Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans
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Objective and design
Comparison of bilastine and cetirizine in inhibiting skin wheal and flare responses over 24 h.
Twenty-one healthy male volunteers (aged 19–44 years).
Treatment and methods
Volunteers were randomised to receive single oral doses of 20 or 50 mg bilastine, 10 mg cetirizine or placebo before provocation of wheal and flare responses to 100 mg/ml histamine by skin prick 1.5, 4, 8, 12 and 24 h later.
There were no significant differences between overall inhibitions of wheal or flare by 20 mg bilastine and 10 mg cetirizine. Bilastine was faster in onset than cetirizine, inhibitions of wheal and flare at 1.5 h being 89 ± 3 versus 44 ± 14% (P = 0.011) and 85 ± 4 versus 45 ± 14% (P = 0.016), respectively (Student’s t test). At 1.5 h, both wheals and flares were inhibited by >70% in 11/12 volunteers taking bilastine and 3/11 taking cetirizine (P = 0.003, Fisher’s exact test). There were no significant differences between the drugs at later times. Bilastine 50 mg had a longer duration of action than bilastine 20 mg.
Both 20 mg bilastine and 10 mg cetirizine are effective and of long duration in reducing histamine-induced wheal and flare responses, the major difference between the two drugs being the more rapid onset of action of bilastine.
KeywordsBilastine Cetirizine Wheal and flare
The author wishes to thank Drs. D. McLaverty, A.J. Stewart and B. Colgan of MDS Pharma Services (Belfast, Northern Ireland), and Román Valiente (Faes Farma SA, Department of Research and Development, Department of Clinical Research, Leioa, Spain) for their valuable comments and advice.
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