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一些14元、15元和16元大环内酯类药物对葡萄球菌属、军团菌属、支原体属和溶脲脲原体的体外活性。

The in vitro activity of some 14-, 15- and 16- membered macrolides against Staphylococcus spp., Legionella spp., Mycoplasma spp. and Ureaplasma urealyticum.

作者信息

Felmingham D, Robbins M J, Sanghrajka M, Leakey A, Ridgway G L

机构信息

Department of Clinical Microbiology, University College Hospital, London, UK.

出版信息

Drugs Exp Clin Res. 1991;17(2):91-9.

PMID:1650694
Abstract

Erythromycin is a macrolide antimicrobial chemically comprised of a 14-membered lactone ring substituted with a neutral (cladinose) and an amino (desosamine) sugar. Recently, a number of new macrolide molecules have been identified containing either 14-, 15- or 16-membered substituted lactone rings. In this study the authors have determined the in vitro activity of roxithromycin and clarithromycin (both 14-membered macrolides), azithromycin (a 15-membered macrolide or azalide) and midecamycin acetate (a 16-membered macrolide) against clinical isolates of Staphylococcus spp., (including methicillin-susceptible and -resistant isolates), Legionella spp., Mycoplasma spp. and Ureaplasma urealyticum. Minimum inhibitory concentrations of the macrolides for the clinical isolates of Staphylococcus spp. examined were widely distributed. However, midecamycin acetate retained activity against those isolates of Staphylococcus spp. exhibiting inducible resistance to erythromycin and the other macrolides tested. Isolates characterised by constitutive resistance to erythromycin were also resistant to midecamycin acetate. All of the macrolides were very active against Legionella spp., with clarithromycin demonstrating the greatest potency (MIC range: less than or equal to 0.03-0.06 mg/l). Isolates of Mycoplasma pneumoniae and Ureaplasma urealyticum were susceptible to all of the macrolides tested. However, erythromycin, roxithromycin, clarithromycin and azithromycin were poorly active against isolates of Mycoplasma hominis. By contrast, the same isolates were susceptible (MIC range: 0.008-0.12 mg/l) to midecamycin acetate.

摘要

红霉素是一种大环内酯类抗菌药物,其化学结构由一个14元内酯环组成,该内酯环被一个中性糖(克拉定糖)和一个氨基糖(去氧氨基糖)取代。最近,已鉴定出许多新的大环内酯类分子,它们含有14元、15元或16元取代的内酯环。在本研究中,作者测定了罗红霉素和克拉霉素(均为14元大环内酯类)、阿奇霉素(15元大环内酯类或氮杂内酯类)以及麦迪霉素醋酸酯(16元大环内酯类)对金黄色葡萄球菌临床分离株(包括甲氧西林敏感和耐药分离株)、军团菌属、支原体属和解脲脲原体的体外活性。所检测的金黄色葡萄球菌临床分离株对大环内酯类药物的最低抑菌浓度分布广泛。然而,麦迪霉素醋酸酯对那些对红霉素和其他所测试大环内酯类药物表现出诱导性耐药的金黄色葡萄球菌分离株仍保持活性。对红霉素具有固有耐药性的分离株对麦迪霉素醋酸酯也耐药。所有大环内酯类药物对军团菌属都非常有效,其中克拉霉素的效力最强(最低抑菌浓度范围:小于或等于0.03 - 0.06毫克/升)。肺炎支原体和解脲脲原体的分离株对所有所测试的大环内酯类药物均敏感。然而,红霉素、罗红霉素、克拉霉素和阿奇霉素对人型支原体分离株的活性较差。相比之下,相同的分离株对麦迪霉素醋酸酯敏感(最低抑菌浓度范围:0.008 - 0.12毫克/升)。

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