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目的 探讨FK506血药浓度与急性排斥反应及毒副反应的关系。方法 10例肾移植术后患者，予FK506为基础的免疫抑制治疗，首次服药后进行药代动力学测定，并记录术后FK506的用药量、急性排斥反应、药物毒副反应的发生情况。结果 峰值时间t（peak）为（1.4797±1.2174）h，分布相半衰期（t1/2β beta）为（10.8065±12.0799）h，平均滞留时间（MRT）为（8.0535±4.4750）h。2例病人在术后1月内发生急性排斥反应； 2例病人在术后1月内发生糖尿病。术后1月内急性排斥反应组与非排斥反应组的FK506浓度无明显差异，术后1月内糖尿病组的FK506浓度显著高于非糖尿病组。结论 我国肾移植成人患者口服FK506药代动力学个体差异大，用药应个体化；FK506具有很强的免疫抑制效应，能很好地预防急性排斥反应；在一定的浓度范围内，FK506的血药浓度与急性排斥反应的发生没有相关性，但随着药物浓度的增加，FK506的毒副反应明显增加；小剂量低谷值浓度用药能取得良好疗效。
Objective To investigate the relationship between plasma concentration of FK506 and acute rejection and toxicity. Methods Ten patients after renal transplantation were treated with FK506 - based immunosuppression. The pharmacokinetics of FK506 was measured after the first dose. The dose of FK506, acute rejection and drug toxicity were recorded. Results The peak time (t) was (1.4797 ± 1.2174) h, the distribution phase half-life was (10.8065 ± 12.0799) h, and the mean retention time (MRT) was (8.0535 ± 4.4750) h. Two patients developed acute rejection within 1 month after operation; 2 patients developed diabetes within 1 month after operation. There was no significant difference in the concentration of FK506 between the acute rejection group and the non-rejection group within 1 month after surgery. The FK506 concentration of the diabetic group was significantly higher than that of the non-diabetic group within 1 month after operation. Conclusions The pharmacokinetics of oral FK506 in adult renal transplant recipients in our country vary widely and should be individualized. FK506 has a strong immunosuppressive effect and can well prevent acute rejection. In a certain range of concentration, FK506 blood drug There was no correlation between the concentration and the occurrence of acute rejection. However, with the increase of drug concentration, the toxicity of FK506 increased obviously. The low dose and low concentration of drug could achieve good effect.