Motohiro T, Tanaka K, Koga T, Shimada Y, Nishiyama T, Ishimoto K, Tominaga K, Yamashita F, Sakaguchi Y, Kimura K
Jpn J Antibiot. 1985 Aug;38(8):2068-86.
Dibekacin (DKB), an antibiotic of aminoglycoside group, was administered at 4 different dosages of 0.5, 1.0, 1.5 and 2.0 mg/kg as intravenous drip infusion taking 30 minutes or 1 hour. For each dose level, 3 cases each were used out of 24 boys from 1 year and 1 month to 14 years and 7 months of age, and serum concentrations as well as urinary concentrations and recovery rate were determined. After removed of 4 cases unassessable of therapeutic efficacy, 7 cases consisting of 1 case of chronic bronchitis, 1 case of lung abscess and 5 cases of urinary tract infections were treated with DKB at a mean daily dosage of 3.3 mg/kg in 2 or 3 divided doses as intravenous drip infusion taking 30 minutes or 1 hour. The mean treatment period was 7 days. The clinical and bacteriological results were analyzed in these cases and for analysis of side effects drop out cases were also included. The following results were obtained. Following 30 minutes intravenous drip infusion of DKB at 0.5, 1.0, 1.5 and 2.0 mg/kg, the serum concentration peaked at the end of infusion for all dose levels. The highest peak concentration of 9.17 mcg/ml was obtained for the dose level of 2.0 mg/kg. The highest dosage with which serum concentration does not exceed concentrations of 10 to 12 mcg/ml was found to be 2.0 mg/kg. The mean highest serum concentrations obtained were 1.65, 3.49, 5.40 and 8.67 mcg/ml for the dosages of 0.5, 1.0, 1.5 and 2.0 mg/kg, respectively, and the mean AUCs determined by the two-compartment model were 2.99, 6.04, 10.5 and 14.2 mcg X hr/ml, respectively, showing dose response relation in terms of peak concentration and AUC among groups. The mean T1/2 values for each dosage were 1.55, 1.54, 1.77 and 2.03 hours, respectively, with a longer tendency in T1/2 for the dose level of 2.0 mg/kg with unknown cause. When 0.5, 1.0, 1.5 and 2.0 mg/kg of DKB were infused taking 1 hour, the peak of serum concentration appeared also at the end of the infusion. The highest concentration was obtained with 2.0 mg/kg and it was 7.02 mcg/ml. Considering from the concentrations obtained for 0.5 mg/kg and 1.0 mg/kg groups the highest dosage at which the serum concentration does not exceed 10 to 12 mcg/ml was estimated to be 2.5 mg/kg.(ABSTRACT TRUNCATED AT 400 WORDS)
双去氧卡那霉素（DKB）是一种氨基糖苷类抗生素，以0.5、1.0、1.5和2.0mg/kg这4种不同剂量通过静脉滴注给药，滴注时间为30分钟或1小时。对于每个剂量水平，从1岁1个月至14岁7个月的24名男孩中各选取3例，测定血清浓度、尿液浓度及回收率。在剔除4例无法评估治疗效果的病例后，对1例慢性支气管炎、1例肺脓肿和5例尿路感染患者使用DKB进行治疗，平均日剂量为3.3mg/kg，分2或3次静脉滴注，滴注时间为30分钟或1小时。平均治疗期为7天。对这些病例的临床和细菌学结果进行分析，分析副作用时也纳入退出病例。得到以下结果。以0.5、1.0、1.5和2.0mg/kg的剂量静脉滴注DKB 30分钟后，所有剂量水平的血清浓度在滴注结束时达到峰值。2.0mg/kg剂量水平的最高峰值浓度为9.17mcg/ml。发现血清浓度不超过10至12mcg/ml的最高剂量为2.0mg/kg。0.5、1.0、1.5和2.0mg/kg剂量的平均最高血清浓度分别为1.65、3.49、5.40和8.67mcg/ml，通过二室模型测定的平均AUC分别为2.99、6.04、10.5和14.2mcg·hr/ml，各组间在峰值浓度和AUC方面呈现剂量反应关系。各剂量的平均T1/2值分别为1.55、1.54、1.77和2.03小时，2.0mg/kg剂量水平的T1/2有延长趋势，原因不明。当以1小时时间滴注0.5、1.0、1.5和2.0mg/kg的DKB时，血清浓度峰值也出现在滴注结束时。2.0mg/kg的浓度最高，为7.02mcg/ml。从0.5mg/kg和1.0mg/kg组的浓度来看，估计血清浓度不超过10至12mcg/ml的最高剂量为2.5mg/kg。（摘要截短至400字）
