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Drugs. 2013 Jun;73(9):959-77. doi: 10.1007/s40265-013-0077-4.
Landiolol (Onoact(®)) is an intravenously administered, ultra short-acting β1-blocker with an elimination half-life of 3-4 min and ≈8-fold greater cardioselectivity than esmolol in vitro. It is approved in Japan for the treatment of intraoperative and postoperative tachyarrhythmias, but in clinical practice is also used to prevent postoperative tachyarrhythmias, such as atrial fibrillation after coronary artery bypass grafting. Randomized controlled trials in patients undergoing open-heart surgery demonstrated that various dosages of landiolol (0.0005-0.04 mg/kg/min) [0.5-40 μg/kg/min] were more effective than diltiazem in converting postoperative atrial fibrillation to normal sinus rhythm during the first 8 h after surgery, and were more effective than placebo (or no landiolol) in preventing the development of atrial fibrillation during the first week after surgery (primary efficacy endpoints). In patients undergoing surgical procedures, landiolol 0.125 mg/kg/min for 1 min followed by 0.04 mg/kg/min for 10 min was superior to placebo in improving intraoperative tachycardia in randomized double-blind trials. The beneficial effects of landiolol in attenuating adverse haemodynamic or other changes that can occur during surgery or invasive procedures (e.g. percutaneous coronary intervention) have been demonstrated in a large number of randomized controlled trials. For example, several studies showed that landiolol attenuated the increase in heart rate associated with tracheal intubation, without adversely affecting blood pressure or other haemodynamic parameters. Landiolol was generally well tolerated in clinical trials, with a relatively low risk of hypotension and bradycardia, although routine monitoring of cardiac function during landiolol administration is important. In general, adverse events such as reduced blood pressure resolve quickly after discontinuation of landiolol. Thus, as an ultra short-acting β1-blocker with a rapid onset of action and readily titratable and rapidly reversible effects, landiolol represents an important agent for the management of intraoperative and postoperative tachyarrhythmias.
兰地洛尔(Onoact(®))是一种静脉内给予的、超短效β1 受体阻滞剂,其消除半衰期为 3-4 分钟,体外比艾司洛尔有约 8 倍的心脏选择性。它在日本被批准用于治疗术中及术后心动过速,但在临床实践中也用于预防术后心动过速,如冠状动脉旁路移植术后的心房颤动。在接受心脏直视手术的患者中进行的随机对照试验表明,兰地洛尔的各种剂量(0.0005-0.04mg/kg/min)[0.5-40μg/kg/min]比地尔硫卓更有效地将术后心房颤动在手术后 8 小时内转为窦性心律,并且比安慰剂(或无兰地洛尔)更有效地预防术后第一周发生心房颤动(主要疗效终点)。在接受手术的患者中,兰地洛尔 0.125mg/kg/min 持续 1 分钟,然后以 0.04mg/kg/min 持续 10 分钟,在随机双盲试验中优于安慰剂,改善术中心动过速。在大量的随机对照试验中已经证明,兰地洛尔在减轻手术或有创性操作过程中可能发生的不良血流动力学或其他变化方面具有有益作用,例如经皮冠状动脉介入治疗。例如,几项研究表明,兰地洛尔减轻了与气管插管相关的心率增加,而不影响血压或其他血流动力学参数。兰地洛尔在临床试验中通常具有良好的耐受性,低血压和心动过缓的风险相对较低,尽管在给予兰地洛尔期间监测心脏功能很重要。一般来说,在停止使用兰地洛尔后,血压降低等不良反应会迅速缓解。因此,作为一种起效迅速、作用可滴定且迅速逆转的超短效β1 受体阻滞剂,兰地洛尔是治疗术中及术后心动过速的重要药物。