癫痫患者首过代谢增强导致利多卡因口服生物利用度降低。
Reduction of oral bioavailability of lignocaine by induction of first pass metabolism in epileptic patients.
作者信息
Perucca E, Richens A
出版信息
Br J Clin Pharmacol. 1979 Jul;8(1):21-31. doi: 10.1111/j.1365-2125.1979.tb05904.x.
Abstract
- The pharmacokinetics of lignocaine following single oral and intravenous doses have been investigated in six normal volunteers and in six patients receiving chronic antiepileptic drug therapy. 2. After intravenous administration, serum lignocaine levels declined biexponentially in all subjects. The serum clearance (mean +/- s.d.) was slightly higher in the patients (0.85 +/- 0.09 v 0.77 +/- 0.07 l/min) but the difference was not statistically significant. 3. Lignocaine bioavailability after oral administration was more than two-fold in the patients than in the normal subjects (0.15 +/- 0.06 v 0.37 +/- 0.09, P < 0.001). 4. It is suggested that the reduced bioavailability of lignocaine in the patients is a consequence of stimulation of hepatic first-pass metabolism by antiepileptic drugs.
摘要
- 已在6名正常志愿者和6名接受慢性抗癫痫药物治疗的患者中研究了单次口服和静脉注射利多卡因后的药代动力学。2. 静脉给药后，所有受试者的血清利多卡因水平呈双指数下降。患者的血清清除率（平均值±标准差）略高（0.85±0.09对0.77±0.07升/分钟），但差异无统计学意义。3. 口服给药后，患者体内利多卡因的生物利用度比正常受试者高出两倍多（0.15±0.06对0.37±0.09，P<0.001）。4. 提示患者体内利多卡因生物利用度降低是抗癫痫药物刺激肝脏首过代谢的结果。
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