Hotta T, Hirabayashi N, Shimizu K, Utsumi M, Katoh T, Maeda H, Hirano A, Ohnishi K, Murate T, Yamada H
Jpn J Antibiot. 1981 Nov;34(11):1457-64.
Investigation was made on absorption, excretion and clinical responses following intravenous drip infusion of amikacin (AMK) and the following results were obtained. 1) Serum concentrations of AMK were determined after completion of a 1 hour-course of its intravenous drip infusion at a dose of 200 mg, involving 2 patients with normal renal function and 1 patient with impaired renal function. In the patients with normal renal function, a mean peak serum concentration of 15.9 micrograms/ml was reached at the termination of the intravenous drip infusion and, then, gradually declined to 0.97 microgram/ml at 6 hours after completion of the intravenous drip infusion. The half-lives were 1.64 and 1.41 hours, respectively. In the patients with impaired renal function, the elimination of AMK from blood flow was markedly delayed and the serum concentration was 5.52 micrograms/ml even at 6 hours after completion of the intravenous drip infusion. The half-life was prolonged, its value being 5.98 hours. 2) The mean urinary excretion rate for the patients with normal renal function was 67.7% within 7 hours, while the patient with impaired renal function had a lower rate of 14.0%. 3) Ten infectious patients with hematological malignant diseases were treated with AMK intravenous drip infusion. Clinical responses were excellent in 6, good in 2, fair in 1 and poor in 1. Thus, 80% of the patients responded to AMK. 4) In order to check the side effects of AMK, investigation was made on the results of various clinical laboratory tests and the subjective and objective findings. But, no side effects attributed to AMK were observed. Therefore, it is thought that the intravenous drip infusion of AMK will be very useful when attention is paid to infusion time, dose and interval.
对静脉滴注阿米卡星（AMK）后的吸收、排泄及临床反应进行了研究，结果如下：1）对2例肾功能正常患者和1例肾功能受损患者以200mg剂量静脉滴注1小时后测定血清阿米卡星浓度。肾功能正常患者在静脉滴注结束时平均血清峰值浓度达到15.9微克/毫升，之后在静脉滴注结束6小时时逐渐降至0.97微克/毫升。半衰期分别为1.64小时和1.41小时。肾功能受损患者中，阿米卡星从血流中的消除明显延迟，即使在静脉滴注结束6小时时血清浓度仍为5.52微克/毫升。半衰期延长，其值为5.98小时。2）肾功能正常患者7小时内平均尿排泄率为67.7%，而肾功能受损患者的排泄率较低，为14.0%。3）对10例血液系统恶性疾病感染患者进行阿米卡星静脉滴注治疗。临床反应优6例，良2例，中1例，差1例。因此，80%的患者对阿米卡星有反应。4）为检查阿米卡星的副作用，对各项临床实验室检查结果及主观和客观表现进行了调查。但未观察到归因于阿米卡星的副作用。因此，认为在注意输注时间、剂量和间隔的情况下，阿米卡星静脉滴注将非常有用。
