title: Comparative efficacy of bilastine, desloratadine and rupatadine in the suppression of wheal and flare response induced by intradermal histamine in healthy volunteers.
abstract: 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 (cm2) 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.
authors.affiliation: a Drug Research Center (CIM), Biomedical Research Institute Sant Pau (IIB Sant Pau) , Barcelona , Spain.|b Pharmacology and Therapeutics Department , Universitat Autònoma de Barcelona (UAB) , Bellaterra , Spain.
authors.forename: Rosa
authors.initials: R
authors.lastname: Antonijoan
authors.affiliation: a Drug Research Center (CIM), Biomedical Research Institute Sant Pau (IIB Sant Pau) , Barcelona , Spain.
authors.forename: Jimena
authors.initials: J
authors.lastname: Coimbra
authors.affiliation: a Drug Research Center (CIM), Biomedical Research Institute Sant Pau (IIB Sant Pau) , Barcelona , Spain.
authors.forename: Consuelo
authors.initials: C
authors.lastname: García-Gea
authors.affiliation: a Drug Research Center (CIM), Biomedical Research Institute Sant Pau (IIB Sant Pau) , Barcelona , Spain.
authors.forename: Montserrat
authors.initials: M
authors.lastname: Puntes
authors.affiliation: a Drug Research Center (CIM), Biomedical Research Institute Sant Pau (IIB Sant Pau) , Barcelona , Spain.|b Pharmacology and Therapeutics Department , Universitat Autònoma de Barcelona (UAB) , Bellaterra , Spain.
authors.forename: Ignasi
authors.initials: I
authors.lastname: Gich
authors.affiliation: c Clinical Research Department , Faes Farma SA , Leioa , Bizkaia , Spain.
authors.forename: Cristina
authors.initials: C
authors.lastname: Campo
authors.affiliation: c Clinical Research Department , Faes Farma SA , Leioa , Bizkaia , Spain.
authors.forename: Román
authors.initials: R
authors.lastname: Valiente
authors.affiliation: c Clinical Research Department , Faes Farma SA , Leioa , Bizkaia , Spain.
authors.forename: Luis
authors.initials: L
authors.lastname: Labeaga
mesh_terms: D000328:Adult; D001562:Benzimidazoles / Q000494:pharmacology*; D018592:Cross-Over Studies; D003533:Cyproheptadine / Q000031:analogs & derivatives* / Q000494:pharmacology; D004311:Double-Blind Method; D005260:Female; D064368:Healthy Volunteers; D006632:Histamine / Q000494:pharmacology; D006633:Histamine Antagonists / Q000494:pharmacology*; D006801:Humans; D007271:Injections, Intradermal; D017336:Loratadine / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D010880:Piperidines / Q000494:pharmacology*; D012867:Skin / Q000187:drug effects*
chemical_list: D001562:Benzimidazoles; D006633:Histamine Antagonists; D010880:Piperidines; C103639:rupatadine; D003533:Cyproheptadine; D017336:Loratadine; D006632:Histamine; C121345:desloratadine; C445659:bilastine
keywords: Antihistamine; bilastine; desloratadine; histamine cutaneous challenge; rupatadine