What are inhibitors of cytochrome P450?

What are inhibitors of cytochrome P450?

Examples of cytochrome P450 inhibitors are erythromycin, ketoconazole, diltiazem, colchicine, and the fluoroquinolones [61].

What is difference between inducer and inhibitor?

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.

What is an inhibitor drug?

Angiotensin-converting enzyme (ACE) inhibitors are medications that help relax the veins and arteries to lower blood pressure. ACE inhibitors prevent an enzyme in the body from producing angiotensin II, a substance that narrows blood vessels.

What are CYP3A4 inhibitors?

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 are cytochrome P450 substrate drugs?

substrates are drugs or other substances (xenobiotics) which are metabolized by cytochrome enzymes including 1. pharmacologically active drugs which require metabolism to inactive form for clearance from the body. metabolically activated drugs (prodrugs) which require conversion to active drug.

What is an inducer drug?

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.

Is pantoprazole a CYP3A4 inhibitor?

Pantoprazole was a competitive inhibitor of both CYP2C9-catalyzed diclofenac 4′-hydroxylation and CYP3A4-catalyzed midazolam 1′-hydroxylation (K(i) of 6 and 22 microM, respectively), which were at least 2 times more potent than the other PPIs.

What are strong CYP3A inducers?

CYP3A inducers include the glucocorticoids, rifampin, carbamazepine, phenobarbital, and phenytoin. Among the many significant CYP3A inhibitors are grapefruit juice, erythromycin, ketoconazole, clarithromycin, and verapamil.