Astemizole: a long-acting, nonsedating antihistamine

Drug Intell Clin Pharm. 1987 Dec;21(12):947-53. doi: 10.1177/106002808702101202.


Astemizole is a long-acting, highly selective histamine1-receptor antagonist with minimal central and anticholinergic effects. Comparison studies have shown astemizole to be equal or superior to currently available antihistamines, beclomethasone nasal spray, and cromolyn sodium in relieving allergic symptoms of seasonal and perennial allergic rhinitis. Other uses include treatment of allergic conjunctivitis and chronic urticaria. Astemizole is not as effective for treatment of acute allergic symptoms because of its delayed onset of action. Astemizole and its active metabolite, desmethylastemizole, have long elimination half-lives permitting once-daily dosing. The incidence of sedation is lower than with conventional antihistamines, but increased appetite and weight gain do occur. Astemizole should be useful for both maintenance and prophylactic therapy in patients with chronic allergic conditions who cannot tolerate the sedative or anticholinergic effects of conventional antihistamines.

Publication types

  • Review

MeSH terms

  • Animals
  • Astemizole
  • Benzimidazoles* / adverse effects
  • Benzimidazoles* / pharmacokinetics
  • Benzimidazoles* / therapeutic use
  • Benzimidazoles* / toxicity
  • Histamine H1 Antagonists* / adverse effects
  • Histamine H1 Antagonists* / pharmacokinetics
  • Histamine H1 Antagonists* / therapeutic use
  • Histamine H1 Antagonists* / toxicity
  • Humans
  • Rhinitis / drug therapy
  • Urticaria / drug therapy


  • Benzimidazoles
  • Histamine H1 Antagonists
  • Astemizole