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老年人过敏性鼻炎的药物治疗:口服抗组胺药的安全性问题

Pharmacological management of allergic rhinitis in the elderly: safety issues with oral antihistamines.

作者信息

Hansen Juga, Klimek Ludger, Hörmann Karl

机构信息

Ear, Nose and Throat Department, Mannheim University Hospital, Mannheim, Germany.

出版信息

Drugs Aging. 2005;22(4):289-96. doi: 10.2165/00002512-200522040-00002.

DOI:10.2165/00002512-200522040-00002
PMID:15839718
Abstract

An increasing number of elderly persons in our society experience allergic rhinoconjunctivitis. Different agents are used in the pharmacological treatment of allergic rhinitis, with histamine H1 receptor antagonists (antihistamines) being the most frequently prescribed class. However, drug therapy of aged persons differs to a degree from that in other age groups primarily because of quantitative pharmacotherapeutic problems. The main problems are co-morbidities and polymedication, which may lead to drug-drug interactions. H1 receptor antagonists block the action of histamine at specific receptors and are available for both topical and systemic administration. First-generation H1 receptor antagonists are lipophilic and therefore may cross the blood-brain barrier; they also lack specificity for the H1 receptor. Second-generation H1 receptor antagonists have reduced capacity to cross the blood-brain barrier and greater specificity for the H1 receptor. Use of first-generation H1 receptor antagonists in the elderly should be considered carefully because of the large number of adverse effects and potential for interactions with these agents. Second-generation H1 receptor antagonists such as desloratadine, levocetirizine and ebastine provide good selective H1 receptor blockade without anticholinergic or alpha-adrenoceptor antagonist activity. Furthermore, they inhibit proinflammatory cytokines and are safe. Second-generation H1 receptor antagonists also offer therapeutic possibilities in patients with severe liver and/or renal dysfunction.

摘要

在我们的社会中,越来越多的老年人患有过敏性鼻结膜炎。过敏性鼻炎的药物治疗使用不同的药物,其中组胺H1受体拮抗剂(抗组胺药)是最常处方的类别。然而,老年人的药物治疗在一定程度上与其他年龄组不同,主要是因为存在定量药物治疗问题。主要问题是合并症和多种药物治疗,这可能导致药物相互作用。H1受体拮抗剂在特定受体处阻断组胺的作用,有局部和全身给药两种剂型。第一代H1受体拮抗剂具有亲脂性,因此可能穿过血脑屏障;它们对H1受体也缺乏特异性。第二代H1受体拮抗剂穿过血脑屏障的能力降低,对H1受体具有更高的特异性。由于第一代H1受体拮抗剂有大量不良反应以及与这些药物相互作用的可能性,在老年人中使用时应谨慎考虑。第二代H1受体拮抗剂,如地氯雷他定、左西替利嗪和依巴斯汀,能提供良好的选择性H1受体阻断作用,而无抗胆碱能或α-肾上腺素能受体拮抗剂活性。此外,它们能抑制促炎细胞因子,且安全性高。第二代H1受体拮抗剂在严重肝和/或肾功能不全的患者中也提供了治疗可能性。

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