Is efavirenz a CYP inducer?
Efavirenz is approximately 99% plasma protein bound. Efavirenz is principally metabolized by CYP450 2B6 and 3A4 to hydroxylated metabolites with subsequent glucuronidation. Efavirenz is an inducer and an inhibitor of the cytochrome P450 system and leads to self-induction.
What is an inducer of CYP3A4?
Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.
What drug exhibits CYP450 induction?
Other chronic inducers of CYP450 enzymes include the anticonvulsant drug phenobarbital and the antimycobacterial drug rifampin. As a potent P450 enzyme inducer, rifampin is associated with drug interactions of substantial clinical significance.
What drugs are 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.
Is efavirenz an enzyme inducer?
Efavirenz has been well described to induce drug-metabolising enzymes and decrease plasma concentrations of a number of antiretrovirals and supportive medications [14].
How is Efavirenz metabolized?
Efavirenz is a non-nucleoside human immunodeficiency virus (HIV)-1 reverse transcriptase inhibitor used in combination therapy to treat HIV-1. Efavirenz metabolism is catalyzed primarily by the polymorphic enzyme P450 2B6. Metabolism of efavirenz by P450 2B6 and the naturally occurring P450 2B6.
Is topiramate a CYP3A4 inducer?
Topiramate is a weak inducer of CYP3A4, which is involved in steroid metabolism. In one case a modest dose of topiramate accelerated the metabolic clearance of dexamethasone and fludrocortisone and caused hypoadrenalism [334A].
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 does CYP3A4 substrate mean?
Drugs metabolized by CYP3A4 are called CYP3A4 substrates. Keep in mind that many drugs are metabolized by more than one CYP450 enzyme, and CYP3A4 may represent only one pathway.
What is the mechanism of action for efavirenz?
Mechanism of action Efavirenz falls in the NNRTI class of antiretrovirals. Both nucleoside and non-nucleoside RTIs inhibit the same target, the reverse transcriptase enzyme, an essential viral enzyme which transcribes viral RNA into DNA.
What is the action of efavirenz?
Efavirenz is used along with other medications to treat human immunodeficiency virus (HIV) infection. Efavirenz is in a class of medications called non-nucleoside reverse transcriptase inhibitors (NNRTIs). It works by decreasing the amount of HIV in the blood.