Some Common Substrates, Inhibitors and Inducers of CYP450 Isoenzymes
| Substrates | Inhibitors | Inducers |
|---|---|---|
| Clomipramine | Cimetidine | Broccoli |
| Clozapine | Ciprofloxacin | Brussels sprouts |
| Imipramine | Fluvoxamine | Cigarette Smoking |
| Theophylline |
What is a CYP3A4 inducer?
CYP3A4 inducers are drugs that increase the activity of CYP3A4. Note that the CYP3A4 enzyme is particularly susceptible to enzyme inducers, and marked reductions in the plasma concentrations of CYP3A4 substrates may occur.
What are CYP3A inhibitors used for?
A CYP3A inhibitor used to increase the systemic exposure of atazanavir or darunavir in combination with other antiretroviral agents in the treatment of HIV-1 infection. A viral protease inhibitor used in the treatment of HIV infection.
Is rifampin a CYP3A4 inhibitor?
Rifampicin can induce both gut (enterocytic) and liver (hepatic) CYP, especially CYP3A4, and increase its own metabolism (autoinduction), but the induced metabolic pathway is still not clear [27].
Is prednisone a CYP3A4 inducer?
Overall, these drugs are considered weak inducers of CYP3A4. Most studies with dexamethasone, prednisone, or methylprednisolone were not conducted as crossover designs but as case-control-type studies or evaluations of patients, which are confounded by other concomitant medications.
What is an inhibitor molecule?
5 Effect of Inhibitors. Enzyme inhibitors are molecules that interact with enzymes (temporary or permanent) in some way and reduce the rate of an enzyme-catalyzed reaction or prevent enzymes to work in a normal manner. The important types of inhibitors are competitive, noncompetitive, and uncompetitive inhibitors.
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 CYP3A inhibitors or 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.
What drugs does CYP3A4 metabolize?
Cytochrome P450 enzymes metabolize approximately 60% of prescribed drugs, with CYP3A4 responsible for about half of this metabolism; substrates include acetaminophen, codeine, ciclosporin (cyclosporin), diazepam, and erythromycin. The enzyme also metabolizes some steroids and carcinogens.
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 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 do CYP3A inhibitors do?
CYP3A Inhibitors. Cytochrome P450 (CYP) proteins are heme-thiolate monooxygenases that mediate NADPH -dependent electron transport and function to oxidize a variety of structurally unrelated compounds, including steroids, fatty acids and xenobiotics. Biochemicals that inhibit CYP3A have many applications in biochemical and physiological research.
What is a CYP3A4 substrate?
Cytochrome P450 enzymes metabolize approximately 60% of prescribed drugs, with CYP3A4 responsible for about half of this metabolism; substrates include acetaminophen, codeine, ciclosporin (cyclosporin), diazepam, and erythromycin. The enzyme also metabolizes some steroids and carcinogens.
