Sustiva Indication:

For use in combination treatment of HIV infection (AIDS)

Sustiva 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 transcriptase interferes with the generation of DNA copies of viral RNA, which, in turn, are necessary for synthesis of new virions. Intracellular enzymes subsequently eliminate the HIV particle that previously had been uncoated, and left unprotected, during entry into the host cell. Thus, reverse transcriptase inhibitors are virustatic and do not eliminate HIV from the body. Even though human DNA polymerase is less susceptible to the pharmacologic effects of triphosphorylated efavirenz, this action may nevertheless account for some of the drug's toxicity.

Sustiva Drug Interactions:

Alprazolam The antiviral agent increases the effect and toxicity of benzodiazepine
Astemizole Increased risk of cardiotoxicity and arrhythmias
Atazanavir Sustiva decreases the levels/effects of atazanavir
Atorvastatin The NNRT inhibitor increases the effect and toxicity of the statin
Cisapride Increased risk of cardiotoxicity and arrhythmias
Clarithromycin Sustiva decreases levels of clarithromycin
Cyclosporine Sustiva decreases the levels of cyclosporine
Dihydroergotamine The antiretroviral agent may increase the ergot derivative toxicity
Dihydroergotoxine The antiretroviral agent may increase the ergot derivative toxicity
Ergotamine The antiretroviral agent may increase the ergot derivative toxicity
Indinavir Sustiva decreases the effect of indinavir
Lovastatin The NNRT inhibitor increases the effect and toxicity of the statin
Methadone The antiretroviral agent decreases the effect of mathadone
Methylergonovine The antiretroviral agent may increase the ergot derivative toxicity
Methysergide The antiretroviral agent may increase the ergot derivative toxicity
Midazolam The antiviral agent increases the effect and toxicity of benzodiazepine
Saquinavir Sustiva decreases the effect of saquinavir
Simvastatin The NNRT inhibitor increases the effect and toxicity of the statin
St. John's Wort St. John's Wort decreases the antiretroviral effect
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Triazolam The antiviral agent increases the effect and toxicity of benzodiazepine
Voriconazole Sustiva decreases the levels/effect of voriconazole

Sustiva Food Interactions:

Take without regard to meals.
Avoid excessive or chronic alcohol consumption.

Sustiva Generic Name:

Synonyms:

  • EFV

Drug Type:

Small Molecule; Approved

Absorption:

Not Available

Toxicity (Overdose):

Not Available

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.

Half Life:

40-55 hours

Dosage Forms of Sustiva:

Tablet Oral
Capsule Oral

Chemical IUPAC Name:

(4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one

Organisms Affected:

Human Immunodeficiency Virus

Sustiva to general, pharmacology

General, pharmacology..
Anti Viral