Abstract
Background: Urticaria is mainly caused by mast cell-derived histamine through the histamine H<sub>1</sub> receptor. Antihistamines are occasionally used on demand upon a recurrence of urticaria; therefore, rapidly acting agents should be explored. The onset of action is assumed to depend on time to maximum concentration (T<sub>max</sub>), but the speed of action needs to be evaluated not only through blood concentration analysis but also by measuring in vivo effectiveness. Methods: In this study, we chose two representative second-generation antihistamines (bepotastine and fexofenadine) with relatively short T<sub>max</sub> values and evaluated their effects on histamine-induced skin responses using both visual and laser Doppler imaging scales. Results: Suppression of histamine-induced flare and itch was observed 3 and 6 h after administration of both antihistamines. Attenuation of itch was seen 30 min after the administration of each drug and thereafter until 6 h. In addition, bepotastine suppressed flare formation after only 30 min following application. Conclusion: These results suggest that antihistamines suppress histamine-induced itch and flare, followed by wheal formation, and that bepotastine suppresses skin symptoms sooner after administration than fexofenadine does, which is relatively consistent with the T<sub>max</sub> results.
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