作者: A. R. Boobis , T. Shiga , R. J. Edwards
DOI: 10.1007/978-3-662-06214-2_3
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摘要: Both the therapeutic and adverse effects of drugs can be profoundly influenced by activity enzymes drug metabolism. Biotransformation is effected a number families structurally functionally related enzymes, which inactivate ultimately enable excretion agents. The metabolism exhibit broad overlapping substrate specificities. Many these are now known to polymorphic expression, due often point mutations in structural gene. result may large difference metabolic activity, consequently pharmacokinetics, between phenotypes. Examples include CYP2D6, CYP2C9, CYP2C19 NAT2. Some transporters such as ABCB1 (P-glycoprotein) also polymorphic. consequences polymorphism will depend upon factors, including steepness concentration-effect curve, contribution pathway overall elimination magnitude other sources variability effect enzyme. In this last case, whilst it might possible demonstrate clear differences phenotypes healthy volunteers, variability, disease itself, dominate response patients. There some examples importance drugs, CYP2C9 warfarin NAT2 hydralazine. However, likely that extent genotyping benefit individual patient established only adequate clinical studies.