奥美拉唑的药物动力学(CYP2C19基质)和比较两个突变的等位基因,CγP2C19m1外显子5和CγP2C19m2外显子4,在日本主题。

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Ieiri我日本久保田公司T Urae,木村M,和田Y,玛米亚K,吉冈年代,老大,Amamoto T,中村K, Nakano年代,Higuchi年代

奥美拉唑的药物动力学(CYP2C19基质)和比较两个突变的等位基因,CγP2C19m1外显子5和CγP2C19m2外显子4,在日本主题。

中国新药杂志。1996年6月,59岁(6):647 - 53。doi: 10.1016 / s0009 - 9236 (96) 90004 - 1。

PubMed ID

8681489 (在PubMed

]

文摘

奥美拉唑的药动学特征是研究日本在27个健康的志愿者,和结果进行了分析与基因型的两个突变,CgammaP2C19m1第5外显子和外显子4 CgammaP2C19m2与穷人代谢表型有关。分析了27个人,10为野生型纯合子(wt)等位基因第5外显子和外显子4 (wt / wt;37.0%,模式GI),五个是杂合的CgammaP2C19m1 (wt / m1;18.5%,G2),五个是杂合的CgammaP2C19m2 (wt /平方米;18.5%,G3),两人杂合的两个缺陷(m1 /平方米;7.4%,G4),五个是纯合子CgammaP2C19m1 (m1 / m1;18.5%,G5)。m1和m2突变的等位基因频率分别为0.31和0.13,分别。奥美拉唑的新陈代谢率之间的相关性,观察基因型。奥美拉唑的平均间隙值模式G1, G2, G3、G4, G5分别为1369.0,332.7,359.0,70.8,和89.5毫升/小时/公斤。 The relative area under the serum concentration-time curve (AUC) ratio of omeprazole to 5-hydroxyomeprazole in patterns G1, G2, G3, G4, and G5 was 1:2.8:3.4:16:17.2. A similar relation was observed in the omeprazole/5-hydroxyomeprazole serum concentration ratio, determined 3 hours after drug intake (1:3:4:18.8:20.3). There were significant (p < 0.05 to 0.01) differences in the disposition kinetics of omeprazole between the subjects with patterns G1, G2, and G3 and the subjects with patterns G4 and G5. The results indicate that the 5-hydroxylation pathway of omeprazole is clearly impaired in subjects with m1/m2 and m1/m1.

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药物酶

药物	酶	类	生物	药理作用	行动
奥美拉唑	细胞色素P450 2 c19	蛋白质	人类	未知的	底物 抑制剂	细节