Fillastre J P, Leroy A, Humbert G, Moulin B, Bernadet P, Josse S
Antimicrob Agents Chemother. 1987 Apr;31(4):575-7. doi: 10.1128/AAC.31.4.575.
The pharmacokinetics of habekacin, a new semisynthetic aminoglycoside antibiotic, were investigated in six healthy subjects and 25 uremic patients (six of whom were on hemodialysis) after administration of a single 3-mg/kg dose. Six healthy subjects received the 3-mg/kg dose both intramuscularly (i.m.) and intravenously (i.v.) (1-h infusion). Uremic patients were given the 3-mg/kg dose as an i.m. injection, except for the hemodialysis patients, who received the dose as a 1-h i.v. infusion. After the i.m. injection, the peak concentrations in serum were higher and the times to peak levels were longer in patients with renal impairment than in healthy subjects. The elimination half-life in serum increased in relation to the degree of renal impairment, from 2 h in normal subjects to 32 h in patients with creatinine clearances of less than 10 ml/min. Renal impairment did not significantly modify the apparent volume of distribution. After the same 3-mg/kg dose as a 1-h i.v. infusion in six hemodialysis patients, the elimination half-life averaged 48 and 5 h off and on a 4- to 5-h hemodialysis session, respectively. The habekacin pharmacokinetic data appeared to be similar to those of the other available aminoglycoside antibiotics.
对一种新型半合成氨基糖苷类抗生素哈贝卡星的药代动力学进行了研究。在6名健康受试者和25名尿毒症患者（其中6名正在接受血液透析）中，给予单次3mg/kg剂量后进行观察。6名健康受试者分别接受了3mg/kg剂量的肌肉注射和静脉注射（1小时输注）。尿毒症患者接受3mg/kg剂量的肌肉注射，但接受血液透析的患者接受1小时静脉输注。肌肉注射后，肾功能损害患者血清中的峰值浓度更高，达到峰值水平的时间更长。血清消除半衰期随着肾功能损害程度的增加而延长，从正常受试者的2小时增加到肌酐清除率低于10ml/min患者的32小时。肾功能损害并未显著改变表观分布容积。在6名血液透析患者接受相同3mg/kg剂量的1小时静脉输注后，在4至5小时的血液透析疗程中，消除半衰期分别平均为48小时和5小时。哈贝卡星的药代动力学数据似乎与其他可用氨基糖苷类抗生素的数据相似。
