Human Immunodeficiency Virus Book

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EfavirenzAka: Sustiva

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  1. Class
    1. Non-Nucleoside Reverse Transcriptase Inhibitor
  2. 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
  3. Adverse Effects
    1. General: CNS effects
      1. Onset 1-3 hours after dose
      2. Symptoms abate over 1-2 weeks
    2. CNS adverse effects
      1. Dizziness
      2. Headache
      3. Insomnia
      4. Difficulty concentrating
      5. Vivid dreams
      6. Nightmares
      7. Hallucinations
  4. Drug Interactions
    1. Induces CYP3A4 enzyme
    2. Decreases serum levels of some Protease Inhibitors
      1. Avoid concurrent use of Saquinavir
      2. Raise dose of Indinavir to 1000 mg PO q8h
    3. Decreases some Macrolide levels
      1. Decreases Clarithromycin level
      2. Azithromycin not effected
  5. Reference
    1. Med Lett Drugs Ther (1998) 40(1041):115

Sustiva (C0674427)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC098320
EnglishBristol-Myers Squibb brand of efavirenz, Du Pont brand of efavirenz, Sustiva, United Drug brand of efavirenz
SourcesCSP, MSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


efavirenz (C0674428)

Definition (CSP)antiHIV 1 agent; reverse transcriptase inhibitor; 6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1, 4-dihydro-2H-3,1-benzoxazin-2-one.
Definition (NCI)A synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral properties. 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 loads, therefore retarding or preventing damage to the immune system, and reducing the risk of developing AIDS. Efavirenz induces activity of the cytochrome P450 system, thereby accelerating its own metabolism. (NCI04)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC098320
Englishefavirenz, EFAVIRENZ PREPARATION, EFV
Spanishefavirenz
Parent ConceptsAntiviral Agents (C0003451), Oxazines (C0030001), Reverse Transcriptase Inhibitors (C0282519), L 743726 (C0387218), Efavirenz and derivatives (C1445636), Anti-HIV Agents, Non-nucleoside Reverse Transcriptase Inhibitors (C1579420)
SourcesCSP, LNC, MSH, MTHSPL, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)



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