Chadwick E G, Yogev R, Shulman S T, Weinfeld R E, Patel I H
J Pediatr. 1983 Jan;102(1):134-7. doi: 10.1016/s0022-3476(83)80311-4.
Ceftriaxone has greater in vitro and in vivo efficacy against many common bacteria than other third-generation cephalosporins. Single-dose ceftriaxone pharmacokinetics were studied in 17 patients, aged 0.6 to 52 months, with infections of the central nervous system. Patients received a randomized dose of 50 or 75 mg/kg ceftriaxone intravenously over 5 minutes on the second to fifth day of illness. Serial blood samples were collected over 24 hours in all patients, and cerebrospinal fluid (CSF) was obtained 1 to 4.5 hours after injection. Ceftriaxone mean peak plasma concentrations, determined by high-power liquid chromatography, were 267 and 184 microgram/ml for the 75 and 50 mg/kg dosage groups, respectively. The harmonic mean elimination half-life was 4.2 hours, and the mean percent drug penetrance into CSF was 4.8 +/- 3.5%. Of CSF studies evaluated, the glucose concentration was correlated most closely (inversely) with CSF penetration of ceftriaxone. Individual CSF concentrations of ceftriaxone exceeded the minimal inhibitory concentrations of the respective bacteria causing infection by 480 to 5,600 times. Ceftriaxone may be useful in the treatment of serious pediatric infections, including meningitis.
与其他第三代头孢菌素相比,头孢曲松对许多常见细菌具有更强的体外和体内疗效。对17例年龄在0.6至52个月之间患有中枢神经系统感染的患者进行了单剂量头孢曲松的药代动力学研究。患者在发病的第二至第五天,在5分钟内静脉注射50或75mg/kg的随机剂量头孢曲松。所有患者在24小时内采集系列血样,并在注射后1至4.5小时获取脑脊液(CSF)。通过高效液相色谱法测定,75mg/kg和50mg/kg剂量组的头孢曲松平均血浆峰浓度分别为267和184μg/ml。谐波平均消除半衰期为4.2小时,药物进入脑脊液的平均百分比为4.8±3.5%。在评估的脑脊液研究中,葡萄糖浓度与头孢曲松的脑脊液渗透率相关性最密切(呈负相关)。头孢曲松的个体脑脊液浓度超过引起感染的相应细菌的最低抑菌浓度480至5600倍。头孢曲松可能对治疗包括脑膜炎在内的严重儿科感染有用。