COMPARATIVE-EVALUATION OF RECENTLY DEVELOPED QUINOLONE COMPOUNDS - WITH A NOTE ON THE FREQUENCY OF RESISTANT MUTANTS
COMPARATIVE-EVALUATION OF RECENTLY DEVELOPED QUINOLONE COMPOUNDS - WITH A NOTE ON THE FREQUENCY OF RESISTANT MUTANTS
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DOI：
10.1159/000238309
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发表时间：
1985-01-01
期刊：
影响因子：
3.3
通讯作者：
OPFERKUCH, W
中科院分区：
文献类型：
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作者：
CULLMANN, W;STIEGLITZ, M;OPFERKUCH, W
研究了新型喹诺酮类化合物依诺沙星、诺氟沙星、氧氟沙星和环丙沙星对300株肠杆菌科细菌、50株铜绿假单胞菌、30株不动杆菌、15株流感嗜血杆菌、50株粪链球菌和70株金黄色葡萄球菌的抗菌活性，并与奈利地酸、庆大霉素和各种β-内酰胺类化合物进行了比较。评估对喹诺酮类化合物耐药的自发突变率。在仅略高于最小抑菌浓度(MIC)的浓度下，突变株可以相当频繁地分离(.apprx。10-6倍)；在至少10倍的浓度下，几乎检测不到MIC抗性突变体。一般而言，与野生株相比，突变体的最低抑菌浓度增加了4到8倍。在粪链球菌中未检测到突变体，而在金黄色葡萄球菌菌株中，突变体出现的频率较低(<；10-8倍)。在所有突变株中，喹诺酮类衍生物之间几乎但不完全存在交叉耐药。
The antibacterial activity of the new quinolone compounds enoxacin, norfloxacin, ofloxacin and ciprofloxacin was evaluated in 300 Enterobacteriaceae, 50 Pseudomonas aeruginosa, 30 Acinetobacter spp., 15 Haemophilus influenzae, 50 Streptococcus faecalis and 70 Straphylococcus aureus isolates and compared to that of nalidixic acid, gentamicin and various .beta.-lactam compounds. The rate of spontaneous mutants resistant to quinolone compounds was evaluated. In concentrations only insignificantly exceeding the minimal inhibitory concentrations (MIC), mutants could be isolated rather frequently (.apprx. 10-6 fold); in concentrations of at least 10 times the MIC resistant mutants were barely detectable. In general, the mutants exhibited a 4- to 8-fold increase of the MIC, as compared to the wild strain. In S. faecalis mutants were not detectable, whereas they occurred in low frequency (< 10-8 fold) in S. aureus strains. In all mutants there was almost, but not entirely, complete cross-resistance between the quinolone derivatives.