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

• Published in: Current medical research and opinion Vol. 33; no. 1; p. 129
• Main Authors: Antonijoan, Rosa, Coimbra, Jimena, García-Gea, Consuelo, Puntes, Montserrat, Gich, Ignasi, Campo, Cristina, Valiente, Román, Labeaga, Luis
• Format: Journal Article
• Language: English
• Published: England 01.01.2017
• Subjects: Adult; Benzimidazoles - pharmacology; Cross-Over Studies; Cyproheptadine - analogs & derivatives; Cyproheptadine - pharmacology; Double-Blind Method; Female; Healthy Volunteers; Histamine - pharmacology; Histamine Antagonists - pharmacology; Humans; Injections, Intradermal; Loratadine - analogs & derivatives; Loratadine - pharmacology; Male; Piperidines - pharmacology; Skin - drug effects; Antihistamine; bilastine; histamine cutaneous challenge; desloratadine; rupatadine
• ISSN: 1473-4877
• DOI: 10.1080/03007995.2016.1240665

To compare the peripheral antihistaminic activity of bilastine, rupatadine and desloratadine in inhibiting the histamine-induced wheal and flare (W&F) response. 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 (cm ) were quantified using the Visitrak System. Itching sensation was evaluated using a 100 mm visual analog scale. EudraCT number: 2015-000790-13. The primary outcome measure was the percentage reduction in W&F areas after each active treatment compared with corresponding basal values. 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. 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.