目的　研究发生环孢素A(CsA)肝损害的肾移植患者口服CsA胶囊的药代动力学特点及意义。方法　测定 32例服用CsA胶囊后发生肝功能异常者的血CsA浓度谷值 (C0 )及峰值(Cmax)、达到峰值的时间 (Tmax)、浓度时间曲线下面积 (AUC)及CsA清除率 (CI) ,统计出现CsA肝损害的时间、肝功能异常的程度、CsA的用量 ,并针对肝功能异常程度的不同给予不同的治疗方案 ;以30例肝功能正常的肾移植患者作对照。结果　随着肝功能异常程度的加重 ,C0 有明显上升的趋势 ,Cmax有明显下降的趋势 ,Tmax明显延长 ,中、重度肝功能异常者的C0 与AUC的相关性差 ;对轻度肝功能异常者 ,可根据其CsA的AUC适当减少CsA的用量 ,而中、重度肝功能异常患者 ,治疗时应增加其它肝毒性较小的免疫抑制剂的用量 ,并根据其CsA的AUC将CsA的用量减少 1/ 3～ 1/ 2 ,甚至停用CsA ,改为肝毒性较小的药物。结论　发生CsA肝损害的患者 ,其CsA药代动力学与肝功能正常者相比 ,差异有显著性 ;中、重度肝功能异常患者需定期监测CsA的AUC ,采取个体化治疗方案 Objective To investigate the pharmacokinetics and significance of CsA capsules in renal transplant recipients with cyclosporine A (CsA) injury. Methods The Cmax and Cmax, the peak time (Tmax), the area under the curve of concentration and time (AUC) and the rate of CsA clearance (CI) were measured in 32 patients with liver dysfunction after taking CsA capsules ), The time of CsA liver damage, the degree of liver dysfunction and the amount of CsA were counted, and different treatment regimens were given according to the different degree of liver dysfunction. Thirty cases with normal liver function were used as control. Results With the aggravation of abnormal liver function, C0 increased obviously, Cmax decreased obviously, Tmax prolonged obviously, and the correlation between C0 and AUC was worse in patients with moderate and severe liver dysfunction. For patients with mild liver dysfunction , According to its CsA AUC appropriate to reduce the amount of CsA, and in patients with moderate and severe liver dysfunction, the treatment should increase the amount of other less toxic hepatotoxicity of immunosuppressive agents, and according to its CsA AUC will reduce the amount of CsA 1 / 3 ~ 1/2, or even disable CsA, to liver less toxic drugs. Conclusions There is significant difference in CsA pharmacokinetics between patients with CsA liver damage and those with normal hepatic function. Patients with moderate and severe hepatic dysfunction need regular monitoring of AUC of CsA and adopt individualized treatment plan