• The variant alleles CYP2C9*2 and CYP2C9*3 are associated with an increased response to warfarin. (ox.ac.uk)
  • About 100 therapeutic drugs are metabolized by CYP2C9, including drugs with a narrow therapeutic index such as warfarin and phenytoin, and other routinely prescribed drugs such as acenocoumarol, tolbutamide, losartan, glipizide, and some nonsteroidal anti-inflammatory drugs. (wikipedia.org)
  • Especially for CYP2C9 substrates such as warfarin and phenytoin, diminished metabolic capacity because of genetic polymorphisms or drug-drug interactions can lead to toxicity at normal therapeutic doses. (wikipedia.org)
  • Warfarin dose requirements with different genotypes of CYP2C9 and VKORC1 for patients with atrial fibrillation and valve replacement. (cdc.gov)
  • Clinical application of a new warfarin-dosing regimen based on the CYP2C9 and VKORC1 genotypes in atrial fibrillation patients. (cdc.gov)
  • DNA sensors to assess the effect of VKORC1 and CYP2C9 gene polymorphisms on warfarin dose requirement in Chinese patients with atrial fibrillation. (cdc.gov)
  • Acenocoumarol is an anticoagulant that functions as a vitamin K antagonist (like warfarin ). (wikidoc.org)
  • Warfarin or acenocoumarol is better in the anticoagulant treatment of chronic atrial fibrillation? (wikidoc.org)
  • Individuals with PM phenotype (i.e. genotypes with homozygous or compound heterozygous *2 or *3 alleles) are at greater risk of severe bleeding during coumarin-based anticoagulation therapy with warfarin, acenocoumarol and - to a lesser extent - phenprocoumon. (viennalab.com)
  • The less important role of CYP2C9 with the clearance of phenprocoumon is due to the involvement of CYP3A4 as a further catalyst for phenprocoumon hydroxylation and considerable excretion of unchanged drug in bile and urine, while the elimination of warfarin and acenocoumarol is sort of absolutely by metabolism. (liveblogspot.com)
  • Amendments of conventional anticoagulant therapy, together with self-checking of international normalized ratio values or future genotyping for specific dose-tailoring may contribute to the continual use of warfarin, phenprocoumon, and acenocoumarol Sooner or later. (liveblogspot.com)
  • Hyper-responsiveness to warfarin in a young patient with the VKORC1 -1639GA/CYP2C9*1*46 genotype: a case report. (cdc.gov)
  • The results of this study1 provide very useful information for clinical practice, ie, DSG may be a safe alternative to oral diclofenac when a pain reliever needs to be co-medicated with CYP2C9 substrates like warfarin antidiabetic sulfonylurea derivatives. (scienceopen.com)
  • Genome-Wide Association Study of VKORC1 and CYP2C9 on acenocoumarol dose, stroke recurrence and intracranial haemorrhage in Spain. (renevas.es)
  • The risk of overanticoagulation in patients with cytochrome P450 CYP2C9*2 or CYP2C9*3 alleles on acenocoumarol or phenprocoumon. (ox.ac.uk)
  • However, an effect on acenocoumarol dose requirements appears to be absent for the CYP2C9*2 allele and the consequences for the metabolism of phenprocoumon have not yet been established. (ox.ac.uk)
  • We investigated CYP2C9 polymorphisms in relation to the international normalized ratio (INR) during the first 6 weeks of treatment and its effect on the maintenance dose in a cohort of 1124 patients from the Rotterdam Study who were treated with acenocoumarol or phenprocoumon. (ox.ac.uk)
  • Phenprocoumon appears to be a clinically useful alternative in patients carrying the CYP2C9*2 and *3 alleles. (ox.ac.uk)
  • Genetic variants of the drug-metabolizing enzyme CYP2C9 lead to high inter-individual dose response variability of certain drugs, in particular coumarin-based anticoagulants. (viennalab.com)
  • Patients with low enzyme activity are at risk of adverse drug reactions or therapeutic failure, particularly for CYP2C9 substrates with a narrow therapeutic window, such as coumarin-based anticoagulants or phenytoin. (viennalab.com)
  • We know, for example, that not everyone responds in the same way to treatment with some oral anticoagulants, such as acenocoumarol, in which two genes are already known whose variants are associated with the differential response to this drug, the genes CYP2C9 and CYP4F2 . (adntro.com)
  • In fact, adverse drug reactions (ADRs) often result from unanticipated changes in CYP2C9 enzyme activity secondary to genetic polymorphisms. (wikipedia.org)
  • Research in the RECAVA network has discovered that two acquired factors (age and body mass index ) and three genetic polymorphisms ( genes VKORC1, CYP2C9 and CYP4F2) are useful to establish the correct dosage . (wikidoc.org)
  • 2011) Proton Pump Inhibitors and the Risk of Overanticoagulation during Acenocoumarol Maintenance Treatment. (scirp.org)
  • Cytochrome P4502C9 (CYP2C9) is the main enzyme implicated in coumarin anticoagulant metabolism. (ox.ac.uk)
  • Cytochrome P450 family 2 subfamily C member 9 (abbreviated CYP2C9) is an enzyme protein. (wikipedia.org)
  • CYP2C9 is a crucial cytochrome P450 enzyme, which plays a significant role in the metabolism, by oxidation, of both xenobiotic and endogenous compounds. (wikipedia.org)
  • The CYP2C9 mpx RealFastâ„¢ Assay allows for the simultaneous detection of CYP2C9*2 and CYP2C9*3 variants exhibiting impaired enzyme function. (viennalab.com)
  • Cytochrome P450 2C9 (abbreviated CYP2C9 ) is an enzyme that in humans is encoded by the CYP2C9 gene . (wikidoc.org)
  • CYP2C9 is an important cytochrome P450 enzyme with a major role in the oxidation of both xenobiotic and endogenous compounds. (wikidoc.org)
  • A clear genotype-dose relationship was found for acenocoumarol-treated patients. (ox.ac.uk)
  • Lack of Association of Clinical Factors (SAMe-TT2R2) with CYP2C9/VKORC1 Genotype and Anticoagulation Control Quality. (cdc.gov)
  • CYP2C9 makes up about 18% of the cytochrome P450 protein in liver microsomes. (wikipedia.org)
  • The enzymes include cytochrome P450 metabolizer classes like the CYP2D6 , CYP2C9, and CYP2CI9 . (dynamicdnalabs.com)
  • Enzalutamide has been described in in vivo studies as a strong inducer of CYP3A4 and a moderate inducer of CYP2C9 and CYP2C19. (altmeyers.org)
  • Investigate the CYP2C9 metabolizer status and individualize coumarin anticoagulation therapy. (viennalab.com)
  • Multiple in vivo studies also show that several mutant CYP2C9 genotypes are associated with significant reduction of in metabolism and daily dose requirements of selected CYP2C9 substrate. (wikidoc.org)
  • In humans, the protein is encoded by the CYP2C9 gene. (wikipedia.org)
  • The CYP2C9 gene is highly polymorphic. (wikipedia.org)
  • The label CYP2C9*1 is assigned by the Pharmacogene Variation Consortium (PharmVar) to the most commonly observed human gene variant. (wikipedia.org)
  • Genetic polymorphism exists for CYP2C9 expression because the CYP2C9 gene is highly polymorphic. (wikidoc.org)
  • this drug appears to be preferable for therapeutic anticoagulation in poor metabolizers of CYP2C9. (liveblogspot.com)
  • Information about how human genetic variation of CYP2C9 affects response to medications can be found in databases such PharmGKB, Clinical Pharmacogenetics Implementation Consortium (CPIC). (wikipedia.org)
  • Individuals with one or more CYP2C9*2 or CYP2C9*3 allele(s) require a significantly lower dose of acenocoumarol compared to wild-type patients. (ox.ac.uk)
  • High prevalence of VKORC1*3 (G9041A) genetic polymorphism in north Indians: A study on patients with cardiac disorders on acenocoumarol. (cdc.gov)
  • By contrast, the known extrahepatic CYP2C9 often metabolizes important endogenous compounds such as serotonin and, owing to its epoxygenase activity, various polyunsaturated fatty acids, converting these fatty acids to a wide range of biological active products. (wikipedia.org)
  • 7. CYP2C9 polymorphism in non-steroidal anti-inflammatory drugs-induced gastropathy. (nih.gov)
  • The result hi-ghlighted a CYP2C9 2 * 2 polymorphism, associated with the C1173T mutation of the VKORC gene, both of which determined an increased sensitivity to com-monly used doses of Warfarin that cause an important hemorrhagic risk. (romanianjournalcardiology.ro)
  • Patients with polymorphisms in CYP2C9 and VKORC1 had a higher risk of overanticoagulation (up to 74%) and a lower risk of underanticoagulation (down to 45%) in the first month of treatment with acenocoumarol, but this effect diminished after 1-6 months. (nih.gov)
  • Treatment with Acenocoumarol was initiated without an effective anticoagulation due to a significant INR variability of 1.2 to 13 in 24 hours, despite exhaustive controls and dose changes (12 mg/day alternating with 4 mg) with the occurrence of frequent episodes of epis-taxis and painful bilateral hematomas. (romanianjournalcardiology.ro)
  • Influence of CYP2C9 and VKORC1 on warfarin dose, anticoagulation attainment and maintenance among European-Americans and African-Americans. (snpedia.com)
  • About 100 therapeutic drugs are metabolized by CYP2C9, including drugs with a narrow therapeutic index such as warfarin and phenytoin, and other routinely prescribed drugs such as acenocoumarol, tolbutamide, losartan, glipizide, and some nonsteroidal anti-inflammatory drugs. (wikipedia.org)
  • Efficiency and effectiveness of the use of an acenocoumarol pharmacogenetic dosing algorithm versus usual care in patients with venous thromboembolic disease initiating oral anticoagulation: study protocol for a randomized controlled trial. (cdc.gov)
  • To determine the cause of a genotype-phenotype discordancy for acenocoumarol sensitivity. (nih.gov)
  • 15. [Significance of cytochrome P450 2C9 genotype for the bleeding complications in patients treated with acenocoumarol]. (nih.gov)
  • Methods A patient, highly sensitive to acenocoumarol, and previously determined to carry only a single CYP2C9*3 allele, was genotyped for additional functionally defective alleles in the CYP2C9 and VKORC1 genes. (nih.gov)
  • Results The acenocoumarol-sensitive patient was found to possess, in addition to CYP2C9*3 allele, a CYP2C9*11 allele and the VKORC1 AA diplotype which were all traced back through the parental lines. (nih.gov)
  • The study provides additional data in support of diminished CYP2C9 activity due to the presence of the rare *11 allele. (nih.gov)
  • 6. CYP2C9*3 Loss-of-Function Allele Is Associated With Acute Upper Gastrointestinal Bleeding Related to the Use of NSAIDs Other Than Aspirin. (nih.gov)
  • Allele frequency for CYP2D6 , CYP2C19 and CYP2C9 . (medscape.com)
  • Conclusions Acenocoumarol sensitivity in this subject is the consequence of inheritance of multiple functionally defective alleles in both the CYP2C9 and VKORC1 genes. (nih.gov)
  • [ 29 ] Individuals who were CYP2C9 IMs or PMs and who also received CYP2C9 inhibitors had a tripling of the overcoagulation risk compared with individuals who were CYP2C19 NMs. (medscape.com)
  • Information about how human genetic variation of CYP2C9 affects response to medications can be found in databases such PharmGKB, Clinical Pharmacogenetics Implementation Consortium (CPIC). (wikipedia.org)