Sangha K S, Miyagawa C I, Healy D P, Bjornson H S
Practitioner-Neurosciences, University of Cincinnati Hospital, OH, USA.
Ann Pharmacother. 1995 Feb;29(2):117-9. doi: 10.1177/106002809502900201.
To compare the first-dose pharmacokinetic parameters of gentamicin 6 mg/kg and 2 mg/kg in stable, nonobese surgical intensive care unit patients with open extremity fractures receiving gentamicin prophylactically.
Serial blood samples were obtained over 8 or 24 hours following the first dose of gentamicin. Serum concentrations of gentamicin were measured using fluorescence polarization immunoassay and analyzed by noncompartmental means.
Eleven patients were enrolled, 7 in the 6 mg/kg group and 4 in the 2 mg/kg group. The median (6 vs. 2 mg/kg) age was 29 versus 28 years; serum creatinine 80 versus 88 mumol/L; and APACHE II score 13 versus 10. The mean +/- SD (micrograms/mL) of concentration at the end of the 30-minute infusion (Cmax), concentration 30 minutes after the end of the infusion (Cpk), and concentration at the end of the dosing interval for 6 versus 2 mg/kg were: 35.0 +/- 19.0 versus 10.1 +/- 1.77; 17.0 +/- 2.7 versus 5.4 +/- 0.4, and 0.45 +/- 0.31 versus 0.69 +/- 0.11, respectively. Area under the curve0-infinity (AUC0-infinity), apparent volume of distribution, and half-life were: 89.0 +/- 28.9 versus 26.1 +/- 1.2 mg.h/L, 0.40 +/- 0.10 versus 0.47 +/- 0.14 L/kg, and 4.0 +/- 1.1 versus 4.3 +/- 1.5 h, respectively.
The first-dose pharmacokinetics of gentamicin 6 mg/kg resulted in a proportional rise in Cmax, Cpk, and AUC0-infinity compared with gentamicin 2 mg/kg in patients with open fractures, but with greater variability.
比较在接受庆大霉素预防性治疗的稳定、非肥胖开放性四肢骨折手术重症监护病房患者中，6mg/kg和2mg/kg庆大霉素的首剂药代动力学参数。
在首剂庆大霉素给药后的8或24小时内采集系列血样。采用荧光偏振免疫分析法测定庆大霉素的血清浓度，并通过非房室方法进行分析。
共纳入11例患者，6mg/kg组7例，2mg/kg组4例。（6mg/kg与2mg/kg相比）年龄中位数分别为29岁和28岁；血清肌酐分别为80和88μmol/L；急性生理学与慢性健康状况评分系统II（APACHE II）评分分别为13分和10分。6mg/kg与2mg/kg在30分钟输注结束时的浓度（Cmax）、输注结束后30分钟的浓度（Cpk）以及给药间隔结束时的浓度（均值±标准差，μg/mL）分别为：35.0±19.0与10.1±1.77；17.0±2.7与5.4±0.4，以及0.45±0.31与0.69±0.11。曲线下面积0至无穷大（AUC0-∞）、表观分布容积和半衰期分别为：89.0±28.9与26.1±1.2mg·h/L，0.40±0.10与0.47±0.14L/kg，以及4.0±1.1与4.3±1.5小时。
在开放性骨折患者中，与2mg/kg庆大霉素相比，6mg/kg庆大霉素的首剂药代动力学导致Cmax、Cpk和AUC0-∞成比例升高，但变异性更大。
