Bergrem H, Ritland S, Opedal I, Bergan A
Scand J Gastroenterol. 1983 Mar;18(2):273-6. doi: 10.3109/00365528309181594.
The pharmacokinetics and protein-binding of orally administered prednisolone have been studied in seven patients with chronic liver disease and portosystemic shunts. The peak prednisolone serum concentration and the time of peak prednisolone concentration were similar to those found in normal subjects, indicating that there is no clinically significant first-pass metabolism of prednisolone. The elimination half-time and the extent of bioavailability of total prednisolone tended to be lower in the patients, and the extent of free, unbound prednisolone higher, but the differences were not statistically significant. The patients had a significantly lower serum protein-binding of prednisolone than the controls. Despite the decreased protein-binding in the patients, however, the results indicate that changes occur in the pharmacokinetics of prednisolone that tend to reduce the bioavailability of free, biologically active prednisolone towards that seen in healthy subjects. Reduction of the prednisolone dose is therefore not indicated in patients with portosystemic shunt and chronic liver disease, even in the presence of hypoalbuminemia.
对7例患有慢性肝病和门体分流的患者进行了口服泼尼松龙的药代动力学和蛋白结合研究。泼尼松龙血清峰值浓度和达峰时间与正常受试者相似，表明泼尼松龙不存在临床上显著的首过代谢。患者体内总泼尼松龙的消除半衰期和生物利用度趋于降低，游离、未结合的泼尼松龙水平较高，但差异无统计学意义。患者体内泼尼松龙的血清蛋白结合率显著低于对照组。然而，尽管患者体内蛋白结合率降低，但结果表明泼尼松龙的药代动力学发生了变化，趋向于使游离的、具有生物活性的泼尼松龙的生物利用度向健康受试者的水平降低。因此，即使存在低白蛋白血症，对于患有门体分流和慢性肝病的患者，也不建议降低泼尼松龙剂量。
