Andritz M H, Smith R P, Baltch A L, Griffin P E, Conroy J V, Sutphen N, Hammer M C
Antimicrob Agents Chemother. 1984 Jan;25(1):33-6. doi: 10.1128/AAC.25.1.33.
The pharmacokinetics of moxalactam were studied in 19 male volunteers 60 years of age or older with normal liver function tests and a creatinine clearance of greater than or equal to 60 ml/min. Moxalactam was administered in single or multiple intravenous or intramuscular doses. Rapid and complete intramuscular bioavailability was demonstrated in a subgroup of the study population. The mean plasma half-life was 2.9 +/- 0.8 h for intravenous doses and 3.5 +/- 0.9 h for intramuscular doses. Average renal clearances of 0.04 liters/kg per h accounted for 74.0 +/- 15.0% of total plasma clearance. Moxalactam plasma clearance showed a statistically significant (P less than 0.01) correlation with measured and calculated creatinine clearance. The major differences in moxalactam pharmacokinetics seen in the elderly appear to be related to diminishing renal function and highly variable nonrenal elimination. Creatinine clearance can be used in estimating moxalactam doses in the elderly without significant renal impairment, but recommendations for the use of serum creatinine as an estimation of renal function or drug half-life are not valid in this population group.
对19名60岁及以上、肝功能检查正常且肌酐清除率大于或等于60 ml/分钟的男性志愿者进行了拉氧头孢的药代动力学研究。拉氧头孢采用单次或多次静脉内或肌内给药。在研究人群的一个亚组中显示了快速且完全的肌内生物利用度。静脉给药的平均血浆半衰期为2.9±0.8小时,肌内给药为3.5±0.9小时。每小时0.04升/千克的平均肾脏清除率占总血浆清除率的74.0±15.0%。拉氧头孢的血浆清除率与测量和计算的肌酐清除率呈统计学显著相关(P<0.01)。在老年人中观察到的拉氧头孢药代动力学的主要差异似乎与肾功能减退和高度可变的非肾清除有关。肌酐清除率可用于估计无明显肾功能损害的老年人的拉氧头孢剂量,但使用血清肌酐作为肾功能或药物半衰期估计值的建议在该人群中无效。