Wagner J G, Wexler D, Ağabeyoğlu I T, Bergstrom R F, Sakmar E, Kay D R
J Lab Clin Med. 1981 Apr;97(4):487-501.
Prednisone and prednisolone bind in plasma to albumin and transcortin. In am attempt to determine whether prednisone side effects and/or type of disease correlated with prednisolone plasma protein binding, multiple plasma samples from 17 patients (three asthma, eight SLE, three RA, two PSS, one PAN) receiving long-term prednisone therapy were monitored during an interval between two prednisone doses. Prednisolone plasma protein binding was nonlinear and exhibited large intrapatient and interpatient variability. For the group, mean association constants of the prednisolone-albumin complex and the prednisolone-transcortin complex were 2.3 X 10(3) M-1 and 2.9 X 10(7) M-1, with coefficients of variation of 82% and 127%, respectively. SLE patients tended to have lower mean prednisolone association constants for albumin and transcortin than did other patients. The presence of corticosteroid side effects did not correlate with prednisolone plasma protein-binding parameters. The wide range of prednisolone free fraction noted in plasma from patients who achieved comparable total prednisolone plasma concentrations implies that administration of a uniform prednisone dose will not lead to a predictable clinical response.
泼尼松和泼尼松龙在血浆中与白蛋白和皮质激素转运蛋白结合。为了确定泼尼松的副作用和/或疾病类型是否与泼尼松龙的血浆蛋白结合相关，在17例接受长期泼尼松治疗的患者（3例哮喘、8例系统性红斑狼疮、3例类风湿关节炎、2例进行性系统性硬化症、1例结节性多动脉炎）的两个泼尼松剂量间隔期间，对多个血浆样本进行了监测。泼尼松龙的血浆蛋白结合呈非线性，且在患者内和患者间存在很大差异。对于该组患者，泼尼松龙 - 白蛋白复合物和泼尼松龙 - 皮质激素转运蛋白复合物的平均缔合常数分别为2.3×10³ M⁻¹和2.9×10⁷ M⁻¹，变异系数分别为82%和127%。系统性红斑狼疮患者的泼尼松龙与白蛋白和皮质激素转运蛋白的平均缔合常数往往低于其他患者。皮质类固醇副作用的存在与泼尼松龙血浆蛋白结合参数无关。在总泼尼松龙血浆浓度相当的患者血浆中观察到的泼尼松龙游离分数范围很广，这意味着给予统一的泼尼松剂量不会导致可预测的临床反应。
