Motohiro T, Maruoka T, Nagai K, Oki S, Tsumura N, Sasaki H, Aramaki M, Koga T, Sakata Y, Tominaga K
Department of Pediatrics, School of Medicine, Kurume University.
Jpn J Antibiot. 1993 Jul;46(7):547-67.
Flomoxef (FMOX), an oxacephem antibiotic of beta-lactam antibiotic family, was administered to 16 infants including 6 neonates and 10 premature infants at a dose of 20 or 40 mg/kg via intravenous injection, and plasma and urinary concentrations and the urinary recovery were determined. In addition, FMOX was administered via intravenous injection at daily doses averaging 85.5 mg/kg divided into 2 to 4 times for durations averaging 9 days to 96 infants from 0- to 90-day old (mainly neonates and premature infants). In 44 of the 96 infants with bacterial infections, clinical and bacteriological efficacies were evaluated, and prophylactic effects of FMOX were determined in the remaining 52 infants. Adverse reaction and laboratory tests abnormalities were evaluated also. The obtained results are summarized as follows. 1. Upon administration of FMOX at 20 or 40 mg/kg to neonates and premature infants via intravenous injection, plasma concentrations, half-lives and AUC were determined. In 3 neonates of 5, 7 and 16 days of ages administered with 20 mg/kg of FMOX, peak plasma concentrations of 62.5 to 99.7 micrograms/ml were achieved in 5 or 15 minutes after injection. Half-lives of FMOX in these neonates were 1.48 to 1.78 hours and AUC's were 112 to 161 micrograms.hr/ml. The same dose (20 mg/kg) of FMOX was administered to 3 premature infants of 5- 16- and 19-day of ages and initial blood samples were obtained at 5 minutes after injection from the 5-day old subject and at 15 minutes after injection from the 16-and 19-day old subjects. Peak plasma concentrations of 63.6 to 79.9 micrograms/ml were observed in the samples. Half-lives were 1.69 to 2.20 hours and AUC's were 174 to 201 micrograms.hr/ml. When 3 neonates (one 17-day old and two 24-day old subjects) were administered with 40 mg/kg of FMOX, peak plasma concentrations obtained at 5 minutes after injection were 99.7 to 122.0 micrograms/ml. Half-lives were 1.28 to 1.92 hours and AUC's were 170 to 357 micrograms.hr/ml.(ABSTRACT TRUNCATED AT 400 WORDS)
氟氧头孢（FMOX）是β-内酰胺抗生素家族中的一种氧头孢烯类抗生素，通过静脉注射以20或40mg/kg的剂量给予16名婴儿，其中包括6名新生儿和10名早产儿，并测定血浆和尿液浓度以及尿回收率。此外，对96名0至90日龄（主要是新生儿和早产儿）的婴儿以平均85.5mg/kg的日剂量静脉注射FMOX，分为2至4次给药，平均持续时间为9天至96天。在96名患有细菌感染的婴儿中的44名中，评估了临床和细菌学疗效，并在其余52名婴儿中确定了FMOX的预防效果。还评估了不良反应和实验室检查异常情况。获得的结果总结如下。1. 通过静脉注射以20或40mg/kg的剂量向新生儿和早产儿给药FMOX后，测定血浆浓度、半衰期和AUC。在3名分别为5、7和16日龄的新生儿中给予20mg/kg的FMOX，注射后5或15分钟血浆峰值浓度达到62.5至99.7μg/ml。这些新生儿中FMOX的半衰期为1.48至1.78小时，AUC为112至161μg·hr/ml。将相同剂量（20mg/kg）的FMOX给予3名分别为5、16和19日龄的早产儿，在5日龄的受试者注射后5分钟以及16和19日龄的受试者注射后15分钟采集初始血样。样本中观察到血浆峰值浓度为63.6至79.9μg/ml。半衰期为1.69至2.20小时，AUC为174至201μg·hr/ml。当3名新生儿（1名17日龄和2名24日龄的受试者）给予40mg/kg的FMOX时，注射后5分钟获得的血浆峰值浓度为99.7至122.0μg/ml。半衰期为1.28至1.92小时，AUC为170至357μg·hr/ml。（摘要截断于400字）
