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Levalbuterol in the treatment of patients with asthma and chronic obstructive lung disease.
J Am Osteopath Assoc 2004; 104(7):288-93JA

Abstract

Effective asthma control requires long-term (anti-inflammatory) controller medications for patients with mild-persistent to severe-persistent disease, and quick-relief bronchodilator medication for all patients with asthma to control intermittent symptoms of cough, wheeze, and bronchoconstriction, as well as acute exacerbations. For patients with chronic obstructive pulmonary disease, quick-relief and long-acting bronchodilators are primarily used in the maintenance and treatment of associated symptoms, including shortness of breath. For many years, the most widely used bronchodilator has been racemic (R, S)-albuterol, a short-acting beta2-adrenergic agonist, commonly dispensed as an inhaled aerosol or solution. Until the introduction of levalbuterol inhalation solution (Xopenex) in 1999, all marketed forms of albuterol (including Ventolin and Proventil brands) were racemic mixtures composed of a 1:1 ratio of (R)- and (S)-stereoisomers. Administered as a proportionally equivalent nebulized dose, levalbuterol [(R)-albuterol] provides greater bronchodilation than racemic albuterol and, in the appropriate clinical setting, offers the possibility for improving clinical outcomes in patients with asthma and other obstructive airway diseases. Additionally, levalbuterol can be given at lower doses than racemic albuterol to provide comparable bronchodilation, with the potential for reduced beta-mediated adverse effects in adults and children. Only since the past decade has the technology to separate stereoisomers become available, and thus the biologic activities of the albuterol stereoisomers had not been established. Binding studies have demonstrated that (R)-albuterol binds to the beta2-adrenergic receptor with a high affinity, whereas (S)-albuterol binds with 100-fold less affinity than (R)-albuterol. Other evaluations have suggested that (R)-albuterol possesses the bronchodilatory, bronchoprotective, and ciliary-stimulatory properties of racemic albuterol, while (S)-albuterol does not contribute beneficially to the therapeutic effects of the racemate and was originally assumed to be inert. However, preclinical evaluations have shown that (S)-albuterol has effects that work in opposition to (R)-albuterol and may diminish the therapeutic effects of (R)-albuterol.

Authors+Show Affiliations

Temple University Hospital, Pulmonary and Critical Care, Philadelphia, PA 19140, USA. dalong@temple.edu

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

15293593

Citation

Dalonzo, Gilbert E.. "Levalbuterol in the Treatment of Patients With Asthma and Chronic Obstructive Lung Disease." The Journal of the American Osteopathic Association, vol. 104, no. 7, 2004, pp. 288-93.
Dalonzo GE. Levalbuterol in the treatment of patients with asthma and chronic obstructive lung disease. J Am Osteopath Assoc. 2004;104(7):288-93.
Dalonzo, G. E. (2004). Levalbuterol in the treatment of patients with asthma and chronic obstructive lung disease. The Journal of the American Osteopathic Association, 104(7), pp. 288-93.
Dalonzo GE. Levalbuterol in the Treatment of Patients With Asthma and Chronic Obstructive Lung Disease. J Am Osteopath Assoc. 2004;104(7):288-93. PubMed PMID: 15293593.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Levalbuterol in the treatment of patients with asthma and chronic obstructive lung disease. A1 - Dalonzo,Gilbert E,Jr PY - 2004/8/6/pubmed PY - 2004/9/3/medline PY - 2004/8/6/entrez SP - 288 EP - 93 JF - The Journal of the American Osteopathic Association JO - J Am Osteopath Assoc VL - 104 IS - 7 N2 - Effective asthma control requires long-term (anti-inflammatory) controller medications for patients with mild-persistent to severe-persistent disease, and quick-relief bronchodilator medication for all patients with asthma to control intermittent symptoms of cough, wheeze, and bronchoconstriction, as well as acute exacerbations. For patients with chronic obstructive pulmonary disease, quick-relief and long-acting bronchodilators are primarily used in the maintenance and treatment of associated symptoms, including shortness of breath. For many years, the most widely used bronchodilator has been racemic (R, S)-albuterol, a short-acting beta2-adrenergic agonist, commonly dispensed as an inhaled aerosol or solution. Until the introduction of levalbuterol inhalation solution (Xopenex) in 1999, all marketed forms of albuterol (including Ventolin and Proventil brands) were racemic mixtures composed of a 1:1 ratio of (R)- and (S)-stereoisomers. Administered as a proportionally equivalent nebulized dose, levalbuterol [(R)-albuterol] provides greater bronchodilation than racemic albuterol and, in the appropriate clinical setting, offers the possibility for improving clinical outcomes in patients with asthma and other obstructive airway diseases. Additionally, levalbuterol can be given at lower doses than racemic albuterol to provide comparable bronchodilation, with the potential for reduced beta-mediated adverse effects in adults and children. Only since the past decade has the technology to separate stereoisomers become available, and thus the biologic activities of the albuterol stereoisomers had not been established. Binding studies have demonstrated that (R)-albuterol binds to the beta2-adrenergic receptor with a high affinity, whereas (S)-albuterol binds with 100-fold less affinity than (R)-albuterol. Other evaluations have suggested that (R)-albuterol possesses the bronchodilatory, bronchoprotective, and ciliary-stimulatory properties of racemic albuterol, while (S)-albuterol does not contribute beneficially to the therapeutic effects of the racemate and was originally assumed to be inert. However, preclinical evaluations have shown that (S)-albuterol has effects that work in opposition to (R)-albuterol and may diminish the therapeutic effects of (R)-albuterol. SN - 0098-6151 UR - https://www.unboundmedicine.com/medline/citation/15293593/Levalbuterol_in_the_treatment_of_patients_with_asthma_and_chronic_obstructive_lung_disease_ L2 - http://jaoa.org/article.aspx?volume=104&page=288 DB - PRIME DP - Unbound Medicine ER -