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Asthma, a heterogeneous disease, is characterized by chronic airway inflammation and hyperreactivity. β 2 -adrenoreceptor agonists (β 2 -agonists) remain pivotal for asthma management. Short-acting β 2 -agonists (SABAs) result in rapid symptomatic alleviation and bronchospasm prevention. Patients experience significant clinical benefits from therapy with long-acting β 2 -agonists (LABAs) with efficacy to bronchodilate, and prolonged lung function betterment. Recently discovered β 2 -agonists with longer half-lives offer once-daily dosing. The authors provide a thorough review of the pharmacokinetics, pharmacodynamics, efficacy, tolerability, classification, and safety of β 2 -agonists through an in-depth review of current literature using these databases: U.S. National Institutes of Health’s National Library of Medicine (NIH/NLM), PubMed Central, and NLM clinical trials. β 2 - agonists act primarily on airway smooth muscle cells and are quintessential for adequate asthma management. Given their pharmacodynamic and pharmacokinetic properties, SABAs are used as rescue medication. Notably, the current Global Initiative for Asthma (GINA) strategy document recommends using LABA/inhaled corticosteroid combinations both as a daily controller and as a rescue medication. Clinicians should assess this new treatment plan on a per-case basis, making sure to evaluate inhaler adherence and treat modifiable risk factors. The development of next-generation β 2 - agonists is an exciting research area that could significantly improve patients’ adherence to treatment regimens and, consequently, asthma control and quality of life.

State-of-the-art beta-adrenoreceptor agonists for the treatment of asthma