Sádaba Díaz de Rada B, Azanza Perea J R, Gomez-Guiu Hormigos A
Servicio de Farmacología Clínica, Clínica Universidad de Navarra, Pamplona, Spain.
Drugs Today (Barc). 2011 Apr;47(4):251-62. doi: 10.1358/dot.2011.47.4.1587029.
Bilastine is a potent inhibitor of the histamine H1 receptor. It was recently approved in 28 countries of the European Union for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria in adults and children older than 12 years. Data from preclinical studies confirmed its selectivity for the histamine H1 receptor over other receptors, and demonstrated antihistaminic and antiallergic properties in vivo. Studies in healthy volunteers and patients have shown that bilastine does not affect driving ability, cardiac conduction or alertness. Bilastine has demonstrated a good safety profile, without serious adverse effects or antimuscarinic effects in clinical trials. There were no significant changes in laboratory tests, electrocardiograms or vital signs. In clinical studies, oral treatment with bilastine 20 mg once daily improved allergic rhinitis with greater efficacy than placebo and comparable to cetirizine and desloratadine. Bilastine 20 mg was more effective than placebo and equivalent to levocetirizine in chronic urticaria, relieving symptoms, improving quality of life and controlling sleep disorders.
比拉斯汀是一种强效的组胺H1受体抑制剂。它最近在欧盟的28个国家获得批准，用于对12岁及以上成人和儿童的过敏性鼻结膜炎和荨麻疹进行对症治疗。临床前研究数据证实了其对组胺H1受体相对于其他受体的选择性，并在体内表现出抗组胺和抗过敏特性。在健康志愿者和患者中进行的研究表明，比拉斯汀不会影响驾驶能力、心脏传导或警觉性。比拉斯汀已显示出良好的安全性，在临床试验中没有严重不良反应或抗毒蕈碱作用。实验室检查、心电图或生命体征均无显著变化。在临床研究中，每天口服一次20毫克比拉斯汀治疗过敏性鼻炎的疗效优于安慰剂，与西替利嗪和地氯雷他定相当。在慢性荨麻疹中，20毫克比拉斯汀比安慰剂更有效，与左西替利嗪相当，可缓解症状、改善生活质量并控制睡眠障碍。
