Safety and efficacy of bilastine: a new H₁-antihistamine for the treatment of allergic rhinoconjunctivitis and urticaria

Abstract

Introduction: New H₁-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 H₁-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 H₁-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 H₁-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 H₁-antihistamines up to fourfold if standard dosing is ineffective.

Keywords:

• allergic rhinoconjunctivitis
• bilastine
• H₁-antihistamines
• safety
• urticaria

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