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依巴斯汀:其药理学特性及治疗过敏性疾病临床疗效的综述

Ebastine. a review of its pharmacological properties and clinical efficacy in the treatment of allergic disorders.

作者信息

Wiseman L R, Faulds D

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1996 Feb;51(2):260-77. doi: 10.2165/00003495-199651020-00006.

DOI:10.2165/00003495-199651020-00006
PMID:8808167
Abstract

Ebastine is a long-acting nonsedating second generation histamine H1 receptor antagonist which binds preferentially to peripheral H1 receptors in vivo. It has shown antihistamine and antiallergic activity in healthy volunteers and patients with allergies, and protected against histamine-induced bronchoconstriction in patients with asthma. Significant symptom improvement is observed in patients with seasonal or perennial allergic rhinitis or chronic idiopathic urticaria following administration of ebastine 10 mg/day, or 20 mg/day in severe rhinitis. In clinical trials, the efficacy of ebastine 10 or 20 mg/day was generally similar to standard dosages of terfenadine, cetirizine, astemizole and loratadine in patients with seasonal allergic rhinitis, astemizole, terfenadine and ketotifen in patients with chronic idiopathic urticaria, and ketotifen, terfenadine, chlorpheniramine and mequitazine in patients with perennial allergic rhinitis. The most frequent adverse events reported during ebastine therapy are drowsiness, headache and dry mouth, the incidence being similar to that reported in placebo recipients. Serious adverse cardiac events, observed on rare occasions with some other histamine H1 receptor antagonists, have not been reported with ebastine, and there has been no evidence of QTc interval prolongation related to ebastine therapy. Thus, once-daily ebastine offers an effective and well-tolerated alternative to other second generation antihistamines in current use for the first-line treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria.

摘要

依巴斯汀是一种长效非镇静性第二代组胺H1受体拮抗剂,在体内优先与外周H1受体结合。它在健康志愿者和过敏患者中显示出抗组胺和抗过敏活性,并可预防组胺诱导的哮喘患者支气管收缩。对于季节性或常年性过敏性鼻炎或慢性特发性荨麻疹患者,每天服用10毫克依巴斯汀,严重鼻炎患者每天服用20毫克依巴斯汀后,症状有显著改善。在临床试验中,对于季节性过敏性鼻炎患者,每天服用10或20毫克依巴斯汀的疗效通常与特非那定、西替利嗪、阿司咪唑和氯雷他定的标准剂量相似;对于慢性特发性荨麻疹患者,与阿司咪唑、特非那定和酮替芬的疗效相似;对于常年性过敏性鼻炎患者,与酮替芬、特非那定、氯苯那敏和美喹他嗪的疗效相似。依巴斯汀治疗期间报告的最常见不良事件是嗜睡、头痛和口干,其发生率与安慰剂组报告的相似。一些其他组胺H1受体拮抗剂偶尔会观察到严重的心脏不良事件,但依巴斯汀尚未报告此类事件,也没有证据表明依巴斯汀治疗会导致QTc间期延长。因此对于目前用于季节性和常年性过敏性鼻炎以及慢性特发性荨麻疹一线治疗的其他第二代抗组胺药而言,每日一次服用依巴斯汀是一种有效且耐受性良好的替代选择。

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本文引用的文献

1
Clinical importance of hepatic cytochrome P450 in drug metabolism.肝细胞色素P450在药物代谢中的临床重要性。
Drug Metab Rev. 1995;27(3):397-417. doi: 10.3109/03602539508998329.
2
Acute and subchronic effects of the H1-histamine receptor antagonist ebastine in 10, 20 and 30 mg dose, and triprolidine 10 mg on car driving performance.10毫克、20毫克和30毫克剂量的H1组胺受体拮抗剂依巴斯汀以及10毫克曲普利啶对驾驶性能的急性和亚慢性影响。
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3
Cimetidine does not influence the metabolism of the H1-receptor antagonist ebastine to its active metabolite carebastine.
富马酸依巴斯汀氢盐的合成与晶体结构
Acta Crystallogr E Crystallogr Commun. 2022 Aug 18;78(Pt 9):916-921. doi: 10.1107/S2056989022008118. eCollection 2022 Sep 1.
4
Carbopol emulgel loaded with ebastine for urticaria: development, characterization, and evaluation.卡波姆巴布剂载埃巴斯汀治疗荨麻疹:制备、表征与评价。
Drug Deliv. 2022 Dec;29(1):52-61. doi: 10.1080/10717544.2021.2015483.
5
Repurpose but also (nano)-reformulate! The potential role of nanomedicine in the battle against SARS-CoV2.重新定位,也要(纳米)重塑!纳米医学在抗击 SARS-CoV2 中的潜在作用。
J Control Release. 2021 Sep 10;337:258-284. doi: 10.1016/j.jconrel.2021.07.028. Epub 2021 Jul 20.
6
Crystal structure of ebastinium 3,5-di-nitro-benzoate.依巴斯汀3,5-二硝基苯甲酸酯的晶体结构。
Acta Crystallogr E Crystallogr Commun. 2017 Sep 19;73(Pt 10):1513-1516. doi: 10.1107/S205698901701324X. eCollection 2017 Oct 1.
7
Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines.依巴斯汀——基于 CONGA 推荐的第三代抗组胺药物研发
J Asthma Allergy. 2009 Aug 31;2:73-92. doi: 10.2147/jaa.s3108.
8
Efficacy and tolerability comparison of ebastine 10 and 20mg with loratadine 10mg: a double-blind, randomised study in patients with perennial allergic rhinitis.依巴斯汀 10mg 和 20mg 与氯雷他定 10mg 的疗效和耐受性比较:一项在常年性变应性鼻炎患者中进行的双盲、随机研究。
Clin Drug Investig. 1998;16(6):413-20. doi: 10.2165/00044011-199816060-00001.
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The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study.CYP2J2、CYP3A4、CYP3A5基因多态性及MDR1基因多态性与性别对H1受体抗组胺药依巴斯汀代谢产物尿排泄的影响:一项初步研究。
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Diazepam effects on the performance of healthy subjects are not enhanced by treatment with the antihistamine ebastine.抗组胺药依巴斯汀治疗不会增强地西泮对健康受试者行为的影响。
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9
Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats.大鼠单次给药后[14C]依巴斯汀的吸收、分布、代谢和排泄
Arzneimittelforschung. 1994 Apr;44(4):527-38.
10
Role of antihistamines in allergic disease.抗组胺药在过敏性疾病中的作用。
Ann Allergy. 1994 Apr;72(4):371-5.