O'Callaghan C H, Acred P, Harper P B, Ryan D M, Kirby S M, Harding S M
Antimicrob Agents Chemother. 1980 May;17(5):876-83. doi: 10.1128/AAC.17.5.876.
GR 20263 is a new broad-spectrum injectable cephalosporin which is stable to most beta-lactamases. Its in vitro activities were of the same order as those of cefotaxime against most gram-negative bacteria, were clearly inferior to cefotaxime against Staphylococcus aureus, but were significantly more active against Pseudomonas aeruginosa. Against the 25 strains used, GR 20263 was significantly more active than any of the other agents tested: piperacillin, azlocillin, gentamicin, amikacin, and carbenicillin. GR 20263 protected mice against experimental infections with P. aeruginosa more effectively than other beta-lactam antibiotics; its general effectiveness in this test was comparable with gentamicin. Studies on human volunteers showed that it produces high, long-lasting blood levels, with much of the antibiotic being recovered in the urine. Intramuscular and intravenous injections were well tolerated by the volunteers, and there were no untoward side effects.
GR 20263是一种新型的广谱注射用头孢菌素，对大多数β-内酰胺酶稳定。其体外活性与头孢噻肟对大多数革兰氏阴性菌的活性相当，对金黄色葡萄球菌的活性明显低于头孢噻肟，但对铜绿假单胞菌的活性显著更高。在所用的25株菌株中，GR 20263的活性明显高于其他任何受试药物：哌拉西林、阿洛西林、庆大霉素、阿米卡星和羧苄西林。GR 20263比其他β-内酰胺抗生素更有效地保护小鼠免受铜绿假单胞菌的实验性感染；其在该试验中的总体有效性与庆大霉素相当。对人类志愿者的研究表明，它能产生高且持久的血药浓度，大部分抗生素从尿液中回收。志愿者对肌肉注射和静脉注射耐受性良好，且无不良副作用。
