Fujita K, Sakata H, Murono K, Yoshioka H, Maruyama S, Sanae N
Jpn J Antibiot. 1984 Dec;37(12):2271-82.
Twenty-eight pediatric patients were treated with ceftriaxone (Ro 13-9904, CTRX) in the doses ranging from 8.75 to 25 mg/kg every 12 hours for 3.5 to 11.5 days, and the clinical efficacy and side effects were evaluated. Among the 21 children with bacterial infections including pneumonia, acute bronchitis, otitis media, tonsillitis and urinary tract infections, the results were excellent in 9, good in 11, and fair in 1 patient. Out of the 28 patients, 2 patients had diarrhea, 3 patients had slightly elevated serum concentrations of transaminases, and 2 patients showed eosinophilia. The serum concentrations of CTRX in 5 children ranged from 50.0 to 93.8 micrograms/ml (mean 75.0 micrograms/ml) at 15 minutes and from 10.2 to 15.6 micrograms/ml (mean 13.4 micrograms/ml at 6 hours after 10 mg/kg intravenous bolus injection of CTRX. The serum half-lives were from 2.61 to 8.30 hours (mean 6.16 hours), and urinary recovery rates were from 43.3 to 58.0% (mean 48.5%) during 0-6 hours and from 52.0 to 66.1% (mean 59.4%) during 0-12 hours. After 20 mg/kg intravenous bolus injection of CTRX in 4 children, the serum concentrations of CTRX were from 118.8 to 162.5 micrograms/ml (mean 139.1 micrograms/ml) at 15 minutes and from 18.0 to 21.1 micrograms/ml (mean 19.2 micrograms/ml) at 6 hours. The serum half-lives were 4.07 to 6.34 hours (mean 5.13 hours), and urinary recovery rates were 38.6 to 51.1% (mean 45.4%) during 0-6 hours and from 54.8 to 64.0% (mean 59.0%) during 0-12 hours. Patients with impairment of renal function were excluded from this pharmacokinetic study.
28名儿科患者接受了头孢曲松（Ro 13-9904，CTRX）治疗，剂量为每12小时8.75至25mg/kg，持续3.5至11.5天，并评估了临床疗效和副作用。在21名患有细菌感染的儿童中，包括肺炎、急性支气管炎、中耳炎、扁桃体炎和尿路感染，9例结果为优，11例为良，1例为中。28例患者中，2例出现腹泻，3例血清转氨酶浓度略有升高，2例出现嗜酸性粒细胞增多。5名儿童在静脉推注10mg/kg CTRX后15分钟时，血清CTRX浓度为50.0至93.8微克/毫升（平均75.0微克/毫升），6小时时为10.2至15.6微克/毫升（平均13.4微克/毫升）。血清半衰期为2.61至8.30小时（平均6.16小时），0至6小时尿回收率为43.3至58.0%（平均48.5%），0至12小时为52.0至66.1%（平均59.4%）。4名儿童静脉推注20mg/kg CTRX后，15分钟时血清CTRX浓度为118.8至162.5微克/毫升（平均139.1微克/毫升），6小时时为18.0至21.1微克/毫升（平均19.2微克/毫升）。血清半衰期为4.07至6.34小时（平均5.13小时），0至6小时尿回收率为38.6至51.1%（平均45.4%），0至12小时为54.8至64.0%（平均59.0%）。肾功能损害患者被排除在本药代动力学研究之外。
