What are CYP enzyme inducers?
CYP enzyme inducers increase the rate of hepatic metabolism, usually through increased transcription of mRNA, and decrease serum concentrations of other drugs metabolized by the same hepatic isoenzyme.
Which drug causes inhibition of CYP 2d6?
CYP2D6 Inhibitors Some drugs, such as fluoxetine, paroxetine, and quinidine, are particularly potent inhibitors of CYP2D6; patients on these drugs may have almost no CYP2D6 activity.
What is CYP inhibitor?
Cytochrome P450 (CYP) are a family of enzymes which play a major role in the metabolism of drugs. Assessment of the potential of a compound to inhibit a specific cytochrome P450 enzyme is important as co-administration of compounds may result in one or both inhibiting the other’s metabolism.
Which of the following is CYP450 enzyme inhibitor?
Examples of cytochrome P450 inhibitors are erythromycin, ketoconazole, diltiazem, colchicine, and the fluoroquinolones [61].
Which of the following is a CYP450 3a4 inducer?
Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.
What are CYP2C19 inhibitors?
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 are CYP1A2 inhibitors?
Strong inhibitor of CYP1A2 and CYP2C19, and moderate inhibitor of CYP2D6 and CYP3A….
| CYP1A2 | |
| Strong inhibitors | ciprofloxacin, enoxacin, fluvoxamine(a) |
| Moderate inhibitors | methoxsalen, mexiletine ,oral contraceptives |
| Weak inhibitors | acyclovir, allopurinol, cimetidine, peginterferon alpha-2a, piperine, zileuton |
How do CYP inhibitors work?
Inhibitors block the metabolic activity of one or more CYP450 enzymes. The extent to which an inhibitor affects the metabolism of a drug depends upon factors such as the dose and the ability of the inhibitor to bind to the enzyme.
What drugs are affected by cytochrome P450?
Examples of Common Drug-Drug Interactions Involving the Cytochrome P450 Enzyme System
| Drug(s)/product | Enzyme inhibitor or inducer |
|---|---|
| Fluoxetine (Prozac), paroxetine (Paxil), | CYP2D6 inhibitor |
| Grapefruit juice | CYP3A4 inhibitor |
| Metronidazole (Flagyl) | CYP2C9 inhibitor |
| Terbinafine (Lamisil) | CYP2D6 inhibitor |
What are CYP2C19 inducers?
Inducers – CYP inducers increase the activity of CYP enzymes. This may increase the metabolism of other drugs that are substrates of the enzyme reducing their exposure.
What are CYP2C9 inhibitors?
| Strong inhibitors | Moderate inhibitors | |
|---|---|---|
| CYP2C9 | – | amiodarone, fluconazole(f), miconazole, piperine |
| CYP2C19 | fluconazole(f), fluoxetine(g), fluvoxamine(a), ticlopidine | felbamate |
| CYP2D6 | bupropion, fluoxetine(g), paroxetine, quinidine(h), terbinafine | abiraterone, cinacalcet, duloxetine, lorcaserin, mirabegron |
What drugs are CYP1A2 inducers?
Cytochrome P-450 CYP1A2 Inducers
| Drug | Target | Type |
|---|---|---|
| Rifampicin | Cytochrome P450 2C19 | enzyme |
| Rifampicin | Canalicular multispecific organic anion transporter 2 | transporter |
| Rifampicin | Multidrug resistance-associated protein 5 | transporter |
| Rifampicin | P-glycoprotein 1 | transporter |