Freysz M, Beal J L, D'Athis P, Mounie J, Wilkening M, Escousse A
Int J Clin Pharmacol Ther Toxicol. 1987 Jul;25(7):392-5.
Severe cardiovascular complications have been associated with regional anesthesia using bupivacaine. Furthermore, in our practice, axillary brachial plexus block is commonly used for surgical emergencies of the hand in out-patients. The pharmacokinetics parameters: peak height (Cmax), peak time (tmax), half life of plasma elimination (t1/2), total apparent clearance (Cl), mean time of plasma retention (t) were studied in 20 male and female patients (mean age 35 and 32 years) receiving axillary local anesthesia by bupivacaine (BU) only (A group = 100 mg), B group BU = 200 mg, or BU + lidocaine (LI) (C group = BU 100 mg + LI 200 mg), plasmatic BU and LI were simultaneously measured by HPLC method. There were no significant differences in the pharmacokinetic data observed in groups A, B and C; total apparent clearances and half times of plasma elimination of BU after brachial plexus block are similar compared to those observed after i.v. administration. Absorption of BU seems to be total while the value of Cmax are very low compared to usual neurotoxic plasma levels, but near that of plasma concentrations observed in cardiac complications. All the tmax observed were under 2 h and the dose independence of the kinetic of BU is not admissible in this study. The association of LI induce no modification of the kinetic of BU. This work concludes that in this way of administration, the absorption of BU seems to be total. Pharmacokinetics of BU is dose dependent and the association of LI induces no significant modification of BU kinetics.
严重的心血管并发症与使用布比卡因的区域麻醉有关。此外,在我们的实践中,腋路臂丛神经阻滞常用于门诊手部手术急诊。在20例男性和女性患者(平均年龄分别为35岁和32岁)中研究了药代动力学参数:峰高(Cmax)、达峰时间(tmax)、血浆消除半衰期(t1/2)、总表观清除率(Cl)、血浆滞留平均时间(t),这些患者仅接受布比卡因(BU)腋路局部麻醉(A组 = 100 mg)、B组BU = 200 mg或BU + 利多卡因(LI)(C组 = BU 100 mg + LI 200 mg),采用高效液相色谱法同时测定血浆中的BU和LI。A、B、C组观察到的药代动力学数据无显著差异;与静脉给药后观察到的数据相比,臂丛神经阻滞后BU的总表观清除率和血浆消除半衰期相似。BU的吸收似乎是完全的,而与通常的神经毒性血浆水平相比,Cmax值非常低,但接近心脏并发症中观察到的血浆浓度。观察到的所有tmax均在2小时以内,本研究中BU动力学的剂量独立性不成立。LI的联合使用未引起BU动力学的改变。这项研究得出结论,以这种给药方式,BU的吸收似乎是完全的。BU的药代动力学是剂量依赖性的,LI的联合使用未引起BU动力学的显著改变。