolol (p less than 0.005). Thus, while intravenous pindolol and metoprolol produced equal reductions in rate-pressure product, pindolol, a beta-adrenergic-blocking drug with intrinsic sympathomimetic activity, evoked less cardiac depression and thus provided a cardiac safety factor not afforded by the beta- 1-selective metoprolol.

摘要

通过多方向超声心动图从左心室周围的八个标准化节段评估局部心肌功能。对36名受试者(健康者、重度心绞痛患者或急性心肌梗死患者)进行了研究,这些受试者在静脉注射总剂量为2毫克和10毫克的β1选择性β受体阻滞剂美托洛尔后15分钟,或在静脉注射总剂量为0.2毫克和1.0毫克的具有内在拟交感活性(ISA)的β受体阻滞剂吲哚洛尔后15分钟接受检查。美托洛尔和吲哚洛尔降低心率血压乘积的方式几乎相同(二者p均小于0.001),降低心率(p小于0.001),降低收缩压(p小于0.05至0.001)。在急性心肌梗死患者中,0.2毫克吲哚洛尔使ST段改善33%,2毫克美托洛尔使ST段改善18%。美托洛尔治疗后左心室直径增加(p小于0.001),射血分数降低(p小于0.05),而吲哚洛尔治疗后则无此现象。吲哚洛尔不会降低健康心肌节段的壁运动幅度,而美托洛尔会降低(p小于0.01)。左心室的整体收缩功能以缺血和健康心室区域的复合节段幅度为特征。在缺血性心脏中,美托洛尔治疗后该功能保持不变,但吲哚洛尔治疗后明显改善(p小于0.005)。因此,虽然静脉注射吲哚洛尔和美托洛尔对心率血压乘积的降低程度相同,但具有内在拟交感活性的β肾上腺素能阻滞剂吲哚洛尔引起的心脏抑制较小,因此提供了β1选择性美托洛尔所没有的心脏安全因素。

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