Safety and efficacy of bilastine: a new H(1)-antihistamine for the treatment of allergic rhinoconjunctivitis and urticaria.

Abstract

INTRODUCTION:

New H(1)-antihistamines should be effective in relieving the symptoms of allergic disease, should have a rapid onset and long duration of action and should neither cause sedation nor interact with cytochrome P450. A review of bilastine was undertaken to determine whether this newer H(1)-antihistamine meets these requirements.

AREAS COVERED:

A Medline search was conducted to identify preclinical and clinical studies of bilastine. This was supplemented with additional articles or abstracts cited in reference lists and/or obtained from online sources and internal reports supplied by Faes Farma. Review of these data indicated that bilastine has high selectivity for H(1)-receptors, is rapidly and effectively absorbed, undergoes negligible metabolism and is a substrate for P-glycoprotein, which limits its passage across the blood-brain barrier. At the recommended dose of 20 mg, bilastine is non-sedative, does not enhance the effects of alcohol or CNS sedatives, does not impair actual driving tests, shows no cardiotoxicity and has a similar efficacy to other second-generation H(1)-antihistamines in the treatment of allergic rhinoconjunctivitis and urticaria.

EXPERT OPINION:

In view of its favorable pharmacological and clinical characteristics, bilastine is likely to have particular benefit in urticaria for which guidelines recommend increasing the dosage of H(1)-antihistamines up to fourfold if standard dosing is ineffective.

• Authors: Martin K Church
• Journal: Expert opinion on drug safety (Expert Opin Drug Saf) Vol. 10 Issue 5 Pg. 779-93 (Sep 2011) ISSN: 1744-764X [Electronic] England
• PMID: 21831011 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Benzimidazoles
• Histamine H1 Antagonists
• Piperidines
• bilastine

Topics

• Animals
• Benzimidazoles (adverse effects, therapeutic use)
• Clinical Trials, Phase I as Topic
• Histamine H1 Antagonists (adverse effects, therapeutic use)
• Humans
• Piperidines (adverse effects, therapeutic use)
• Randomized Controlled Trials as Topic
• Rhinitis, Allergic, Seasonal (drug therapy)
• Urticaria (drug therapy)