Midtvedt K
Department of Medicine, Nephrology Unit, Rikshospitalet, Oslo, Norway.
Transplant Proc. 2004 Mar;36(2 Suppl):430S-433S. doi: 10.1016/j.transproceed.2004.01.025.
Therapeutic drug monitoring of cyclosporine has been established as part of the routine clinical treatment for patients after organ transplantation. The inability to define optimal dose (maximize efficacy/minimize toxicity) has been a problem related to drug monitoring of cyclosporine. The original cyclosporine formula showed high intra-patient and inter-patient variability and low bioavailability. The microemulsion formulation of cyclosporine (Neoral) was introduced to address the absorption problems related to the original cyclosporine formulation. With the introduction of Neoral, renewed interest in methods of therapeutic drug monitoring brought us from trough monitoring (C0) to levels measured 2 hours after dosing (C2). The pharmacokinetic rationale for using C2 to monitor patients receiving Neoral has demonstrated a reduced incidence of rejection in de novo patients and improvements in safety profile in both renal and hepatic transplant recipients. Monitoring C2 levels is a more precise method for optimizing cyclosporine dosing and a better way to individualize therapy. Further data are required from prospective trials to evaluate the clinical benefits of adopting C2 monitoring in cardiac and lung transplant recipients as well as in long-term maintenance patients.
环孢素的治疗药物监测已成为器官移植患者常规临床治疗的一部分。无法确定最佳剂量（使疗效最大化/毒性最小化）一直是与环孢素药物监测相关的一个问题。最初的环孢素制剂显示出患者内和患者间的高变异性以及低生物利用度。环孢素微乳剂（新山地明）的推出是为了解决与最初环孢素制剂相关的吸收问题。随着新山地明的引入，对治疗药物监测方法的重新关注使我们从谷浓度监测（C0）转向给药后2小时测量的血药浓度（C2）。使用C2监测接受新山地明治疗患者的药代动力学原理已证明，初治患者的排斥反应发生率降低，肾移植和肝移植受者的安全性均有所改善。监测C2水平是优化环孢素给药的更精确方法，也是实现个体化治疗的更好方式。需要前瞻性试验提供更多数据，以评估在心脏和肺移植受者以及长期维持治疗患者中采用C2监测的临床益处。
