Bartucci M R, Bayer L, Brooks B K, Chandler L, Himes V, Meiergerd D, Newby B, Satmary N T, Shieck V
University Hospital of Cleveland, USA.
J Transpl Coord. 1998 Dec;8(4):227-33; quiz 234-5. doi: 10.7182/prtr.1.8.4.t272k7g0717144h1.
The pharmacokinetic profiles of Sandimmune and Neoral vary considerably among transplant recipients. Cyclosporine exposure is far more consistent with Neoral than it is with Sandimmune. Because intrapatient variability of drug exposure has been demonstrated to be a risk factor for chronic rejection, this difference becomes important. Neoral also has a linear dose response and a stronger correlation between trough level and drug exposure. Dose linearity greatly facilitates accurate dose titration. Results of controlled studies in which kidney, liver, and heart transplant recipients were converted from Sandimmune to Neoral have shown that conversion on a 1:1 mg basis results in more predictable bioavailability and often in reductions in cyclosporine dose. Carefully monitored conversion has not been associated with increased side effects, and any side effects that do emerge can usually be managed by taking Neoral with food, changing the dose from every 12 hours to every 8 hours, or through dose reduction.
山地明(Sandimmune)和新山地明(Neoral)在移植受者中的药代动力学特征差异很大。与山地明相比,新山地明的环孢素暴露情况更为稳定。由于已证明患者体内药物暴露的变异性是慢性排斥反应的一个危险因素,因此这种差异变得很重要。新山地明还具有线性剂量反应,谷浓度与药物暴露之间的相关性更强。剂量线性极大地便于准确的剂量滴定。在肾脏、肝脏和心脏移植受者从山地明转换为新山地明的对照研究结果表明,按1:1毫克的基础进行转换可产生更可预测的生物利用度,并且环孢素剂量通常会降低。经过仔细监测的转换与副作用增加无关,出现的任何副作用通常可通过与食物同服新山地明、将给药间隔从每12小时改为每8小时或减少剂量来处理。