Sheffer A L, Samuels L L
Department of Medicine, Harvard Medical School, Boston, MA.
J Allergy Clin Immunol. 1990 Dec;86(6 Pt 2):1040-6. doi: 10.1016/s0091-6749(05)80251-9.
For three decades, traditional H1 antihistamines have been used in the treatment of allergic diseases. They are effective in reducing histamine-related symptoms, but the use of such agents has been limited by sedation and anticholinergic side effects. These adverse effects are fewer with the recently introduced H1 antihistamines. One of these, cetirizine, a human metabolite of hydroxyzine, is characterized by its high selectivity for the H1 receptor site and its reliable and consistent inhibition of histamine-induced allergic reactions. It also blocks eosinophil infiltration to the site of allergen-induced cutaneous reactions. Cetirizine has proved effective in the treatment of seasonal and perennial allergic rhinitis and urticaria. It is excreted primarily by renal mechanisms. It is well tolerated by elderly patients. Cetirizine has a low rate of penetration of the blood-brain barrier, and it has minimal central nervous system impairment. Furthermore, it can be given once a day. Cetirizine's low incidence of sedation and anticholinergic side effects contribute to its high profile of safety. In this article the characteristics, pharmacology, pharmacokinetics, and mode of action of cetirizine are reviewed.
三十年来，传统的H1抗组胺药一直用于治疗过敏性疾病。它们在减轻组胺相关症状方面有效，但此类药物的使用受到镇静作用和抗胆碱能副作用的限制。最近推出的H1抗组胺药的这些不良反应较少。其中之一西替利嗪，是羟嗪的人体代谢产物，其特点是对H1受体位点具有高选择性，对组胺诱导的过敏反应具有可靠且持续的抑制作用。它还能阻止嗜酸性粒细胞浸润到变应原诱导的皮肤反应部位。西替利嗪已被证明在治疗季节性和常年性过敏性鼻炎及荨麻疹方面有效。它主要通过肾脏机制排泄。老年患者对其耐受性良好。西替利嗪血脑屏障的穿透率低，对中枢神经系统的损害最小。此外，它可以每天服用一次。西替利嗪的低镇静发生率和抗胆碱能副作用促成了其高安全性。本文综述了西替利嗪的特性、药理学、药代动力学和作用方式。
