Levalbuterol versus albuterol

Abstract

Albuterol has been used for more than 40 years to treat acute asthma exacerbations as a racemic mixture of isomers: the active form, (R)-albuterol, or levalbuterol, and (S)-albuterol, classically considered inert. The single-isomer formulation, levalbuterol, has been synthesized recently and used therapeutically when the racemate is deemed less desirable. Basic investigations indicate that racemic albuterol and levalbuterol can produce effects that favor asthma remediation, including corticosteroid amplification and reduction of inflammatory mediators; in contrast, (S)-albuterol produces opposite effects. With inhalation of racemic albuterol, circulating (S)-albuterol persists 12 times longer than levalbuterol, suggesting potential for paradoxical effects observed clinically. Although mainly consistent with basic findings, clinical studies suggest no overwhelming superiority of levalbuterol over racemic albuterol; however, levalbuterol's effects may be greatest in moderate to severe asthma patients, especially with racemic albuterol overuse. Recent adoption of the hydrofluoroalkane formulation has narrowed the cost gap between levalbuterol and racemic albuterol metered-dose inhalers, but it remains for the nebulized formulations. Thus, physician selection of these drugs has remained dependent on experience, pharmaceutical knowledge, and established prescribing habits combined with cost factors, formulary structures, and availability, such that racemic albuterol is still used significantly compared with levalbuterol to treat acute asthma exacerbations.