What are inhibitors of cytochrome p450?
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.
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 happens if you inhibit cytochrome P450?
IRREVERSIBLE INHIBITION In some cases, CYP450 inhibition is irreversible. The formation of a stable complex, between a drug and the metabolizing enzyme, is one mechanism that can result in irreversible inhibition. The inhibitor can be a drug or one of its metabolites.
Is clopidogrel CYP2C19 inhibitor?
Clopidogrel is an inactive prodrug that requires hepatic bioactivation via several cytochrome P450 enzymes, including CYP2C19. The active metabolite irreversibly inhibits the platelet ADP receptor, P2Y12.
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.
What is CYP induction?
CYP induction is a relatively slow phenomenon due to gene regulation events, such as nuclear receptor activation and synthesis of mRNA and enzyme. Each assay delivers CYP induction relative to vehicle control (x-fold) and / or EC50 values if feasible (concentration where 50 % of maximal induction is achieved).
What drugs inhibit enzymes?
Examples of enzyme-inhibiting agents are cimetidine, erythromycin, ciprofloxacin, and isoniazid.
Which GI drugs interact with CYP450?
Clinical example of P450-based interactions
- Terfenadine. Terfenadine is the first non-sedating H1-antihistamine drug.
- Cimetidine. Cimetidine inhibits antihistamine H2-receptor binding and is used in the treatment of gastric ulcers.
- Grapefruit juice.
- Omeprazole.
- Erythromycin.
- Cyclosporin.
- Rifampicin.
What medications are metabolized by CYP2C19?
The CYP2C19 enzyme is responsible for the breakdown of several popular drugs including proton pump inhibitors (Prilosec, Nexium, Prevacid), certain anti-epileptics, and an antiplatelet drug (Plavix). CYP2C19 is also involved in activating and breaking down some hormones such as progesterone.
Is pantoprazole a CYP2C19 inhibitor?
Pantoprazole, a proton pump inhibitor (PPI) frequently used in the treatment of GERD and related conditions, is ideally suited for such a study, given the predominant role of CYP2C19 (Cytochrome P450 subtype 2C19) in its metabolism and its favorable safety and efficacy profile in pediatric medicine.
Which drugs are metabolized by CYP2D6?
Overview. The impact of CYP2D6 activity in drug metabolism is further complicated by the activity of the drug itself on CYP2D6. Some SSRIs, such as paroxetine (Paxil), fluoxetine (Prozac), and citalopram (Celexa), as well as statins, are known to inhibit CYP2D6 activity and may make EMs resemble IMs or PMs.
What are P450 inhibitors?
The CYP450 enzymes are essential for the production of numerous agents including cholesterol and steroids. Additionally, these enzymes are necessary for the detoxification of foreign chemicals and the metabolism of drugs.