What is a CYP2C19 intermediate metabolizer?
An enzyme called cytochrome P450 2C19 (CYP2C19 “Sip – 2 – See – 19”) helps to process a variety of medications including clopidogrel (Plavix®), voriconazole (Vfend®), and many antidepressants. Like many medicines, how well the medicine works and side effects are different from person to person.
What does it mean to be an intermediate metabolizer?
Intermediate Metabolizer. An intermediate-metabolizing enzyme is considered to be less active. It doesn’t break down a drug as completely as a normal metabolizer, which means you might require a lower dose. A lower dose prevents the unmetabolized drug from building up in your body and possibly causing side effects.
What is CYP2C19 responsible for?
The CYP2C19 gene provides instructions for making an enzyme that is found primarily in liver cells in a cell structure called the endoplasmic reticulum, which is involved in protein processing and transport.
What drug is a major substrate of CYP2C19?
3.2 CYP2C19. CYP2C19 metabolizes numerous commonly used drugs including citalopram, clomipramine, clopidogrel, diazepam, omeprazole, S-mephenytoin, and biguanides [97–99].
What drugs do CYP2C19 metabolize?
CYP2C19 catalyzes the metabolism of several drugs, including proton pump inhibitors (PPIs) (e.g., omeprazole, lansoprazole, pantoprazole), antidepressants (e.g., citalopram and amitriptyline), antiplatelet drugs (e.g., clopidogrel), antifungals (e.g., voriconazole), and anticancer compounds (e.g., cyclophosphamide).
What does it mean to be a CYP2C19 rapid metabolizer?
In people who are rapid metabolizers, the CYP2C19 enzyme has high activity. People who are rapid metabolizers break down some medicines quickly and may need different doses or a different medicine. About 29% of our patients are rapid metabolizers.
What drugs are metabolized by CYP2C19?
What happens when CYP2C19 is inhibited?
Loss-of-function alleles (e.g., CYP2C19∗2) thus impair formation of the active principle (i.e., metabolite), resulting in decreased platelet inhibition and increased risk for adverse cardiovascular events, especially in PM patients undergoing percutaneous coronary intervention [91].
What happens if CYP2C19 is inhibited?
CYP2C19 Inhibitors Drugs that inhibit CYP2C19 activity (Table 2) are likely to increase the plasma concentrations of the medications listed with an asterisk in Table 1, and in some cases adverse outcomes may occur.
What drugs inhibit CYP2C19?
CYP2C19 strong inhibitors
- Amitriptyline (Elavil®) [9]
- Clomipramine (Anafranil®) [9]
- Fluconazole (Diflucan®) [1]
- Fluvoxamine (Luvox®) [1]
- Imipramine (Tofranil®) [9]
- Ticlopidine (Ticlid®) [1]
What drugs are affected by CYP2C19?
14.4. CYP2C19 metabolizes numerous commonly used drugs including citalopram, clomipramine, clopidogrel, diazepam, omeprazole, S-mephenytoin, and biguanides [97–99]. Approximately 2000 SNPs and more than 35 variants have been identified in the CYP2C19 gene.