What is the function of CYP2C9?
What is the function of CYP2C9?
The CYP2C9 enzyme breaks down (metabolizes) compounds including steroid hormones and fatty acids. The CYP2C9 enzyme also plays a major role in breaking down the drug warfarin, which thins the blood and prevents blood clots from forming.
What is the role of CYP2C9 gene in prescribing warfarin?
A patient’s CYP2C9 and VKORC1 genotype can be used to help determine the optimal starting dose of warfarin. The CYP2C9 gene encodes one of the main enzymes involved in the metabolism of warfarin. Several variant CYP2C9 alleles are associated with reduced enzyme activity and lower clearance rates of warfarin.
What is the chromosomal location of the CYP2C9 gene?
The enzyme is involved in metabolism, by oxidation, of both xenobiotics, including drugs, and endogenous compounds, including fatty acids. In humans, the protein is encoded by the CYP2C9 gene….
|Location (UCSC)||Chr 10: 94.94 – 94.99 Mb||Chr 19: 39.06 – 39.09 Mb|
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What is the function of cytochrome P450?
Background: The cytochrome P450 (CYP) enzymes are membrane-bound hemoproteins that play a pivotal role in the detoxification of xenobiotics, cellular metabolism and homeostasis. Induction or inhibition of CYP enzymes is a major mechanism that underlies drug-drug interactions.
What drugs are affected by CYP2C9?
|NSAIDs||Celecoxib, diclofenac, etodolac, ibuprofen, indomethacin, lornoxicam, mefenamic acid, suprofen, tenoxicam|
|Oral hypoglycemic agents||Chlorpropamide, glibenclamide, gliclazide, glimepiride, nateglinide, tolbutamide|
What is the CYP3A4 responsible for?
CYP3A4 is responsible for the metabolism of more than 50% of medicines. Potent inhibitors of CYP3A4 include clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal and grapefruit. Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St.
How does CYP2C19 affect metabolism?
Most often, changes in the CYP2C19 gene lead to impaired metabolism of these drugs, which reduces their effectiveness. One change in the CYP2C19 gene (known as CYP2C19*17) increases the enzyme’s ability to metabolize drugs.
Does everyone have CYP2C9?
Studies have shown that approximately 18% of the total CYP proteins in the human liver microsomes are CYP2C9 . CYP2C9 metabolizes about 25% of clinically administered drugs including warfarin and phenytoin, for which actionable PGx-based adjustments exist [104,105].
What are CYP450 inhibitors?
Inhibition of cytochrome P450 (CYP450) enzymes is the most common mechanism leading to drug–drug interactions . CYP450 inhibition can be categorized as reversible (including competitive and non-competitive inhibition) or irreversible (or quasi-irreversible), such as mechanism-based inhibition.
What happens when CYP2C9 is inhibited?
Once a CYP enzyme is combined with a certain xenobiotic compound, its catalytic activity may be decreased, which will trigger drug-drug interactions when it is coadministrated with substrates of the same enzyme. Generally, inhibitors of CYP enzymes can be classified as reversible and irreversible types.
What drugs are strong CYP3A4 inducers?
Potent inhibitors of CYP3A4 include clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal and grapefruit. Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.