Ebastine. a review of its pharmacological properties and clinical efficacy in the treatment of allergic disorders

Drugs. 1996 Feb;51(2):260-77. doi: 10.2165/00003495-199651020-00006.

Abstract

Ebastine is a long-acting nonsedating second generation histamine H1 receptor antagonist which binds preferentially to peripheral H1 receptors in vivo. It has shown antihistamine and antiallergic activity in healthy volunteers and patients with allergies, and protected against histamine-induced bronchoconstriction in patients with asthma. Significant symptom improvement is observed in patients with seasonal or perennial allergic rhinitis or chronic idiopathic urticaria following administration of ebastine 10 mg/day, or 20 mg/day in severe rhinitis. In clinical trials, the efficacy of ebastine 10 or 20 mg/day was generally similar to standard dosages of terfenadine, cetirizine, astemizole and loratadine in patients with seasonal allergic rhinitis, astemizole, terfenadine and ketotifen in patients with chronic idiopathic urticaria, and ketotifen, terfenadine, chlorpheniramine and mequitazine in patients with perennial allergic rhinitis. The most frequent adverse events reported during ebastine therapy are drowsiness, headache and dry mouth, the incidence being similar to that reported in placebo recipients. Serious adverse cardiac events, observed on rare occasions with some other histamine H1 receptor antagonists, have not been reported with ebastine, and there has been no evidence of QTc interval prolongation related to ebastine therapy. Thus, once-daily ebastine offers an effective and well-tolerated alternative to other second generation antihistamines in current use for the first-line treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria.

Publication types

  • Review

MeSH terms

  • Animals
  • Butyrophenones / administration & dosage
  • Butyrophenones / adverse effects
  • Butyrophenones / pharmacokinetics
  • Butyrophenones / pharmacology*
  • Butyrophenones / therapeutic use*
  • Histamine H1 Antagonists / administration & dosage
  • Histamine H1 Antagonists / adverse effects
  • Histamine H1 Antagonists / pharmacokinetics
  • Histamine H1 Antagonists / pharmacology*
  • Histamine H1 Antagonists / therapeutic use*
  • Humans
  • Hypersensitivity / drug therapy*
  • Piperidines / administration & dosage
  • Piperidines / adverse effects
  • Piperidines / pharmacokinetics
  • Piperidines / pharmacology*
  • Piperidines / therapeutic use*

Substances

  • Butyrophenones
  • Histamine H1 Antagonists
  • Piperidines
  • ebastine