Corcóstegui Reyes, Labeaga Luis, Innerárity Ana, Berisa Agustín, Orjales Aurelio
Department of Research, FAES FARMA, SA, Leioa, Spain.
Drugs R D. 2006;7(4):219-31. doi: 10.2165/00126839-200607040-00002.
We set out to establish the in vivo histamine H(1) receptor antagonistic (antihistaminic) and antiallergic properties of bilastine.
In vivo antihistaminic activity experiments consisted of measurement of: inhibition of increase in capillary permeability and reduction in microvascular extravasation and bronchospasm in rats and guinea pigs induced by histamine and other inflammatory mediators; and protection against lethality induced by histamine and other inflammatory mediators in rats. In vivo antiallergic activity experiments consisted of measurement of passive and active cutaneous anaphylactic reactions as well as type III and type IV allergic reactions in sensitised rodents.
In the in vivo antihistaminic activity experiments, bilastine was shown to have a positive effect, similar to that of cetirizine and more potent than that of fexofenadine. The results of the in vivo antiallergic activity experiments showed that the properties of bilastine in this setting are similar to those observed for cetirizine and superior to fexofenadine in the model of passive cutaneous anaphylactic reaction. When active cutaneous anaphylactic reaction experiments were conducted, bilastine showed significant activity, less potent than that observed with cetirizine but superior to that of fexofenadine. Evaluation of the type III allergic reaction showed that of the antihistamines only bilastine was able to inhibit oedema in sensitised mice, although its effect in this respect was much less potent than that observed with dexamethasone. In terms of the type IV allergic reaction, neither bilastine, cetirizine nor fexofenadine significantly modified the effect caused by oxazolone.
The results of our in vivo preclinical studies corroborate those obtained from previously conducted in vitro experiments of bilastine, and provide evidence that bilastine possesses antihistaminic as well as antiallergic properties, with similar potency to cetirizine and superior potency to fexofenadine.
我们旨在确定比拉斯汀的体内组胺H(1)受体拮抗（抗组胺）和抗过敏特性。
体内抗组胺活性实验包括测量：组胺和其他炎症介质诱导的大鼠和豚鼠毛细血管通透性增加的抑制、微血管渗出减少和支气管痉挛；以及对组胺和其他炎症介质诱导的大鼠致死性的保护。体内抗过敏活性实验包括测量致敏啮齿动物的被动和主动皮肤过敏反应以及III型和IV型过敏反应。
在体内抗组胺活性实验中，比拉斯汀显示出积极作用，类似于西替利嗪，且比非索非那定更有效。体内抗过敏活性实验结果表明，在此环境下比拉斯汀的特性与西替利嗪相似，在被动皮肤过敏反应模型中优于非索非那定。进行主动皮肤过敏反应实验时，比拉斯汀显示出显著活性，效力低于西替利嗪但优于非索非那定。III型过敏反应评估显示，在抗组胺药中只有比拉斯汀能够抑制致敏小鼠的水肿，尽管其在这方面的作用远不如地塞米松。就IV型过敏反应而言，比拉斯汀、西替利嗪和非索非那定都未显著改变恶唑酮引起的效应。
我们体内临床前研究的结果证实了先前对比拉斯汀进行的体外实验所获得的结果，并提供证据表明比拉斯汀具有抗组胺和抗过敏特性，效力与西替利嗪相似，优于非索非那定。
