Chapter 3
ADME Pharmacogenetics and Its Impact on Drug–Drug Interactions
Abstract
- CYP酶CYP2B6, CYP2C9, CYP2C19, and CYP2D6和转运体 ABCB1 and OAT1B1具有genetic polymorphisms, 约占人群的1%
3.1 Introduction
- pharmacogenetics的关注重点已由最开始的药物代谢酶(M),扩展到影响ADE的膜转运体
- Genetic variants not only determine to which extent a drug is metabolized, taken up or excreted by ADME genes, but they also influence the various mechanisms of how two or more drugs interact with the resulting protein.
- 某些基因型会直接影响the induction potential of a drug; 通常酶活性的基线水平越低,被诱导剂诱导的越高,但如果absent or low baseline activity是null alleles或其他遗传因素导致的话,就可能会出现不诱导的现象;
- 遗传多态性对药物代谢酶和转运体对drug exposure的影响的研究很多,直到最近才有少数研究者关注是否这些polymorphisms会改变inter individual susceptibility to or the degree of induction or inhibition.
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