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八种新型喹诺酮类药物与萘啶酸的体外活性比较

The comparative in-vitro activity of eight newer quinolones and nalidixic acid.

作者信息

King A, Phillips I

出版信息

J Antimicrob Chemother. 1986 Nov;18 Suppl D:1-20. doi: 10.1093/jac/18.supplement_d.1.

DOI:10.1093/jac/18.supplement_d.1
PMID:3468100
Abstract

The in-vitro antibacterial activity of nalidixic acid and the 4-quinolones, ciprofloxacin, norfloxacin, enoxacin, ofloxacin, pefloxacin, A-56619, A-56620 and CI-934 was assessed by determination of MICs. The 4-quinolones were all highly active against most isolates of Enterobacteriaceae, including nalidixic acid-resistant strains. Ciprofloxacin (MICs 0.002-2 mg/l) was the most active and A-56619 (MICs 0.008-32 mg/l) was the least active. A-56619, A-56620, ofloxacin, ciprofloxacin and CI-934 were highly active against Acinetobacter strains, pefloxacin and enoxacin were slightly less active, and a few strains were resistant to norfloxacin. All the compounds, including nalidixic acid, were active against Aeromonas strains (MICs 0.001-0.12 mg/l). Ciprofloxacin (MICs 0.06-1 mg/l) was the most active compound against Pseudomonas aeruginosa; A-56619 and CI-934 (MICs 1-16 mg/l) were the least active against this species. All the compounds were highly active against Haemophilus influenzae, Branhamella catarrhalis and Neisseria gonorrhoeae but the activity of all the compounds was poor against most isolates of Gardnerella vaginalis. All the 4-quinolones were active against staphylococci and CI-934 (MICs 0.03-0.25 mg/l) was the most active. CI-934 (MICs 0.06-2 mg/l) was also the most active compound against all streptococci. Most streptococci were sensitive also to ciprofloxacin (MICs 0.25-4 mg/l) but there were many isolates resistant to the other 4-quinolones. Against the anaerobic bacteria CI-934 was again the most active compound, particularly against the Gram-positive anaerobic cocci. Pefloxacin, enoxacin and norfloxacin had poor activity against most anaerobes. Ofloxacin, ciprofloxacin, A-56619 and A-56620 had good to moderate activity against all species of anaerobes except the Bacteroides fragilis group, against which none of the compounds was very active.

摘要

通过测定最低抑菌浓度(MIC)来评估萘啶酸及4-喹诺酮类药物环丙沙星、诺氟沙星、依诺沙星、氧氟沙星、培氟沙星、A-56619、A-56620和CI-934的体外抗菌活性。4-喹诺酮类药物对大多数肠杆菌科细菌分离株均具有高度活性,包括对萘啶酸耐药的菌株。环丙沙星(MIC为0.002 - 2mg/L)活性最强,A-56619(MIC为0.008 - 32mg/L)活性最弱。A-56619、A-56620、氧氟沙星、环丙沙星和CI-934对不动杆菌属菌株具有高度活性,培氟沙星和依诺沙星活性稍弱,少数菌株对诺氟沙星耐药。所有化合物,包括萘啶酸,对气单胞菌属菌株均有活性(MIC为0.001 - 0.12mg/L)。环丙沙星(MIC为0.06 - 1mg/L)是对铜绿假单胞菌活性最强的化合物;A-56619和CI-934(MIC为1 - 16mg/L)对该菌活性最弱。所有化合物对流感嗜血杆菌、卡他布兰汉菌和淋病奈瑟菌均具有高度活性,但对大多数阴道加德纳菌分离株活性较差。所有4-喹诺酮类药物对葡萄球菌均有活性,CI-934(MIC为0.03 - 0.25mg/L)活性最强。CI-934(MIC为0.06 - 2mg/L)也是对所有链球菌活性最强的化合物。大多数链球菌对环丙沙星(MIC为0.25 - 4mg/L)也敏感,但有许多分离株对其他4-喹诺酮类药物耐药。对于厌氧菌,CI-934同样是活性最强的化合物,尤其是对革兰氏阳性厌氧球菌。培氟沙星、依诺沙星和诺氟沙星对大多数厌氧菌活性较差。氧氟沙星、环丙沙星、A-56619和A-56620对除脆弱拟杆菌群以外的所有厌氧菌均具有良好至中等活性,而所有化合物对脆弱拟杆菌群的活性均不强。

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