Jonsson M, Walder M
Department of Community Health Sciences, University of Lund, Värnhem Hospital, Malmö, Sweden.
Eur J Clin Microbiol Infect Dis. 1992 Jan;11(1):15-21. doi: 10.1007/BF01971265.
The i.v. and i.m. dose pharmacokinetics of ceftazidime 1 g b.i.d. were investigated in steady state in 52 consecutive cases of hospitalised patients with underlying diseases and serious supervening bacterial infections. Following i.v. bolus injection, serum concentrations of greater than 4 mg/l persisted for 8 h in all patients. Compared to values found in younger patients studied previously, clearance was markedly reduced in the elderly, t1/2 beta more than doubled, the area under the curve four times enlarged and the apparent volume of distribution reduced. The values obtained in serum after i.m. injection were similar, though the peak concentration was delayed by about 2 h. The serum uptake was approximately 70%, and serum concentration was greater than 4 mg/l for 8 h. The concentrations in tissue fluid after i.v. administration were similar to those in serum, but the penetration into tissue fluid was slower and only 20% of that reported previously for young people. The elimination was slow, with greater than 4 mg/l maintained for 7 h. Tissue concentrations after i.m. injection were almost comparable with those after i.v. injection, but lagged behind by about 1 h. In conclusion, suitable concentrations in blood and tissue are attained with 1 g ceftazidime b.i.d., whether administered by the i.v. or i.m. route.
对52例患有基础疾病并伴有严重继发细菌感染的住院患者，在稳态下研究了头孢他啶1g每日两次静脉注射和肌肉注射的药代动力学。静脉推注后，所有患者血清浓度大于4mg/L持续8小时。与先前研究的年轻患者相比，老年人的清除率明显降低，β半衰期增加一倍多，曲线下面积扩大四倍，表观分布容积减小。肌肉注射后血清中的值相似，尽管峰值浓度延迟约2小时。血清摄取率约为70%，血清浓度大于4mg/L持续8小时。静脉给药后组织液中的浓度与血清中的浓度相似，但进入组织液的速度较慢，仅为先前报道的年轻人的20%。消除缓慢，大于4mg/L维持7小时。肌肉注射后的组织浓度与静脉注射后的几乎相当，但滞后约1小时。总之，无论通过静脉注射还是肌肉注射途径，每日两次1g头孢他啶均可在血液和组织中达到合适的浓度。
