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在体外药代动力学系统中研究达巴万星的药效学。

Pharmacodynamics of dalbavancin studied in an in vitro pharmacokinetic system.

作者信息

Bowker Karen E, Noel Alan R, MacGowan Alasdair P

机构信息

Bristol Centre for Antimicrobial Research & Evaluation, North Bristol NHS Trust and University of Bristol Bristol, UK.

出版信息

J Antimicrob Chemother. 2006 Oct;58(4):802-5. doi: 10.1093/jac/dkl311. Epub 2006 Aug 5.

DOI:10.1093/jac/dkl311
PMID:16891629
Abstract

OBJECTIVES

The antibacterial effect of dalbavancin was studied against Staphylococcus aureus using stepwise declining concentrations designed to model a range of free drug concentrations observed in human serum.

METHODS

Initial concentrations ranged from 0.6 to 21 mg/L and experiments were conducted over 240 h. Three vancomycin-susceptible and one vancomycin-intermediate strain of S. aureus were used.

RESULTS AND CONCLUSIONS

Dalbavancin showed non-concentration-dependent killing against the three vancomycin-susceptible strains in the range 3-21 mg/L and the vancomycin-intermediate strain at 15 and 21 mg/L. AUC/MIC could be related to antibacterial effect. The AUC/MIC for a bacteriostatic effect was 36 at 24 h, 55 at 120 h and 100 at 240 h. A larger AUC/MIC was required to produce a 2 log reduction in counts, being 214 at 24 h, 195 at 120 h and 331 at 240 h.

摘要

目的

使用逐步降低浓度的方法来模拟人血清中观察到的一系列游离药物浓度,研究达巴万星对金黄色葡萄球菌的抗菌作用。

方法

初始浓度范围为0.6至21mg/L,实验持续240小时。使用了三株对万古霉素敏感和一株对万古霉素中介的金黄色葡萄球菌菌株。

结果与结论

达巴万星在3至21mg/L范围内对三株对万古霉素敏感的菌株以及在15和21mg/L时对万古霉素中介菌株显示出非浓度依赖性杀菌作用。AUC/MIC可能与抗菌效果相关。抑菌作用的AUC/MIC在24小时时为36,120小时时为55,240小时时为100。要使菌数减少2个对数,需要更大的AUC/MIC,在24小时时为214,120小时时为195,240小时时为331。

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