Bergrem H
Acta Med Scand. 1983;213(5):333-7. doi: 10.1111/j.0954-6820.1983.tb03747.x.
The pharmacokinetics and protein binding of prednisolone have been compared in 6 uremic patients and 6 healthy controls after intravenous injection of 20 mg prednisolone. The uremic patients had a 53% longer elimination half-time (p less than 0.01) and a 34% larger area under the time-concentration curve (AUC) (p less than 0.05) of total prednisolone than the controls. The total body clearance of total prednisolone was 26% lower and of free prednisolone 40% lower in the uremic patients than in the controls (p less than 0.01). The volume of distribution at steady state was 17% larger in the patients than in the controls, but the difference was not statistically significant. The protein binding of prednisolone was decreased in the patients, the proportion of free prednisolone being 26% higher than in the controls (p less than 0.05). The amount of free prednisolone, expressed as the AUC of free prednisolone, was 67% larger in the patients than in the controls (p less than 0.01). These results indicate that uremic patients taking prednisolone may be more prone to develop glucocorticoid side-effects because of higher concentration of free, biologically active prednisolone, secondary to a reduced rate of elimination and a decreased serum protein binding of prednisolone.
在6名尿毒症患者和6名健康对照者静脉注射20毫克泼尼松龙后，对泼尼松龙的药代动力学和蛋白结合情况进行了比较。与对照组相比，尿毒症患者的总泼尼松龙消除半衰期长53%（p<0.01），时间-浓度曲线下面积（AUC）大34%（p<0.05）。尿毒症患者总泼尼松龙的全身清除率比对照组低26%，游离泼尼松龙低40%（p<0.01）。患者的稳态分布容积比对照组大17%，但差异无统计学意义。患者体内泼尼松龙的蛋白结合率降低，游离泼尼松龙的比例比对照组高26%（p<0.05）。以游离泼尼松龙的AUC表示的游离泼尼松龙量，患者比对照组大67%（p<0.01）。这些结果表明，服用泼尼松龙的尿毒症患者可能更容易出现糖皮质激素副作用，因为泼尼松龙的消除速率降低和血清蛋白结合率下降，导致游离的、具有生物活性的泼尼松龙浓度升高。
