Fujita K, Kakehashi H, Murono K, Sakata H, Ohmi H, Yoshioka H, Maruyama S, Sanae N, Inyaku F
Jpn J Antibiot. 1986 Jul;39(7):1681-92.
Nineteen episodes of infection in 17 children (one had 3 episodes) were treated with imipenem/cilastatin sodium (MK-0787/MK-0791), and the clinical efficacy and side effects were evaluated. The ages of patients ranged from 1 month to 8 years 1 month and their body weights ranged from 3.9 to 25.2 kg. The MK-0787/MK-0791 was administered intravenously by a 30-60 minutes infusion, in doses ranging from 8-42 mg/8-42 mg/kg every 6 to 12 hours for 3 to 40.5 days. Among 18 episodes in 16 patients (one patient proved to have rubella meningoencephalitis and was excluded from evaluation of the clinical efficacy) with bacterial infections including sepsis, pneumonia, acute suppurative thyroiditis and urinary tract infections, the results were excellent in 10, good in 5, fair in 2, and poor in 1 episode. Some side effects were noted; among all 19 episodes in the 17 patients diarrhea was noted in 3, rash in 1, slightly elevated serum transaminases in 1 and thrombocytosis in 1 episode. Pharmacokinetic studies were done in 7 patients whose ages ranged from 3 years 2 months to 13 years 1 month. Plasma concentrations of MK-0787 in 2 children were 19.6 and 20.0 micrograms/ml at 15 minutes and 5.6 and 2.1 micrograms/ml at 2 hours after a 10 mg/10 mg/kg intravenous 30-minute drip infusion of MK-0787/MK-0791. Plasma half-lives of MK-0787 were 1.52 and 0.74 hour, and total urinary recoveries were 54.6 and 71.4% during 0-6 hours. After a 20 mg/20 mg/kg intravenous 30-minute drip infusion into 2 other children, plasma concentrations of MK-0787 were 46.8 and 44.0 micrograms/ml at 15 minutes and 7.8 and 7.4 micrograms/ml at 2 hours. Plasma half-lives were 0.82 and 0.83 hour, and total urinary recoveries were 110.2 and 80.5% during 0-6 hours. Plasma concentrations of MK-0787 were less than 0.2, 0.2 and 1.2 micrograms/ml just before the next doses in 3 patients given 11-20 mg/11-20 mg/kg of MK-0787/MK-0791 every 6-8 hours. The time course of the plasma levels and urinary excretion in these patients were similar to those noted in the previous 4 patients following a single dose. Plasma concentrations of MK-0787 in a girl were 0.3 micrograms/ml just before the next dose and 8.2 micrograms/ml at 2 hours after multiple doses of 14 mg/14 mg/kg every 6 hours for 3 days and then 28 mg/28 mg/kg every 6 hours for 35 days.(ABSTRACT TRUNCATED AT 400 WORDS)
对17名儿童（其中1名儿童有3次感染发作）的19次感染发作采用亚胺培南/西司他丁钠（MK - 0787/MK - 0791）进行治疗，并评估其临床疗效和副作用。患者年龄范围为1个月至8岁1个月，体重范围为3.9至25.2千克。MK - 0787/MK - 0791通过静脉输注30 - 60分钟给药，剂量为每6至12小时8 - 42毫克/8 - 42毫克/千克，持续3至40.5天。在16名患者的18次感染发作中（1名患者被证实患有风疹性脑膜脑炎，被排除在临床疗效评估之外），感染类型包括败血症、肺炎、急性化脓性甲状腺炎和尿路感染，结果为优10例，良5例，中2例，差1例。观察到一些副作用；在17名患者的所有19次感染发作中，3例出现腹泻，1例出现皮疹，1例血清转氨酶轻度升高，1例出现血小板增多。对7名年龄范围为3岁2个月至13岁1个月的患者进行了药代动力学研究。在静脉滴注10毫克/10毫克/千克的MK - 0787/MK - 0791 30分钟后，2名儿童在15分钟时MK - 0787的血浆浓度分别为19.6和20.0微克/毫升，2小时时分别为5.6和2.1微克/毫升。MK - 0787的血浆半衰期分别为1.52和0.74小时，0 - 6小时的总尿回收率分别为54.6%和71.4%。在另外2名儿童中静脉滴注20毫克/20毫克/千克的MK - 0787/MK - 0791 30分钟后，15分钟时MK - 0787的血浆浓度分别为46.8和44.0微克/毫升，2小时时分别为7.8和7.4微克/毫升。血浆半衰期分别为0.82和0.83小时，0 - 6小时的总尿回收率分别为110.2%和80.5%。在3名每6 - 8小时给予11 - 20毫克/11 - 20毫克/千克MK - 0787/MK - 0791的患者中，下次给药前MK - 0787的血浆浓度分别低于0.2、0.2和1.2微克/毫升。这些患者的血浆水平和尿排泄的时间过程与之前4名单次给药患者中观察到的相似。一名女孩在每6小时多次给予14毫克/14毫克/千克共3天，然后每6小时给予28毫克/28毫克/千克共35天后，下次给药前MK - 0787的血浆浓度为0.3微克/毫升，2小时时为8.2微克/毫升。（摘要截于400字）
