Ellenbogen K A, McCarthy E A, Pritchett E L
Clin Pharmacol Ther. 1987 Apr;41(4):455-9. doi: 10.1038/clpt.1987.56.
Esmolol is an investigational ultra-short-acting beta-adrenergic blocker that has potential application in many clinical cardiology settings. The purpose of this study was to investigate the effect of a bolus dose of esmolol on heart rate, blood pressure, and PR interval in healthy, exercising male subjects. We gave a single esmolol bolus over 30 seconds to 13 men who exercised to a predetermined target heart rate. Each subject performed the exercise protocol twice, receiving a different dose between 10 and 300 mg each time. An additional eight subjects received two esmolol boluses 5 minutes apart while performing the same exercise protocol. Esmolol doses of 180 mg or greater caused a 13% to 18% decrease in heart rate, an 11% to 18% decrease in blood pressure, and a 13% to 22% prolongation of the PR interval. The median time to peak esmolol effect was 1 minute for heart rate, 2 minutes for blood pressure, and 4 minutes for PR interval. The median time required to recover 50%, 75%, and 90% of the decrement in heart rate was 8, 10, and 13 minutes, respectively. The rapid onset and disappearance of esmolol effects may make it an appealing drug in acute care settings.
艾司洛尔是一种正在研究的超短效β-肾上腺素能阻滞剂，在许多临床心脏病学场景中具有潜在应用价值。本研究的目的是调查静脉推注艾司洛尔对健康、正在运动的男性受试者的心率、血压和PR间期的影响。我们在30秒内给13名运动至预定目标心率的男性单次静脉推注艾司洛尔。每名受试者进行两次运动方案，每次接受10至300毫克之间的不同剂量。另外8名受试者在进行相同运动方案时，间隔5分钟接受两次艾司洛尔静脉推注。180毫克及以上剂量的艾司洛尔可使心率降低13%至18%，血压降低11%至18%，PR间期延长13%至22%。艾司洛尔达到峰值效应的中位时间，心率为1分钟，血压为2分钟，PR间期为4分钟。心率下降恢复50%、75%和90%所需的中位时间分别为8分钟、10分钟和13分钟。艾司洛尔效应的快速起效和消失可能使其成为急性护理场景中一种有吸引力的药物。
