Patamasucon P, McCracken G H
Antimicrob Agents Chemother. 1982 Mar;21(3):390-2. doi: 10.1128/AAC.21.3.390.
The pharmacokinetics and bacteriological efficacy of N-formimidoyl thienamycin were determined in rabbits infected with Escherichia coli K1. After a single intravenous dose of 25 mg/kg, a peak N-formimidoyl thienamycin concentration in cerebrospinal fluid (CSF) of 2.5 micrograms/ml was attained at 45 min. The penetration into CSF was calculated to be 31%. In animals that received continuous intravenous infusions of the drug for 9 h, the mean CSF concentration was 8.2 microgram/ml, and the CSF bactericidal titers against the E. coli K1 strain were from 1:16 to 1:32. This infusion produced a reduction in the numbers of E. coli in the CSF of 4 log10 colony-forming units per ml. N-Formimidoyl thienamycin might prove to be useful for therapy of meningitis caused by E. coli and other susceptible bacteria.
测定了N-甲酰亚胺硫霉素在感染大肠杆菌K1的家兔体内的药代动力学和细菌学疗效。单次静脉注射剂量为25mg/kg后，45分钟时脑脊液（CSF）中N-甲酰亚胺硫霉素的峰值浓度达到2.5μg/ml。计算得出其进入脑脊液的渗透率为31%。在接受该药物持续静脉输注9小时的动物中，脑脊液平均浓度为8.2μg/ml，针对大肠杆菌K1菌株的脑脊液杀菌效价为1:16至1:32。这种输注使脑脊液中大肠杆菌数量每毫升减少4个对数10集落形成单位。N-甲酰亚胺硫霉素可能被证明对治疗由大肠杆菌和其他易感细菌引起的脑膜炎有用。
