瑞格列奈药物基因组学的研究进展

发布时间：2018-01-18 00:34

本文关键词：瑞格列奈药物基因组学的研究进展　出处：《中国药房》2017年35期 　论文类型：期刊论文

【摘要】：目的:了解瑞格列奈药物基因组学的研究进展,为瑞格列奈的临床个体化给药提供参考。方法:查阅近年来国内外相关文献,就瑞格列奈的药物基因组学的研究进行归纳和总结。结果:瑞格列奈相关的药物基因组学研究主要集中于药物代谢和转运相关基因、药物作用靶点和受体的编码基因、2型糖尿病(T2DM)易感基因等方面,其中KCNQ1、Neuro D1/BETA2、PAX4、NOS1AP、SLC30A8、IGF2BP2、UCP2、NAMPT为代表的T2DM易感基因对瑞格列奈药效学的影响是目前研究的重点。T2DM易感基因可能通过影响胰岛B细胞的增殖、腺苷三磷酸敏感性钾通道(KATP)和电压门控Ca~(2+)通道的表达和活性以及胰岛素分泌,从而增加T2DM的易感性并影响药物治疗反应性。CYP2C8、CYP3A4、SLCO1B1和MDR1等与药物代谢和转运有关的基因多态性可能影响瑞格列奈的药-时曲线下面积、峰浓度、半衰期和清除率等,间接影响药物疗效和安全性。在开展药物基因组学研究时,还应根据不同种族的等位基因频率来选择基因多态性位点,以期获得更大的临床应用价值。结论:基因多态性是瑞格列奈治疗反应性个体差异的部分原因,有望通过基因导向的个体化治疗提高疗效、减少不良反应。
[Abstract]:Objective: to understand the research progress of pharmacogenomics of repaglinide and to provide a reference for clinical individualized administration of repaglinide. Methods: to review the relevant literature at home and abroad in recent years. Results: the pharmacogenomics of repaglinide was mainly focused on drug metabolism and transport related genes. KCNQ1 / Neuro D1 / BETA2 / PAX4 / NOS1AP was identified as the target of drug action and the receptor encoding gene T2DM2, among them KCNQ1 / Neuro D1 / BETA2 / PAX4 / NOS1AP. SLC30A8,IGF2BP2,UCP2. The effect of T2DM susceptibility gene represented by NAMPT on pharmacodynamics of repaglinide is the focus of current research. T2DM susceptibility gene may affect the proliferation of islet B cells. Expression and activity of K ATP and voltage-gated Ca~(2 channels and insulin secretion. Thus, the susceptibility of T2DM was increased and the response to drug therapy was affected. CYP2C8 / CYP3A4. Gene polymorphisms related to drug metabolism and transport, such as SLCO1B1 and MDR1, may affect the area, peak concentration, half-life and clearance of repaglinide under the drug time curve. Indirectly affect the efficacy and safety of drugs. In the development of pharmacogenomics research, we should also select gene polymorphism sites according to the allele frequency of different races. Conclusion: gene polymorphism is part of the reason of individual difference in the treatment of reaglinide, which is expected to improve the curative effect and reduce the adverse reaction through the individualized therapy directed by gene.
【作者单位】：无锡市第三人民医院药学部;
【基金】：江苏省药学会奥赛康医院药学基金科研课题(No.201513)
【分类号】：R966
【正文快照】： 2型糖尿病(Type 2 diabetes mellitus,T2DM)是机体在环境因素和遗传因素作用下,发生胰岛素分泌受损和/或胰岛素抵抗,主要表现为慢性血糖升高的一种临床综合征[1]。T2DM患者Ⅰ相胰岛素分泌缺陷,而瑞格列奈快速、短效促胰岛素分泌作用可模拟Ⅰ相胰岛素分泌过程,能有效控制餐后血

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