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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,而血透可明显清除药物使血透后需要再次补充
Objective To determine the pharmacokinetics of intravenous levocarnitine in patients with hemodialysis to guide the clinical treatment. Methods After intravenous injection of levocarnitine 1 g at d 2 at 8:00 after hemodialysis, before treatment, 0-5, 1, 2, 4, 8, 12 and 24 h after drug treatment, and before and after hemodialysis Blood were collected to measure plasma free L-carnitine concentration. A two-compartment open model was used to study the pharmacokinetics of L-carnitine using a non-linear regression analysis. The effect of hemodialysis on L-carnitine metabolism was also analyzed. Results ① The pharmacokinetics of intravenous L-carnitine in patients with hemodialysis was in accordance with the two-compartment open model. The AUC was 3738 m mol · h-1 after administration, ② the half-life of elimination was 8-40 h, and the elimination phase constant was 0 -083 h-1, plasma levocarnitine clearance rate of 1-65 L · h-1. Hemodialysis can be significantly cleared of L-carnitine, a hemodialysis plasma free L-carnitine concentration can be reduced by 66%. Conclusion L-carnitine in patients with uremia to maintain hemodialysis slow clearance after treatment can be maintained for a longer period of high levels of drug concentration, and hemodialysis can clear the drug to make hemodialysis need to replenish