Wiseman L R, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs. 1996 Feb;51(2):260-77. doi: 10.2165/00003495-199651020-00006.
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.
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。