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目的探讨五酯片用于肾移植受者他克莫司(FK506)药代动力学的影响及其长期疗效。方法选取38例处于稳定期的肾移植患者,包括主动要求FK506减量、药物快代谢型以及治疗其他疾病需加用五酯片治疗者。加用五酯片治疗后根据血药浓度调整FK506用量。对11例患者在五酯片使用前、后,多时间点采血测定FK506药代动力学参数的变化。对38例患者定期随访,记录其存活情况、移植物功能及并发症等。结果与加用五酯片前相比,11例自身对照患者的FK506谷浓度(C0)、峰浓度(Cmax)和药物剂量-时间曲线下面积(AUC0-12h)分别提高了192%、133%和124%,达峰时间(tmax)显著推迟(P<0.05)。加用五酯片后,38例患者随访21～50个月,FK506用量为(2.8±1.0)mg/d,C0为(5.8±2.2)ng/ml。38例患者中,1例死于巨细胞病毒肺炎;1例自行减药致急性体液性排斥反应,最终恢复血液透析;1例病理证实慢性排斥反应;1例病理证实肾炎复发;2例因新发糖尿病改用环孢素;其余移植肾功能正常。结论加用五酯片可显著影响肾移植患者FK506口服生物利用度,长期使用未见明显与之相关的不良反应。
Objective To investigate the effects and the long-term effects of pentasil tablets on the pharmacokinetics of tacrolimus (FK506) in renal transplant recipients. Methods Thirty-eight patients with stable renal transplant recipients were enrolled in this study, including the active reduction of FK506, rapid metabolism of drugs and the treatment of other diseases. Plus five-chip treatment based on blood concentration adjusted FK506 dosage. Eleven patients were tested for changes in the pharmacokinetic parameters of FK506 before and after the pentacetate tablets were taken at various time points. 38 patients were followed up regularly, record the survival, graft function and complications. Results The areas under the C0, Cmax and AUC0-12h of FK506 were increased by 192%, 133% And 124% respectively. The peak time (tmax) was significantly delayed (P <0.05). Fifty-eight patients were followed up for 21-50 months. The dosage of FK506 was (2.8 ± 1.0) mg / d and the C0 was (5.8 ± 2.2) ng / ml. Of the 38 patients, 1 died of cytomegalovirus pneumonia, 1 case of acute hypoxemia caused by self-administration of drug and finally hemodialysis, 1 case of chronic rejection confirmed by pathology, 1 case of recurrent nephritis and 2 cases of new Diabetes switch to cyclosporine; other graft normal function. Conclusion The use of pentasil tablets can significantly affect the oral bioavailability of FK506 in renal transplant recipients, and there is no obvious adverse reaction associated with long-term use of FK506 in renal transplant recipients.