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奈多罗米钠(替乐定):临床前研究综述

Nedocromil sodium (Tilade): a review of preclinical studies.

作者信息

Rainey D K

机构信息

Loughborough, Leicestershire, UK.

出版信息

Eur Respir J Suppl. 1989 Jun;6:561s-565s.

PMID:2553033
Abstract

Nedocromil sodium (Tilade) is a novel pyranoquinoline dicarboxylic acid, developed for the treatment of reversible obstructive airway disease (ROAD). The drug exhibits specific anti-inflammatory properties when administered topically to the airways. These properties are illustrated by the activity of the drug in a number of in vitro and in vivo models. Thus, in vitro, nedocromil sodium inhibits activation of, and mediator release from, a wide range of inflammatory cells (neutrophils, eosinophils, macrophages/monocytes, mast cells and platelets) in both animals and man, initiated by either specific or non-specific stimuli. In vivo, the drug is effective in models of anaphylactic bronchospasm, increased vascular permeability, cellular influx, late reaction and bronchial hyperreactivity. Although as yet the mechanism of action has not been fully clarified, nedocromil sodium (Tilade) has demonstrated unequivocal efficacy in the treatment of ROAD in controlled therapeutic studies of up to twelve weeks in duration.

摘要

奈多罗米钠(替乐)是一种新型吡喃并喹啉二羧酸,用于治疗可逆性阻塞性气道疾病(ROAD)。该药物局部应用于气道时具有特定的抗炎特性。这些特性在许多体外和体内模型中通过药物的活性得到了体现。因此,在体外,奈多罗米钠可抑制动物和人类多种炎症细胞(中性粒细胞、嗜酸性粒细胞、巨噬细胞/单核细胞、肥大细胞和血小板)由特异性或非特异性刺激引发的激活及介质释放。在体内,该药物在过敏性支气管痉挛、血管通透性增加、细胞内流、迟发反应和支气管高反应性模型中有效。尽管目前其作用机制尚未完全阐明,但在长达12周的对照治疗研究中,奈多罗米钠(替乐)已在ROAD的治疗中显示出明确的疗效。

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