血液透析患者静脉应用左旋肉碱（可益能）的药代动力学研究

刘惠兰; 张晓洁; 曹峰

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中国血液净化 ›› 2003, Vol. 2 ›› Issue (6) : 298-300.

论著

血液透析患者静脉应用左旋肉碱（可益能）的药代动力学研究

刘惠兰张晓洁曹峰

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摘要

目的研究血液透析患者静脉应用左旋肉碱的药代动力学特点，探讨治疗肉碱缺乏的给药途径、剂量、疗程。方法选择9例本透析中心病情稳定的患者，男5例，女4例。于每次血液透析结束回血前3分钟，静脉推注1g左旋肉碱，共用药8周（26次透析）。应用酶法检测首次给药前（0时）、给药后1.5分钟、3分钟、15分钟、30分钟、1小时、2小时、4小时、8小时、12小时、24小时肉碱的血药浓度，分析单次静脉应用左旋肉碱的药代动力学特点。另外，于首次给药、给药2周、4周、6周、8周分别检测透析前后、透析液中肉碱浓度，研究多次用药后血浆肉碱水平变化和透析液中的清除量。结果维持性血液透析患者用药前血浆肉碱浓度大大低于正常值40～50umol/L；首次于透析结束时静脉给予1g左旋肉碱的药代动力学符合二室开放模型。给药后血药浓度很快增加，然后迅速下降，AUC大，但半衰期与正常人接近；每次透析过程中均可清除大量的肉碱，并且随着血药浓度增加而清除增加；连续给药期6至8周后透析前后肉碱水平基本维持稳定。结论血液透析患者外源性补充肉碱的药代动力学特点与正常人不同，透析清除是药物排泄的主要途径，因此须6～8周连续透析后补充用药，使组织及血浆肉碱水平恢复。

Abstract

Objective To evaluate the pharmacokinetic characters of intravenous administered L-carnitine in hemodialysis patients. Methods One gram L-carnitine was given by intravenous after hemodialysis in 9 patients, blood samples were taken at 0, 1.5, 3, 15min and 0.5、1、2、4、8、12、24h to investigate the pharmacokinetic parameters for single dose L-carnitine. Then study the carnitine levels in plasma before /after hemodialysis and in hemodialysates at 0、2、4、6、8 weeks during. Results The plasma carnitine level were lower than normal in hemodialysis patients； The pharmacokinetic parameters for single dose L-carnitine were fitted two-compartment open model； L-carnitine conformed to during hemodialysis greatly；After repeated administration of L-carnitine for 6～8 weeks, the plasma carnitine level can keep stable. Conclusion The pharmacokinetic characters of intravenous administered L-carnitine in hemodialysis patients were different from normal. L-carnitine was significantly eliminated to hemodialysate, so repeated supplementations were needed for 6～8 weeks after each hemodialysis. 