Cheymol G
Service de Pharmacologie Hôpital Saint-Antoine, Paris.
Bull Acad Natl Med. 1992 Oct;176(7):1023-31; discussion 1031-2.
Cyclosporine (CsA) has played a major role in the development of organ transplantation. However, its use in the prevention of liver graft rejection is somewhat delicate because the liver plays an essential role in the intestinal absorption, metabolism and excretion of CsA. Interindividual differences in CsA pharmacokinetics are large, and clearance can vary by a factor of 40 in liver transplant recipients. During CsA therapy, the intact molecule is assayed in whole blood by means of specific technique. The margin between immunosuppressive and nephrotoxic concentration is poorly defined. The interpretation of blood concentrations must take into account the mode of administration, associated drug therapy, the time since grafting, and pathological episodes. The recommend trough concentrations are 150-200 ng/ml during the first three months.
环孢素（CsA）在器官移植发展过程中发挥了重要作用。然而，其用于预防肝移植排斥反应时情况较为复杂，因为肝脏在CsA的肠道吸收、代谢及排泄过程中起着至关重要的作用。CsA药代动力学的个体差异很大，肝移植受者的清除率可能相差40倍。在CsA治疗期间，通过特定技术在全血中检测完整分子。免疫抑制浓度与肾毒性浓度之间的界限尚不明确。血药浓度的解读必须考虑给药方式、联合药物治疗、移植后的时间以及病理情况。前三个月推荐的谷浓度为150 - 200 ng/ml。
