Beskid G, Christenson J G, Cleeland R, DeLorenzo W, Trown P W
Antimicrob Agents Chemother. 1981 Aug;20(2):159-67. doi: 10.1128/AAC.20.2.159.
Ceftriaxone (Ro 13-9904) was compared with other newer beta-lactam antibiotics for activity in experimental infections of mice with Enterobacteriaceae, Haemophilus influenzae, Pseudomonas aeruginosa, and gram-positive bacteria. Overall, ceftriaxone was equal or superior to cefotaxime and cefoperazone against systemic infections. All three drugs were highly potent against most organisms but were considerably less active against P. aeruginosa. However, ceftriaxone tended to be more active than the other two agents against 8 of the 10 P. aeruginosa strains tested. Ceftriaxone, cefmenoxime (SCE 1365), and moxalactam were all highly active against systemic infections with 16 strains of Enterobacteriaceae, whereas ceftriaxone was more active against infections with two strains of streptococci. When the drugs were administered at various time intervals before infection, ceftriaxone was superior to cefotaxime, cefmenoxime, and moxalactam. This suggested that ceftriaxone might be eliminated from mice more slowly than the other drugs. In the case of cefotaxime, this was directly confirmed by microbiological assays of plasma samples. In a murine meningitis model induced by Klebsiella pneumoniae or Streptococcus pneumoniae, ceftriaxone was more active than ampicillin or cefotaxime. Ceftriaxone was more active than ampicillin, cefotaxime, piperacillin, cefamandole, or carbenicillin in a pneumococcal, pneumonia model in mice. These studies indicate that ceftriaxone is a potent, broad-spectrum cephalosporin with unusual pharmacokinetic properties.
将头孢曲松（Ro 13-9904）与其他新型β-内酰胺类抗生素进行比较，观察其对感染肠杆菌科细菌、流感嗜血杆菌、铜绿假单胞菌和革兰氏阳性菌的小鼠的实验性感染的活性。总体而言，在全身感染方面，头孢曲松与头孢噻肟和头孢哌酮相当或更优。这三种药物对大多数微生物都具有高效活性，但对铜绿假单胞菌的活性则显著较低。然而，在测试的10株铜绿假单胞菌菌株中，头孢曲松对其中8株的活性往往高于其他两种药物。头孢曲松、头孢甲肟（SCE 1365）和拉氧头孢对16株肠杆菌科细菌引起的全身感染均具有高效活性，而头孢曲松对两株链球菌感染的活性更高。当在感染前不同时间间隔给药时，头孢曲松优于头孢噻肟、头孢甲肟和拉氧头孢。这表明头孢曲松从小鼠体内消除的速度可能比其他药物慢。对于头孢噻肟，通过对血浆样本的微生物学测定直接证实了这一点。在由肺炎克雷伯菌或肺炎链球菌诱导的小鼠脑膜炎模型中，头孢曲松比氨苄西林或头孢噻肟更具活性。在小鼠肺炎球菌性肺炎模型中，头孢曲松比氨苄西林、头孢噻肟、哌拉西林、头孢孟多或羧苄西林更具活性。这些研究表明，头孢曲松是一种具有独特药代动力学特性的高效、广谱头孢菌素。
