Kirshenbaum J M, Kloner R A, Antman E M, Braunwald E
Circulation. 1985 Oct;72(4):873-80. doi: 10.1161/01.cir.72.4.873.
Esmolol is a new ultra short-acting (half-life [t1/2] beta 9 min) beta 1-adrenergic-receptor antagonist reported to have no intrinsic sympathomimetic activity. The safety and efficacy of esmolol in lowering the ventricular rate and rate-pressure product in patients with acute myocardial infarction (n = 5), postmyocardial infarction angina (n = 10), or acute unstable angina (n = 4), and without cardiogenic shock were studied. After a 30 min observation period, esmolol was titrated to a maximum dose of 300 micrograms/kg/min and infused for up to 420 min. The ventricular rate fell from 92 +/- 11 (mean +/- SD) to 77 +/- 13 beats/min (p less than .01) and the systolic arterial pressure decreased from 120 +/- 13 to 97 +/- 11 mm Hg (p less than .01) during the initial 30 min titration period. There was no significant change during the maintenance phase, and both the ventricular rate and arterial pressure returned rapidly toward baseline values within 30 min of termination of the infusion. The cardiac index fell from 2.8 +/- 0.6 to 2.2 +/- 0.6 liters/min/m2 (p less than .01) during the same period, and also returned to the baseline level 30 min after termination of the infusion. There was no significant change in the pulmonary capillary wedge pressure, respiratory rate, or PR interval. Five patients required termination of infusion because of hypotension and all recovered uneventfully within 30 min of stopping the esmolol. One patient required a brief infusion of dopamine to restore hemodynamic stability.(ABSTRACT TRUNCATED AT 250 WORDS)
艾司洛尔是一种新型超短效(半衰期[t1/2]为9分钟)的β1肾上腺素能受体拮抗剂,据报道无内在拟交感活性。本研究了艾司洛尔在急性心肌梗死患者(n = 5)、心肌梗死后心绞痛患者(n = 10)或急性不稳定型心绞痛患者(n = 4)且无心源性休克时降低心室率和心率 - 血压乘积的安全性和有效性。在30分钟观察期后,将艾司洛尔滴定至最大剂量300微克/千克/分钟,并输注长达420分钟。在最初30分钟的滴定期内,心室率从92±11(平均值±标准差)降至77±13次/分钟(p <.01),收缩动脉压从120±13降至97±11毫米汞柱(p <.01)。维持期无显著变化,输注终止后30分钟内心室率和动脉压均迅速恢复至基线值。同期心脏指数从2.8±0.6降至2.2±0.6升/分钟/平方米(p <.01),输注终止后30分钟也恢复至基线水平。肺毛细血管楔压、呼吸频率或PR间期无显著变化。5例患者因低血压需要终止输注,且在停用艾司洛尔后30分钟内均顺利恢复。1例患者需要短暂输注多巴胺以恢复血流动力学稳定性。(摘要截短至250字)