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左卡巴斯汀。对其作为局部抗组胺药在变应性鼻炎和结膜炎中的药理特性及治疗潜力的综述。

Levocabastine. A review of its pharmacological properties and therapeutic potential as a topical antihistamine in allergic rhinitis and conjunctivitis.

作者信息

Dechant K L, Goa K L

机构信息

Adis Drug Information Services, Auckland, New Zealand.

出版信息

Drugs. 1991 Feb;41(2):202-24. doi: 10.2165/00003495-199141020-00006.

Abstract

Levocabastine is a long acting, highly potent and selective histamine H1-receptor antagonist, which has been developed for nasal and ocular administration. In controlled trials performed to date levocabastine was effective and well tolerated in the treatment of allergic rhinitis and allergic conjunctivitis. Comparative studies have demonstrated that levocabastine is superior to placebo and at least as effective as sodium cromoglycate (cromolyn sodium) in alleviating symptoms associated with seasonal allergic conditions. Although levocabastine appears to be less effective than the topical corticosteroid beclomethasone with regard to relieving runny and blocked nose, further comparative trials between these 2 agents would be desirable. Similar to other antihistamines, levocabastine provides minimal relief of nasal blockage, but this symptom is believed to be mediated by receptors other than histamine H1. The prompt onset of antiallergic activity after application differentiates levocabastine from the reference topical antiallergic, sodium cromoglycate, which has an onset of efficacy characterised by a lag period, thereby necessitating maintenance treatment. The incidence of adverse effects associated with levocabastine therapy is low and is similar to that observed with placebo and sodium cromoglycate. Levocabastine provides prophylactic protection as well as acute relief from nasal and ocular symptoms in patients with seasonal allergic disorders. With the ever increasing trend towards topical therapy for the treatment of allergic rhinitis and allergic conjunctivitis, levocabastine is a useful addition to the range of drugs currently available. Possible avenues for additional research should include determining whether the antiallergic efficacy of topical levocabastine is superior to that of oral agents such as astemizole and terfenadine, and whether topical therapy is indeed preferred, considering the relative ease of administration of effective oral antiallergic agents.

摘要

左卡巴斯汀是一种长效、高效且具有选择性的组胺H1受体拮抗剂,已开发用于鼻腔和眼部给药。在迄今为止进行的对照试验中,左卡巴斯汀在治疗过敏性鼻炎和过敏性结膜炎方面有效且耐受性良好。比较研究表明,左卡巴斯汀在缓解季节性过敏相关症状方面优于安慰剂,且至少与色甘酸钠(色甘酸二钠)效果相当。尽管在缓解流涕和鼻塞方面,左卡巴斯汀似乎不如局部用皮质类固醇倍氯米松有效,但这两种药物之间还需要进一步的对比试验。与其他抗组胺药类似,左卡巴斯汀对鼻塞的缓解作用极小,但据信这种症状是由组胺H1以外的受体介导的。用药后抗过敏活性迅速起效,这使左卡巴斯汀有别于对照局部用抗过敏药色甘酸钠,后者的起效具有滞后性,因此需要维持治疗。左卡巴斯汀治疗相关的不良反应发生率较低,与安慰剂和色甘酸钠观察到的情况相似。左卡巴斯汀可为季节性过敏性疾病患者提供预防性保护,并能迅速缓解鼻和眼症状。随着过敏性鼻炎和过敏性结膜炎局部治疗的趋势不断增加,左卡巴斯汀是现有药物种类中的一种有用补充。进一步研究的可能途径应包括确定局部用左卡巴斯汀的抗过敏疗效是否优于口服药物如阿司咪唑和特非那定,以及考虑到有效口服抗过敏药物相对易于给药,局部治疗是否确实更受青睐。

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