Sanders C C, Sanders W E, Goering R V
Antimicrob Agents Chemother. 1978 Aug;14(2):178-84. doi: 10.1128/AAC.14.2.178.
In vitro tests were performed with Sch 21420 and Sch 22591 to determine (i) their activity in comparison to six other aminoglycosides against 343 clinical isolates, and (ii) whether synergy with penicillin G could be demonstrated with enterococci. In broth dilution tests, Sch 22591 was more active than the seven other aminoglycosides against Staphylococcus aureus, Enterobacteriaceae, and most nonfermenting gram-negative bacilli. Sch 22591 was as active as tobramycin against Pseudomonas aeruginosa. The activity of Sch 21420 was comparable to gentamicin, sisomicin, netilmicin, and tobramycin but greater than amikacin or kanamycin against S. aureus and most genera of Enterobacteriaceae. Sch 21420, amikacin, and kanamycin were (i) more active than the other five aminoglycosides against Proteus rettgeri and Providencia stuartii, but (ii) less active than the other five aminoglycosides against Neisseria gonorrhoeae, enterococci, most nonfermenting gram-negative bacilli, Proteus mirabilis, and Proteus morganii. Studies on the bactericidal activity of Sch 22591 with penicillin indicated a synergistic interaction against enterococci, including strains highly resistant to streptomycin and kanamycin. This could be demonstrated with combinations containing 3.0 to 6.0 mug of Sch 22591 per ml and was comparable to that observed with penicillin/gentamicin. Penicillin plus Sch 21420 (25 mug/ml) also demonstrated synergy against enterococci, including strains highly resistant to streptomycin. However, synergy did not occur against strains highly resistant to kanamycin. These latter results were similar to those obtained in tests with penicillin/kanamycin.
使用Sch 21420和Sch 22591进行了体外试验,以确定:(i)与其他六种氨基糖苷类药物相比,它们对343株临床分离菌的活性;(ii)是否能证明与青霉素G对肠球菌有协同作用。在肉汤稀释试验中,Sch 22591对金黄色葡萄球菌、肠杆菌科细菌和大多数非发酵革兰氏阴性杆菌的活性比其他七种氨基糖苷类药物更强。Sch 22591对铜绿假单胞菌的活性与妥布霉素相当。Sch 21420对金黄色葡萄球菌和大多数肠杆菌科菌属的活性与庆大霉素、西索米星、奈替米星和妥布霉素相当,但强于阿米卡星或卡那霉素。Sch 21420、阿米卡星和卡那霉素:(i)对雷氏普罗威登斯菌和斯氏普罗威登斯菌的活性比其他五种氨基糖苷类药物更强,但(ii)对淋病奈瑟菌、肠球菌、大多数非发酵革兰氏阴性杆菌、奇异变形杆菌和摩根氏变形杆菌的活性低于其他五种氨基糖苷类药物。关于Sch 22591与青霉素杀菌活性的研究表明,其对肠球菌有协同相互作用,包括对链霉素和卡那霉素高度耐药的菌株。这在每毫升含3.0至6.0微克Sch 22591的组合中得到证实,且与青霉素/庆大霉素观察到的情况相当。青霉素加Sch 21420(25微克/毫升)也证明对肠球菌有协同作用,包括对链霉素高度耐药的菌株。然而,对卡那霉素高度耐药的菌株未出现协同作用。后一组结果与青霉素/卡那霉素试验中获得的结果相似。