Simons F E, Simons K J
Department of Pediatrics and Child Health, Faculty of Medicine, University of Manitoba.
Ann Allergy. 1991 Jan;66(1):5-16, 19.
The second-generation H1-receptor antagonists do not penetrate into the central nervous system as readily as the first-generation H1-receptor antagonists do. They bind preferentially to peripheral rather than central H1-receptors. They cause no more sedation than placebo does. These medications differ considerably from one another in some aspects of basic pharmacology and in pharmacokinetics and pharmacodynamics. An understanding of these differences will facilitate their optimal clinical usage. The second-generation H1-receptor antagonists are replacing the first generation H1-receptor antagonists in the symptomatic treatment of allergic rhinoconjunctivitis, and in relieving pruritus in patients with urticaria. They have a mild beneficial effect in patients with chronic asthma. They have not supplanted the first generation H1-receptor antagonists in atopic dermatitis treatment or as adjunctive treatment of pruritus and other symptoms in patients with anaphylaxis.
第二代H1受体拮抗剂不像第一代H1受体拮抗剂那样容易渗透到中枢神经系统。它们优先与外周而非中枢H1受体结合。它们引起的镇静作用不超过安慰剂。这些药物在基础药理学、药代动力学和药效学的某些方面彼此有很大差异。了解这些差异将有助于它们的最佳临床应用。第二代H1受体拮抗剂正在取代第一代H1受体拮抗剂用于过敏性鼻结膜炎的症状治疗以及缓解荨麻疹患者的瘙痒。它们对慢性哮喘患者有轻微的有益作用。在特应性皮炎的治疗或作为过敏反应患者瘙痒及其他症状的辅助治疗中，它们尚未取代第一代H1受体拮抗剂。
