Expert opinion on pharmacotherapy

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

PMID 21453221


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

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