Jahre J A, Fu K P, Neu H C
Clin Pharmacol Ther. 1978 May;23(5):591-7. doi: 10.1002/cpt1978235591.
The kinetic parameters of netilmicin were studied in normal human subjects. In the intravenous study a steady-state was obtained in 4 subjects by the constant infusion of 2 mg/kg of netilmicin during the first hour followed by 0.5 mg/kg/hr for each of three successive hours. Creatinine clearance was greater than the simultaneous serum and renal clearance of netilmicin. In the intramuscular study 6 subjects received a single injection of 1 mg/kg of netilmicin followed by the same dose of gentamicin 1 wk later. A mean peak serum levels of 3.9 microgram/ml was found for both antibiotics, but the mean serum half-life of netilmicin was shorter than that of gentamicin. Doubling the intramuscular dose of netilmicin approximately doubled the peak serum level. In both studies 75% to 90% of the netilmicin was recovered in the urine within the first 24 hr. Netilmicin appears to be primarily excreted by glomerular filtration. The apparent volume of distribution was similar to that reported for other related aminoglycosides. Netilmicin and gentamicin have similar kinetic parameters. There were wide individual differences among normal subjects with both drugs.
在正常人体受试者中研究了奈替米星的动力学参数。在静脉给药研究中，4名受试者在第1小时内以2mg/kg的奈替米星持续输注，随后连续3小时每小时输注0.5mg/kg，从而达到稳态。肌酐清除率高于同时期奈替米星的血清清除率和肾脏清除率。在肌肉注射研究中，6名受试者单次注射1mg/kg的奈替米星，1周后注射相同剂量的庆大霉素。两种抗生素的平均血清峰值水平均为3.9微克/毫升，但奈替米星的平均血清半衰期短于庆大霉素。将奈替米星的肌肉注射剂量加倍，血清峰值水平约加倍。在两项研究中，75%至90%的奈替米星在最初24小时内从尿液中回收。奈替米星似乎主要通过肾小球滤过排泄。表观分布容积与其他相关氨基糖苷类药物报道的相似。奈替米星和庆大霉素具有相似的动力学参数。正常受试者中使用这两种药物时个体差异很大。
