Lau A, Lee M, Sharifi R
Int J Clin Pharmacol Ther Toxicol. 1985 Aug;23(8):391-4.
Piperacillin is an extended-spectrum penicillin active against Pseudomonas. It has been documented to be effective in the treatment of complicated urinary tract infections and urosepsis. Much of the pharmacokinetic information available is obtained from normal subjects. The purpose of this study is to evaluate piperacillin pharmacokinetics in hospitalized patients. Ten clinically stable hospitalized urology patients were given 4 grams of piperacillin intravenously in a single dose. Serial blood samples were then obtained and serum piperacillin concentrations were determined by high performance liquid chromatography. The following pharmacokinetic parameters (mean +/- SD) were determined: half-life = 1.09 +/- 0.31 h, elimination rate constant = 0.69 +/- 0.22 h-1, volume of distribution = 0.36 +/- 0.13 l/kg, total body clearance = 0.230 +/- 0.054 l/h/kg. These parameters are comparable to those obtained in normal subjects except for the volume of distribution which is slightly higher than that reported in healthy volunteers. Pharmacokinetic information obtained in healthy subjects may, therefore, be applied to the clinically stable hospitalized urology patient. However, changes in pharmacokinetic characteristics may be found in the critically ill patient with compromise in hemodynamics and significant third spacing of fluid.
哌拉西林是一种对假单胞菌有效的广谱青霉素。已证明它在治疗复杂性尿路感染和尿脓毒症方面有效。现有的许多药代动力学信息是从正常受试者获得的。本研究的目的是评估住院患者的哌拉西林药代动力学。10名临床稳定的住院泌尿外科患者静脉注射4克哌拉西林,剂量为单次。然后采集系列血样,通过高效液相色谱法测定血清哌拉西林浓度。确定了以下药代动力学参数(平均值±标准差):半衰期=1.09±0.31小时,消除速率常数=0.69±0.22小时-1,分布容积=0.36±0.13升/千克,总体清除率=0.230±0.054升/小时/千克。除分布容积略高于健康志愿者报告的值外,这些参数与正常受试者获得的参数相当。因此,在健康受试者中获得的药代动力学信息可应用于临床稳定的住院泌尿外科患者。然而,在血流动力学受损和有明显液体第三间隙的重症患者中可能会发现药代动力学特征的变化。