Fujii R, Fujita K, Murono K, Saijo M, Kakuya F, Yoshioka H, Maruyama S, Sakata H, Hiramoto A, Inyaku F
Department of Pediatrics, Asahikawa Medical College.
Jpn J Antibiot. 1993 Jul;46(7):518-38.
We investigated pharmacokinetics and clinical effects of flomoxef sodium (6315-S, FMOX) in neonates and premature infants. These results are summarized as follows: 1. Pharmacokinetics (1) Plasma concentration (Ct) and half-lives (T1/2) were determined upon after intravenous one-shot injection (i.v.) of FMOX to neonates of different day-age groups (0-3 (n = 25), 4-7 (n = 18), 8-28 (n = 32) days of birth). At a dose of 10 mg/kg. i.v., mean C30 (30 minutes concentration) values were 21.2, 21.8 and 21.3 micrograms/ml, respectively, in the different groups mentioned above, and the mean T1/2 values were 3.37, 1.85 and 1.63 hours. At 20 mg/kg i.v., mean C15 (15 minutes concentration) values were 54.4, 51.4 and 50.7 micrograms/ml, and mean T1/2's were 2.99, 2.32 and 1.79 hours, respectively. At a dose of 40 mg/kg i.v., mean C15 values were 104.0, 95.9 and 99.2 micrograms/ml, and the mean T1/2's were 3.40, 1.20 and 1.80 hours, respectively. (2) Plasma concentrations and T1/2 after intravenous one-shot injection of FMOX in premature infants in group (0-3 (n = 14), 4-7 (n = 10), 8-28 (n = 13) days of birth). Mean C15's at doses of 10, 20 and 40 mg/kg in the different groups of infants were 24.0, 28.6, 21.7 and 54.0, 54.6, 55.5 and 98.2, 93.0, 106.0 micrograms/ml, and T1/2's were 4.10, 2.53, 2.57 and 4.28, 2.27, 3.02 and 4.66, 2.86, 2.09 hours, respectively. Mean Cmax values were clearly dose dependent, and mean T1/2 values tended to be longer in premature infants compared to neonates. (3) Urinary recovery rate of FMOX after intravenous injection in neonates and premature infants. Mean urinary recovery rates of FMOX in the first 6 hours after i.v. (one-shot) at doses of 10, 20 and 40 mg/kg to neonates and premature infants were 38.9-62.8% in the neonates and 30.7-61.5% in the premature infants. (4) Plasma concentrations and urinary recovery rates upon 1 hour drip infusion of 20 mg/kg in the neonate groups (or the premature infant groups) as follows: Mean C50 values were 31.0, 32.7 and 23.4 micrograms/ml, and T1/2 were 2.94, 3.68 and 2.25 hours, respectively. The recovery rates were 35.2-52.9% in the first 6 hours after administration. 2. Clinical studies The number of clinically evaluable cases in the FMOX treatment of premature infants was 199, in which the causative pathogens were identified in 71 cases (A group) and not identified in 128 cases (B group).(ABSTRACT TRUNCATED AT 400 WORDS)
我们研究了氟氧头孢钠（6315 - S，FMOX）在新生儿和早产儿中的药代动力学及临床效果。结果总结如下：1. 药代动力学（1）对不同日龄组（出生0 - 3天（n = 25）、4 - 7天（n = 18）、8 - 28天（n = 32））的新生儿静脉一次性注射FMOX后测定血浆浓度（Ct）和半衰期（T1/2）。静脉注射剂量为10mg/kg时，上述不同组的平均C30（30分钟浓度）值分别为21.2、21.8和21.3微克/毫升，平均T1/2值分别为3.37、1.85和1.63小时。静脉注射剂量为20mg/kg时，平均C15（15分钟浓度）值分别为54.4、51.4和50.7微克/毫升，平均T1/2分别为2.99、2.32和1.79小时。静脉注射剂量为40mg/kg时，平均C15值分别为104.0、95.9和99.2微克/毫升，平均T1/2分别为3.40、1.20和1.80小时。（2）对出生日龄分组为0 - 3天（n = 14）、4 - 7天（n = 10）、8 - 28天（n = 13）的早产儿静脉一次性注射FMOX后的血浆浓度和T1/2。不同组婴儿静脉注射剂量为10、20和40mg/kg时的平均C15值分别为24.0、28.6、21.7；54.0、54.6、55.5；98.2、93.0、106.0微克/毫升，T1/2分别为4.10、2.53、2.57；4.28、2.27、3.02；4.66、2.86、2.09小时。平均Cmax值明显呈剂量依赖性，与新生儿相比，早产儿的平均T1/2值往往更长。（3）新生儿和早产儿静脉注射FMOX后的尿回收率。新生儿和早产儿静脉注射（一次性）剂量为10、20和40mg/kg后，前6小时FMOX的平均尿回收率在新生儿中为38.9 - 62.8%，在早产儿中为30.7 - 61.5%。（4）新生儿组（或早产儿组）静脉滴注20mg/kg 1小时后的血浆浓度和尿回收率如下：平均C50值分别为31.0、32.7和23.4微克/毫升，T1/2分别为2.94、3.68和2.25小时。给药后前6小时的回收率为35.2 - 52.9%。2. 临床研究FMOX治疗早产儿的临床可评估病例数为199例，其中71例（A组）明确了致病病原体，128例（B组）未明确致病病原体。
