Allocco Frances T, Votypka Virginia, deTineo Marcy, Naclerio Robert M, Baroody Fuad M
Section of Otolaryngology-Head and Neck Surgery, The Pritzker School of Medicine, The University of Chicago, Chicago, Illinois 60637, USA.
Ann Allergy Asthma Immunol. 2002 Dec;89(6):578-84. doi: 10.1016/S1081-1206(10)62105-9.
Previous studies using nasal allergen challenge models have shown that terfenadine, an H1 antihistamine, inhibits histamine release during the early response to allergen provocation. Fexofenadine, the active metabolite of terfenadine, has strong H1-antihistaminic activity and no cardiac effects. Clinical studies have documented the efficacy of fexofenadine in the treatment of allergic rhinitis.
To determine whether fexofenadine, like terfenadine, inhibits histamine and tryptase release during the early allergic response.
Randomized, double blind, placebo-controlled, two-way crossover study in 20 subjects with seasonal allergic rhinitis, out of their allergy season (median age 27.5 years, 13 males and 7 females). Subjects were medicated with either placebo or fexofenadine 180 mg orally daily for 1 week followed by nasal challenge with allergen. After each challenge, sneezes and nasal symptoms were recorded, and a nasal lavage was obtained for the assay of albumin, an indicator of vascular permeability, and histamine and tryptase, indicators of mast cell degranulation.
When patients were on placebo, allergen challenges led to significant increases in all measured parameters compared with the sham challenges with diluent. Treatment with fexofenadine resulted in inhibition of allergen-induced symptoms and increased vascular permeability, but not the release of histamine and tryptase.
Fexofenadine is an effective H1 antihistamine, but in contrast to its parent compound, terfenadine, it does not affect the release of the mast cell mediators histamine and tryptase.
既往使用鼻过敏原激发模型的研究表明，H1抗组胺药特非那定可抑制过敏原激发早期反应过程中的组胺释放。特非那定的活性代谢产物非索非那定具有较强的H1抗组胺活性且无心脏效应。临床研究已证实非索非那定治疗变应性鼻炎的疗效。
确定非索非那定是否像特非那定一样，在早期过敏反应中抑制组胺和类胰蛋白酶释放。
对20例季节性变应性鼻炎患者（处于非过敏季节，中位年龄27.5岁，男13例，女7例）进行随机、双盲、安慰剂对照、双向交叉研究。受试者口服安慰剂或非索非那定180 mg，每日1次，共1周，随后进行过敏原鼻激发试验。每次激发后，记录喷嚏和鼻部症状，并采集鼻灌洗液检测血管通透性指标白蛋白以及肥大细胞脱颗粒指标组胺和类胰蛋白酶。
患者服用安慰剂时，与用稀释液进行的假激发试验相比，过敏原激发导致所有测量参数均显著增加。非索非那定治疗可抑制过敏原诱发的症状并减轻血管通透性增加，但不影响组胺和类胰蛋白酶释放。
非索非那定是一种有效的H1抗组胺药，但与其母体化合物特非那定不同，它不影响肥大细胞介质组胺和类胰蛋白酶的释放。
