Simons F E
Department of Pediatrics and Child Health, Faculty of Medicine, University of Manitoba, Winnipeg, Canada.
Ann Allergy. 1993 Sep;71(3):282-7.
The introduction of relatively nonsedating H1-receptor antagonists ushered in a new era in the symptomatic treatment of allergic disorders. Unlike first-generation H1-receptor antagonists, the second-generation compounds (such as astemizole, cetirizine, loratadine, and terfenadine) do not cross the blood-brain barrier readily and are thus comparatively free of central nervous system effects. The pharmacokinetic and pharmacodynamic profiles vary considerably by agent, but most of the second-generation drugs are suitable for once-daily dosing. Efficacy of the H1 antagonists is maintained during chronic therapy. The second-generation H1-receptor antagonists are appropriate for use as first-line treatment of allergic rhinoconjunctivitis and urticaria. These agents also have a modest, direct beneficial effect in patients with chronic asthma. The role of the newer H1-receptor antagonists in the treatment of atopic dermatitis, upper respiratory tract infections, and otitis media remains undefined. Recently, the gene encoding the histamine H1 receptor was cloned from bovine adrenal medullae. Emerging evidence suggests that more than one subtype of H1 receptor may exist. It is hoped these advances will pave the way for further improvements in H1-antagonist therapy.
相对无镇静作用的H1受体拮抗剂的引入开创了过敏性疾病症状治疗的新时代。与第一代H1受体拮抗剂不同，第二代化合物（如阿司咪唑、西替利嗪、氯雷他定和特非那定）不易穿过血脑屏障，因此相对没有中枢神经系统效应。不同药物的药代动力学和药效学特征差异很大，但大多数第二代药物适合每日一次给药。在慢性治疗期间，H1拮抗剂的疗效得以维持。第二代H1受体拮抗剂适合用作过敏性鼻结膜炎和荨麻疹的一线治疗药物。这些药物对慢性哮喘患者也有一定的直接有益作用。新型H1受体拮抗剂在特应性皮炎、上呼吸道感染和中耳炎治疗中的作用仍不明确。最近，编码组胺H1受体的基因从牛肾上腺髓质中克隆出来。新出现的证据表明可能存在不止一种H1受体亚型。希望这些进展将为H1拮抗剂治疗的进一步改进铺平道路。
