What drugs are metabolized by CYP3A?

What drugs are metabolized by CYP3A?

	Sensitive index substrates unless otherwise noted
CYP2C9	tolbutamide(c), S-warfarin(c)
CYP2C19	lansoprazole (c,d), omeprazole
CYP2D6	desipramine, dextromethorphan, nebivolol
CYP3A	midazolam, triazolam

What drugs are CYP450 inhibitors?

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

What does CYP3A4 enzyme do?

Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14. 13.97) is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body.

What drugs are CYP2C8 inhibitors?

CYP2C8 substrate drugs include amodiaquine, cerivastatin, dasabuvir, enzalutamide, imatinib, loperamide, montelukast, paclitaxel, pioglitazone, repaglinide, and rosiglitazone, and the number is increasing. Similarly, many drugs have been identified as CYP2C8 inhibitors or inducers.

Is diltiazem a CYP3A inhibitor?

Diltiazem is a calcium channel blocker used to treat angina pectoris and mild-to-moderate arterial hypertension19. This compound is an inhibitor of CYP3A activity20,21 and is classified as a moderate inhibitor of this enzyme10.

What is the difference between CYP3A4 and CYP3A?

CYP3A5 is 83% homologous to CYP3A4, is expressed at a much lower level than CYP3A4 in the liver, but is the main CYP3A isoform in the kidney. CYP3A7 is the major CYP isoform detected in human embryonic, fetal and newborn liver, but is also detected in adult liver, although at a much lower level than CYP3A4.

What do CYP450 inhibitors do?

The cytochrome P450 (CYP450) enzymes are essential to produce numerous agents, including cholesterol and steroids. CYP450 inhibitors are used to minimize or prevent such reactions. Drugs are metabolized in many sites of our body; however, the liver is the primary organ for drug metabolism.

Is omeprazole a CYP450 inhibitor?

The human clearance of omeprazole and lansoprazole is conducted primarily by the hepatic cytochrome P450 (CYP) system. Since its inhibition is very potent and has a broad “window of selectivity,” omeprazole seems to be a useful, selective inhibitor of CYP2C19.

How many drugs does CYP3A4 metabolize?

1900 drugs
CYP3A4 metabolizes more than 1900 drugs: 1033 act as substrates (897 major, 136 minor); 696, as inhibitors (118 weak, 437 moderate, and 141 strong); and 241, as inducers of the CYP3A4 enzyme [113].

What drugs are strong 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.

Is clopidogrel a CYP2C8 inhibitor?

Clopidogrel, a CYP2C8 inhibitor, causes a clinically relevant increase in the systemic exposure to the active metabolite of selexipag in healthy subjects.

What drugs are metabolized by CYP1A2?

CYP1A2 plays an important role in metabolism of drugs like clozapine, olanzapine, fluvoxamine, haloperidol, theophylline; biotransformation of endogenous compounds like melatonin, bilirubin, estrogens, procarcinogens, aflatoxin B1, and aromatic/heterocyclic amines as well as caffeine (Gunes and Dahl, 2008).

What are some common medications classified as weak, moderate and strong inhibitors of CYP3A4?

Common Medications Classified as Weak, Moderate and Strong Inhibitors of CYP3A4. Strong inhibitors of CYP3A4 include: Clarithromycin , telithromycin, nefazodone, itraconazole, ketoconazole, atazanavir, darunavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, tipranavir.

What drugs are CYP3A4 inducers?

A small number of drugs such as rifampin, phenytoin and ritonavir are identified as inducers of CYP3A4. The orphan nuclear receptor, pregnane X receptor (PXR), have been found to play a critical role in the induction of CYP3A4.

What drugs are CYP3A4 inhibitors?

CYP3A4 Inhibitors. Some drugs, such as clarithromy- cin, itraconazole, ketoconazole, nefazo- done, nelfinavir, and ritonavir , are particu- larly potent inhibitors of CYP3A4; patients on these drugs may have markedly reduced CYP3A4 activity.

What are strong CYP3A4 inhibitors?

Strong inhibitors of CYP3A4 include: Clarithromycin, telithromycin, nefazodone, itraconazole, ketoconazole, atazanavir, darunavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, tipranavir. It is important to note that not all drugs within a class of medications are known to be inhibitors of CYP3A4.