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Bilastine in allergic rhinoconjunctivitis and urticaria

机译：过敏性鼻结膜炎和荨麻疹中的比拉汀

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To cite this article: Bachert C, Kuna P, Zuberbier T. Bilastine in allergic rhinoconjunctivitis and urticaria. Allergy 2010; 65 (SUPPL.93): 1-13. Abstract Allergic rhinoconjunctivitis and urticaria are increasing in prevalence in many developed countries. The role of histamine in such conditions is well documented and clinical guidelines recommend non-sedating H 1-receptor antagonists as first-line treatment choices. Bilastine is a novel non-sedating histamine H 1-receptor antagonist developed for the treatment of allergic rhinoconjunctivitis and urticaria. The aim of this review is to critique the scientific evidence relating to the pharmacological properties of bilastine and the clinical evidence regarding its potential as an antihistamine. In vitro binding studies and investigations in animal tissue have demonstrated the high specificity of bilastine for H 1-receptors, and preclinical animal studies have also yielded promising results in terms of a reduction of histamine-mediated inflammatory effects, including capillary permeability and bronchospasm. In pharmacodynamic studies bilastine was found to down-regulate histamine-induced flare and wheal responses in healthy volunteers. Preclinical and clinical pharmacokinetic studies showed that bilastine has dose-dependent kinetics following oral administration. Excretion is almost exclusively via urine and faeces as unchanged drug. Early clinical trials have shown that bilastine has similar efficacy to other second-generation H 1-receptor antagonists such as cetirizine, desloratadine, fexofenadine and levocetirizine, in terms of reducing allergic symptoms. Clinical findings also indicate that bilastine has a rapid onset of action and a 20 mg single dose is effective throughout a 24-h period. Furthermore, bilastine has been associated with improved quality of life in allergic rhinoconjunctivitis and urticaria patients. Adverse effects have generally been minimal in these studies and doses up to twice those proposed did not exhibit differences in adverse events compared to placebo. Moreover, in vivo investigations have found no evidence of accumulation of bilastine in the central nervous system, and various studies have confirmed minimal effects on psychomotor performance in healthy volunteers administered up to four times the usual dose. Clinical studies have also found no effect of bilastine on the QTc interval and other ECG parameters, even at supratherapeutic dosages, confirming the good cardiac safety profile of this newer antihistamine. Given its pharmacodynamic profile, which appears to be similar to other second-generation H 1-receptor antagonists, and its favourable safety and tolerability, bilastine has the attributes of a potentially clinically useful non-sedating antihistamine. Larger clinical studies are now necessary to fully elucidate the clinical potential of this novel antihistamine.
机译：引用本文：Bachert C，Kuna P，Zuberbier T. Bilastine在变应性鼻结膜炎和荨麻疹中的应用。过敏2010; 65（SUPPL.93）：1-13。摘要在许多发达国家，过敏性鼻结膜炎和荨麻疹的发病率正在增加。组胺在这种情况下的作用已得到充分证明，临床指南建议将非镇静性的H 1受体拮抗剂作为一线治疗选择。 Bilastine是开发用于治疗变应性鼻结膜炎和荨麻疹的新型非镇静组胺H 1受体拮抗剂。这篇综述的目的是批判与生物素的药理特性有关的科学证据，以及有关其作为抗组胺药的潜力的临床证据。在动物组织中进行的体外结合研究和研究表明，双向弹性蛋白对H 1受体具有高度特异性，并且在减少组胺介导的炎症作用（包括毛细血管通透性和支气管痉挛）方面，临床前动物研究也产生了可喜的结果。在药效学研究中，在健康志愿者中发现了生物弹性蛋白下调了组胺诱导的耀斑和风团反应。临床前和临床药代动力学研究表明，在口服后，比斯汀具有剂量依赖性的动力学。排泄几乎完全是通过尿液和粪便作为未改变的药物。早期的临床试验表明，在减少过敏症状方面，比拉汀具有与其他第二代H 1受体拮抗剂（例如西替利嗪，地氯雷他定，非索非那定和左西替利嗪）相似的功效。临床发现还表明，比拉汀具有快速起效的作用，单剂量20 mg在整个24小时内都是有效的。此外，在过敏性鼻结膜炎和荨麻疹患者中，比拉汀与改善生活质量有关。在这些研究中，不良反应通常很小，与安慰剂相比，两倍于建议剂量的不良反应无差异。此外，体内研究还没有证据显示中枢神经系统中存在双氨苯丁酸的积累，各种研究已经证实，健康志愿者服用普通剂量至普通剂量的四倍对精神运动能力的影响极小。临床研究还发现，即使在超治疗剂量下，双氨嘧啶对QTc间隔和其他ECG参数也没有影响，证实了这种新型抗组胺药的良好心脏安全性。鉴于其药效学特征似乎与其他第二代H 1受体拮抗剂相似，并且其有利的安全性和耐受性，比拉司汀具有潜在的临床有用的非镇静抗组胺药特性。为了充分阐明这种新型抗组胺药的临床潜力，现在需要进行更大的临床研究。

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