Haruta T, Okura K, Kuroki S, Nikami H, Kobayashi Y
Department of Pediatrics, Kobe City General Hospital, Japan.
Jpn J Antibiot. 1996 May;49(5):517-21.
The transferability of cefozopran (CZOP) to cerebrospinal fluid (CSF) was studied employing rabbits with experimental meningitis caused by Staphylococcus aureus. The mean plasma concentration was 293 +/- 17.6 micrograms/ml at 15 minutes after intravenous administration of CZOP at a dose level of 100 mg/kg. The mean concentration in CSF reached its maximum, 16.5 +/- 2.74 micrograms/ml at 60 minutes after administration. Pharmacokinetic parameters calculated from these values were as follows: Cmax (CSF/plasma) 5.72%, AUC (CSF/plasma) 6.61% between 15 and 60 minutes, 9.38% between 15 and 120 minutes and 11.2% between 15 and 180 minutes, T 1/2 for CZOP in CSF: 138 minutes, T 1/2 (CSF/plasma): 2.81. In comparison to those of beta-lactams that were obtained in the same way, the transferability of CZOP to CSF was moderate but concentration in CSF was high, hence, in consideration of the antimicrobial potency against the main pathogens of meningitis, it appears worthwhile of running clinical trials for CZOP.
采用由金黄色葡萄球菌引起实验性脑膜炎的家兔，研究了头孢唑啉（CZOP）向脑脊液（CSF）的转移情况。以100mg/kg的剂量静脉注射CZOP后15分钟时，平均血浆浓度为293±17.6μg/ml。给药后60分钟时，脑脊液中的平均浓度达到最高值，为16.5±2.74μg/ml。根据这些值计算的药代动力学参数如下：15至60分钟时Cmax（脑脊液/血浆）为5.72%，AUC（脑脊液/血浆）为6.61%；15至120分钟时为9.38%；15至180分钟时为11.2%。CZOP在脑脊液中的T 1/2为138分钟，T 1/2（脑脊液/血浆）为2.81。与以同样方式获得的β-内酰胺类药物相比，CZOP向脑脊液的转移能力中等，但脑脊液中的浓度较高，因此，考虑到对脑膜炎主要病原体的抗菌效力，对CZOP进行临床试验似乎是值得的。
