Bergrem H, Refvem O K
Proc Eur Dial Transplant Assoc. 1983;19:552-7.
Prednisolone pharmacokinetics and protein binding were studied after i.v. injection before and after three weeks of rifampicin therapy. The elimination half-time for prednisolone fell by 44.8% +/- 8.1% (p less than 0.01) and the area under the time-concentration curve by 47.5% +/- 7.3% (p less than 0.01). The reduction in area under the time concentration curve of free, non-protein bound prednisolone was 56.5% +/- 9.8% (p less than 0.01). The reduction in AUC was greater (p less than 0.05) for free prednisolone than for total prednisolone because of non-linear protein binding of prednisolone. The total body clearance of prednisolone increased from 73.5 +/- 14.6ml/min to 142.7 +/- 35.8ml/min (p less than 0.01). There was no change in the volume of distribution of prednisolone. Because of the marked reduction in the extent of bioavailability of total, and especially free, prednisolone, dosage adjustments should be made accordingly if prednisolone and rifampicin are prescribed concomitantly.
在利福平治疗三周前后，静脉注射泼尼松龙后对其药代动力学和蛋白结合情况进行了研究。泼尼松龙的消除半衰期下降了44.8%±8.1%（p<0.01），药时曲线下面积下降了47.5%±7.3%（p<0.01）。游离的、未与蛋白结合的泼尼松龙药时曲线下面积减少了56.5%±9.8%（p<0.01）。由于泼尼松龙的非线性蛋白结合，游离泼尼松龙的AUC下降幅度大于总泼尼松龙（p<0.05）。泼尼松龙的全身清除率从73.5±14.6ml/min增至142.7±35.8ml/min（p<0.01）。泼尼松龙的分布容积没有变化。由于总泼尼松龙尤其是游离泼尼松龙的生物利用度显著降低，如果同时开具泼尼松龙和利福平，应相应调整剂量。
