title: [Transferability of cefozopran to cerebrospinal fluid in rabbits with meningitis caused by Staphylococcus aureus].
abstract: 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.
authors: Department of Pediatrics, Kobe City General Hospital, Japan.
authors: T
authors: T
authors: Haruta
authors: K
authors: K
authors: Okura
authors: S
authors: S
authors: Kuroki
authors: H
authors: H
authors: Nikami
authors: Y
authors: Y
authors: Kobayashi
mesh_terms: D000818:Animals; D001692:Biological Transport; D002511:Cephalosporins / Q000097:blood / Q000134:cerebrospinal fluid / Q000493:pharmacokinetics*; D006207:Half-Life; D016920:Meningitis, Bacterial / Q000097:blood / Q000134:cerebrospinal fluid / Q000188:drug therapy*; D011817:Rabbits; D013203:Staphylococcal Infections / Q000097:blood / Q000134:cerebrospinal fluid / Q000188:drug therapy*; D014018:Tissue Distribution; D000097586:Cefozopran
chemical_list: D002511:Cephalosporins; D000097586:Cefozopran