Tolerance & resistance to β₂-agonist bronchodilators

Paediatr Respir Rev. 2013 Sep;14(3):195-8. doi: 10.1016/j.prrv.2012.11.002. Epub 2013 Mar 16.


For the past half-century, β₂-agonists have been the mainstay of treatment of the bronchoconstriction associated with asthma. Although their usefulness in reversing acute bronchospasm remains undiminished, there is increasing evidence that chronic use may lead to development of tolerance and thus, potentially increasing morbidity and even mortality. In addition, genetic studies have shown that certain individuals carrying specific mutations may be prone to developing resistance to β₂-agonists regardless of the duration of treatment. This article reviews the current evidence regarding the underlying mechanisms that cause or contribute to the development of the resistance, as well as the strategies for the evaluation and management of patients who are at risk for or have developed tolerance to β₂-agonists.

Keywords: Resistance; Tolerance; β(2)-agonists.

Publication types

  • Review

MeSH terms

  • Adrenergic beta-2 Receptor Agonists / administration & dosage
  • Adrenergic beta-2 Receptor Agonists / pharmacology*
  • Adrenergic beta-2 Receptor Agonists / therapeutic use*
  • Albuterol / administration & dosage
  • Albuterol / therapeutic use
  • Asthma / drug therapy*
  • Asthma / physiopathology
  • Bronchoconstriction / drug effects*
  • Bronchoconstriction / genetics
  • Bronchodilator Agents / pharmacology
  • Bronchodilator Agents / therapeutic use
  • Drug Resistance / drug effects
  • Drug Resistance / physiology
  • Drug Tolerance / genetics
  • Drug Tolerance / physiology*
  • Humans
  • Polymorphism, Genetic
  • Receptors, Adrenergic, beta-2 / drug effects*
  • Receptors, Adrenergic, beta-2 / physiology*


  • Adrenergic beta-2 Receptor Agonists
  • Bronchodilator Agents
  • Receptors, Adrenergic, beta-2
  • Albuterol