Impact of CYP2C9 genotype on pharmacokinetics: are all cyclooxygenase inhibitors the same?
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Rodrigues AD
Impact of CYP2C9 genotype on pharmacokinetics: are all cyclooxygenase inhibitors the same?
Drug Metab Dispos. 2005 Nov;33(11):1567-75. Epub 2005 Aug 23.
- PubMed ID
- 16118328 [ View in PubMed]
- Abstract
The market withdrawals of rofecoxib (Vioxx) and valdecoxib (Bextra) have focused considerable attention on the side effect profiles of cyclooxygenase (COX) inhibitors. As a result, attempts will be made to identify risk factors in the hope that physicians might be able to ensure patient safety. At first glance, CYP2C9 genotype might be considered a risk factor because many COX inhibitors are CYP2C9 substrates in vitro. This observation has led some to hypothesize that a reduction in clearance, in subjects expressing variant forms of the enzyme (e.g., CYP2C9*1/*3 or CYP2C9*3/*3 genotype), will lead to increased exposure and a greater risk of cardiovascular or gastrointestinal side effects. For any drug, however, one has to consider all clearance pathways. Therefore, a number of COX inhibitors were surveyed and it was determined that CYP2C9 plays a relatively minor role in the overall clearance (
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Celecoxib Cytochrome P450 2C9 Protein Humans UnknownSubstrateDetails Lornoxicam Cytochrome P450 2C9 Protein Humans UnknownSubstrateDetails Meloxicam Cytochrome P450 2C8 Protein Humans UnknownSubstrateDetails Naproxen Cytochrome P450 2C9 Protein Humans UnknownSubstrateDetails Rofecoxib Cytochrome P450 2C9 Protein Humans UnknownSubstrateDetails Tenoxicam Cytochrome P450 2C9 Protein Humans UnknownSubstrateDetails