Role of histamine in the pathophysiology of asthma: immunomodulatory and anti-inflammatory activities of H1-receptor antagonists

Am J Med. 2002 Dec 16;113 Suppl 9A:2S-7S. doi: 10.1016/s0002-9343(02)01431-6.


Cumulative clinical and laboratory evidence on histamine and its actions suggests that it has a pathophysiologic role in asthma. These findings have renewed interest in the potential therapeutic role of H1 antihistamines in this disease. A murine model of allergen-induced airway inflammation and methacholine-induced airway hyperresponsiveness has been used to clarify mechanisms of airway function, to identify potential therapeutic targets, and to investigate the effects of the H1-receptor antagonist fexofenadine. Findings suggest that there may be a role for second-generation antihistamines in treating asthma, with patient selection as well as dosing both important therapeutic considerations. Because high-dose therapy may be required to achieve a clinical response, agents with the widest therapeutic window and the lowest potential for sedation would offer the greatest therapeutic potential.

Publication types

  • Review

MeSH terms

  • Adjuvants, Immunologic / pharmacology
  • Adjuvants, Immunologic / therapeutic use*
  • Anti-Inflammatory Agents / immunology*
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Asthma / immunology*
  • Asthma / physiopathology*
  • Histamine / immunology*
  • Histamine / physiology*
  • Histamine H1 Antagonists / immunology*
  • Histamine H1 Antagonists / pharmacology
  • Histamine H1 Antagonists / therapeutic use*
  • Humans


  • Adjuvants, Immunologic
  • Anti-Inflammatory Agents
  • Histamine H1 Antagonists
  • Histamine