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抗组胺药对肥大细胞介质释放的体内和体外作用:在过敏性疾病治疗中一项潜在的重要特性。

In vivo and in vitro effects of antihistamines on mast cell mediator release: a potentially important property in the treatment of allergic disease.

作者信息

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

机构信息

Department of Medicine, Division of Clinical Immunology, Hopkins University School of Medicine, Baltimore, Maryland.

出版信息

Ann Allergy. 1989 Nov;63(5):465-9.

PMID:2573301
Abstract

A nasal antigen challenge model of allergic individuals was used to evaluate whether antihistamines could inhibit human mast cell and basophil mediator release in vivo. In placebo-controlled trials, topically applied azatadine base, a tricyclic antihistamine with in vitro antirelease action, effectively reduced symptoms and mediator levels in nasal lavage fluids after antigen challenge, suggesting mast cell inhibition. Both terfenadine and cetirizine, systemically administered antihistamines, were clinically effective in reducing sneezing and changes in vascular permeability. Only terfenadine significantly reduced histamine in antigen-induced nasal secretions. However, cetirizine did reduce the level of leukotriene C4 in these fluids. These results indicate that some antihistamines may be capable of suppressing mediator release from nasal mast cells. The significance of this property in those compounds' overall clinical effect is unclear because of their other concomitant activities.

摘要

使用变应性个体的鼻内抗原激发模型来评估抗组胺药是否能在体内抑制人肥大细胞和嗜碱性粒细胞介质的释放。在安慰剂对照试验中,局部应用阿扎他定碱(一种具有体外抗释放作用的三环类抗组胺药)能有效减轻抗原激发后鼻灌洗液中的症状和介质水平,提示肥大细胞受到抑制。特非那定和西替利嗪这两种全身给药的抗组胺药在临床上均能有效减轻打喷嚏和血管通透性变化。只有特非那定能显著降低抗原诱导的鼻分泌物中的组胺水平。然而,西替利嗪确实降低了这些液体中白三烯C4的水平。这些结果表明,一些抗组胺药可能能够抑制鼻内肥大细胞释放介质。由于这些化合物还具有其他伴随活性,因此该特性在其整体临床效果中的意义尚不清楚。

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In vivo and in vitro effects of antihistamines on mast cell mediator release: a potentially important property in the treatment of allergic disease.抗组胺药对肥大细胞介质释放的体内和体外作用:在过敏性疾病治疗中一项潜在的重要特性。
Ann Allergy. 1989 Nov;63(5):465-9.
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引用本文的文献

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Drugs. 2005;65(3):341-84. doi: 10.2165/00003495-200565030-00004.
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Overview of allergic mechanisms. Ebastine has more than an antihistamine effect.过敏机制概述。依巴斯汀具有多种作用,不止是抗组胺作用。
Drugs. 1996;52 Suppl 1:15-9. doi: 10.2165/00003495-199600521-00005.
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Direct effects of second-generation H1-receptor antagonists on the activation of human basophils.第二代H1受体拮抗剂对人嗜碱性粒细胞激活的直接作用。
Agents Actions. 1994 Jun;41 Spec No:C45-6. doi: 10.1007/BF02007760.
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Pharmacokinetic optimisation of histamine H1-receptor antagonist therapy.组胺H1受体拮抗剂治疗的药代动力学优化
Clin Pharmacokinet. 1991 Nov;21(5):372-93. doi: 10.2165/00003088-199121050-00005.