安定扩张宫颈作用的药动学与药效学关系探讨

TUDY ON THE CORRELATION BETWEEN THE PHARMACOKINETICS AND PHARMACODYNAMICS OF CERVICAL DILATION OF DIAZEPAM

本实验用高效液相色谱法测定静脉推注安定１０ｍｇ的１０例产妇血浆中安定和儿茶酚胺浓度，并观察宫口扩张情况，经实用药动学程序处理，安定在产妇体内血药浓度分布呈二室模型。为３．１７±１．２ｍｉｎ，为１７７．８±３７．３ｍｉｎ，ｖｄ为２．４４±１．２６１／ｋｇ，ｃｌ为７１．９±２１．１８ｍｌ／ｍｉｎ。安定血药浓度与血浆儿茶酚胺浓度的降低为正相关（ｙ＝３．６９＋９０．３１ｘ，ｒ＝０．８６，Ｐ＜０．０５），而宫口扩张速度与血浆儿茶酚胺浓度为负相关（ｙ＝１３．６３－０．０４ｘ），ｒ＝－０．９４，Ｐ＜（０．０５）．用药组与对照组有显著差异（Ｐ＜００１）．结果表明安定扩张宫颈可能不是直接作用，而是通过降低血浆中儿茶酚胺浓度而显效。

iasepam 10mg was given by iv to 10 women with active phase inlabor and changes of cervicaldila tion were observed. The plasma concentration of diazepam and catecholamine level weremeasure by high performance liquid chromatography simultaneusly during labor. Thepharmacokinetics parameters were calculated with pharmacokinetic program 3p87.The resultsshowed that the distribution of plasma concentration of diazepam in laber women were twocompartment model and the pharmacokinetic parameters were t1/2α:3.17± 1. 2min; t1/2β:177. 8 ± 37.3min; Vd:2.44 ± 126;C 1:71.9±21.18ml/min respectively.The correlation anaysis between the plasma concentration of diazepma and its effect ondecreasing plasma catecholamin was positive correlation(y=3.69 ± 90.31x,r=0.86,P<0.05).Therewas significant difference between the diazepam group and ihe control(P<0. 01).This experunentbdicated that diazepam could dilatc cervix by decreasing plasma catecholamines.