Sastre J
Fundación Jiménez Díaz, Allergy Service, CIBERES-Inst Salud Carlos III, Madrid, Spain.
Allergy. 2008 Dec;63 Suppl 89:1-20. doi: 10.1111/j.1398-9995.2008.01897.x.
Histamine is a key mediator in the development of allergy symptoms, and oral H(1)-antihistamines are among the most widely used treatments for symptomatic relief in conditions such as allergic rhinitis and chronic urticaria. Ebastine is a second-generation antihistamine which has been shown to be an effective treatment for both seasonal and perennial allergic rhinitis. In controlled clinical trials in adult and adolescent patients with allergic rhinitis, ebastine 10 mg once-daily improved symptoms to a significantly greater extent than placebo and to a similar extent as loratadine 10 mg and cetirizine 10 mg (both once-daily), while ebastine 20 mg proved to be more effective than these two comparator antihistamines. In addition, ebastine was significantly more effective than placebo at relieving the symptoms of chronic idiopathic urticaria. Ebastine provides efficacy throughout the 24-h dosing interval with once-daily administration and clinical benefit is seen from the first day of treatment. Small studies have found beneficial effects for ebastine in patients with other disorders, including cold urticaria, dermographic urticaria, atopic asthma, mosquito bites and (in combination with pseudoephedrine) the common cold. In addition to the regular ebastine tablet, a fast-dissolving tablet (FDT) formulation, which disintegrates in the mouth without the aid of a drink, is also available. It has been shown to be bioequivalent to the regular tablet, and to be significantly more effective than desloratadine at reducing histamine-induced cutaneous wheals. A number of patient surveys demonstrated that the majority of individuals who tried the fast-dissolving formulation reported it to be convenient for use, fast-acting and preferred it to their previous antihistamine medication. Perhaps most importantly, a large proportion of patients indicated that they would prefer to use this new formulation in the future. Ebastine has a rapid onset of action and it can be administered once-daily, with or without food. Dose modifications are not needed in elderly patients, or in those with renal or mild to moderate hepatic impairment. Ebastine is generally well-tolerated, and clinical studies showed that at usual therapeutic doses of 10 and 20 mg once-daily, it had no clinically relevant adverse effects on cognitive function and psychomotor performance or on cardiovascular function. In conclusion, ebastine is an effective and generally well-tolerated treatment for allergic rhinitis and chronic idiopathic urticaria. In addition to the regular tablet formulation, ebastine is available as a FDT, providing a treatment option that is particularly convenient for patients.
组胺是过敏症状发展过程中的关键介质,口服H(1)抗组胺药是过敏性鼻炎和慢性荨麻疹等疾病中最广泛用于缓解症状的治疗药物之一。依巴斯汀是第二代抗组胺药,已被证明是季节性和常年性过敏性鼻炎的有效治疗药物。在针对成年和青少年过敏性鼻炎患者的对照临床试验中,每日一次服用10毫克依巴斯汀比安慰剂能更显著地改善症状,且改善程度与每日一次服用10毫克氯雷他定和10毫克西替利嗪相似,而每日一次服用20毫克依巴斯汀比这两种对照抗组胺药更有效。此外,依巴斯汀在缓解慢性特发性荨麻疹症状方面比安慰剂显著更有效。依巴斯汀每日一次给药,在整个24小时给药间隔内均有疗效,且从治疗第一天即可看到临床益处。小型研究发现依巴斯汀对患有其他疾病的患者有有益作用,包括寒冷性荨麻疹、皮肤划痕症、特应性哮喘、蚊虫叮咬以及(与伪麻黄碱联合使用时)普通感冒。除了常规的依巴斯汀片剂外,还有一种口腔崩解片(FDT)剂型,无需用水即可在口腔中崩解。已证明其与常规片剂生物等效,且在减少组胺诱导的皮肤风团方面比地氯雷他定显著更有效。多项患者调查表明,大多数试用过口腔崩解片剂型的人报告其使用方便、起效快,且比他们之前使用的抗组胺药物更受青睐。也许最重要的是,很大一部分患者表示他们未来更愿意使用这种新剂型。依巴斯汀起效迅速,每日服用一次,无论是否与食物同服。老年患者或肾或轻度至中度肝功能损害患者无需调整剂量。依巴斯汀一般耐受性良好,临床研究表明,每日一次服用10毫克和20毫克的常用治疗剂量对认知功能、精神运动表现或心血管功能均无临床相关的不良反应。总之,依巴斯汀是治疗过敏性鼻炎和慢性特发性荨麻疹的一种有效且一般耐受性良好的药物。除了常规片剂剂型外,依巴斯汀还有口腔崩解片剂型,为患者提供了一种特别方便的治疗选择。