加替沙星（BMS-284756）对不同氟喹诺酮敏感性的流感嗜血杆菌分离株的体外活性。
In vitro activities of garenoxacin (BMS-284756) against Haemophilus influenzae isolates with different fluoroquinolone susceptibilities.
作者信息
Pérez-Vázquez María, Román Federico, Aracil Belen, Cantón Rafael, Campos José
机构信息
Centro Nacional de Microbiología, Instituto de Salud Carlos III, Majadahonda-Madird, Spain.
出版信息
Antimicrob Agents Chemother. 2003 Nov;47(11):3539-41. doi: 10.1128/AAC.47.11.3539-3541.2003.
The in vitro activity of garenoxacin (BMS-284756) against 62 clinical Haemophilus influenzae isolates with different fluoroquinolone susceptibilities was determined by the microdilution susceptibility testing method and compared with the activities of other oral quinolones and nonquinolone oral antimicrobial agents. Cefixime presented the highest intrinsic activity (MIC at which 50% of the isolates tested were inhibited [MIC(50)], 0.01 microg/ml), followed by garenoxacin, moxifloxacin, and ciprofloxacin (MIC(50), 0.06 microg/ml), levofloxacin (MIC(50), 0.12 microg/ml), cefuroxime (MIC(50), 1.0 microg/ml), and amoxicillin-clavulanate (MIC(50), 1.0/0.5 microg/ml), amoxicillin (MIC(50), 2 microg/ml), azithromycin (MIC(50), 4 microg/ml), and erythromycin (MIC(50), 8 microg/ml). In strains with ciprofloxacin MICs of < or =0.06 microg/ml, ciprofloxacin and garenoxacin displayed similar MIC(50)s and MIC(90)s, one dilution lower than those of moxifloxacin and levofloxacin. For strains for which ciprofloxacin MICs were > or = 0.12 microg/ml, MIC(50)s were similar for the four quinolones tested, although garenoxacin presented the widest activity range (0.03 to 32 microg/ml) and the highest MIC at which 90% of the isolates tested were inhibited (16.0 microg/ml). For strains without amino acid changes in the quinolone resistance determining region (QRDR) of GyrA and ParC, garenoxacin MICs were < or =0.03 microg/ml; with a single amino acid change in GyrA, garenoxacin MICs were 0.06 to 0.12 microg/ml; with one amino acid change each in GyrA and ParC, garenoxacin MICs were 0.5 to 2.0 micro g/ml; one amino acid change in ParC combined with two amino acid changes in GyrA increased the MICs to > or = 4 microg/ml for all assayed quinolones. We conclude that garenoxacin has excellent activity against H. influenzae, although progressive acquired resistance was observed by step-by-step mutation in the QRDR of gyrA and parC.
采用微量稀释药敏试验方法测定了加替沙星（BMS-284756）对62株不同氟喹诺酮敏感性的临床流感嗜血杆菌分离株的体外活性，并与其他口服喹诺酮类药物和非喹诺酮类口服抗菌药物的活性进行了比较。头孢克肟表现出最高的内在活性（使50%受试分离株受到抑制的最低抑菌浓度[MIC(50)]，0.01μg/ml），其次是加替沙星、莫西沙星和环丙沙星（MIC(50)，0.06μg/ml）、左氧氟沙星（MIC(50)，0.12μg/ml）、头孢呋辛（MIC(50)，1.0μg/ml）、阿莫西林-克拉维酸（MIC(50)，1.0/0.5μg/ml）、阿莫西林（MIC(50)，2μg/ml）、阿奇霉素（MIC(50)，4μg/ml）和红霉素（MIC(50)，8μg/ml）。在环丙沙星MIC≤0.06μg/ml的菌株中，环丙沙星和加替沙星显示出相似的MIC(50)和MIC(90)，比莫西沙星和左氧氟沙星低一个稀释度。对于环丙沙星MIC≥0.12μg/ml的菌株，所测试的四种喹诺酮的MIC(50)相似，尽管加替沙星的活性范围最宽（0.03至32μg/ml），且使90%受试分离株受到抑制的最高MIC（16.0μg/ml）。对于在GyrA和ParC的喹诺酮耐药决定区（QRDR）没有氨基酸变化的菌株，加替沙星的MIC≤0.03μg/ml；GyrA中有一个氨基酸变化时，加替沙星的MIC为0.06至0.12μg/ml；GyrA和ParC中各有一个氨基酸变化时，加替沙星的MIC为0.5至2.0μg/ml；ParC中有一个氨基酸变化并结合GyrA中有两个氨基酸变化时，所有测定的喹诺酮的MIC均增加至≥4μg/ml。我们得出结论，加替沙星对流感嗜血杆菌具有优异的活性，尽管通过gyrA和parC的QRDR中的逐步突变观察到了渐进性获得性耐药。
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