Abstract

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.

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