Comparative efficacy of bilastine, desloratadine and rupatadine in the suppression of wheal and flare response induced by intradermal histamine in healthy volunteers

Abstract

Objective: To compare the peripheral antihistaminic activity of bilastine, rupatadine and desloratadine in inhibiting the histamine-induced wheal and flare (W&F) response.

Research design and methods: Twenty-four healthy volunteers aged 18–40 years participated in this crossover, randomized, double-blind, placebo-controlled clinical study. Subjects received single doses of bilastine 20 mg, desloratadine 5 mg, rupatadine 10 mg and placebo. W&F responses induced by intradermal injection of histamine 5 μg were evaluated before treatment (basal value) and at 0.5, 1, 2, 4, 6, 9, 12 and 24 hours after treatment. Fifteen minutes after histamine injection, W&F surface areas (cm²) were quantified using the Visitrak System. Itching sensation was evaluated using a 100 mm visual analog scale.

EudraCT number: 2015-000790-13.

Main outcome measures: The primary outcome measure was the percentage reduction in W&F areas after each active treatment compared with corresponding basal values.

Results: Bilastine induced the greatest inhibition in wheal area and was significantly superior to desloratadine and rupatadine from 1 to 12 hours (both p < .001). Rupatadine and desloratadine were better than placebo without differences between them. Maximum wheal inhibition occurred at 6 hours (bilastine 83%, desloratadine 38%, rupatadine 37%). Onset of action was 1 hour for bilastine and 4 hours for desloratadine and rupatadine. Bilastine was significantly superior to desloratadine and rupatadine for flare inhibition from 1–24 hours (both p < .001) with an onset of action at 30 minutes. Bilastine was significantly better than desloratadine (2–12 hours; at least p < .05) and rupatadine (2–9 hours; at least p < .01) for reducing itching sensation. Neither desloratadine nor rupatadine significantly reduced itching compared to placebo. All active treatments were well tolerated.

Conclusions: Bilastine 20 mg induced significantly greater inhibition of the W&F response compared with desloratadine 5 mg and rupatadine 10 mg throughout the 24 hour study period, and had the fastest onset of action. Only bilastine significantly reduced itching sensation versus placebo.

Keywords:

• Antihistamine
• bilastine
• desloratadine
• histamine cutaneous challenge
• rupatadine

Transparency

Declaration of funding

This study was funded by Faes Farma SA.

Declaration of financial/other relationships

C.C., L.L. and R.V. have disclosed that they are employees of Faes Farma SA. R.A., J.C., C.G.-G., M.P. and I.G. have disclosed that they have no significant relationships with or financial interests in any commercial companies related to this study or article. CMRO peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Acknowledgments

Editorial support was provided by Kerry Dechant of Content Ed Net (Madrid, Spain) and was funded by Faes Farma SA.