AbstractRacemic albuterol, a commonly used bronchodilator, is an exact 50:50 mixture of two enantiomers, R‐ and S‐albuterol. Concern regarding increased mortality associated with the use of this beta‐2 (β2) agonist triggered the study of both of these enantiomers separately.In vitro studies suggest that the two enantiomers have different binding affinities for β‐adrenoreceptors, may exert opposing effects on inflammation, demonstrate different effects on mucocilary transport, and display differing pharmacokinetics. Clinical studies comparing both enantiomers are few, of short duration, and often in small patient populations, and their results vary. R‐albuterol has greater bronchodilatory effects than the racemate and may have anti‐inflammatory properties. S‐albuterol has markedly less affinity for the β‐adrenoreceptor. It was found to cause bronchoconstriction in animal models, but neither bronchoconstrictive nor pro‐inflammatory effects have been conclusively demonstrated in human studies.The data available at present, while suggestive, are insufficient to conclusively recommend R‐albuterol over the racemate. Further basic research and investigations in humans comparing both enantiomers at increasing doses over longer time periods are required to clarify the precise roles of R‐ and S‐albuterol. Pediatr Pulmonol. 2002; 33:151–157. © 2002 Wiley‐Liss, Inc.