What is a strong CYP3A inhibitor?

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.

What is a potent enzyme inducer?

Potent enzyme inducers may, for example, reduce serum levels of several steroidal drugs, ciclosporin A, oral anticoagulants, and cardiovascular, antineoplastic and psychotropic drugs (Perucca, 2006).

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.

Is dexamethasone a strong CYP3A4 inducer?

Dexamethasone (10μM) proved to be the most efficacious inducer increasing the rate of synthesis of CYP3A4 from 0.05% of total cellular protein synthesis in incubated control cultures to almost 9.5% in dexamethasone treated cultures [12].

Which drug is an enzyme inducer?

Examples of enzyme inducers include aminoglutethimide, barbiturates, carbamazepine, glutethimide, griseofulvin, phenytoin, primidone, rifabutin, rifampin, and troglitazone. Some drugs, such as ritonavir, may act as either an enzyme inhibitor or an enzyme inducer, depending on the situation.

Are corticosteroids CYP3A4 inducers?

Is dexamethasone a CYP450 inducer?

Evidence for CYP3A4 induction in primary cultures of human hepatocytes. For several years, dexamethasone has been recognized as an inducer of CYP450 expressed in animal liver microsome.

Is atorvastatin a strong CYP3A4 inhibitor?

Fluvastatin, pravastatin and rosuvastatin are not significantly metabolised by CYP3A4….Key Messages.

Interacting medicines Simvastatin Atorvastatin
Minor CYP3A4 Inhibitors Azithromycin Roxithromycin Case reports of rhabdomyolysis. Use with caution and monitor No clinically significant interactions

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 metabolized by CYP3A4?

– alfentanil – buprenorphine ( analgesic, addiction maintenance treatment) – codeine ( analgesic, antitussive, antidiarrheal) – fentanyl – hydrocodone (partial involvement, not the bioactivation factor) – methadone ( analgesic, addiction maintenance treatment) – levacetylmethadol – tramadol (to inactive metabolites, do not confuse with metabolism via CYP2D6)

What does CYP3A4 do?

CYP3A4 is responsible for the metabolism of more than 50% of medicines.

  • CYP3A4 activity is absent in new-borns but reaches adult levels at around one year of age.
  • The liver and small intestine have the highest CYP3A4 activity.
  • Some important CYP3A4 interactions are due to intestinal rather than hepatic enzyme inhibition (eg,grapefruit).
  • What are CYP3A4 inhibitors?

    CYP3A4 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 CYP3A4 have many applications in biochemical and physiological research.