紫锥菊的影响(紫锥菊根紫竹)体内的细胞色素P450活动。

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黄Gorski JC, SM,平托,洗澡,Hilligoss JK, Zaheer NA,德赛M, SD米勒M,大厅

紫锥菊的影响(紫锥菊根紫竹)体内的细胞色素P450活动。

中国新药杂志。2004年1月,75 (1):89 - 100。doi: 10.1016 / j.clpt.2003.09.013。

PubMed ID

14749695 (在PubMed

]

文摘

背景:紫锥菊是一种广泛使用的非处方草药。药酒的紫锥菊已被证明在体外抑制细胞色素P450 (CYP)。紫锥菊的影响(紫锥菊根紫竹)CYP体内活动评估使用CYP探针药物咖啡因(CYP1A2)、甲苯磺丁脲(CYP2C9),右美沙芬(CYP2D6)和咪达唑仑(肝脏和肠道CYP3A)。方法:12个健康受试者(6人)-周期,完成了这个非盲、固定的时间表。咖啡因、甲苯磺丁脲、右美沙芬和口服给药和静脉注射咪达唑仑是管理前后短疗程的紫锥菊(400毫克每天4次,8天)来确定体内CYP的活动。结果:紫锥菊管理系统性的咪达唑仑间隙显著增加了34%,从32 + / - 7 L / h 43 + / - 16 L / h (P = .003;90%可信区间(CI), 116% - -150%),并显著降低咪达唑仑曲线下面积减少23%,从127 + / - 36 microg。h / L - 102 + / - 43 microg。h / L (P = .024;90%可信区间,63% - -88%)。 In contrast, the oral clearance of midazolam was not significantly altered (P =.655; 90% CI, 75%-124%), 137 +/- 19 L/h compared with 146 +/- 71 L/h. The oral availability of midazolam after echinacea dosing was significantly increased (P =.028; 90% CI, 108%-153%), from 0.23 +/- 0.06 to 0.33 +/- 0.13. Hepatic availability (0.72 +/- 0.08 versus 0.61 +/- 0.16; P =.006; 90% CI, 73%-90%) and intestinal availability (0.33 +/- 0.11 versus 0.61 +/- 0.38; P =.015; 90% CI, 125%-203%) were significantly altered in opposite directions. Echinacea dosing significantly reduced the oral clearance of caffeine, from 6.6 +/- 3.8 L/h to 4.9 +/- 2.3 L/h (P =.049; 90% CI, 58%-96%). The oral clearance of tolbutamide was reduced by 11%, from 0.81 +/- 0.18 L/h to 0.72 +/- 0.19 L/h, but this change was not considered to be clinically relevant because the 90% CIs were within the 80% to 125% range. The oral clearance of dextromethorphan in 11 CYP2D6 extensive metabolizers was not affected by echinacea dosing (1289 +/- 414 L/h compared with 1281 +/- 483 L/h; P =.732; 90% CI, 89%-108%). CONCLUSIONS: Echinacea (E purpurea root) reduced the oral clearance of substrates of CYP1A2 but not the oral clearance of substrates of CYP2C9 and CYP2D6. Echinacea selectively modulates the catalytic activity of CYP3A at hepatic and intestinal sites. The type of drug interaction observed between echinacea and other CYP3A substrates will be dependent on the relative extraction of drugs at hepatic and intestinal sites. Caution should be used when echinacea is coadministered with drugs dependent on CYP3A or CYP1A2 for their elimination.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
紫锥菊	细胞色素P450 3 a4	蛋白质	人类	未知的	诱导物	细节