[蝙蝠葛碱的首过效应]
[First-pass effect of dauricine].
作者信息
Gui Y T, Du Z H, Zeng F D, Hu C J
机构信息
Department of Clinical Pharmacology, Tongji Medical University, Hankou, China.
出版信息
Zhongguo Yao Li Xue Bao. 1993 Mar;14(2):173-5.
The first-pass effect of dauricine (Dau) was compared with that of lidocaine (Lid) by measuring the ventricular fibrillation threshold (VFT) and dauricine plasma concentration in rats or rabbits. After forelimb or mesenteric vein (imv) infusion of Dau at a rate of 1 mg.kg-1 x min-1 in rats, the VFT were 1.64-3.17 or 1.60-2.11 V, respectively. In the case of Lid at 2.5 mg.kg-1 x min-1, the VFT were 1.69-4.79 or 1.67-2.80 V, respectively, after ear vein (iev) or imv infusion of Dau at a rate of 0.5 mg.kg-1 x min-1 in rabbits, the VFT were 6.50-12.14 or 5.81-7.43 V, respectively. Plasma Dau concentration through iev infusion was significantly higher than that through imv route. As the dose of imv infusion increased, AUC of Dau showed a nonlinear increase. The results suggested that Dau showed a considerable first-pass effect, which was dose-dependent.
通过测量大鼠或家兔的心室颤动阈值（VFT）和蝙蝠葛碱（Dau）血浆浓度，比较了蝙蝠葛碱（Dau）和利多卡因（Lid）的首过效应。大鼠前肢或肠系膜静脉（imv）以1 mg·kg⁻¹·min⁻¹的速率输注Dau后，VFT分别为1.64 - 3.17 V或1.60 - 2.11 V。对于以2.5 mg·kg⁻¹·min⁻¹的速率输注的Lid，大鼠耳静脉（iev）或imv输注后，VFT分别为1.69 - 4.79 V或1.67 - 2.80 V。家兔iev或imv以0.5 mg·kg⁻¹·min⁻¹的速率输注Dau后，VFT分别为6.50 - 12.14 V或5.81 - 7.43 V。通过iev输注的血浆Dau浓度显著高于通过imv途径的浓度。随着imv输注剂量增加，Dau的AUC呈非线性增加。结果表明，Dau显示出相当大的首过效应，且具有剂量依赖性。
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