Long-acting beta-adrenoceptor agonist

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Long-acting beta-adrenoceptor agonist
Drug class
Salmeterol—an example of long-acting β2 adrenoreceptor agonist
In Wikidata

Long-acting β adrenoceptor agonists (LABAs, more specifically, long-acting β2 adrenergic receptor agonists) are usually prescribed for moderate-to-severe persistent asthma patients or patients with chronic obstructive pulmonary disease (COPD). They are designed to reduce the need for shorter-acting β2 agonists such as salbutamol (albuterol), as they have a duration of action of approximately 12 hours in comparison with the 4-to-6-hour duration of salbutamol, making them candidates for sparing high doses of corticosteroids[citation needed] or treating nocturnal asthma and providing symptomatic improvement in patients with COPD. With the exception of formoterol, long-acting β2 agonists are not recommended for the treatment of acute asthma exacerbations because of their slower onset of action compared to salbutamol. Their long duration of action is due to the addition of a long, lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to continuously bind and unbind at β2 receptors in the smooth muscle in the lungs.

Medical uses

When combined with inhaled steroids, β adrenoceptor agonists can improve symptoms.[1][2] In children this benefit is uncertain and they may be potentially harmful.[2] They should not be used without an accompanying steroid due to an increased risk of severe symptoms, including exacerbation in both children and adults.[3] A 2018 meta-analysis was unable to determine whether an increase serious adverse events reported in the previous meta-analysis on regular salmeterol alone is abolished by the additional use of regular inhaled corticosteroid.[4] Large surveillance studies are ongoing to provide more information. There were no asthma-related deaths and few asthma-related serious adverse events when salmeterol is used with an inhaled steroid.[5][6] At least with formoterol, an increased risk appears to be present even when steroids are used[7] and this risk has not been ruled out for salmeterol.[8]


Some of the currently available long-acting β2 adrenoceptor agonists include:
International nonproprietary name (INN): Trade (brand) name


Several long-acting β adrenoreceptor agonists have a duration of action of 24 hours, allowing for once-daily dosing. They are considered to be ultra-long-acting β adrenoreceptor agonists (ultra-LABAs)[10] and are now approved.

Ultra-LABAs under development

Failed agents


A meta-analysis study from 2006 (pooled results of 19 trials, 33,826 participants) raised concerns that Salmeterol may increase the risk of death in asthmatics, and that the additional risk was not reduced with the adjunctive use of inhaled steroids (e.g., as with the combination product fluticasone/salmeterol).[22] The proposed mechanism is that while LABAs relieve asthma symptoms, they can also promote bronchial inflammation and sensitivity without warning.[23] On February 18, 2011, the FDA issued a safety alert for long-acting β agonists.[24] Following new clinical safety trials however, the FDA issued updated guidance on 20 December 2017, that there is no significant increased risk of serious asthma outcomes with LABAs when used together with inhaled corticosteroids.[25]


  1. ^ Higashi, AS; Zhu S; Stafford RS; Alexander GC (2011). "National trends in outpatient asthma treatment, 1997-2009". Journal of General Internal Medicine. 26 (12): 1465–70. doi:10.1007/s11606-011-1796-4. PMC 3235617. PMID 21769507.
  2. ^ a b Ducharme, Francine M; Ni Chroinin, Muireann; Greenstone, Ilana; Lasserson, Toby J (12 May 2010). "Addition of long-acting beta2-agonists to inhaled corticosteroids versus same dose inhaled corticosteroids for chronic asthma in adults and children". The Cochrane Database of Systematic Reviews (5): CD005535. doi:10.1002/14651858.CD005535.pub2. PMC 4169792. PMID 20464739.
  3. ^ Fanta CH (March 2009). "Asthma". New England Journal of Medicine. 360 (10): 1002–14. doi:10.1056/NEJMra0804579. PMID 19264689.
  4. ^ Cates, Christopher J.; Schmidt, Stefanie; Ferrer, Montse; Sayer, Ben; Waterson, Samuel (3 December 2018). "Inhaled steroids with and without regular salmeterol for asthma: serious adverse events". The Cochrane Database of Systematic Reviews. 2018 (12): CD006922. doi:10.1002/14651858.CD006922.pub4. ISSN 1469-493X. PMC 6524619. PMID 30521673.
  5. ^ Cates CJ, Cates MJ (2008). Cates, Christopher J (ed.). "Regular treatment with salmeterol for chronic asthma: serious adverse events". Cochrane Database Syst Rev (3): CD006363. doi:10.1002/14651858.CD006363.pub2. PMC 4015854. PMID 18646149.
  6. ^ "FDA Drug Safety Communication: New safety requirements for long-acting inhaled asthma medications called Long-Acting Beta-Agonists (LABAs)". U.S. Food and Drug Administration (FDA). Feb 2010. Archived from the original on 2017-11-02. Retrieved 2019-12-16. Based on the available information, FDA concludes there is an increased risk for severe exacerbation of asthma symptoms, leading to hospitalizations in pediatric and adult patients as well as death in some patients using LABAs for the treatment of asthma. The agency is requiring the REMS and class-labeling changes to improve the safe use of these products.
  7. ^ Cates, CJ; Cates, MJ (Apr 18, 2012). "Regular treatment with formoterol for chronic asthma: serious adverse events". Cochrane Database of Systematic Reviews. 4 (4): CD006923. doi:10.1002/14651858.CD006923.pub3. PMC 4017186. PMID 22513944.
  8. ^ Cates, CJ; Cates, MJ (Jul 16, 2008). "Regular treatment with salmeterol for chronic asthma: serious adverse events". Cochrane Database of Systematic Reviews (3): CD006363. doi:10.1002/14651858.CD006363.pub2. PMC 4015854. PMID 18646149.
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  13. ^ "New once-daily Striverdi (olodaterol) Respimat gains approval in first EU countries". Boehringer-Ingelheim. 18 October 2013.
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