肾移植后他克莫司普通剂型转换为缓释剂型时基于基线谷浓度的调整方案  

Conversion of tacrolimus from general dosage form to sustained release based upon baseline trough concentration in renal transplant recipients

作　　者：李景 赵娟芝 舒婧娴 黄斌 梁嘉碧[1] 田琳[1] 郭振宇[1] Li Jing;Zhao Juanzhi;Shu Jingxian;Huang Bin;Liang Jiabi;Tian Lin;Guo Zhenyu(Department of Clinical Pharmacy,Fifth Affiliated hospital,Sun Yat-Sen University,Zhuhai 519000,China)

机构地区：[1]中山大学附属第五医院,广东珠海519000

出　　处：《中华器官移植杂志》2020年第8期482-486,共5页Chinese Journal of Organ Transplantation

摘　　要：目的分析肾移植术后不同基线血他克莫司谷浓度(C0)的受者,将他克莫司普通剂型转换为他克莫司缓释胶囊后C0的变化情况及效果。方法根据肾移植受者术后基线C0,将130例受者分为两组,A组受者转换前基线C0≥6μg/L,普通剂型与缓释剂型他克莫司剂量按1∶1转换,B组受者基线C0<6μg/L,普通剂型与缓释剂型他克莫司剂量按1∶1.1转换。比较两组在药物转换前后C0的变化情况及相关肾脏指标的变化。结果与转换前相比,转换后两组间他克莫司日平均用量和单位体重平均用量的差异均有统计学意义(P<0.001)。与转换前相比,两组受者在转换后第7天的C0明显降低,差异均有统计学意义(P<0.001)。转换4周(第28天)时B组受者C0波动范围较小,与转换前比较,差异无统计学意义(P=0.126);而未调整初始剂量的A组受者转换第28天的C0仍明显下降,与转换前比较,差异统计学意义(P<0.001)。结论当受者基线C0低于6μg/L,在将他克莫司普通剂型转换成他克莫司缓释制剂时增加10%~20%左右的用药剂量,以维持C0的稳定,避免C0出现大范围波动。Objective To explore the changes of blood trough concentration of tacrolimus(C0)at different baselines after renal transplantation and the change of C0 after converting tacrolimus into tacrolimus sustained-release capsules to provide rationales for dose adjustment of immunosuppressants.Methods According to different baseline values of C0,130 renal transplant recipients were divided into two groups.In group A,C0 was>6 ng/ml and the conversion ratio between sustained-release and ordinary dosage forms was 1:1.At a baseline C0 of<6μg/L in group B,conversion dose should be raised appropriately.The changes of C0 after drug conversion and the effects of related renal parameters were compared between two groups.Results The daily average dosage of tacrolimus and the average dosage of unit weight per recipient pre-and post-conversion were significantly different between two groups(P<0.001).As compared with its pre-conversion value,C0 was statistically significant at Day 7 post-conversion.At Day 28 post-conversion,there was a small fluctuation range of C0 in group B and no significant difference existed in blood drug concentration pre-and post-conversion(P=0.126)in group A without adjusting an initial dose(C0>6μg/L).Yet significant statistical difference in C0 existed between Day 28 and pre-conversion(P<0.001).Conclusions At a steady-state value of C0<6μg/L in Chinese renal transplant population,dosage should be boosted by 10%-20%.This adjustment maintains the stability of blood concentration and avoids a large fluctuation of C0.

关 键 词：肾移植 他克莫司 血药浓度 免疫抑制剂 

分 类 号：R699.2[医药卫生—泌尿科学]