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布比卡因和依替卡因在人体中的内脏清除率及全身毒性

Splanchnic elimination and systemic toxicity of bupivacaine and etidocaine in man.

作者信息

Wiklund L, Berlin-Wahlén A

出版信息

Acta Anaesthesiol Scand. 1977;21(6):521-8. doi: 10.1111/j.1399-6576.1977.tb01255.x.

Abstract

Fifteen healthy young volunteers were studied in connection with an intravenous infusion of a local anaesthetic agent. Seven received bupivacaine and eight etidocaine in a dose rate of 2 mg.min-1 over a period of 150 min. The hepatic blood flow and arterial-hepatic venous differences of the two drugs were measured. The estimated hepatic blood flow increased during the infusion of both drugs. While the splanchnic extraction ratio decreased during infusion of bupivacaine to 0.41 +/- 0.13, the same variable did not change (0.76 +/- 0.07) when etidocaine was infused. After 150 min infusion, the splanchnic clearance of bupivacaine and etidocaine was 0.76 +/- 0.27 and 1.32 +/- 0.21 1.min-1, respectively. Slight symptoms of central nervous toxicity were noted towards the end of the bupivacaine infusion, while no such symptoms appeared with etidocaine. A comparison between earlier published data on the blocking properties and the disposition pharmacokinetics of the two drugs shows that etidocaine is likely to confer a clinical advantage over bupivacaine as regards toxicity.

摘要

对15名健康年轻志愿者进行了一项与静脉输注局部麻醉剂有关的研究。7名受试者接受布比卡因,8名接受依替卡因,给药速率为2毫克·分钟⁻¹,持续150分钟。测量了两种药物的肝血流量以及动脉-肝静脉差值。在两种药物输注期间,估计的肝血流量均增加。在输注布比卡因期间,内脏提取率降至0.41±0.13,而输注依替卡因时该变量未发生变化(0.76±0.07)。输注150分钟后,布比卡因和依替卡因的内脏清除率分别为0.76±0.27和1.32±0.21升·分钟⁻¹。在布比卡因输注接近尾声时,出现了轻微的中枢神经毒性症状,而依替卡因未出现此类症状。对两种药物先前发表的关于阻滞特性和处置药代动力学的数据进行比较表明,就毒性而言,依替卡因可能比布比卡因具有临床优势。

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