Jankowski R, Wagenmann M, Baroody F M, Naclerio R
Department of Medicine (Division of Clinical Immunology), Johns Hopkins University School of Medicine, Baltimore, Md.
Int Arch Allergy Immunol. 1993;101(3):311-7. doi: 10.1159/000236469.
The effect of premedication with terfenadine, an H1 antagonist, on nasal challenge with antigen, histamine and methacholine was evaluated. A single dose of terfenadine had no effect on the response to a localized challenge with methacholine but completely blocked the secretory response to histamine on both the ipsilateral and contralateral sides. These results suggest that terfenadine has no anticholinergic activity and that the direct and reflex secretory response to challenge with histamine is mediated by the H1 receptor. A single dose of terfenadine significantly reduced sneezing and nasal secretion after challenge with antigen but had no effect on nasal congestion. A double-blind placebo-controlled clinical trial was undertaken to compare the effects of pretreatment with terfenadine for 1 week on the response to sequential nasal challenge with antigen and histamine. Terfenadine significantly reduced the number of sneezes and the levels of kinins, albumin and TAME esterase activity following challenge with antigen. The levels of histamine were also significantly reduced, suggesting inhibition of the degranulation of mast cells. The number of sneezes and the levels of albumin were also significantly reduced by terfenadine following challenge with histamine.
评估了H1拮抗剂特非那定预处理对抗原、组胺和乙酰甲胆碱鼻腔激发试验的影响。单剂量特非那定对乙酰甲胆碱局部激发试验的反应无影响，但完全阻断了同侧和对侧对组胺的分泌反应。这些结果表明特非那定无抗胆碱能活性，且组胺激发试验的直接和反射性分泌反应由H1受体介导。单剂量特非那定显著减少抗原激发试验后的打喷嚏和鼻分泌物，但对鼻充血无影响。进行了一项双盲安慰剂对照临床试验，比较特非那定预处理1周对依次进行抗原和组胺鼻腔激发试验反应的影响。特非那定显著减少抗原激发试验后的打喷嚏次数以及激肽、白蛋白和TAME酯酶活性水平。组胺水平也显著降低，提示肥大细胞脱颗粒受到抑制。组胺激发试验后，特非那定也显著减少打喷嚏次数和白蛋白水平。
