异丙酚对人肝微粒体的影响细胞色素P450的活动。
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•麦基洛普爵士D,野生MJ,黄油CJ, Simcock C
异丙酚对人肝微粒体的影响细胞色素P450的活动。
Xenobiotica。1998年9月28日(9):845 - 53。doi: 10.1080 / 004982598239092。
- PubMed ID
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9764927 (在PubMed]
- 文摘
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1。潜在的异丙酚抑制主要人类细胞色素P450酶的活动检查使用人类肝微粒体体外。异丙酚产生抑制CYP1A2(非那西汀O-deethylation), CYP2C9(甲苯磺丁脲4羟基化),CYP2D6(右美沙芬O-demethylation)和CYP3A4(睾酮6 beta-hydroxylation)活动与IC50 = 40, 49岁,分别为213和32 microM。Ki异丙酚对所有这些CYP2D6酶除了,异丙酚显示小抑制活动,30岁,分别为30和19 microM cyp 1 a2, 2 c9和3 a4。2。Furafylline、sulphaphenazole奎尼丁和酮康唑的选择性抑制剂cyp 1 a2, 2 c9, 2 d6和3 a4分别比异丙酚更强有力的IC50 = 0.8, 0.5, 0.2和0.1 microM;furafylline sulphaphenazole产生Ki = 0.6和0.7分别microM。3所示。治疗血药浓度的异丙酚(20 microM;3 - 4 microg /毫升)的体外Ki估计为每个主要的人类P450酶被用来估计细胞色素P450抑制的程度,可能产生体内的异丙酚。 This in vitro-in vivo extrapolation indicates that the degree of inhibition of CYP1A2, 2C9 and 3A4 activity which could theoretically be produced in vivo by propofol is relatively low (40-51%); this is considered unlikely to have any pronounced clinical significance. 4. Although propofol has now been used in > 190 million people since its launch in 1986, there are only single reports of possible drug interactions between propofol and either alfentanil or warfarin. Consequently, it is difficult to conclude from either the published literature or the ZENECA safety database whether there is any evidence to indicate that propofol produces clinically significant drug interactions through inhibition of cytochrome P450-related drug metabolism.
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药物 酶 类 生物 药理作用 行动 酮康唑 细胞色素P450 2 c9 蛋白质 人类 未知的抑制剂细节 异丙酚 细胞色素P450 1 a2 蛋白质 人类 未知的抑制剂细节 甲苯磺丁脲 细胞色素P450 2 c9 蛋白质 人类 未知的底物细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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