(R)-salbutamol in the treatment of asthma and chronic obstructive airways disease

Expert Opin Pharmacother. 2011 May;12(7):1133-41. doi: 10.1517/14656566.2011.571210. Epub 2011 Apr 1.


Introduction: Asthma and chronic obstructive pulmonary disease (COPD) are inflammatory disorders that have an increasing prevalence and associated morbidity and mortality. β(2)-adrenoceptor agonists (β(2)-agonists) act by stimulating the β(2)-adrenoceptor present on airway smooth muscle and other cells in the airway, resulting in bronchodilatation. β(2)-agonists are among the most commonly used drugs in the world and remain pivotal in the treatment of symptoms in patients with asthma and COPD. Salbutamol is a chiral drug with (R)- and (S)- isomers. Almost all β(2)-agonists that are used at present are racemic mixtures of (R)- and (S)-salbutamol.

Areas covered: In this review the authors show that (R)-salbutamol alone (generically known as levosalbutamol) provides beneficial β(2)-agonist effects at a cellular level and in experimental models of airways disease. In addition the authors demonstrate that (S)-salbutamol opposes the desirable effects of (R)-salbutamol and can actually cause features of asthma and COPD in vitro and in experimental asthma.

Expert opinion: Despite this strong body of experimental evidence, (R)-salbutamol has not shown consistent superiority over (S)- or racemic salbutamol in human asthma or COPD.

Publication types

  • Review

MeSH terms

  • Adrenergic beta-2 Receptor Agonists / adverse effects
  • Adrenergic beta-2 Receptor Agonists / chemistry
  • Adrenergic beta-2 Receptor Agonists / therapeutic use*
  • Albuterol / adverse effects
  • Albuterol / chemistry
  • Albuterol / therapeutic use*
  • Asthma / drug therapy*
  • Asthma / epidemiology
  • Bronchodilator Agents / adverse effects
  • Bronchodilator Agents / chemistry
  • Bronchodilator Agents / therapeutic use*
  • Humans
  • Pulmonary Disease, Chronic Obstructive / drug therapy*
  • Pulmonary Disease, Chronic Obstructive / epidemiology
  • Receptors, Adrenergic, beta-2 / metabolism
  • Respiratory System / drug effects
  • Stereoisomerism


  • Adrenergic beta-2 Receptor Agonists
  • Bronchodilator Agents
  • Receptors, Adrenergic, beta-2
  • Albuterol