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测定国产氟罗沙星对493株临床分离细菌的最低抑菌浓度(MIC),并与氧氟沙星、洛美沙星、环丙沙星和几种头孢菌素、氨基糖苷类抗生素作了比较。结果表明:氟罗沙星对革兰氏阴性细菌有强大抗菌活性,对肠杆菌科细菌的MIC90≤1μg/ml。对铜绿假单胞菌亦有较强抗菌活性,其MIC50、MIC90分别为2和4μg/ml。金葡球菌(含MRSA菌株)对氟罗沙星亦很敏感,MIC90≤1μg/ml。链球菌属对其基本耐药,MIC90为8~16μg/ml。对大多数常见致病菌,氟罗沙星体外抗菌活性与氧氟沙星、洛美沙星相近,稍逊于环丙沙星。对革兰氏阴性菌,氟罗沙星与头孢噻肟、头孢他啶、阿米卡星相当,优于头孢唑林、氨苄西林、哌拉西林、庆大霉素。耐庆大霉素、头孢菌素菌株对氟罗沙星仍敏感。细菌对氟罗沙星单步自发耐药突变频率极低,但通过连续传代培养可以培育出对氟罗沙星高度耐药菌株。
The minimum inhibitory concentrations (MICs) of domestic fleroxacin against 493 clinically isolated bacteria were determined and compared with ofloxacin, lomefloxacin, ciprofloxacin and several cephalosporins and aminoglycoside antibiotics. The results showed that fleroxacin had strong antibacterial activity against Gram-negative bacteria, and MIC90 of Enterobacteriaceae was less than or equal to 1μg / ml. Pseudomonas aeruginosa also have strong antibacterial activity, the MIC50, MIC90 were 2 and 4μg / ml. Staphylococcus aureus (including MRSA strain) is also very sensitive to fleroxacin, MIC90 ≤ 1μg / ml. Streptococcus is resistant to its basic, MIC90 is 8 ~ 16μg / ml. For most common pathogenic bacteria, fleroxacin antibacterial activity in vitro and ofloxacin, lomefloxacin similar, slightly inferior to ciprofloxacin. For gram-negative bacteria, fleroxacin and cefotaxime, ceftazidime, amikacin rather superior to cefazolin, ampicillin, piperacillin, gentamicin. Resistant to gentamycin, cephalosporin strains are still sensitive to fleroxacin. The frequency of single-step spontaneous mutagenesis of fleroxacin by bacteria is extremely low, but highly resistant to fleroxacin can be produced by continuous subculturing.