Skip to main content
Log in

Evidence based review on levosalbutamol

  • Special Article
  • Published:
The Indian Journal of Pediatrics Aims and scope Submit manuscript

Abstract

Salbutamol, the most commonly used bronchodilator, is a chiral drug with R (levosalbutamol) and S — isomers (also known as enantiomer). The commonly used formulation is a racemic mixture that contains equal amounts of both R and S isomers. Levosalbutamol is the therapeutically active isomer and has all the β2 agonist activity. Until recently S-salbutamol was considered inert filler in the racemic mixture but animal as well as human studies have shown that S-salbutamol is not inert rather it may have some deleterious effects. Enantioselective metabolism of salbutamol leads to higher and sustained plasma levels of S-salbutamol with repeated dosing. There has been concern that chronic use of racemic salbutamol may lead to loss of effectiveness and clinical deterioration. Formulation of salbutamol containing only R-isomer (levosalbutamol) has been available in international market since last few years. Clinical trials in acute as well as chronic asthma in adults as well as children have shown that it has therapeutic advantage over racemic salbutamol and also is more cost effective. But, large multicenter trials are needed to prove its therapeutic superiority and cost-effectiveness in long term.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Clive P, Jhon M. Contrasting properties of Albuterol stereoisomers. J Allergy Clin Immuno 1999; 104: S31–41.

    Article  Google Scholar 

  2. Penn RB, Friele T, McCullough JR, Aberg G, Benovie JL. Comparision of R-, S-, RS-albuterol, interaction with human β2 adrenergic receptors. Clin Rev Allergy Immunol 1996; 14: 37–45.

    PubMed  CAS  Google Scholar 

  3. Canning B. Pharmacological properties of S-albuterol in human airway smooth muscle preparations. Am J Resp Crit Care Med 2002; 165: A770.

    Google Scholar 

  4. Van Essen-Zandvliet EE, Hughes MD et al. Effects of 22 months of treatment with inhaled salbutamol lung function, airway responsiveness, and symptom in children with asthma. Am Rev Resp Dis 1992; 146: 547–554.

    PubMed  Google Scholar 

  5. Waheda I, Wong CS, Wisniewski Afz et al. Asthma control during and after cessation of regular β2 agonist treatment. Am Rev Resp Dis 1993; 148: 707–712.

    Google Scholar 

  6. Taylor DR, Sears MR. Bronchodilators and bronchial hyperresponsiveness. Thorax 1994; 49(2): 190–191.

    PubMed  CAS  Google Scholar 

  7. Mazzoni L, Naef R, Chapman ID, Morley J. Hyperresponsiveness of the airways to histamine following exposure of guinea pigs to racemic mixtures and distomers of β2-selective sympathomimetics. Pulm Pharmacol 1994; 7: 367–376.

    Article  PubMed  CAS  Google Scholar 

  8. Keir S, Page C, Spina D. Bronchial hyper-responsiveness induced by chronic treatment with albuterol: role of sensory nerves. J Allergy Clin Immunol 2002; 110: 388–394.

    Article  PubMed  CAS  Google Scholar 

  9. Templeton AGB, Chapman ID, Chilvers E, Morley J, Handley DA. Effects of (S)-albuterol on isolated human bronchus. Pulm Pharmacol 1998; 11: 1–6.

    Article  CAS  Google Scholar 

  10. Mazzoni L, Naef R, Chapman ID, Morley J. Hyperresponsiveness of the airways to histamine following exposure of guinea pigs to racemic mixtures and distomers of β2-selective sympathomimetics. Pulm Pharmacol 1994; 7: 367–376.

    Article  PubMed  CAS  Google Scholar 

  11. Cockcroft DW, Swystun VA. Effect of single doses of S-salbutamol, R-salbutamol, racemic salbutamol, and placebo on the airway response to methacholine. Thorax 1997; 52: 845–848.

    Article  PubMed  CAS  Google Scholar 

  12. Ramsay CM, Cowan J, Flannery E, McLachlan C, Taylor DR. Bronchoprotective and bronchodilator effects of single doses of (S)-salbutamol, (R)-salbutamol and racemic salbutamol in patients with bronchial asthma. Eur J Clin Pharmacol 1999; 55: 353–359.

    Article  PubMed  CAS  Google Scholar 

  13. Chang MM, Zhao YH, Chen Y et al. S-albuterol but not other β2 agonist isomers, has stimulatory effects on mucin secretion and changes in gene expression on airway epithelium. Am J Resp Crit Care Med 2001; 161:A 144.

    Google Scholar 

  14. Perterson BT, Miller EJ, Effect of enatiomers of albuterol on lung epithelial permeability. Am J Resp Crit Care Med 2000; 161: A 416.

    Google Scholar 

  15. O’sullivan S, Cormican L, Faul JL, Ichinohe S, Johnston SL et al. Activated, cytotoxic CD8 + T lymphocytes contribute to the pathology of asthma death. Am J Resp Crit Care Med 2001; 164: 560–564.

    PubMed  CAS  Google Scholar 

  16. Volcheck GW, Gleich GJ, Kita H. Pro-and anti-inflammatory effects of β2 adrenergic agonists on eosinophil response to IL-5. J Allergy Clin Immunolo 1998; 111: S35.

    Google Scholar 

  17. Cho SH, Haartleroad JY, Oh CK. S-albuterol increases the production of histamine and IL-4 in mast cells. Int Arch Allergy Imunolo 2001; 124: 478–484.

    Article  CAS  Google Scholar 

  18. Friere M, Pergolizzi R, Millon C, Dominguez PJ. Cytokine, chemokine, and nitric oxide release in stimulated small airway epithelial cells treated with β2 agonist enantiomers of salbutamol. J Allergy Clin Immunolo 2000; 105: S 292–293.

    Article  Google Scholar 

  19. Kwong CC, Chung QN, Choi SS et al. Effects of isomers of albuterol, R-albuterol, and S-albuterol, on human granulocytic function. J Invest Med 2002; 50: 72 A.

    Google Scholar 

  20. Walle T, Walle UK, Thornburg KR, Schey KL. Stereoselective sulfation of albuterol in humans. Drug Meabo Dispos 1993; 21: 76–80.

    CAS  Google Scholar 

  21. Boulton DW, Fawcett JP. Enantioselective disposition of salbutamol in man following oral and inhaled administration. J Clin Pharmacol 1996; 41: 35–40.

    Article  CAS  Google Scholar 

  22. Schmekel B, Rydberg I, Norlandar B, Sjosward KN. Stereoselective pharmacokinetics of S-salbutamol after administration of the racemate in healthy volunteers. Eur Respir J 1999; 13: 1230–1235.

    PubMed  CAS  Google Scholar 

  23. Maier G, Henry A, Baumbgartner R et al. The effects of (S)-albuterol, is not through the alteration of the pharmacokinetics of (R)-albuterol: a population PK analysis. J Allergy Clin Immunol 2002; 109: S 237–239.

    Article  Google Scholar 

  24. Nelson HS, Bensch G, Pleskow WW, DiSantostefano R, DeGraw S, Reasner DS, Rollins TE, Rubin PD. Improved bronchodilation with levalbuterol compared with racemic albuterol in patients with asthma. J Allergy Clin Immunol 1998; 102: 943–952.

    Article  PubMed  CAS  Google Scholar 

  25. Gawchik SM, Saccar CL, Noonan M, Reasner DS, DeGraw SS. The safety and efficacy of nebulized levalbuterol compared with racemic albuterol and placebo in the treatment of asthma in pediatric patients. J Allergy Clin Immunol 1999; 103(4): 615–621.

    Article  PubMed  CAS  Google Scholar 

  26. Milgrom H, Skoner DP, Bensch G, Kim KT, Claus R, Baumgartner RA for the Levalbuterol Pediatric Study Group. Low-dose levalbuterol in children with asthma: safety and efficacy in comparison with placebo and racemic albuterol. J Allergy Clin Immunol 2001; 108: 938–945.

    Article  PubMed  CAS  Google Scholar 

  27. Skoner DP, Greos LS, Kim KT, Roach JM, Parsey M, Baumgartner RA. Evaluation of the safety and efficacy of levalbuterol in 2-5-year-old patients with asthma. Pediatr Pulmonol 2005; 40: 477–486.

    Article  PubMed  Google Scholar 

  28. Lotvall J, Palmqvist M, Arvidsson P, Maloney A, Ventresca GP, Ward J. The therapeutic ratio of R-albuterol is comparable with that of RS-albuterol in asthmatic patients. J Allergy Clin Immunol 2001; 108: 726–731.

    Article  PubMed  CAS  Google Scholar 

  29. Handley DA, Tinkelman D, Noonan M, Rollins TE, Snider ME, Caron J. Dose-response evaluation of levalbuterol versus racemic albuterol in patients with asthma. J Asthma 2000; 37: 319–327.

    PubMed  CAS  Google Scholar 

  30. Carl JC, Myers TR, Kirchner HL, Kercsmar CM. Comparison of racemic albuterol and levalbuterol for treatment of acute asthma. J Pediatr 2003; 143: 731–736.

    Article  PubMed  CAS  Google Scholar 

  31. Ralston ME, Euwema MS, Knecht KR, Ziolkowski TJ, Coakley TA, Cline SM. Comparison of levalbuterol and racemic albuterol combined with ipratropium bromide in acute pediatric asthma: a randomized controlled trial. J Emerg Med 2005; 29: 29–35.

    Article  PubMed  Google Scholar 

  32. Haider D. Levalbuterol affords superior health and cost benefit over racemic albuterol in the emergency department. Resp Care 2001; 46: 1081.

    Google Scholar 

  33. Truitt T, Witko J, Halpern M. Levalbuterol compared to racemic albuterol: efficacy and outcomes in patients hospitalized with COPD or asthma. Chest 2003; 123: 128–135.

    Article  PubMed  Google Scholar 

  34. Nowak RM, Emerman CL, Schaefer K, Disantostefano RL, Vaickus L, Roach JM. Levalbuterol compared with racemic albuterol in the treatment of acute asthma: results of a pilot study. Am J Emerg Med 2004; 22: 29–36.

    Article  PubMed  Google Scholar 

  35. Berger We, Ames DE, Harrison D. A patient satisfaction survey comparing Levalbuterol with racemic salbutamol in children. Allergy Asthma Proc 2004; 25: 437–444.

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Mukesh Kumar Gupta.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Gupta, M.K., Singh, M. Evidence based review on levosalbutamol. Indian J Pediatr 74, 161–167 (2007). https://doi.org/10.1007/s12098-007-0010-5

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s12098-007-0010-5

Key words

Navigation