Hesselink Dennis A, Ngyuen Hien, Wabbijn Marike, Gregoor Peter J H Smak, Steyerberg Ewout W, van Riemsdijk Iza C, Weimar Willem, van Gelder Teun
Department of Internal Medicine, Renal Transplant Unit, Room D 412, Erasmus Medical Centre, PO Box 2040, 3000 CA Rotterdam, the Netherlands.
Br J Clin Pharmacol. 2003 Sep;56(3):327-30. doi: 10.1046/j.0306-5251.2003.01882.x.
To evaluate the effect of corticosteroids on tacrolimus pharmacokinetics.
In a randomized trial, kidney transplant recipients were treated with tacrolimus and mycophenolate mofetil with either daclizumab (n = 31) or 3 months of prednisone (n = 34). Tacrolimus dose-adjusted predose concentrations (C0) at month 1-6 were compared between both groups and within the corticosteroid group before and after prednisone withdrawal.
At month 1 the tacrolimus dose-adjusted C0 in the corticosteroid group was 83 +/- 8 vs 119 +/- 17 ng ml-1 mg-1 kg-1 in the daclizumab group. The tacrolimus dose-adjusted C0 within the corticosteroid group at month 1 and 2 was 42% and 29% lower compared with month 4 (P < 0.001).
A higher tacrolimus dose is required to reach target concentrations when used in combination with corticosteroids.
评估皮质类固醇对他克莫司药代动力学的影响。
在一项随机试验中，肾移植受者接受他克莫司和霉酚酸酯治疗，其中一组使用达利珠单抗（n = 31），另一组使用3个月的泼尼松（n = 34）。比较两组在第1至6个月时他克莫司剂量调整后的给药前浓度（C0），以及皮质类固醇组在停用泼尼松前后的情况。
第1个月时，皮质类固醇组他克莫司剂量调整后的C0为83±8 ng/ml·mg⁻¹·kg⁻¹，而达利珠单抗组为119±17 ng/ml·mg⁻¹·kg⁻¹。皮质类固醇组在第1个月和第2个月时他克莫司剂量调整后的C0比第4个月分别低42%和29%（P < 0.001）。
与皮质类固醇联合使用时，需要更高的他克莫司剂量才能达到目标浓度。
