Iwai N, Miyazu M, Katayama M, Taneda Y, Nakamura H, Ozaki T, Tauchi N, Yamaguchi H
Department of Pediatrics, Meitetsu Hospital.
Jpn J Antibiot. 1988 Aug;41(8):1087-105.
Pharmacokinetic, bacteriological and clinical studies of ceftizoxime (CZX) were performed in neonates. 1. Serum concentrations and urinary excretion of CZX were investigated in 12 neonates ranging ages from 1 to 27 days (gestational age, 35-41 weeks; birth weight, 2,150-4,030 g) and 2 infants ranging ages from 55 to 57 days (gestational age, 39-40 weeks; birth weight, 2,320-2,650 g). Each of the subjects was given a single intravenous dose of 20 mg/kg by one shot. Serum concentrations of CZX in the neonates were 24.9-53.7 micrograms/ml at 1/4 hour after intravenous injection, with an average of 40.6 +/- 7.6 micrograms/ml. Serum half-lives of CZX were 1.32-4.75 hours and averaged 2.60 +/- 1.06 hours. Serum concentrations ranged from 2.01 to 14.6 micrograms/ml at 6 hours after injection with an average of 7.70 +/- 3.89 micrograms/ml. In the 2 infants, serum concentrations were 42.0 and 46.2 micrograms/ml at 1/4 hour (average: 44.1 +/- 3.0 micrograms/ml), and 2.91 and 5.04 micrograms/ml at 6 hours after injection (average: 3.98 +/- 1.51 micrograms/ml). Half-lives were 1.54 hours in 1 infant and 1.93 hours in the other (average: 1.74 +/- 0.28 hours). Furthermore, 6-hour urinary recovery rates were 28.5-71.7% (average: 49.3 +/- 12.8%) in the neonates and 42.1-55.5% (average: 48.8 +/- 9.5%) in the infants. The above results suggest that the following 3 points are accepted; 1) peak serum concentrations (at 1/4 hour) in neonates were similar to those in infants and older children irrespective of age (days after birth). 2) Serum half-lives of CZX in neonates shortly after birth were 4 or 5 times longer than those in older children, but decreased rapidly with the advance of day-ages. The half-life in neonates of 2 weeks of age or so became shorter to about twice the normal value in infants. Furthermore, half-lives of the drug in those at an age of the first half of infancy were similar to those in older children. 3) The urinary excretion rates tended to be somewhat low with neonates soon after birth, but became very similar to those in infants and older children at a relatively early stage.(ABSTRACT TRUNCATED AT 400 WORDS)
对新生儿进行了头孢唑肟（CZX）的药代动力学、细菌学和临床研究。1. 对12名年龄在1至27天（胎龄35 - 41周；出生体重2150 - 4030克）的新生儿和2名年龄在55至57天（胎龄39 - 40周；出生体重2320 - 2650克）的婴儿进行了CZX的血清浓度和尿排泄研究。每个受试者单次静脉注射20毫克/千克。新生儿静脉注射后1/4小时血清CZX浓度为24.9 - 53.7微克/毫升，平均为40.6±7.6微克/毫升。CZX的血清半衰期为1.32 - 4.75小时，平均为2.60±1.06小时。注射后6小时血清浓度范围为2.01至14.6微克/毫升，平均为7.70±3.89微克/毫升。在这2名婴儿中，注射后1/4小时血清浓度分别为42.0和46.2微克/毫升（平均：44.1±3.0微克/毫升），注射后6小时分别为2.91和5.04微克/毫升（平均：3.98±1.51微克/毫升）。一名婴儿的半衰期为1.54小时，另一名为1.93小时（平均：1.74±0.28小时）。此外，新生儿的6小时尿回收率为28.5 - 71.7%（平均：49.3±12.8%），婴儿为42.1 - 55.5%（平均：48.8±9.5%）。上述结果表明以下三点成立：1）无论年龄（出生后天数）如何，新生儿的血清峰值浓度（1/4小时时）与婴儿和大龄儿童相似。2）出生后不久新生儿CZX的血清半衰期比大龄儿童长4或5倍，但随着日龄增加迅速缩短。2周龄左右新生儿的半衰期缩短至婴儿正常水平的约两倍。此外，婴儿期前半段年龄组的药物半衰期与大龄儿童相似。3）新生儿出生后不久尿排泄率往往略低，但在相对较早阶段就变得与婴儿和大龄儿童非常相似。（摘要截断于400字）
