咪达唑仑和1 '的药物-hydroxymidazolam CYP3A5基因型在中国不同。
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Shih PS,黄JD
咪达唑仑和1 '的药物-hydroxymidazolam CYP3A5基因型在中国不同。
药物金属底座Dispos。2002; 12月30 (12):1491 - 6。doi: 10.1124 / dmd.30.12.1491。
- PubMed ID
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12433824 (在PubMed]
- 文摘
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CYP3A的亚科代表最丰富的细胞色素p450在人类肝脏和胃肠道和在异型生物质新陈代谢中扮演着非常重要的作用。CYP3A5表达在一个相对较小的白人人口和东方人。我们招募了42个中国志愿者确定CYP3A5基因型聚合酶链reaction-restriction片段长度多态性。基因型分析显示,CYP3A5 * 3等位基因存在于39的42个志愿者。CYP3A5 * 4和CYP3A5 * 5等位基因被发现在一个志愿者;和CYP3A5 * 2和CYP3A5 * 6等位基因也不见了。最常见的CYP3A5 * 3等位基因不表达CYP3A5而闻名。我们排除了其他CYP3A5基因型研究的意义CYP3A5 * 3咪达唑仑药物动力学。在这项研究中,每个志愿者被咪达唑仑片(7.5毫克)口服。收集血液样本分析时间浓度的咪达唑仑和1的-hydroxymidazolam高性能液相色谱法。 The average area under plasma concentration curve (AUC, 0-8 h) of midazolam was 9237 +/- 1050 ng-min/ml (mean +/- S.E.M.) in homozygous CYP3A5*3 (n = 14) subjects and 7934 +/- 768 ng-min/ml in heterozygous CYP3A5*1/*3 (n = 12) subjects, respectively. The average AUC (0-8 h) of 1'-hydroxymidazolam was 3748 +/- 427 ng-min/ml in homozygous CYP3A5*3 subjects and 3920 +/- 402 ng-min/ml in heterozygous CYP3A5*1/*3 subjects. The results indicated that the pharmacokinetics of midazolam and 1'-hydroxymidazolam was independent of CYP3A5 expression. Although the genetic polymorphism of CYP3A5 is well known, the results of this study suggested that the clinical consequence might be insignificant.
