Suzuki Yumiko, Nishinari Chisato, Endo Harumi, Hiramatsu Nobuyoshi, Akiyama Kazumitsu, Koyama Tsuneo
Section of Studies, Tokyo Clinical Research Center.
Jpn J Antibiot. 2003 Aug;56(4):294-308.
The in vitro antibacterial activities of cefozopran (CZOP), an agent of cephems, against various clinical isolates obtained between 1996 and 2001 were yearly evaluated and compared with those of other cephems, oxacephems, carbapenems, and penicillins. A total of 1,274 strains in 15 species of Gram-positive bacteria were isolated from the clinical materials annually collected from January to December, and consisted of methicillin-susceptible Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus epidermidis, Staphylococcus haemolyticus, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus pneumoniae, Enterococcus faecalis, Enterococcus faecium, Enterococcus avium, and Peptostreptococcus spp. CZOP possessed stable antibacterial activities against all strains tested throughout 6 years. The MIC90 of CZOP against MRSA and S. haemolyticus tended to decrease while against S. pneumoniae and Peptostreptococcus spp., tended to increase year by year. However, the MIC90 just changed a little and were consistent with the results from the studies performed until the new drug application approval. Increases in the MIC90 against S. pneumoniae were also observed with ceftazidime (CPR), cefepime (CFPM), flomoxef (FMOX), sulbactam/cefoperazone (SBT/CPZ), and imipenem (IPM). Increases in the MIC90 against Peptostreptococcus spp. were also observed with FMOX, SBT/CPZ, and IPM. In conclusion, the annual antibacterial activities of CZOP against the Gram-positive bacteria did not considerably change. It, therefore, was suggested that CZOP had maintained high antibacterial activity during 6 years of post marketing.
头孢唑肟(CZOP)是一种头孢菌素类药物,对1996年至2001年间分离出的各种临床分离株进行了体外抗菌活性的年度评估,并与其他头孢菌素类、氧头孢烯类、碳青霉烯类和青霉素类药物进行了比较。每年1月至12月从临床材料中分离出15种革兰氏阳性菌的1274株菌株,包括甲氧西林敏感金黄色葡萄球菌(MSSA)、甲氧西林耐药金黄色葡萄球菌(MRSA)、表皮葡萄球菌、溶血葡萄球菌、化脓性链球菌、无乳链球菌、肺炎链球菌、粪肠球菌、屎肠球菌、鸟肠球菌和消化链球菌属。在6年期间,CZOP对所有测试菌株均具有稳定的抗菌活性。CZOP对MRSA和溶血葡萄球菌的MIC90呈下降趋势,而对肺炎链球菌和消化链球菌属则逐年上升。然而,MIC90变化不大,与新药申请批准前进行的研究结果一致。头孢他啶(CPR)、头孢吡肟(CFPM)、氟氧头孢(FMOX)、舒巴坦/头孢哌酮(SBT/CPZ)和亚胺培南(IPM)对肺炎链球菌的MIC90也有升高。FMOX、SBT/CPZ和IPM对消化链球菌属的MIC90也有升高。总之,CZOP对革兰氏阳性菌的年度抗菌活性没有显著变化。因此,提示CZOP在上市后的6年中保持了较高的抗菌活性。