Lanao J M, Pedraz J L, Navarro A S, Dominguez-Gil A
Int J Clin Pharmacol Ther Toxicol. 1984 Oct;22(10):538-42.
The urinary excretion kinetics of amikacin was studied in 28 healthy volunteers who received doses of 125, 250 and 500 mg of the antibiotic. The average percentages of the dose excreted were 67.67, 79.4 and 68.65% for each dose, respectively. The elimination constant (Ke), the urinary excretion constant (Ku) and the extra-renal excretion constant (Knr) had similar values for the three groups studied. The average value obtained for Knr showed the existence of a moderate extra-renal excretion of amikacin. A linear relationship was observed between the maximum excretion rate (Vmax) and the dose administered (D), according to the equation: Vmax (mg/h) = 3.714 + 0.207 X D (mg); r = 1.000 This relationship reveals the linear kinetics of renal excretion in the dose range studied. In view of the high urinary concentrations obtained, it is concluded that amikacin doses of 4 mg/kg/day should ensure therapeutic urinary concentrations sufficient to combat most amikacin-susceptible organisms.
对28名健康志愿者进行了研究，这些志愿者分别接受了125毫克、250毫克和500毫克的阿米卡星剂量，以研究其尿排泄动力学。各剂量的平均排泄剂量百分比分别为67.67%、79.4%和68.65%。在所研究的三组中，消除常数（Ke）、尿排泄常数（Ku）和肾外排泄常数（Knr）具有相似的值。所获得的Knr平均值表明存在中等程度的阿米卡星肾外排泄。根据方程：Vmax（毫克/小时）=3.714 + 0.207×D（毫克）；r = 1.000，观察到最大排泄率（Vmax）与给药剂量（D）之间存在线性关系。这种关系揭示了在所研究的剂量范围内肾排泄的线性动力学。鉴于获得的高尿浓度，得出结论：4毫克/千克/天的阿米卡星剂量应确保足以对抗大多数对阿米卡星敏感的生物体的治疗性尿浓度。
