Pierson W E
Department of Pediatrics, University of Washington, Seattle.
Clin Ther. 1991 Jan-Feb;13(1):92-9.
The recent development of selective H1-antagonists that minimally cross the blood-brain barrier has greatly improved the management of allergic rhinitis and chronic urticaria. These new agents have much reduced anticholinergic and sedative side effects, which were the major drawbacks of the classic H1-antihistamines. Cetirizine, a new second-generation H1-antagonist, offers several properties that may further improve the treatment of allergic rhinitis and chronic urticaria. Cetirizine is the only antihistamine known to possess activity against both the histamine-mediated early phase of the allergic response and the late-phase response of immediate hypersensitivity characterized by migration of inflammatory cells to the site of the reaction. Its efficacy has been demonstrated in clinical trials of patients with seasonal rhinitis and urticaria. The most common side effects associated with cetirizine, such as sedation, are similar to those of other second-generation antihistamines. These properties, combined with a once-daily dosage regimen, should help improve patient compliance and optimize antihistamine therapy.
近期开发的选择性H1拮抗剂极少透过血脑屏障,这极大地改善了变应性鼻炎和慢性荨麻疹的治疗。这些新药的抗胆碱能和镇静副作用大幅减少,而这些副作用是经典H1抗组胺药的主要缺点。西替利嗪是一种新型第二代H1拮抗剂,具有多种特性,可能会进一步改善变应性鼻炎和慢性荨麻疹的治疗。西替利嗪是唯一已知对组胺介导的变应性反应早期阶段和以炎症细胞迁移至反应部位为特征的速发型超敏反应晚期阶段均有活性的抗组胺药。其疗效已在季节性鼻炎和荨麻疹患者的临床试验中得到证实。与西替利嗪相关的最常见副作用,如镇静作用,与其他第二代抗组胺药相似。这些特性,再加上每日一次的给药方案,应有助于提高患者的依从性并优化抗组胺药治疗。