Department of Dermatology and Allergy, Allergy Centre Charité, Charité Universitätsmedizin, Berlin, Germany.
Medical Department, FAES Farma, S.A., Bilbao, Spain.
J Eur Acad Dermatol Venereol. 2017 Sep;31(9):1447-1452. doi: 10.1111/jdv.14305. Epub 2017 Jun 1.
This review set out to examine published papers detailing the efficacy of bilastine in skin models and urticaria to assess whether it meets the optimal profile for updosing in urticaria, that is, strong clinical efficacy and freedom from unwanted side effects, particularly sedation. Bilastine is a highly effective H -antihistamine even when used at the basic dose of 20 mg daily. Its facilitated uptake after oral dosage gives it a rapid onset and long duration of action. In both wheal and flare studies and in urticaria updosing fourfold showed increased effectiveness. With respect to somnolence, bilastine is a substrate for P-glycoprotein, a membrane pump which prevents it crossing the blood-brain barrier. Consequently, bilastine is a practically 'non-sedating' H -antihistamine. In conclusion, the excellent profile of bilastine in both efficacy and safety make it the ideal H -antihistamine for updosing the daily dose fourfold in difficult-to-treat urticaria as recommended by the EAACI/GA LEN/EDF/WAO guideline for the management of urticaria.
这篇综述旨在研究详细描述比拉斯汀在皮肤模型和荨麻疹中疗效的已发表论文，以评估其是否符合荨麻疹增量治疗的最佳特征，即具有强大的临床疗效且无不良副作用，尤其是镇静作用。即使使用基本剂量的每日 20 毫克，比拉斯汀也是一种非常有效的 H1 抗组胺药。其口服后易于吸收，起效迅速，作用持续时间长。在风团和瘙痒研究以及荨麻疹四倍剂量增量中均显示出更高的疗效。关于嗜睡，比拉斯汀是 P 糖蛋白的底物，P 糖蛋白是一种膜泵，可防止其穿过血脑屏障。因此，比拉斯汀实际上是一种“非镇静”的 H1 抗组胺药。总之，比拉斯汀在疗效和安全性方面的出色表现使其成为治疗困难性荨麻疹的理想 H1 抗组胺药，四倍剂量增量符合 EAACI/GA LEN/EDF/WAO 荨麻疹管理指南的推荐。
