Albuterol enantiomers: Pre-clinical and clinical value?

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

Albuterol has been used in the acute treatment of asthma exacerbations for over 25 years. Its cost is low, and delivery can be tailored to allow dose-effect titration. Like other beta-2-adrenergic receptor agonists, it can exist as a racemate of two enantiomers, one active [(R)-albuterol], and one traditionally considered inert [(S)-albuterol]. Basic investigations in airway cells and models from animals and humans have shown that (R)-albuterol, in both racemic and single enantiomer formulations, produces changes consistent with both relaxation of airway smooth muscle cells, and the reduction of inflammation. In contrast, (S)-albuterol typically has produces effects opposite to those of (R)-albuterol, i.e., antagonistic to the beneficial desired effects. Coupled with the fact that (S)-albuterol can persist 12 times longer than (R)-albuterol within the human circulation, findings suggest that paradoxical effects, sometimes seen with chronic racemic albuterol use, are due to (S)-albuterol. A number of clinical studies, to date, have been generally consistent with these findings; however, overwhelming evidence for clinical superiority of the (R)-albuterol single enantiomer over that within racemic albuterol remains to be obtained.

Original languageEnglish (US)
Pages (from-to)1081-1092
Number of pages12
JournalFrontiers in Bioscience - Elite
Volume2 E
Issue number3
StatePublished - Jun 1 2010

Keywords

  • (R)-albuterol
  • (S)-Albuterol
  • Airway smooth muscle
  • Beta-2-receptor agonists
  • Bronchoconstriction
  • Racemic albuterol
  • Review

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Immunology and Microbiology(all)

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