Levalbuterol: pharmacologic properties and use in the treatment of pediatric and adult asthma

Ann Allergy Asthma Immunol. 2003 Jun;90(6):583-91; quiz 591-2, 659. doi: 10.1016/S1081-1206(10)61859-5.


Learning objectives: To review the rationale supporting the use of levalbuterol [(R)-albuterol] for the treatment of pediatric and adult asthma.

Data sources: Peer-reviewed articles, selected abstracts from studies presented at recent professional meetings, and the Xopenex [levalbuterol, (R)-albuterol; Sepracor, Marlborough, MA] Summary Basis of Approval and package insert.

Study selection: Institutional review board-approved clinical study protocols.

Results: Levalbuterol is a single isomer beta2-agonist that differs from racemic albuterol by elimination of (S)-albuterol. Levalbuterol is an effective bronchodilator whose primary mechanism of action is unimpeded by (S)-albuterol. Thus, when compared with racemic albuterol, clinically comparable bronchodilation can be achieved with doses that substantially lessen beta-mediated side effects. In chronic or acute treatment of asthma, this favorable therapeutic profile cannot apparently be duplicated by increasing or decreasing the dose of racemic albuterol or by the addition of anticholinergic agents such as ipratropium bromide.

Conclusions: Levalbuterol seems to provide efficacy and safety advantages in pediatric and adult patients suffering from asthma. Its use may afford a cost benefit as well. More clinical studies are required to extend these observations for use in the treatment of other pulmonary diseases in both adults and children and to determine levalbuterol's impact on long-term therapy of respiratory diseases.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adrenergic beta-Agonists / administration & dosage
  • Adrenergic beta-Agonists / pharmacology*
  • Adrenergic beta-Agonists / therapeutic use
  • Adult
  • Albuterol / administration & dosage
  • Albuterol / pharmacology*
  • Albuterol / therapeutic use
  • Asthma / drug therapy
  • Bronchodilator Agents / administration & dosage
  • Bronchodilator Agents / pharmacology*
  • Bronchodilator Agents / therapeutic use
  • Child
  • Dose-Response Relationship, Drug
  • Humans
  • United States


  • Adrenergic beta-Agonists
  • Bronchodilator Agents
  • Albuterol