Benfield P, Sorkin E M
Drugs. 1987 Apr;33(4):392-412. doi: 10.2165/00003495-198733040-00004.
Esmolol is a relatively cardioselective beta-adrenoceptor antagonist. Since esmolol is rapidly metabolised by blood-borne esterases, it has a very short half-life (about 9 mins) and a short duration of action. In this respect esmolol is unique amongst currently available beta-adrenoceptor antagonists, and it is anticipated that it will be particularly useful in critical care situations where administration by continuous intravenous infusion should permit a level of control over beta-adrenoceptor antagonism that has previously been unattainable. In perioperative settings, esmolol attenuates tachycardia induced by a variety of surgical stimuli such as endotracheal intubation, sternotomy and aortic dissection, suggesting a clinical use of the drug to prevent potentially serious complications in surgical patients with cardiovascular disease. Additionally, clinical studies have shown that titrated dosages of esmolol achieved therapeutic response rates of 66 to 79% in patients with supraventricular tachyarrhythmias, which favourably compared with response rates achieved with propranolol. In most of these patients esmolol produced a reduction in ventricular rate which was well maintained during infusion but disappeared within 30 minutes following esmolol withdrawal. Preliminary studies involving small numbers of patients have reported that esmolol exerts significant antihypertensive effects in patients with postoperative hypertension, and beneficial effects in patients with myocardial ischaemia and infarction, but support for these results is required from additional large, well-controlled studies. Esmolol has been generally well tolerated, and although hypotension has occurred in up to 44% of patients it resolved during or soon after the infusion of esmolol. Thus, esmolol is the first titratable beta-adrenoceptor antagonist able to be rapidly 'switched on' and 'off', a property that is expected to offer a major contribution to safety in critical care patients requiring beta-adrenoceptor antagonism for short durations.
艾司洛尔是一种相对具有心脏选择性的β肾上腺素能受体拮抗剂。由于艾司洛尔可被血液中的酯酶迅速代谢，其半衰期非常短（约9分钟），作用持续时间也很短。在这方面，艾司洛尔在目前可用的β肾上腺素能受体拮抗剂中是独一无二的，预计它在重症监护情况下将特别有用，通过持续静脉输注给药应能实现对β肾上腺素能受体拮抗作用的一定程度的控制，而这在以前是无法实现的。在围手术期，艾司洛尔可减轻由各种手术刺激（如气管插管、胸骨切开术和主动脉夹层分离）引起的心动过速，这表明该药物在临床上可用于预防患有心血管疾病的手术患者发生潜在的严重并发症。此外，临床研究表明，在室上性快速心律失常患者中，滴定剂量的艾司洛尔达到了66%至79%的治疗有效率，与普萘洛尔的有效率相比更具优势。在大多数这些患者中，艾司洛尔使心室率降低，在输注期间能很好地维持，但在停用艾司洛尔后30分钟内消失。涉及少数患者的初步研究报告称，艾司洛尔对术后高血压患者有显著的降压作用，对心肌缺血和梗死患者有有益作用，但需要更多大型、严格对照的研究来支持这些结果。艾司洛尔总体耐受性良好，尽管高达44%的患者出现了低血压，但在输注艾司洛尔期间或之后很快就得到缓解。因此，艾司洛尔是第一种可滴定的β肾上腺素能受体拮抗剂，能够迅速“开启”和“关闭”，预计这一特性将对需要短期进行β肾上腺素能受体拮抗的重症监护患者的安全性做出重大贡献。
