利多卡因及其代谢物作为肝功能标志物在犬体内的药代动力学研究。

B E Pérez-Guillé, F Villegas-Alvarez, A Toledo-López, M A Jiménez-Bravo, J F González-Zamora, M C Carrasco-Portugal, F J Flores-Murrieta, R E Soriano-Rosales
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摘要

测量肝脏代谢功能是检测和治疗肝功能衰竭的关键。几种测试已被广泛用于表征肝脏的完整性;然而,它们不评估器官的代谢功能,大多数需要多次抽血。本研究的目的是确定静脉注射利多卡因30分钟后,利多卡因代谢物单乙基甘氨酸乙酯(MEGX)与利多卡因浓度之比是否是肝脏代谢活性的良好标志。9只健康的狗和2只部分肝切除和自体移植的狗被纳入研究。单次静脉给药1.5 mg/kg利多卡因,在指定时间取血清样本,持续150分钟。采用高效液相色谱法测定血清利多卡因和MEGX浓度。采用非室室法获得药动学参数,测定每只狗MEGX的AUC除以利多卡因AUC的比值。该比值与给药后30分钟所获得的化合物浓度比值相关。得到了很好的一致性,表明单样本所得的比值可能有助于预测肝脏代谢功能。为了验证该测试,绘制了切除和自动移植的狗的肝脏,所得结果在健康狗的数值范围内。提示给药30 min后MEGX/利多卡因比值可作为肝脏代谢功能的良好指标。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmacokinetics of lidocaine and its metabolite as a hepatic function marker in dogs.

Measuring hepatic metabolic function is critical for detection and treatment of liver failure. Several tests have been widely used to characterize the integrity of liver; however, they do not evaluate the metabolic function of the organ, most requiring multiple blood draws. The purpose of this study was to establish if the ratio of the lidocaine metabolite monoethylglycinexylidide (MEGX) divided by lidocaine concentration at 30 min post intravenous lidocaine administration is a good marker of metabolic activity of the liver. Nine healthy and two partially hepatectomized and auto-transplanted dogs were included in the study. A single 1.5 mg/kg intravenous dose of lidocaine and serum samples were obtained at selected times for 150 minutes. Serum concentrations of lidocaine and MEGX were determined by a validated high-performance liquid chromatographic method. Pharmacokinetic parameters were obtained by non-compartmental methods and ratio of AUC of MEGX divided by AUC of lidocaine was determined for each dog. This ratio was correlated with the ratio of the concentration of the compounds obtained 30 minutes after drug administration. A good concordance was obtained, suggesting that ratio obtained with a single sample may be useful to predict the hepatic metabolism function. To validate the test, dogs hepatectomized and auto-transplanted were plotted and the results obtained were within the values obtained in healthy dogs. These results suggest that ratio of MEGX/lidocaine obtained 30 min after administration could be a good marker of hepatic metabolic function.

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