Bergrem H, Refvem O K
Acta Med Scand. 1983;213(5):339-43. doi: 10.1111/j.0954-6820.1983.tb03748.x.
The pharmacokinetics and protein binding of prednisolone were studied in 7 patients before and after 3 weeks of rifampicin therapy. The elimination half-time for prednisolone decreased by 45 +/- 8.1% (p less than 0.01), and the total body clearance of prednisolone increased by 91 +/- 26% (p less than 0.01). The area under the time-concentration curve (AUC) of total (free plus protein-bound) prednisolone decreased by 48 +/- 7.3% (p less than 0.01) and of free, unbound prednisolone by 57 +/- 9.8% (p less than 0.01). The reduction in AUC was greater for free than for total prednisolone (p less than 0.05) mainly due to the non-linear nature of prednisolone protein binding. There was no significant change in the volume of distribution. Because of the marked reduction in total and especially free prednisolone, the dosage should be adjusted accordingly if prednisolone and rifampicin are prescribed concomitantly.
在7名患者中研究了利福平治疗3周前后泼尼松龙的药代动力学和蛋白结合情况。泼尼松龙的消除半衰期降低了45±8.1%（p<0.01），泼尼松龙的全身清除率增加了91±26%（p<0.01）。总（游离加蛋白结合）泼尼松龙的时间-浓度曲线下面积（AUC）降低了48±7.3%（p<0.01），游离、未结合泼尼松龙的AUC降低了57±9.8%（p<0.01）。游离泼尼松龙的AUC降低幅度大于总泼尼松龙（p<0.05），这主要是由于泼尼松龙蛋白结合的非线性性质。分布容积没有显著变化。由于总泼尼松龙尤其是游离泼尼松龙显著减少，如果同时开具泼尼松龙和利福平，应相应调整剂量。
