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WU Yin-hua��FANG Hong. Department of Dermatology, First Affiliated Hospital of Zhejiang University, Hangzhou 310003, China Corresponding author��FANG Hong, Email: fanghongzy@sina.com ��Abstract�� The binding of histamine to H1 receptors may result in an increase in the capacity of antigen-presenting cells and in the release of histamine and other mediators from mast cells and basophils, which plays an important role in the pathogenesis of urticaria and other allergic diseases. First-generation H1-antihistamines, which have lipophilicity and low molecular weight, can penetrate blood-brain barrier easily and induce a number of side effects, especially on alertness and consciousness. By contrast, second-generation H1-antihistamines have higher molecular weight, specificity and affinity for receptor, stronger antihistamine activity, and superior safety. International treatment guidelines all recommend second-generation H1-antihistamines as first-choice therapy for chronic urticaria, which permits a dose increase up to 4 times the standard dose when needed with a good security. H3- and H4- antihistamines are under clinical investigations, and are expected to be used for the treatment of allergic diseases and pruritus. ��Key words�� Urticaria�� Histamine�� Histamine H1 antagonists

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