Eickhoff T C, Ehret J
Antimicrob Agents Chemother. 1981 Mar;19(3):435-42. doi: 10.1128/AAC.19.3.435.
The in vitro activity of Ro 13-9904, a new cephalosporin derivative, was compared with the activities of cephalothin, cefamandole, cefoxitin, cefotaxime, and moxalactam against 591 clinical isolates of gram-negative and gram-positive organisms. The spectra of activity and potency of Ro 13-9904 and cefotaxime were quite similar; they were the most active agents against Enterobacteriaceae, Streptococcus pyogenes, Haemophilus influenzae, Neisseria gonorrhoeae, and Neisseria meningitidis. Moxalactam was only slightly less active against these organisms. Ro 13-9904, cefotaxime, and moxalactam were approximately equal in activity against Pseudomonas aeruginosa; concentrations of 50 to 100 microgram/ml inhibited over 90% of the strains tested. Cefamandole and cephalothin were the most active drugs tested against staphylococci. Moxalactam demonstrated the highest intrinsic activity against Bacteroides fragilis; a concentration of 1.6 microgram/ml inhibited over 50% of the strains. All six of the antibiotics were essentially inactive against group D streptococci. The action of all of the antibiotics was bactericidal, with minimal bactericidal concentrations generally being no more than twofold greater than minimal inhibitory concentrations. The only exception to this was found when large inocula of Staphylococcus aureus were tested. Increased inoculum size generally sharply reduced the activity of Ro 13-9904, cefotaxime, and moxalactam against Enterobacteriaceae and P. aeruginosa.
将新型头孢菌素衍生物Ro 13-9904的体外活性与头孢噻吩、头孢孟多、头孢西丁、头孢噻肟和莫西沙星对591株革兰氏阴性和革兰氏阳性临床分离菌的活性进行了比较。Ro 13-9904和头孢噻肟的活性谱和效价非常相似;它们是对肠杆菌科、化脓性链球菌、流感嗜血杆菌、淋病奈瑟菌和脑膜炎奈瑟菌最具活性的药物。莫西沙星对这些菌的活性略低。Ro 13-9904、头孢噻肟和莫西沙星对铜绿假单胞菌的活性大致相当;50至100微克/毫升的浓度可抑制90%以上的受试菌株。头孢孟多和头孢噻吩是受试药物中对葡萄球菌最具活性的。莫西沙星对脆弱拟杆菌显示出最高的内在活性;1.6微克/毫升的浓度可抑制50%以上的菌株。所有六种抗生素对D组链球菌基本无活性。所有抗生素的作用均为杀菌性,最小杀菌浓度通常不超过最小抑菌浓度的两倍。唯一的例外是在测试金黄色葡萄球菌的大接种量时发现的。接种量增加通常会大幅降低Ro 13-9904、头孢噻肟和莫西沙星对肠杆菌科和铜绿假单胞菌的活性。