Arpi M, Gahrn-Hansen B, Søgaard P, Bentzon M W
Acta Pathol Microbiol Immunol Scand B. 1987 Apr;95(2):141-6. doi: 10.1111/j.1699-0463.1987.tb03102.x.
The antibacterial activity of four new fluoroquinolone carboxylic acids, pefloxacin, ofloxacin, enoxacin and ciprofloxacin, against 256 clinical isolates was investigated by means of an agar dilution method. Generally, all quinolones tested had a high activity against Gram-negative bacteria. More than 90% of Enterobacteriaceae strains were inhibited by a quinolone concentration of 0.4 microgram/ml. Also strains usually resistant to conventional beta-lactam antibiotics, and sometimes to third-generation cephalosporins, like Enterobacter spp., Serratia spp, and Yersinia spp. were susceptible to the tested quinolones. Ciprofloxacin was 5 to 25-fold more potent on a weight basis against Enterobacteriaceae than the other quinolones. Neisseria meningitidis, Neisseria gonorrhoeae, and Haemophilus influenzae were extremely susceptible to the new quinolones. Ciprofloxacin was about 10 times more potent against Pseudomonas aeruginosa than the other quinolones, and was the only quinolone that was sufficiently active against all tested P. aeruginosa strains (MIC less than or equal to 0.4 microgram/ml). The activity against Gram-positive bacteria was considerably lower. All the quinolones investigated had an acceptable activity against many of the methicillin-sensitive and methicillin-resistant Staphylococcus aureus and coagulase-negative staphylococci. The majority of the Streptococcus spp. tested was quinolone-resistant, and was Listeria monocytogenes. Generally, it was evident that ciprofloxacin was more potent on a weight basis than the other quinolones, but this difference was counterbalanced by a higher achievable serum concentration for ofloxacin. Some of the investigated fluoroquinolones might constitute valid therapeutical alternatives to beta-lactam antibodies and aminoglycosides in the treatment of serious bacterial infections.
采用琼脂稀释法研究了四种新型氟喹诺酮羧酸类药物，即培氟沙星、氧氟沙星、依诺沙星和环丙沙星对256株临床分离菌的抗菌活性。总体而言，所有测试的喹诺酮类药物对革兰氏阴性菌均具有高活性。浓度为0.4微克/毫升的喹诺酮类药物可抑制90%以上的肠杆菌科菌株。此外，通常对传统β-内酰胺类抗生素耐药，有时对第三代头孢菌素耐药的菌株，如肠杆菌属、沙雷氏菌属和耶尔森菌属，对测试的喹诺酮类药物敏感。以重量计，环丙沙星对肠杆菌科的活性比其他喹诺酮类药物高5至25倍。脑膜炎奈瑟菌、淋病奈瑟菌和流感嗜血杆菌对新型喹诺酮类药物极为敏感。环丙沙星对铜绿假单胞菌的活性比其他喹诺酮类药物高约10倍，并且是唯一对所有测试的铜绿假单胞菌菌株均具有足够活性（最低抑菌浓度小于或等于0.4微克/毫升）的喹诺酮类药物。其对革兰氏阳性菌的活性明显较低。所有研究的喹诺酮类药物对许多甲氧西林敏感和甲氧西林耐药的金黄色葡萄球菌及凝固酶阴性葡萄球菌均具有可接受的活性。大多数测试的链球菌属对喹诺酮类药物耐药，单核细胞增生李斯特菌也耐药。总体而言，很明显以重量计环丙沙星比其他喹诺酮类药物更有效，但氧氟沙星可达到的更高血清浓度抵消了这种差异。一些研究的氟喹诺酮类药物在治疗严重细菌感染方面可能构成β-内酰胺类抗体和氨基糖苷类药物的有效治疗替代方案。
