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地红霉素与其他新型及已上市大环内酯类药物的体外活性比较。

In-vitro activity of dirithromycin in comparison with other new and established macrolides.

作者信息

Bauernfeind A

机构信息

Max von Pettenkofer-Institut, Munich, Germany.

出版信息

J Antimicrob Chemother. 1993 Mar;31 Suppl C:39-49. doi: 10.1093/jac/31.suppl_c.39.

Abstract

Improvements with regard to the in-vitro activity of new macrolides are marginal and apply mainly to Haemophilus spp., Moraxella catarrhalis and Neisseria gonorrhoeae (e.g. azithromycin is two to eight times more active than erythromycin) and to non-enterococcal streptococci (e.g. clarithromycin is two to four times more active than erythromycin). The increase in activity against staphylococci is even less striking, being restricted to a few species and limited to clarithromycin (twice as active as erythromycin). The Enterobacteriaceae, as well as glucose non-fermenting Gram-negative bacilli, remain outside the therapeutic range of the new macrolides, as they were for the established compounds. The majority of enterococci and Corynebacterium jeikeium are resistant to all macrolides, whereas Corynebacterium diphtheriae is highly susceptible. In-vitro susceptibilities both of Campylobacter jejuni/coli and Helicobacter pylori indicate only moderate susceptibility to macrolides and the azalide. In the case of anaerobic organisms, clarithromycin is the most active macrolide against the majority of species. Dirithromycin, clarithromycin, roxithromycin and josamycin, and the azalide azithromycin, are similar in their antibacterial spectrum to erythromycin. New macrolides differ from established compounds largely in their pharmacokinetic behaviour and only minor progress has been achieved in improving their antibacterial spectrum.

摘要

新型大环内酯类药物在体外活性方面的改善很有限,主要适用于嗜血杆菌属、卡他莫拉菌和淋病奈瑟菌(例如阿奇霉素的活性比红霉素高两到八倍)以及非肠球菌性链球菌(例如克拉霉素的活性比红霉素高两到四倍)。对葡萄球菌活性的增加甚至更不显著,仅限于少数几种葡萄球菌,且仅限于克拉霉素(活性是红霉素的两倍)。肠杆菌科细菌以及葡萄糖非发酵革兰氏阴性杆菌仍不在新型大环内酯类药物的治疗范围内,就像它们对已有的化合物一样。大多数肠球菌和杰氏棒状杆菌对所有大环内酯类药物耐药,而白喉棒状杆菌则高度敏感。空肠弯曲菌/结肠弯曲菌和幽门螺杆菌的体外药敏试验表明,它们对大环内酯类药物和氮杂内酯类药物仅中度敏感。对于厌氧菌,克拉霉素是对大多数菌种活性最强的大环内酯类药物。地红霉素、克拉霉素、罗红霉素和交沙霉素,以及氮杂内酯类药物阿奇霉素,它们的抗菌谱与红霉素相似。新型大环内酯类药物与已有的化合物在很大程度上的区别在于它们的药代动力学行为,在改善抗菌谱方面仅取得了微小进展。

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