尿毒症血透病人静脉应用左旋卡尼汀的药代动力学  

Pharmacokinetics following administration of single 1 g L carnitine intravenous dose inhemodialyzed patients with uremia

作　　者：徐洪实[1] 沈兰贞[1] 梅长林[1] 顾书华[2] 陈蕾[1] 

机构地区：[1]第二军医大学附属长征医院肾内科,上海200003 [2]常州三维工业技术研究所,常州213003

出　　处：《中国药理学通报》1999年第5期467-469,共3页Chinese Pharmacological Bulletin

摘　　要：目的　测定血透病人静脉应用左旋卡尼汀的药代动力学，以指导临床治疗。方法　于血透后ｄ ２ ８：００ 静脉推注左旋卡尼汀１ ｇ，在用药前、用药后０－５ ，１ ，２，４，８，１２ ，２４ ｈ 以及下次血透前、后分别取血测定血浆游离左旋卡尼汀浓度。采用二室开放模型，用非线性回归分析研究左旋卡尼汀的药代动力学。同时分析血透对左旋卡尼汀代谢的影响。结果　①血透病人静脉应用左旋卡尼汀的药代动力学符合二室开放模型，用药后ＡＵＣ为３７３８ ｍ ｍｏｌ·ｈ·Ｌ－１ ，②清除半衰期为８－４０ ｈ，清除相常数为０－０８３ ｈ－１ ，血浆左旋卡尼汀清除率为１－６５ Ｌ·ｈ－１ 。血透可明显清除左旋卡尼汀，一次血透血浆游离左旋卡尼汀浓度可下降６６％ 。结论　左旋卡尼汀在尿毒症维持血透病人中清除缓慢，用药后可维持更长时间的高水平药物浓度。AIM Pharmacokinetic parameters following L carnitine administration of single intravenous dose in hemodialyzed patients was determined. METHODS L carnitine 1 0 g was intravenously given at 8:00 am of next day after hemodialysis.Blood samples were taken at 0, 0 5, 1, 2, 4, 8, 12, 24 h after administration and before and after next hemodialysis session.Plasma free carnitine(FC) concentration was determined. Two compartment open model and nonlinear regrssion analyses were taken to study pharmacokinetics of L carnitine.Effect of hemodialysis on L carnitine clearance was also analyzed. RESULTS ①The plasma concentration versus time profiles following administration of the injectable solution L carnitine were best fitted two compartment open model.AUC was much higher than that in normal subjects. Elimination half life was longer than in normal subjects. ② L carnitine was obiviously eliminated during hemodialysis. There was a 66% decline in plasma FC cocentration during one hemodialysis session. CONCLUSION Elimination of L carnitine was slower in hemodialyzed patients. L carnitine was given to maintain high plasma level for a longer time. L carnitine was significantly eliminated by hemodialysis. So further supplementation was needed after hemodialysis.

关 键 词：尿毒症 血液透析 左旋卡尼汀 药代动力学 

分 类 号：R969.1[医药卫生—药理学] R459.5[医药卫生—药学]