An Overview of the Pharmacokinetics and Pharmacodynamics of Landiolol (an Ultra-Short Acting β1 Selective Antagonist) in Atrial Fibrillation

Abstract

Landiolol is an ultra-short-acting, selective β1-adrenergic receptor blocker that was originally approved in Japan for the treatment of intraoperative tachyarrhythmias. It has gained attention for its use in the management of tachyarrhythmias and perioperative tachycardia, especially atrial fibrillation for both cardiac and non-cardiac surgeries. It can be the ideal agent for heart rate control due to its high β1-selectivity, potent negative chronotropic effect, a limited negative inotropic potential, and an ultrashort elimination half-life (around 4 min); moreover, it may have a potential therapeutic effects for sepsis and pediatric patients. Landiolol seems to be superior to other short-acting and selective beta-blockers such as esmolol. This review aims to provide a comprehensive overview of landiolol, a new ultra-short-acting β1 selective antagonist, including its pharmacology, clinical applications, efficacy, safety profile, and future directions in research and clinical data.

Keywords: arrhythmias; atrial fibrillation; beta-blockers; cardiac surgery; landiolol; perioperative tachyarrhythmias.

Figure 1

The mechanism of action for Landiolol. This image was created with Biorender.com (accessed on 23 March 2024). β–ADR: β adrenergic receptor; I_Na: sodium current; I_Ks: slow delayed rectifier potassium current; If: funny current; I_NaK: sodium–potassium pump current; cAMP: cyclic adenosine monophosphate; RyR2: ryanodine receptor 2; ATP: adenosine triphosphate; AC: adenylyl cyclase.