[Transferability of biapenem (L-627) to cerebrospinal fluid in rabbits with meningitis caused by Staphylococcus aureus].
The transferability of biapenem (L-627) to cerebrospinal fluid (CSF) was studied employing rabbits with experimental meningitis caused by Staphylococcus aureus. The mean plasma concentration was 192 +/- 12.8 micrograms/ml at 15 minutes after intravenous administration of the drug at a dose level of 100 mg/kg. The mean concentration in CSF was maximum at 45 minutes after administration at 11.4 +/- 2.19 micrograms/ml. Pharmacokinetic parameters calculated from these values were as follows, Cmax (CSF/plasma): 5.96%; AUC (CSF/plasma): 8.15% between 15 and 60 minutes, 12.1% between 15 and 120 minutes and 15.0% between 15 and 180 minutes; T1/2 for L-627 in CSF: 152 minutes; T1/2 (CSF/plasma): 3.34. In comparison with those of other beta-lactam antibiotics that were obtained in the same way, the transferability of L-627 was intermediate, and in consideration of the antimicrobial potency against the main pathogens of meningitis, it appears worthwhile of running clinical trials for this drug.
Haruta
T
T
Department of Pediatrics, Kobe City General Hospital.
Kuroki
S
S
Okura
K
K
Nikami
H
H
Nishio
T
T
Kobayashi
Y
Y
D000818:Animals; 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; D013845:Thienamycins / Q000134:cerebrospinal fluid / Q000493:pharmacokinetics*
D013845:Thienamycins; C065257:biapenem