Ptachcinski R J, Burckart G J, Venkataramanan R
J Clin Pharmacol. 1986 May-Jun;26(5):358-66. doi: 10.1002/j.1552-4604.1986.tb03538.x.
The availability of the immunosuppressant cyclosporin has led to significant improvements in the recent success of clinical organ transplantation. Problems associated with cyclosporine therapy include serious adverse reactions, such as nephrotoxicity, wide variability in the drug's pharmacokinetics, and several complex drug interactions. Monitoring of drug concentrations is accepted as a part of the routine care of patients receiving cyclosporine. However, cyclosporine concentrations can be determined in different biologic fluids by either radioimmunoassay or high-performance liquid chromatographic techniques. Controversy exists regarding the optimal analytic technique to be used for cyclosporine monitoring and pharmacokinetic studies. This commentary addresses factors including: why the monitoring of cyclosporine concentrations is important, the differences between the biologic fluids and analytic techniques, when monitoring and special pharmacokinetic studies are indicated, what some major transplant centers have established as a "therapeutic range" for cyclosporine concentrations, and provides guidelines for the optimal clinical monitoring of cyclosporine concentrations.
免疫抑制剂环孢素的应用使临床器官移植近期成功率有了显著提高。与环孢素治疗相关的问题包括严重不良反应,如肾毒性、药物药代动力学的广泛变异性以及多种复杂的药物相互作用。药物浓度监测被视为接受环孢素治疗患者常规护理的一部分。然而,环孢素浓度可通过放射免疫测定法或高效液相色谱技术在不同生物体液中测定。关于用于环孢素监测和药代动力学研究的最佳分析技术存在争议。本评论涉及以下因素:为何监测环孢素浓度很重要、生物体液与分析技术之间的差异、何时进行监测及特殊药代动力学研究、一些主要移植中心确定的环孢素浓度“治疗范围”,并提供环孢素浓度最佳临床监测的指导原则。