Nahata M C, Kohlbrenner V M, Barson W J
College of Pharmacy, Ohio State University, Columbus 43210.
Chemotherapy. 1993;39(1):1-5. doi: 10.1159/000238966.
Limited data are available about cefixime pharmacokinetics and cerebrospinal fluid (CSF) penetration in infants and young children. Ten patients with bacterial meningitis and 8 undergoing CSF shunt placement, aged 2-22 months (mean 9.5 +/- 6.5 months), were given a single dose of cefixime suspension, 8 mg/kg, before undergoing a routine lumbar puncture. Patients were fasted for 2 h before and 2 h after drug administration. Blood samples were collected just before drug administration (0 h) and at 1, 2, 3, 4, 6, 8 h; CSF was obtained at 1-8.8 h after drug administration. Cefixime was measured by a high-performance liquid chromatographic method. The peak serum concentration of cefixime ranged from 0.85 to 6.2 (mean 3.1) micrograms/ml and occurred at 2-8 h (mean 4.5). The area under the serum concentration-time curve ranged from 5.3 to 28.4 micrograms h/ml, and the elimination half-life ranged from 2.6 to 5.6 h. CSF concentrations ranged from 0.02 to 0.57 micrograms/ml. The mean CSF concentration of cefixime was 0.22 micrograms/ml in patients with meningitis and 0.10 microgram/ml in those undergoing shunt placement (p < 0.02). The mean CSF concentration/serum concentration ratio was 11.7 in patients with meningitis compared with 5.4 in those undergoing shunt procedures (p < 0.02). These data indicate that cefixime can be considered as an alternative to other antimicrobials for infants and children with respiratory and urinary tract infections, since the observed peak serum concentration exceeded the minimum inhibitory concentrations of the common pathogens by severalfold.(ABSTRACT TRUNCATED AT 250 WORDS)
关于头孢克肟在婴幼儿中的药代动力学及脑脊液穿透情况的数据有限。10例细菌性脑膜炎患儿及8例接受脑脊液分流术的患儿,年龄2 - 22个月(平均9.5±6.5个月),在进行常规腰椎穿刺前给予单剂量8mg/kg的头孢克肟混悬液。给药前2小时及给药后2小时患儿禁食。在给药前(0小时)及给药后1、2、3、4、6、8小时采集血样;给药后1 - 8.8小时采集脑脊液。采用高效液相色谱法测定头孢克肟。头孢克肟的血清峰值浓度为0.85至6.2(平均3.1)μg/ml,出现在给药后2 - 8小时(平均4.5小时)。血清浓度 - 时间曲线下面积为5.3至28.4μg·h/ml,消除半衰期为2.6至5.6小时。脑脊液浓度为0.02至0.57μg/ml。脑膜炎患儿头孢克肟的平均脑脊液浓度为0.22μg/ml,接受分流术患儿为0.10μg/ml(p<0.02)。脑膜炎患儿的平均脑脊液浓度/血清浓度比值为11.7,接受分流术患儿为5.4(p<0.02)。这些数据表明,对于患有呼吸道和泌尿道感染的婴幼儿,头孢克肟可被视为其他抗菌药物的替代药物,因为观察到的血清峰值浓度超过常见病原体的最低抑菌浓度数倍。(摘要截短至250字)