Table of Contents
What is a sensitive substrate of CYP3A4?
These sensitive substrates are: budesonide, buspirone, eplerenone, eletriptan, felodipine, fluticasone, lovastatin, midazolam, saquinavir, sildenafil, simvastatin, triazolam and vardenafil.
Is rifampin a CYP3A4 inhibitor?
Rifampicin is a well-known CYP3A4 inducer, and is commonly used as a positive control for evaluating the CYP3A4 induction potential of test compounds.
What medications interact with CBD oil?
CBD can alter the effects of other drugs
- a common blood thinner, warfarin.
- a heart rhythm medication, amiodarone.
- a thyroid medication, levothyroxine.
- several medications for seizure, including clobazam, lamotrigine, and valproate.
How long is CYP3A4 inhibited?
The interaction potential of even high amounts of grapefruit juice with CYP3A4 substrates dissipates within 3 to 7 days after ingestion of the last dose of grapefruit juice.
Is isoniazid a CYP3A4 inhibitor?
Conclusions: As the peak plasma concentrations of isoniazid are around 30-50 microM, isoniazid at clinically relevant concentrations reversibly inhibits CYP2C19 and CYP3A4 activities, and mechanistically inactivates CYP1A2, CYP2A6, CYP2C19 and CYP3A4 in human liver microsomes.
What are CYP3A inhibitors?
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 are moderate CYP3A4 inhibitors?
Moderate inhibitors of CYP3A4 include: amiodarone, erythromycin, fluconazole, miconazole, diltiazem, verapamil, delavirdine, amprenavir, fosamprenavir, conivaptan.
What is a CYP3A drug?
Is methylprednisolone 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 rifampin a CYP inducer?
Rifampicin is involved in drug-drug interaction by its induction of CYPs, especially CYP3A4, and CYP3A4 mRNA is induced by rifampicin in blood mononuclear and liver HepG2 cells [64-66]. The CYP3A4 gene has also been isolated and cloned.
What class of drug is isoniazid?
Isoniazid is in a class of medications called antituberculosis agents. It works by killing the bacteria that cause tuberculosis.
What drugs are CYP3A inhibitors?
What drugs are inhibitors of CYP3A4?
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. Drugs that induce (increase) activity of CYP3A4 are listed in Table 4.
What are the drug interactions between CYP3A4 inhibitors and other cyto-chrome P450 substrates?
Keep in mind that many drugs are metabolized by more than one cyto- chrome P450 enzyme, and CYP3A4 may represent only 1 pathway. Unfortunately, many CYP3A4 substrates have substantial toxicity and some patients may develop severe toxicosis when CYP3A4 inhibitors are taken concurrently. A selected list of such interactions appears in Table 2.
What is an example of a CYP3A4 inducer?
For example, a patient taking the potent CYP3A4 inducer rifampin may have a roughly 90% reduction in serum concen- trations of CYP3A4 substrates, such as buspirone, triazolam, and verapamil. CYP3A4 is the most important of the CYP450 enzymes for drug metabolism and for drug interactions.
How common is CYP3A4 toxicity?
It has been estimated that CYP3A4 metabolizes about half of all drugs on the market. Since many other commonly used drugs are moderate to potent inhibitors of CYP3A4, it is not surprising that the drug toxicity of CYP3A4 substrates, due to inhi- bition of CYP3A4, is relatively common.