What is a CYP2C19 inducer?
Drugs that stimulate CYP2C19 (enzyme inducers) often induce several drug metabolism pathways, so enzyme induction often markedly decreases in the plasma concentrations of drugs with multiple metabolic pathways.
What drugs are CYP2C19 inhibitors?
CYP2C19 strong inhibitors
- Amitriptyline (Elavil®) [9]
- Clomipramine (Anafranil®) [9]
- Fluconazole (Diflucan®) [1]
- Fluvoxamine (Luvox®) [1]
- Imipramine (Tofranil®) [9]
- Ticlopidine (Ticlid®) [1]
What do CYP2C19 inhibitors do?
Drugs and compounds which inhibit or antagonize the biosynthesis or actions of CYTOCHROME P-450 CYP2C19. A selective serotonin-reuptake inhibitor used to treat obsessive-compulsive disorder.
What is the function of CYP2C19?
Normal Function 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 are inducers of CYP450?
Cytochrome P-450 enzyme inducers (e.g., rifampin, phenytoin, phenobarbital) decrease the bioavailability and increase the clearance of verapamil and diltiazem. St. John’s wort also significantly decreases verapamil bioavailability through induction of first-pass metabolism in the gut.
What do drug inducers do?
Inducers increase CYP450 enzyme activity by increasing enzyme synthesis. Unlike metabolic inhibition, there is usually a delay before enzyme activity increases, depending on the half-life of the inducing drug.
How does CYP2C19 affect metabolism?
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 are the Inhibitors of CYP2C19?
Inhibitors of CYP2C19 can be classified by their potency, such as: Strong being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance of substrates. Moderate being one that causes at least a 2-fold increase in the plasma AUC values, or 50-80% decrease in clearance of substrates.
Does hyperforin induce CYP2C19?
CYP2C19 induction has been demonstrated with baicalin-containing Chinese multicomponent herbal preparation Yin Zhi Huangand hyperforin-containing St. John’s wort (Fan et al. 2007; Wang et al. 2004a, b) (Table 14), while no environmental chemical is known to induce CYP2C19.
Why do drugs that stimulate CYP2C19 induce multiple metabolic pathways?
Drugs that stimulate CYP2C19 (enzyme inducers) often induce several drug metabolism pathways, so enzyme induction often markedly decreases in the plasma concentrations of drugs with multiple metabolic pathways.
Are there any new inducers and inhibitors in new drugs?
Thus, especially the number of new inducers has been low among the recently approved drugs. However, there may still be unidentified inducers and inhibitors among the compounds present in our diet and various herbal remedies as well as in the environment as chemical toxicants.