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Review
. 2011 May;163(1):4-17.
doi: 10.1111/j.1476-5381.2011.01216.x.

β(2) -adrenoceptor agonists: current and future direction

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Review

β(2) -adrenoceptor agonists: current and future direction

Mario Cazzola et al. Br J Pharmacol. 2011 May.

Abstract

Despite the passionate debate over the use of β(2) -adrenoceptor agonists in the treatment of airway disorders, these agents are still central in the symptomatic management of asthma and COPD. A variety of β(2) -adrenoceptor agonists with long half-lives, also called ultra long-acting β(2) -adrenoceptor agonists (ultra-LABAs; indacaterol, olodaterol, vilanterol, carmoterol, LAS100977 and PF-610355) are currently under development with the hopes of achieving once-daily dosing. It is likely that the once-daily dosing of a bronchodilator would be a significant convenience and probably a compliance-enhancing advantage, leading to improved overall clinical outcomes. As combination therapy with an inhaled corticosteroid (ICS) and a LABA is important for treating patients suffering from asthma, and a combination with an inhaled long-acting antimuscarinic agent (LAMA) is important for treating COPD patients whose conditions are not sufficiently controlled by monotherapy with a β(2) -adrenoceptor agonist, some novel once-daily combinations of LABAs and ICSs or LAMAs are under development.

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Figures

Figure 1
Figure 1
Chemical structures of salmeterol, formoterol and emerging ultra-LABAs.

References

    1. Agarwal SK, Marshall GD., Jr Beta-adrenergic modulation of human type-1/type-2 cytokine balance. J Allergy Clin Immunol. 2000;105:91–98. - PubMed
    1. Aldridge RE, Hancox RJ, Taylor DR, Cowan JO, Winn MC, Frampton CM, et al. Effects of terbutaline and budesonide on sputum cells and bronchial hyperresponsiveness in asthma. Am J Respir Crit Care Med. 2000;161:1459–1464. - PubMed
    1. Aparici M, Gómez-Angelats M, Vilella D, Cortijo J, Morcillo EJ, Carcasona C, et al. The in vitro pharmacological profile of LAS100977 – a potent, selective and long-acting beta-2 receptor agonist [abstract] Am J Respir Crit Care Med. 2010;181:A5675.
    1. Appleton S, Poole P, Smith B, Veale A, Lasserson TJ, Chan MM. Long-acting β2-agonists for poorly reversible chronic obstructive pulmonary disease. Cochrane Database Syst Rev. 2006;3:CD001104. - PMC - PubMed
    1. Balint B, Watz H, Amos C, Owen R, Higgins M, Kramer B. Onset of action of indacaterol in patients with COPD: comparison with salbutamol and salmeterol-fluticasone. Int J Chron Obstruct Pulmon Dis. 2010;5:311–318. - PMC - PubMed

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