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特非那定,一种H1抗组胺药,可抑制人体体内组胺的释放。

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

作者信息

Naclerio R M, Kagey-Sobotka A, Lichtenstein L M, Freidhoff L, Proud D

机构信息

Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland.

出版信息

Am Rev Respir Dis. 1990 Jul;142(1):167-71. doi: 10.1164/ajrccm/142.1.167.

DOI:10.1164/ajrccm/142.1.167
PMID:1695070
Abstract

A double-blind, placebo-controlled clinical trial was performed on 12 subjects 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-esterase activity, 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, kinins, 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.

摘要

对12名变应性鼻炎患者进行了一项双盲、安慰剂对照临床试验,以评估特非那定(每日两次,每次60毫克或每日两次,每次300毫克)进行1周预处理对依次用变应原和组胺进行鼻腔激发试验反应的影响。通过计数喷嚏次数以及对回收的鼻腔灌洗液中的组胺、激肽、TAME酯酶活性和白蛋白水平进行定量,来监测对变应原激发试验的反应。在组胺激发试验后,记录喷嚏次数和白蛋白水平。特非那定显著减少了抗原激发试验后出现的喷嚏次数以及组胺、激肽、TAME酯酶活性和白蛋白水平。此外,特非那定减少了组胺激发试验后以白蛋白水平衡量的喷嚏次数增加和血管通透性增加。两种剂量的特非那定之间未发现显著差异。我们的数据表明,特非那定不仅在速发型过敏反应期间拮抗释放的组胺的H1活性,而且在当前规定剂量下还抑制组胺的释放。

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