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两种新型喹诺酮类药物:芦氟沙星和MF 961的体外活性

The in-vitro activity of two new quinolones: rufloxacin and MF 961.

作者信息

Wise R, Andrews J M, Matthews R, Wolstenholme M

机构信息

Department of Medical Microbiology, Dudley Road Hospital, Birmingham, UK.

出版信息

J Antimicrob Chemother. 1992 Jun;29(6):649-60. doi: 10.1093/jac/29.6.649.

Abstract

The in-vitro activity of two new quinolone antimicrobials, rufloxacin and MF 961, together with the desmethylated metabolite of rufloxacin (MF 922) were compared with other orally administered agents against 622 bacterial strains. Against Enterobacteriaceae and Pseudomonas aeruginosa rufloxacin was generally active (MIC90 1-8 mg/L) with the exception of Klebsiella and Serratia spp. (MIC90 32 mg/L and Enterobacter spp. (MIC90) 64 mg/L. The respiratory pathogens Haemophilus influenzae and Moraxella catarrhalis were susceptible to rufloxacin (MIC90 0.5 and 1 mg/L respectively) but Streptococcus pneumoniae was less susceptible (MIC90 32 mg/L). Staphylococcus aureus were susceptible to rufloxacin (MIC90 2 mg/L). The rufloxacin metabolite MF 922 was generally as active as its parent. MF 961 was usually two-fold more active than rufloxacin. All three compounds were four to 16 times less active than norfloxacin, but rufloxacin was as active or somewhat more active than norfloxacin against Staphylococcus spp. Any strains showing decreased susceptibility to other quinolones exhibited cross resistance to these new agents. The MBC of rufloxacin and MF 922 was within one dilution of the MIC and human serum had little effect upon the activity of both agents. The protein binding of rufloxacin and MF 922 at 1 and 10 mg/L were 55% and 63.8% and 30.3% and 32.6% respectively. The activity of rufloxacin against four strains of Chlamydia trachomatis and one strain of Chlamydia pneumoniae was determined. The MICs for C. trachomatis were 4-8 mg/L and 4 mg/L for C. pneumoniae.

摘要

将两种新型喹诺酮类抗菌药物鲁氟沙星和MF 961及其去甲基代谢产物鲁氟沙星(MF 922)的体外活性与其他口服制剂对622株细菌进行了比较。对于肠杆菌科和铜绿假单胞菌,鲁氟沙星通常具有活性(MIC90为1 - 8mg/L),但肺炎克雷伯菌和沙雷菌属(MIC90为32mg/L)以及阴沟肠杆菌(MIC90为64mg/L)除外。呼吸道病原体流感嗜血杆菌和卡他莫拉菌对鲁氟沙星敏感(MIC90分别为0.5和1mg/L),但肺炎链球菌敏感性较低(MIC90为32mg/L)。金黄色葡萄球菌对鲁氟沙星敏感(MIC90为2mg/L)。鲁氟沙星代谢产物MF 922的活性通常与其母体相当。MF 961的活性通常比鲁氟沙星高两倍。所有这三种化合物的活性比诺氟沙星低4至16倍,但鲁氟沙星对葡萄球菌属的活性与诺氟沙星相当或略高。任何对其他喹诺酮类药物敏感性降低的菌株对这些新药物均表现出交叉耐药性。鲁氟沙星和MF 922的MBC在MIC的一个稀释度范围内,人血清对这两种药物的活性影响很小。鲁氟沙星和MF 922在1mg/L和10mg/L时的蛋白结合率分别为55%和63.8%以及30.3%和32.6%。测定了鲁氟沙星对四株沙眼衣原体和一株肺炎衣原体的活性。沙眼衣原体的MIC为4 - 8mg/L,肺炎衣原体的MIC为4mg/L。

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