目的:对碳酸利多卡因在硬膜外麻醉中的临床药物动力学及药效学特性进行探讨。方法:研究对象为15例实施硬膜外麻醉患者。采用荧光偏振免疫分析方法(FPIA)测定利多卡因血药浓度;放射免疫方法测定血浆肾素浓度。通过临床观察及测定血浆肾素水平评价药效学;将药代动力学及药效学研究结果与其盐酸盐进行比较。结果:药物动力学参数:达峰时间,达峰浓度,吸收速率常数及末端相半衰期分别为(0.30±0.04)h,(3.96±1.14)mg·L^-1,(10.92±2.36)h^-1和(1.95±0.08)h;药效学参数;麻醉起效时间,阻滞完善时间及麻醉持续时间分别为(4.38±0.78)min,(8.23±1.84)min和(57.22±10.35)min。结论:碳酸利多卡因吸收速率明显高于其盐酸盐;达峰时间亦快于其盐酸盐;体内消除半衰期与其盐酸盐的消除半衰期接近。临床麻醉杭州起效时间及阻滞完善时间快于盐酸利多卡因。研究结果证明:碳酸利多卡因用于硬膜外麻醉起效较快,但体内消除过程无明显改变。

OBJECTIVE:Pharmacokinetics and pharmacodynamics of lidocaine carbonate in patients during epidural anesthesia were investigated.METHODS:There were 15 patients performed epidural anesthesia enroed in this study.Serum levels of lidocaine and plasma renin concentrations were measured using FPIA and RIA,respectively.Pharmacodynamics was evaluated by subjective observation of an anesthetist and was assessed indirectly by plasma renin levels.The results of pharmacokinetics and pharmacodynamics of lidocaine carbonate were compared with those of lidocaine hydrochloride.RESULTS:The peak time,the maximal concentrations,constant of absorption rate and half life were (0.30±0.04)min,(3.96±1.14)mg·L^-1,(10.92±2.36)h^-1 and (1.95±0.08)h,respectively.Blockade,the onset time,finished time and persistent time of blockade were (4.38±0.78)min,(8.23±1.84)min and (57.22±10.35)min,respectively.CONCLUSION:The results shown constant of absorption rate of lidocaine carbonate was singificantly bigger than that of lidocaine hydrochloride;the peak time was shorter than that of lidocaine hydrochloride too;half life of lidocaine carbonate was almost identical with that of lidocaine hydrochloride.Onset time and finished time of blockade of lidocaine carbonate were shorter than those of its hydrochloride.The study suggested that onset of blockade of lidocaine carbonate was faster,but elimination of lidocaine in human body was not changed during epidural anesthesia.