Cheymol G
Service de Pharmacologie, Hôpital Saint-Antoine, Paris.
Therapie. 1992 Jul-Aug;47(4):319-21.
The therapeutic drug monitoring of cyclosporine (CsA) requires not only correct methodological conditions but also taking into consideration of numerous other factors involved in the value of blood drug concentrations. Main factors concern: the clinical state of patients. Liver function and bile flow act predominantly on drug clearance; the choice of monitoring parameters and of sampling time. Comparison was done of information given respectively by area under the curve and different sampling times. Usually blood concentration is monitored with trough level plus eventually another concentration measured 4-6 h after drug administration; the time-table. Blood concentrations are measured at steady-state period. Bioavailability of CsA increases in the immediate postoperative period after transplantation; ways of CsA administration. Trough level is influenced by dividing up of the daily dose. In case of continuous i.v. infusion mean blood concentration, but not trough concentration, is measured; drug interactions. Several drugs modify blood concentrations of CsA. Others induce an additive nephrotoxicity or immunosuppressive effect. Recommended blood trough concentrations vary with clinical indications, experience and therapeutic habits of each transplant center. Currently recommended values (CsA whole blood concentration determined by specific method) are 150-250 ng/ml in renal, heart, liver and bone marrow grafts, during the 3 months after transplantation, with good renal function. Concentrations are often higher for lung transplantation.
环孢素(CsA)的治疗药物监测不仅需要正确的方法学条件,还需要考虑许多其他影响血药浓度值的因素。主要因素包括:患者的临床状态。肝功能和胆汁流量主要影响药物清除率;监测参数和采样时间的选择。对曲线下面积和不同采样时间分别给出的信息进行了比较。通常在谷浓度时监测血药浓度,并最终在给药后4至6小时测量另一个浓度;时间表。在稳态期测量血药浓度。CsA的生物利用度在移植后的术后即刻会增加;CsA的给药方式。谷浓度受每日剂量分配的影响。在持续静脉输注的情况下,测量的是平均血药浓度而非谷浓度;药物相互作用。几种药物会改变CsA的血药浓度。其他药物会产生相加的肾毒性或免疫抑制作用。推荐的血药谷浓度因各移植中心的临床指征、经验和治疗习惯而异。目前推荐的值(通过特定方法测定的CsA全血浓度)在移植后3个月内,对于肾功能良好的肾、心、肝和骨髓移植患者为150 - 250 ng/ml。肺移植时的浓度通常更高。