摘要
在非甾体抗炎药氯诺昔康的生物等效性试验中发现1名药物慢代谢者携带药物代谢基因CYP2C9*3突变位点,并携带一个新CYP2C9多态性位点—CYP2C9*13。CYP2C9酶的基因多态性通过影响酶的活力,改变底物药在体内的清除率。因此,CYP2C9突变体的携带者将面临着底物药的用药安全问题,特别是有效剂量和毒性剂量距离近的药物,如华法林、甲苯磺丁脲和苯妥英钠等。筛查CYP2C9基因型,有助于提高CYP2C9酶底物药的用药安全,减少不良反应的发生。
A poor metabolizer was found in a bioequiavailability experiment about lornoxicam, a non-steroidal anti-inflammatory drug. The genetic analysis revealed the study subject is heterozygous for reported CYP2C9＊3 and a novel mutation CYP2C9＊13. This shows the CYP2C9 gene polymor-phisms affect the intrinsic clearance of a variety of CYP2C9 substrates by changing the catalytic effi-ciency of enzyme. The individuals carrying the CYP2C9 variant alleles will face with the drug safety, especially towards the drugs such as warfarin, tolbutamide and phenytoin with the narrow range between effective dose and venenosus dose. The screening of CYP2C9 genotype will provide a basis for increasing the safety of CYP2C9 substrates.
出处
《中国药物警戒》
2008年第4期231-234,共4页
Chinese Journal of Pharmacovigilance
关键词
药物代谢酶
底物药
用药安全
启示
drug-metabolizing enzyme
drug efficacy
drug safety
revelation
