Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy

Drugs. 1984 Jul;28(1):38-61. doi: 10.2165/00003495-198428010-00003.


Astemizole is an H1-histamine receptor antagonist with a long duration of action permitting once daily administration. Its efficacy in seasonal and perennial allergic rhinitis has been convincingly demonstrated, and several comparative studies suggest that astemizole is at least as effective as some other H1-histamine receptor antagonists. A few smaller studies have shown beneficial effects on the symptoms of allergic conjunctivitis and chronic urticaria (but not atopic dermatitis). While astemizole appears to share with other H1-histamine receptor antagonists a tendency to increase appetite and cause weight gain after prolonged use, it offers the important advantage of an absence of significant central nervous system depression or anticholinergic effects with usual doses. Thus, astemizole offers a worthwhile improvement in side effect profile over 'traditional' H1-histamine receptor antagonists, especially in patients bothered by the sedative effects of these drugs.

Publication types

  • Review

MeSH terms

  • Animals
  • Astemizole
  • Benzimidazoles / administration & dosage
  • Benzimidazoles / metabolism
  • Benzimidazoles / pharmacology*
  • Benzimidazoles / therapeutic use
  • Conjunctivitis / drug therapy
  • Dermatitis, Contact / drug therapy
  • Histamine H1 Antagonists / therapeutic use*
  • Histamine Release / drug effects
  • Humans
  • Hypersensitivity / drug therapy
  • Hypnotics and Sedatives
  • Intestinal Absorption
  • Mast Cells / drug effects
  • Nausea / drug therapy
  • Parasympatholytics
  • Psychomotor Performance / drug effects
  • Reaction Time / drug effects
  • Rhinitis, Allergic, Seasonal / drug therapy
  • Serotonin Antagonists
  • Tissue Distribution


  • Benzimidazoles
  • Histamine H1 Antagonists
  • Hypnotics and Sedatives
  • Parasympatholytics
  • Serotonin Antagonists
  • Astemizole