Metabolized by CYP isoenzymes, principally CYP2D6 and CYP2C9; to a lesser extent by CYP3A4, CYP2C19, CYP1A2, CYP2E1.Drugs Affecting Hepatic Microsomal EnzymesPotent inhibitors of CYP2D6 (e.g., fluoxetine, paroxetine, propafenone, quinidine): potential pharmacokinetic interaction (increased plasma...
5. These data indicate that, although not substrates for CYP2E1, some clinically used drugs have the capacity to inhibit this enzyme and hence have the potential to modulate the toxicity of non-drug xenobiotics metabolized by CYP2E1.Tassaneeyakul...
Studieshave shown that CBD is metabolized by the CYP450 enzyme system, which includes CYP2C9, CYP2C19, CYP3A4, UGT1A9, UGT2B7, CYP2C8, CYP1A2, CYP2B6, CYP2D6, CYP2C8, CYP2E1, CYP3A, and CYP3A4 enzymes. Approximately 60% of prescription medications are also metabolized by these en...
The results from the present in vivo study suggested that HEI showed no effects on rat CYP1A2, CYP2C11 and CYP2E1, however, it demonstrated potential inhibitory effects on rat CYP2D4 and CYP3A2. Therefore, caution is needed when HEI is co-administered with drugs metabolized by human CYP2D...
Metabolized principally by sulfate and glucuronide conjugation; small amounts (5–10%) oxidized by CYP-dependent pathways (mainly CYP2E1) to a toxic metabolite, N-acetyl-p-benzoquinoneimine (NAPQI). NAPQI is detoxified by glutathione and eliminated; any remaining toxic metabolite may bind to ...
micafungin is observed in vitro, and the blood concentrations of cyclosporine and tacrolimus are not affected by coadministration of micafungin in vivo, suggesting that micafungin would not cause clinically significant interactions with drugs that are metabolized by CYPs via the inhibition of metabolism....
(phaseIIbiotransformation)withwatersolublesubstances.•Watersolubledrugsaremorereadilyexcretedintheurine.Theymaybemetabolized,butgenerallynotbytheCYPenzymesystems.Biotransformation&urinaryexcretion•Drugswithmajorfirstpasseffect(bioavailability)[%urinaryexcretion]imipramine(39)[<2]lidocaine(35)[2]morphine(24)[8]...
CYP2D6, CYP2E1, or CYP3A4 in vitro. Similarly oral vorinostat is 71% bound to proteins and is metabolized via glucuronidation and hydrolysis followed by beta-oxidation into two inactive metabolites. Biotransformation by cytochrome P450 is negligible. It is renally excreted with <1% of the dose ...
Inhibits CYP2C9 and CYP2C19. Does not inhibit CYP2E1, and does not inhibit CYP2D6 or CYP1A2 at clinically relevant concentrations.Induces CYP3A and CYP2B6.Drugs Affecting or Metabolized by Hepatic Microsomal EnzymesInducers of CYP3A and CYP2B6 expected to reduce efavirenz plasma concentrations. ...
Not metabolized by CYP isoenzymes; undergoes spontaneous hydrolysis and deamination by cytidine deaminase.Elimination RouteAzacitidine and its metabolites are eliminated principally in urine.Half-lifeElimination half-life of injectable azacitidine in adult patients is about 4 hours, regardless of IV or sub...