Influence of Panax ginseng on cytochrome P450 (CYP)3A and P-glycoprotein (P-gp) activity in healthy participants.
Influence of Panax ginseng on cytochrome P450 (CYP)3A and P-glycoprotein (P-gp) activity in healthy participants.
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DOI：
10.1177/0091270011407194
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发表时间：
2012-06
影响因子：
2.9
通讯作者：
Penzak SR
中科院分区：
文献类型：
--
作者：
Malati CY;Robertson SM;Hunt JD;Chairez C;Alfaro RM;Kovacs JA;Penzak SR
许多草药制剂已被证明与处方药物相互作用，继发于细胞色素P450 （CYP）和/或p糖蛋白（P-gp）的调节。本研究以咪达唑仑和非索非那定为探针底物，研究人参对CYP3A和P-gp功能的影响。12名健康受试者（8名男性）完成了这项开放标签、单序列药代动力学研究。健康志愿者分别口服咪达唑仑8毫克和非索非那定120毫克，28天前后分别服用人参500毫克，每天两次。计算咪达唑仑和非索非那定给药前后药动学参数值并进行比较。从0到无穷远（AUC0-∞）、半衰期（T1/2）和最大浓度（Cmax）的几何平均比（参后/参前）显著降低，分别为0.66（0.55 ~ 0.78）、0.71（0.53 ~ 0.90）和0.74（0.56 ~ 0.93）。相反，非索非那定的药代动力学不受人参给药的影响。基于这些结果，人参似乎可以诱导肝脏和胃肠道的CYP3A活性。人参与CYP3A底物联用治疗范围窄的患者应密切监测底物用药是否有足够的治疗反应。
A number of herbal preparations have been shown to interact with prescription medications secondary to modulation of cytochrome P450 (CYP) and/or P-glycoprotein (P-gp). The purpose of this study was to determine the influence of Panax ginseng on CYP3A and P-gp function using the probe substrates midazolam and fexofenadine, respectively. Twelve healthy subjects (8 males) completed this open label, single sequence pharmacokinetic study. Healthy volunteers received single oral doses of midazolam 8 mg and fexofenadine 120 mg, before and after 28 days of P. ginseng 500 mg twice daily. Midazolam and fexofenadine pharmacokinetic parameter values were calculated and compared pre-and post P. ginseng administration. Geometric mean ratios (post-ginseng/pre-ginseng) for midazolam area under the concentration vs. time curve from zero to infinity (AUC0-∞), half life (T1/2), and maximum concentration (Cmax) were significantly reduced at 0.66 (0.55 – 0.78), 0.71 (0.53 – 0.90), and 0.74 (0.56 – 0.93), respectively. Conversely, fexofenadine pharmacokinetics were unaltered by P. ginseng administration. Based on these results, Panax ginseng appeared to induce CYP3A activity in the liver and possibly the gastrointestinal tract. Patients taking Panax ginseng in combination with CYP3A substrates with narrow therapeutic ranges should be monitored closely for adequate therapeutic response to the substrate medication.
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影响因子：
7.9
作者：
Budzinski, JW;Foster, BC;Arnason, JT
通讯作者：
Arnason, JT
影响因子：
2.8
作者：
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Ang, CYW
影响因子：
6.7
作者：
Gurley, BJ;Gardner, SF;Ang, CYW
通讯作者：
Ang, CYW
影响因子：
6.1
作者：
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通讯作者：
Stresser, DM
影响因子：
6.7
作者：
HUNT, CM;WATKINS, PB;GUZELIAN, PS
通讯作者：
GUZELIAN, PS