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离体兔心肌对硫喷妥钠的摄取动力学研究 |
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毛卫克 蒲倩 曹林森 J.X.Mazoit
摘要 目的：研究硫喷妥钠在离体兔心肌的摄取动力学过程。方法：以三种浓度硫喷妥钠(500μmol、1500μmol、500μmol)持续灌注兔心肌共15分钟，应用高效液相色谱法测定心肌灌出液内硫喷妥钠浓度，用左室压力最大上升速率(LV+dp/dtmax)作为效应指标。结果：硫喷妥钠在心肌内摄取分布符合二室开放模型，它能较快分布于心肌组织(T1／2α=0.5±0.1分钟)，但从心肌清除较慢(T1／2β=25.3±10.1分钟)。药物自中央室向周边室的转运速率快于自周边室向中央室的转运。对LV+dp/dtmax的最大理论抑制效应(Emax)为19.0+11.2kPa*s－1。结论：离体兔心肌对硫喷妥钠的摄取过程符合二室开放模型，其特点为快速分布而清除较慢。
关键词 硫喷妥钠 药代动力学 心肌 在体外
Myocardial uptake of thiopental in the isolated rabbit heart：the study of pharmacokinetics and pharmacodynamics Mao Weike，Pu Qian，Cao Linsen，et al．Department of Anesthesiology，Union Hospital，Tongji Medical University，Wuhan 430022
Abstract Objective：To study the dynamic process of myocardial uptake of thiopental in the isolated rabbit hearts．Method：Thiopental at doses of 500μmol，1500μmol and 500μmol was given sequentially to the perfused rabbit heart in a total time of 15 min．The outflow concentration of thiopental was measured with high performance liquid chromatography and the left ventricular +dp／dtmax served as a effective parameter.Result：The disposition and elimination of thiopental can be best described by a two-compartment open model．It can disposed into myocardium rapidly（T1／2α=0.5±0.1 min),but elimination was relatively slow （T1／2β＝25．3±10．1 min）．The transfer rate was slower from peripheral to central compartment than from central to peripheral compartment．The theoritical maximum depressant effect of thiopental on ＋dp/dt(Emax）was 19．0±11．2 kPa．s－1corresponding to 1／10 E０．Conclusion：The myocardial uptake of thiopental can be fitted to a two-compartment open model with rapid disposition and relative slow elimination process．
Key words Thiopental Pharmacokinetics Mycardium In vitro
硫喷妥钠(Sodium pentothal，SP）是常用的静脉麻醉药之一，它在临床剂量范围内即有直接心肌抑制作用，既往多侧重研究其全身药代动力学与药效学的关系。实际上，药物从血管内透过多层生物屏障到达作用位点并产生相应效应，与组织器官对它的摄取与分布密切相关，而对上述摄取规律的研究能更精确地反映其体内过程。为此本文在离体兔[1] [2] [3] 下一页
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