II. Class

III. Indications: HIV and AIDS

  1. Most commonly used NNRTI in 2011 and available in combination (Atripla)

IV. Dosing

  1. Adult
    1. Efavirenz 600 mg qhs
  2. Child
    1. Weight 10-14 kg: 200 mg qhs
    2. Weight 15-19 kg: 250 mg qhs
    3. Weight 20-24 kg: 300 mg qhs
    4. Weight 25-32 kg: 350 mg qhs
    5. Weight 32-40 kg: 400 mg qhs

V. Adverse Effects

  1. General: CNS effects
    1. Onset 1-3 hours after dose
    2. Symptoms abate over 1-2 weeks
  2. CNS adverse effects (affects 50% at 1 month, 23% at 3 months, baseline at 6 months)
    1. Dizziness
    2. Headache
    3. Insomnia
    4. Difficulty concentrating
    5. Vivid dreams
    6. Nightmares
    7. Hallucinations

VI. Pregnancy

  1. Potentially Teratogenic

VII. Drug Interactions

  1. Take on empty Stomache at bedtime
  2. Induces CYP3A4 enzyme
  3. Decreases serum levels of some Protease Inhibitors
    1. Avoid concurrent use of Saquinavir
    2. Raise dose of Indinavir to 1000 mg PO q8h
  4. Decreases some Macrolide levels
    1. Decreases Clarithromycin level
    2. Azithromycin not effected

VIII. Labs

  1. Causes false positive drug screen for cannabinoids, Benzodiazepines

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Cost: Medications

sustiva (on 1/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
SUSTIVA 200 MG CAPSULE $10.50 each
SUSTIVA 600 MG TABLET $31.34 each

Ontology: Sustiva (C0674427)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C098320
English Sustiva, sustiva, Bristol-Myers Squibb brand of efavirenz, Du Pont brand of efavirenz, United Drug brand of efavirenz

Ontology: efavirenz (C0674428)

Definition (NCI) A synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity. Efavirenz binds directly to the human immunodeficiency virus type 1 (HIV-1) RT, an RNA-dependent DNA polymerase, blocking its function in viral DNA replication. In combination with other antiretroviral drugs, this agent has been shown to significantly reduce HIV viral load, retarding or preventing damage to the immune system and reducing the risk of developing AIDS. Efavirenz induces activity of the cytochrome P450 system, accelerating its own metabolism.
Definition (NCI_NCI-GLOSS) A drug used with other drugs to treat infection with the human immunodeficiency virus (HIV). It blocks HIV from making copies of itself. It is a type of non-nucleoside reverse transcriptase inhibitor and a type of antiviral agent.
Definition (CSP) antiHIV 1 agent; reverse transcriptase inhibitor; 6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1, 4-dihydro-2H-3,1-benzoxazin-2-one.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C098320
SnomedCT 116078005, 387001004
LNC LP21310-5, MTHU013845
English efavirenz, efavirenz (medication), EFAVIRENZ, efavirenz [Chemical/Ingredient], EFV, (s)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, efavirenz, (S)-isomer, Efavirenz (product), Efavirenz (substance), Efavirenz
Spanish efavirenz (producto), efavirenz (sustancia), efavirenz