The pharmacogenetics of ibuprofen: Exploring variants in CYP2C9

Increasingly, clinicians and researchers are recognizing the importance of understanding how genes can influence the efficacy and safety of drugs. In this article, we will focus on one of the most studied genetic variants, specifically the CYP2C9 gene, and how these variants may affect the response to ibuprofen, a commonly used pain reliever.

The role of CYP2C9 in ibuprofen metabolism: Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) widely used to relieve pain and reduce inflammation. However, ibuprofen is not metabolized in the same way in all people. The CYP2C9 gene encodes an enzyme called cytochrome P450 2C9, which plays a crucial role in the metabolism of many drugs, including ibuprofen.

Genetic variants in CYP2C9: There are different genetic variants in the CYP2C9 gene that can affect the enzymatic activity of the CYP2C9 enzyme. The two most common variants that have been studied are CYP2C9*2 and CYP2C9*3. These variants are associated with reduced enzyme activity, which means that individuals who carry them may have difficulty adequately metabolizing ibuprofen and other drugs that are CYP2C9 substrates.

Effects of variants on ibuprofen response: The presence of CYP2C9*2 and CYP2C9*3 variants can have a significant impact on ibuprofen response. Individuals with these variants may experience less clearance of the drug from their system, which may lead to increased exposure to the drug. This may result in a longer duration of action and a greater likelihood of experiencing side effects, such as gastrointestinal bleeding.

Clinical recommendations: Given the influence of genetic variants in CYP2C9 on the response to ibuprofen, it is important to consider pharmacogenetics when prescribing this drug. Genetic testing to identify CYP2C9*2 and CYP2C9*3 variants can help clinicians customize doses of ibuprofen and other CYP2C9-metabolized drugs.

In addition, patients known to have these variants may require dose adjustments to avoid unwanted side effects. For example, they may be recommended a lower dose of ibuprofen or prescribed an alternative NSAID that is not metabolized primarily through CYP2C9.

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