Terfenadine, an H1 antihistamine, inhibits histamine release in vivo in the human.

Terfenadine, an H1 antihistamine, inhibits histamine release in vivo in the human.
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Terfenadine 是一种 H1 抗组胺药,可抑制人体内组胺的释放。

DOI:
10.1164/ajrccm/142.1.167
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发表时间:
1990
期刊:
The American review of respiratory disease
影响因子:
--
通讯作者:
Proud,D
Proud,D
中科院分区:
--
文献类型:
--
作者:
Naclerio,RM;Kagey-Sobotka,A;Lichtenstein,LM;Freidhoff,L;Proud,D

文献摘要

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对12例过敏性鼻炎受试者进行了一项双盲、安慰剂对照的临床试验,以评价特非那定(60 mg,每日两次或300 mg,每日两次)预处理1周对过敏原和组胺连续鼻激发反应的影响。通过计数喷嚏次数和定量回收鼻灌洗液中组胺、激肽、TAME-酯酶活性和白蛋白的水平来监测对过敏原激发的反应。组胺激发后,记录打喷嚏和白蛋白水平。特非那定显著降低抗原激发后的喷嚏和组胺、亲属、TAME-酯酶活性和白蛋白水平。此外,特非那定降低了组胺激发后喷嚏和血管通透性的增加,如通过白蛋白水平测量的。两种剂量的特非那定之间无显著差异。我们的数据表明,特非那定不仅拮抗H1活性释放组胺在立即过敏反应,但也在目前规定的剂量,抑制组胺的释放。
SUMMARY A double-blind, placebo-controlled clinical trial was performed on 12subjects with allergic rhinitis to evaluate the effect of 1-wk pretreatment with terfenadine (60 mg twice daily or 300 mg twice daily) on the response to sequential nasal challenges with allergen and histamine. The response to allergen challenge was monitored by counting sneezes and by quantifying the levels of histamine, kinins, TAME-esteraseactivity, and albumin in recovered nasal lavages. Following histamine challenges, sneezing and the levels of albumin were recorded. Terfenadine significantly reduced sneezing and the levels of histamine, kin ins, TAME-esterase activity, and albumin seen after antigen challenge. In addition, terfenadine reduced the increase in sneezing and vascular permeability, as measured by albumin levels, following challenge with histamine. No significant differences were found between the two doses of terfenadine. Our data suggest that terfenadine not only antagonizes the H1 activity of released histamine during the immediate allergic reaction but also, at currently prescribed doses, inhibits the release of histamine.