Sintetos A L, Hulse J, Pritchett E L
Clin Pharmacol Ther. 1987 Jan;41(1):112-7. doi: 10.1038/clpt.1987.19.
Esmolol is a new ultra-short-acting beta-adrenergic receptor blocking agent that may be useful in the treatment of patients with heart disease. We gave esmolol as an intravenous bolus injection (over 30 seconds) to 12 healthy men in a dose-ranging study; each subject received two doses. Our dosing schedule began with 30 mg in the first subject and ended with 100 mg and 150 mg in the final four subjects. We measured blood esmolol concentration, PR interval, QRS duration, QTc interval, cardiac cycle, systolic blood pressure, and diastolic blood pressure. Esmolol doses of 150 mg produced blood esmolol concentrations of 0.868 to 1.47 micrograms/ml. The peak PR interval recorded after esmolol was significantly longer than the control PR interval in four subjects who received 100 and 150 mg doses (192 +/- 7.9 msec vs. 177 +/- 10.6 msec; P = 0.00002). Peak prolongation of the PR interval was recorded 6 to 10 minutes after the bolus, at which time blood esmolol concentrations were negligible. Esmolol did not consistently affect any other pharmacodynamic variable. Giving esmolol as an intravenous bolus injection may be a simple alternative to loading and maintenance infusion in some clinical settings.
艾司洛尔是一种新型超短效β-肾上腺素能受体阻滞剂，可能对心脏病患者的治疗有用。在一项剂量范围研究中，我们对12名健康男性进行静脉推注（30秒内）给予艾司洛尔；每名受试者接受两剂。我们的给药方案从第一名受试者的30毫克开始，最后四名受试者的剂量为100毫克和150毫克。我们测量了血液中艾司洛尔浓度、PR间期、QRS时限、QTc间期、心动周期、收缩压和舒张压。150毫克的艾司洛尔剂量产生的血液艾司洛尔浓度为0.868至1.47微克/毫升。在接受100毫克和150毫克剂量的四名受试者中，艾司洛尔给药后记录的峰值PR间期明显长于对照PR间期（192±7.9毫秒对177±10.6毫秒；P = 0.00002）。推注后6至10分钟记录到PR间期的峰值延长，此时血液中艾司洛尔浓度可忽略不计。艾司洛尔并未持续影响任何其他药效学变量。在某些临床环境中，静脉推注艾司洛尔可能是负荷和维持输注的一种简单替代方法。
