摘要
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 explore the relationship of the whole blood concentrations of FK506 with the occurrence of acute rejection after renal transplantation and further, with the toxicity of this medication. Methods Ten patients with renal transplantation were given FK506-based immunosuppressive regimen 24 h after the operation. Heparinized blood samples were obtained after the initial oral administration of the drug for the pharmacokinetic evaluation. The FK506 dosage, the episodes of acute rejection and the toxicity of the medication were recorded in detail. Results t(peak) was (1.4797±1.2174) h，t1/2 beta was (10.8065±12.0799) h, and the mean residence time (MRT) was (8.0535±4.4750) h. Within the first postoperative month, 2 patients experienced acute rejection and 2 others developed diabetes which necessirare insulin therapy. The blood concentrations of the drug were not significantly different between patients with acute rejection and those without, but were significantly different between diabetic and non-diabetic patients. Conclusions FK506 is an effective prophylactic immunosuppressant for renal transplantation. The whole blood concentrations, in a certain range, are not corresponding to the episode of acute rejection. There was a significant tendency for side effects with increase of the dose concentrations, and small dose low concentrations of Fk506 can achieve good effect and reduce its toxicity.
出处
《第一军医大学学报》
CSCD
2000年第6期539-540,545,共3页
Journal of First Military Medical University
关键词
FK506
肾移植
药代动力学
血药浓度
Fk506
pharmacokinetics
kidney transplantation toxicity
side effect
