Kirby W M, Clarke J T, Libke R D, Regamey C
J Infect Dis. 1976 Nov;134 SUPPL:S312-5. doi: 10.1093/infdis/135.supplement_2.s312.
During and after a 4-hr intravenous infusion of amikacin and kanamycin in a cross-over study in healthy adult male volunteers, average concentrations of drug in serum were similar, with half-lives of approximately 2 hr. Apparent volumes of distribution at the steady state averaged 30% of body weight, and the rate of renal clearance was less than the rate of creatinine clearance (83 vs. 120 ml/min), a finding that indicates tubular reabsorption. The rate of serum clearance was greater than the rate of renal clearance (100 vs 83 ml/min). Urinary excretion in 24 hr averaged 94% of the dose, and there was no binding of serum proteins. In another cross-over study, volunteers received single intramuscular injections of these antibiotics. Peak concentrations of drug in serum after 45 min to 2 hr averaged 19.9 and 19.0 mug/ml for amikacin and kanamycin, respectively. Serum half-lives between 4 and 8 hr after administration of drug were 2 hr, and an average of 94% of the dose was recovered in the urine in 24 hr. Thus, the pharmacologic properties of amikacin and kanamycin were virtually identical.
在一项针对健康成年男性志愿者的交叉研究中,在4小时静脉输注阿米卡星和卡那霉素期间及之后,血清中药物的平均浓度相似,半衰期约为2小时。稳态时的表观分布容积平均为体重的30%,肾脏清除率低于肌酐清除率(83对120 ml/分钟),这一发现表明存在肾小管重吸收。血清清除率大于肾脏清除率(100对83 ml/分钟)。24小时内尿液排泄量平均为给药剂量的94%,且不存在血清蛋白结合。在另一项交叉研究中,志愿者接受了这些抗生素的单次肌肉注射。给药后45分钟至2小时,血清中阿米卡星和卡那霉素的药物峰值浓度分别平均为19.9和19.0μg/ml。给药后4至8小时的血清半衰期为2小时,24小时内平均94%的给药剂量在尿液中回收。因此,阿米卡星和卡那霉素的药理特性几乎相同。