Human Immunodeficiency Virus Book

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Protease Inhibitor

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  1. Mechanism
    1. Prevent HIV from being assembled
    2. Prevent release from infected CD4 cells
  2. Preparations
    1. Amprenavir (Agenerase)
    2. Atazanavir (Reyataz)
    3. Fosamprenavir (Lexiva)
      1. Converted to Agenerase in vivo
      2. Less gastrointestinal side effects than Agenerase
      3. CYP3A4 inhibitor
    4. Indinavir (Crixivan)
    5. Lopinavir with Ritonavir (Kaletra)
    6. Nelfinavir (Viracept)
    7. Ritonavir (Norvir)
    8. Saquinavir (Fortovase)
    9. Saquinavir mesylate (Invirase)
    10. Tipranavir (Aptivus)
      1. Indicated for resistance to other protease inhibitors
      2. Avoid if sulfa allergy
  3. Precautions
    1. Saquinavir and Saquinavir mesylate are not equivalent
  4. Adverse Effects
    1. Nephrolithiasis (Indinavir)
    2. Severe Diarrhea (Nelfinavir)
    3. Hepatotoxicity
      1. Associated with concurrent use of other HIV agents
      2. Associated with comorbid Hepatitis C
    4. Lipodystrophy
    5. Osteopenia
    6. Insulin Resistance
      1. Manage with lifestyle changes (diet, Exercise)
      2. Consider medications
        1. Thiazolidinediones (eg Rosiglitazone, Pioglitazone)
        2. Glucophage
    7. Severe lipid abnormalities
      1. Effects
        1. Hypertriglyceridemia
        2. Low HDL
      2. Management
        1. Can be treated with Pravastatin (see below)
        2. Resolves with discontinuation of Protease Inhibitor
  5. Drug Interactions
    1. Drug interactions are common
      1. PIs cause most interactions of all Antiretrovirals
    2. Statin drugs (used for PI-induced lipid abnormalities)
      1. Pravastatin is first choice Statin for use with PI
      2. Do not use Simvastatin or Lovastatin with PI
      3. Use Atorvastatin and Fluvastatin with caution with PI
  6. Monitoring
    1. Fasting lipid panel with glucose every 3-6 months

HIV Protease Inhibitors (C0162714)

Definition (MSH)Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly.
ConceptsPharmacologic Substance (T121)
EnglishHIV PROTEASE INHIB, HIV protease inhibitor, HIV Protease Inhibitors
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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