The pharmacology and use of H1-receptor-antagonist drugs

N Engl J Med. 1994 Jun 9;330(23):1663-70. doi: 10.1056/NEJM199406093302307.


The second-generation H1-antagonist drugs are supplanting their predecessors in the treatment of allergic rhinoconjunctivitis and chronic urticaria. Their use can be justified mainly on the basis of a more favorable risk-benefit ratio, because they are less toxic to the central nervous system. Future research into H1 antagonists should include additional dose-response studies in patients with allergic disorders, especially children and the elderly; objective studies of adverse effects; studies of topical mucosal application of H1 antagonists; and studies of H1-antagonist enantiomers and active metabolites. With the cloning of the gene encoding the H1 receptor and increased understanding of the precise structural requirements for H1-receptor activity, H1 antagonists with an even more favorable therapeutic index may be developed.

Publication types

  • Review

MeSH terms

  • Animals
  • Histamine H1 Antagonists* / adverse effects
  • Histamine H1 Antagonists* / pharmacology
  • Histamine H1 Antagonists* / therapeutic use
  • Humans
  • Hypersensitivity / drug therapy


  • Histamine H1 Antagonists