What are CYP1A2 inducers?
CYP1A2 Polymorphism Environmental and genetic factors are shown to influence the activity of CYP1A2. These can account for up to a 60-fold difference in activity. Tobacco byproducts produced from smoking and oral contraceptive steroids have been well established as CYP1A2 inducers.
Which drug is an inducer of CYP450 enzymes?
Cimetidine, a typical CYP450 enzyme inducer, can increase both plasma concentration and elimination half-life, but the clinical significance of this is unclear.
Which TB drug is a powerful inducer of cytochrome P450?
Rifampin, for example, is a potent inducer of cytochrome P450 enzyme 3A, the enzyme subfamily responsible for metabolizing a large proportion of drugs currently on the market, as well as other cytochrome P450 enzymes.
What does inducer of CYP450 mean?
Drugs that cause CYP450 drug interactions are referred to as either inhibitors or inducers. An inducing agent can increase the rate of another drug’s metabolism by as much as two- to threefold that develops over a period of a week.
What drugs are CYP1A2 substrates?
Typical CYP1A2 substrates generally contain planar ring that can fit the narrow and planar active site of the enzyme, such as propranolol, clozapine, guanabenz, flutamide, imatinib, thalidomide, carbamazepine, lidocaine, theophylline, tacrine, tizanidine, zolpidem, riluzole, zileuton, and leflunomide.
What are CYP1A2 and CYP3A drugs?
CYP1A2 and CYP3A are members of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids.
What drug inhibits cytochrome P450?
Jump to a Section
| CYP | Inducers | Inhibitors |
|---|---|---|
| 2C9 | Barbiturates, carbamazepine, rifampin | Fluconazole, fluvoxamine, sulfaphenazole, tienilic acid |
| 2C18 | Phenobarbital | |
| 2C19 | Barbiturates, rifampin | N3-benzylnirvanol, N3-benzylphenobarbital, fluconazole, nootkatone, ticlopidine |
| 2D6 | Unknown | Bupropion, fluoxetine, paroxetine, quinidine |
Which drugs inhibit CYP450?
Medicines that are potent CYP3A4 inhibitors include (but are not limited to) clarithromycin, diltiazem, erythromycin, itraconazole, ketoconazole, ritonavir, and verapamil9.
Which drug inhibits the cytochrome P450 system?
Examples of cytochrome P450 inhibitors are erythromycin, ketoconazole, diltiazem, colchicine, and the fluoroquinolones [61].
What does it mean when a drug is an inducer?
An enzyme inducer is a type of drug that increases the metabolic activity of an enzyme either by binding to the enzyme and activating it, or by increasing the expression of the gene coding for the enzyme. It is the opposite of an enzyme repressor.
What is the difference between inhibitor and inducer?
The key difference between enzyme inhibitor and enzyme inducer is that enzyme inhibitor decreases the activity of an enzyme by binding with the active site of the enzyme. In contrast, enzyme inducer increases the metabolic activity of an enzyme either by binding to it or by increasing the gene expression.