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[阿奇霉素与支气管肺部感染]

[Azithromycin and bronchopulmonary infections].

作者信息

Leophonte P

机构信息

Service de Pneumologie, Hôpital Rangueil, Toulouse, France.

出版信息

Pathol Biol (Paris). 1995 Jun;43(6):534-41.

PMID:8539078
Abstract

Azithromycin is a molecule of the macrolide family, belonging to the azalides class. Several of its characteristics allow for its use in the treatment of the community-acquired lower respiratory tract infections. Commonly isolated pathogens in bronchial infections are most frequently H. influenzae, S. pneumoniae, M. catarrhalis, C. pneumoniae and M. pneumoniae, and more rarely or in the context of a particular background, S. aureus, Gram negative bacteria and L. pneumophila. MIC90 of these germs is generally low or slightly elevated, displaying an inhibitory activity of the azithromycin on these bacteria. Nevertheless, the frequency of macrolide-resistant S. pneumoniae is not negligible and this germ must be considered as inconstantly susceptible to the macrolide family. Pharmacokinetics studies evidenced from high to very high azithromycin concentrations in the pulmonary tissues, reaching values well above MIC of pathogens commonly isolated. Given the long half-life, these concentrations persist a long time after oral administration. As azithromycin concentrates much in polymorphonuclear leucocytes, they release azithromycin after having migrated into the infectious site by chimiotactism, thus allowing to increase the antibiotic concentration at infection site. These requirements have been confirmed in vivo in animal models and in clinical studies. Two experimental models on macrolide susceptible S. pneumoniae, and H. influenzae evidenced a better activity of azithromycin in comparison to other macrolides tested against these two germs.

摘要

阿奇霉素是大环内酯类家族的一种分子,属于氮杂内酯类。其若干特性使其可用于治疗社区获得性下呼吸道感染。支气管感染中常见分离出的病原体最常见的是流感嗜血杆菌、肺炎链球菌、卡他莫拉菌、肺炎衣原体和肺炎支原体,较少见或在特定背景下还包括金黄色葡萄球菌、革兰氏阴性菌和嗜肺军团菌。这些病菌的MIC90通常较低或略有升高,显示出阿奇霉素对这些细菌的抑制活性。然而,耐大环内酯类肺炎链球菌的频率不可忽视,这种病菌必须被视为对大环内酯类家族的敏感性不稳定。药代动力学研究表明,肺组织中阿奇霉素浓度从高到非常高,达到远高于常见分离出病原体MIC的值。鉴于半衰期长,口服给药后这些浓度会持续很长时间。由于阿奇霉素在多形核白细胞中大量浓缩,它们通过趋化作用迁移到感染部位后会释放阿奇霉素,从而使感染部位的抗生素浓度增加。这些条件在动物模型和临床研究中已在体内得到证实。针对对大环内酯类敏感的肺炎链球菌和流感嗜血杆菌的两个实验模型表明,与针对这两种病菌测试的其他大环内酯类相比,阿奇霉素具有更好的活性。

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