Uchida M, Nakahara H
Sumitomo Pharmaceuticals Research Center, Discovery Research Laboratories II, Osaka, Japan.
Nihon Yakurigaku Zasshi. 2000 Apr;115(4):229-35. doi: 10.1254/fpj.115.229.
A number of reports have characterized cetirizine as a potent histamine H1-receptor antagonist possessing inhibitory effects on eosinophil chemotaxis. In clinical pharmacological tests, cetirizine markedly reduced wheal and flare responses induced by histamines. The inhibition was fast onset, potent and long-lasting. A single clinical dose of cetirizine was more potent in inhibiting wheal response than other antihistamines such as terfenadine, loratadine, epinastine and ebastine. Cetirizine also inhibited eosinophil chemotaxis in vitro at a concentration easily attained after a clinical dose of 10 mg. Eosinophil infiltration into a site challenged with allergen in vivo was also inhibited. Potent antihistaminic effects of cetirizine afforded fast and strong relief from histamine-induced symptoms such as sneezing and rhinorrhoea in allergic rhinitis and itchy sensation in idiopathic chronic urticaria. Inhibitory effect of cetirizine on eosinophil chemotaxis may alleviate minimal persistent inflammation due to faintly but repeated intake of allergen. Such anti-inflammatory properties of cetirizine may be beneficial in reducing hypersensitivity to normalize the upper respiratory tract and eosinophil-related skin inflammation.
多项报告将西替利嗪描述为一种强效组胺H1受体拮抗剂，对嗜酸性粒细胞趋化性具有抑制作用。在临床药理试验中，西替利嗪显著降低组胺诱导的风团和潮红反应。这种抑制起效迅速、作用强大且持久。单次临床剂量的西替利嗪在抑制风团反应方面比其他抗组胺药如特非那定、氯雷他定、依匹斯汀和依巴斯汀更有效。西替利嗪在临床剂量10mg后很容易达到的浓度下，也能在体外抑制嗜酸性粒细胞趋化性。在体内，其对变应原攻击部位的嗜酸性粒细胞浸润也有抑制作用。西替利嗪强大的抗组胺作用能迅速且有力地缓解组胺诱导的症状，如过敏性鼻炎中的打喷嚏和鼻漏，以及特发性慢性荨麻疹中的瘙痒感。西替利嗪对嗜酸性粒细胞趋化性的抑制作用可能减轻因轻微但反复摄入变应原引起的轻微持续性炎症。西替利嗪的这种抗炎特性可能有助于降低超敏反应，使上呼吸道和嗜酸性粒细胞相关的皮肤炎症恢复正常。
