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QuickView for Efavirenz (compound)

Name: efavirenz
PubChem Compound ID: 3203
Molecular formula: C14H9ClF3NO2
Molecular weight: 315.675 g/mol
154635-17-3; 2H-3,1-Benzoxazin-2-one, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-; 177530-93-7; 6-Chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; 2H-3,1-Benzoxazin-2-one, 6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-, (+-)-; 6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-3-one; L 741211
Name: efavirenz
Name (isomeric): DB00625
Drug Type: small molecule
Brand: Sustiva, Stocrin
Category: Anti-HIV Agents, Nonnucleoside Reverse Transcriptase Inhibitors, Reverse Transcriptase Inhibitors
CAS number: 154598-52-4
Indication: For use in combination treatment of HIV infection (AIDS)
Efavirenz (dideoxyinosine, ddI) is an oral nucleoside reverse transcriptase inhibitor (NRTI). It is a synthetic purine derivative and, similar to zidovudine, zalcitabine, and stavudine. Efavirenz was originally approved specifically for the treatment of HIV infections in patients who failed therapy with zidovudine. Currently, the CDC recommends tha...
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Mechanism of Action:
Similar to zidovudine, efavirenz inhibits the activity of viral RNA-directed DNA polymerase (i.e., reverse transcriptase). Antiviral activity of efavirenz is dependent on intracellular conversion to the active triphosphorylated form. The rate of efavirenz phosphorylation varies, depending on cell type. It is believed that inhibition of reverse tran...
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Protein binding: 99.5-99.75%
Biotransformation: Efavirenz is principally metabolized by the cytochrome P450 system to hydroxylated metabolites with subsequent glucuronidation of these hydroxylated metabolites. These metabolites are essentially inactive against HIV-1.
Route of elimination: Nearly all of the urinary excretion of the radiolabeled drug was in the form of metabolites.
Half Life: 40-55 hours
Affected organisms: Human Immunodeficiency Virus
Food interaction:
Avoid excessive or chronic alcohol consumption.
Take without regard to meals.
Drug interaction:
DihydroergotamineEfavirenze may increase the adverse/toxic effects of dihydroergotamine. Concomitant therapy is contraindicated.
MidazolamThe antiviral agent, efavirenz, may increase the effect and toxicity of the benzodiazepine, midazolam.
IndinavirEfavirenz decreases the effect of indinavir
TemsirolimusEfavirenz may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
TrazodoneThe CYP3A4 inhibitor and inducer, Efavirenz, may alter Trazodone efficacy/toxicity by altering Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Efavirenz is initiated, discontinued or dose changed.
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