Slater J W, Zechnich A D, Haxby D G
College of Pharmacy, Oregon State University, Portland, USA.
Drugs. 1999 Jan;57(1):31-47. doi: 10.2165/00003495-199957010-00004.
Second-generation histamine H1 receptor antagonists (antihistamines) have been developed to reduce or eliminate the sedation and anticholinergic adverse effects that occur with older H1 receptor antagonists. This article evaluates second-generation antihistamines, including acrivastine, astemizole, azelastine, cetirizine, ebastine, fexofenadine, ketotifen, loratadine, mizolastine and terfenadine, for significant features that affect choice. In addition to their primary mechanism of antagonising histamine at the H1 receptor, these agents may act on other mediators of the allergic reaction. However, the clinical significance of activity beyond that mediated by histamine H1 receptor antagonism has yet to be demonstrated. Most of the agents reviewed are metabolised by the liver to active metabolites that play a significant role in their effect. Conditions that result in accumulation of astemizole, ebastine and terfenadine may prolong the QT interval and result in torsade de pointes. The remaining agents reviewed do not appear to have this risk. For allergic rhinitis, all agents are effective and the choice should be based on other factors. For urticaria, cetirizine and mizolastine demonstrate superior suppression of wheal and flare at the dosages recommended by the manufacturer. For atopic dermatitis, as adjunctive therapy to reduce pruritus, cetirizine, ketotifen and loratadine demonstrate efficacy. Although current evidence does not suggest a primary role for these agents in the management of asthma, it does support their use for asthmatic patients when there is coexisting allergic rhinitis, dermatitis or urticaria.
第二代组胺H1受体拮抗剂（抗组胺药）已被研发出来，以减少或消除第一代H1受体拮抗剂所出现的镇静和抗胆碱能不良反应。本文评估了第二代抗组胺药，包括阿伐斯汀、阿司咪唑、氮卓斯汀、西替利嗪、依巴斯汀、非索非那定、酮替芬、氯雷他定、咪唑斯汀和特非那定，以探讨影响用药选择的显著特征。除了在H1受体处拮抗组胺的主要机制外，这些药物可能还作用于过敏反应的其他介质。然而，除组胺H1受体拮抗作用外的其他活性的临床意义尚未得到证实。所评估的大多数药物在肝脏中代谢为活性代谢产物，这些代谢产物在其作用中发挥重要作用。导致阿司咪唑、依巴斯汀和特非那定蓄积的情况可能会延长QT间期并导致尖端扭转型室速。所评估的其余药物似乎没有这种风险。对于过敏性鼻炎，所有药物均有效，用药选择应基于其他因素。对于荨麻疹，按照制造商推荐的剂量，西替利嗪和咪唑斯汀在抑制风团和潮红方面表现出更好的效果。对于特应性皮炎，作为减轻瘙痒的辅助治疗，西替利嗪、酮替芬和氯雷他定显示出疗效。虽然目前的证据并不表明这些药物在哮喘治疗中起主要作用，但当哮喘患者同时存在过敏性鼻炎、皮炎或荨麻疹时，确实支持使用这些药物。
