Title | Acenocoumarol pharmacogenetics: correlation between CYP2C9 polymorphisms and dose requirements | ||
Authors | G. Seretakis1, E. Kyriakou2 and N. Drakoulis1
1. Dept of Pharmaceutical Technology, School of Pharmacy, University of Athens, Greece 2. Dept of Laboratory Haematology and Blood Bank, Attikon University Hospital,Athens, Greece |
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Citation | Seretakis, G., Kyriakou, E., Drakoulis, N.: Acenocoumarol pharmacogenetics: correlation between CYP2C9 polymorphisms and dose requirements, Epitheorese Klin. Farmakol. Farmakokinet. 24(2): 208-210 (2010) | ||
Publication Date | 2010 | ||
Full Text Language | English | ||
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Keywords | Vitamin K antagonists, thromboembolism, CYP2C9, polymorphism. | ||
Other Terms | Review article | ||
Summary | CYP2C9 is the major enzyme involved in the metabolism of oral anticoagulants warfarin, phenprocouman and acenocoumarol. Allelic variants, CYP2C9*2 and CYP2C9*3 have been reported to have reduced enzymatic activity in the metabolism of warfarin6. Carriers of CYP2C9*2 and CYP2C9*3 variants are poor metabolizers and therefore sensitive to cou-marins. Significantly lower warfarin dose requirements have been reported for patients carrying either the CYP2C9*2 or the CYP2C9*3 polymorphism (6). Likewise, CYP2C9*3 has been related to a lower clearance and to an increased half-life of elimination of S-acenocoumarol. The influence of the CYP2C9 polymorphism on sensitivity to acenocoumarol is less known (40. Aim of this project was to investigate the relation of the CYP2C9*2 and CYP2C9*3 polymorphisms in Greek population, to the variability of acenocoumarol dose requirements. | ||
References | 1. Ansell J. et al.: The pharmacology and management of the vitamin K antagonists, The seventh ACCP conference on antithrombotic and thrombolytic therapy. Chest 126: 204S-33S (2004)
2. Markatos C., et al.: VKORC1 and CYP2C9 allelic variants influence acenocourol dose requirements in Greek patients. Pharmacogenomics 9: 1631-1638 (2008) 3. Tassies D., et al. Pharmacogenetics of acenocoumarol: cytochrome P450 CYP2C9 polymorphisms influence dose requirements and stability of anticoagulation. Haematologica 87: 1185-1191 (2002) 4. Thijssen H.H.W., et al.: The possession of the CYP2C9*3 allele is associated with low dose requirements of acenocoumarol. Pharmacogenetics 10: 757-760 (2000) 5. Thijssen H.H.W., et al.: Altered pharmacokinetics of R- and S-acenocoumarol in a subject of heterozygous for CYP2C9*3. Clin. Pharmacol. Ther. 70: 292-298 (2001) 6. Aithal G.P., et al.: Association of polymorphisms in the cytochrome P450 CYP2C9 with warfarin dose requirement and risk of bleeding complications. Lancet 353: 717-719 (1999) |
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Online ISSN 1011-6575
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Articles published in this Journal are Indexed or Abstracted in: • Chemical Abstracts • Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE SCImago Journal and Country Rank Factor
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