II. Mechanism

  1. Prevent HIV from being assembled
  2. Prevent release from infected CD4+ Cells

III. Protocols

  1. Most Protease Inhibitors are "boosted" with concurrent use of Ritonavir (Norvir)
    1. Limited by adverse gastrointestinal effects

IV. Preparations- suffix '/r' added when combined with Ritonavir

  1. Amprenavir (Agenerase)
  2. Atazanavir (Reyataz, ATV or ATV/r)
    1. Unboosted (without Ritonavir) has least adverse effect on lipids
  3. Darunavir (DRV or DRV/r)
    1. Less adverse effects on lipid profile
  4. Fosamprenavir (Lexiva, FPV or FPV/r)
  5. Indinavir (Crixivan)
  6. Lopinavir with Ritonavir (Kaletra, LPV/r)
  7. Nelfinavir (Viracept)
  8. Ritonavir (Norvir, /r)
  9. Saquinavir (Fortovase)
  10. Saquinavir mesylate (Invirase)
  11. Tipranavir (Aptivus)

V. Precautions

  1. Saquinavir and Saquinavir mesylate are not equivalent

VI. Adverse Effects

  1. See each individual agent for specific adverse effects
    1. Nephrolithiasis (Indinavir)
    2. Severe Diarrhea (Nelfinavir)
  2. Gastrointestinal upset
  3. Lipodystrophy
  4. Insulin Resistance
    1. Manage with lifestyle changes (diet, Exercise)
    2. Consider medications
      1. Thiazolidinediones (eg Rosiglitazone, Pioglitazone)
      2. Glucophage
  5. Severe lipid abnormalities
    1. Effects
      1. Hypertriglyceridemia
      2. Low HDL
    2. Management
      1. Consider Atazanavir (unboosted or boosted) or boosted Darunavir (DRV)
      2. Can be treated with Pravastatin (see below)
      3. Resolves with discontinuation of Protease Inhibitor
  6. Hepatotoxicity
    1. Associated with concurrent use of other HIV agents
    2. Associated with comorbid Hepatitis C
  7. Osteopenia

VII. Drug Interactions

  1. Drug Interactions are common
    1. Protease Inhibitors cause the most Drug Interactions of all Antiretrovirals
  2. Statin drugs (used for PI-induced lipid abnormalities)
    1. Pravastatin is first choice Statin for use with PI
    2. Rosuvastatin (Crestor) or Atorvastatin (Lipitor) may also be used with caution
    3. Do not use Simvastatin or Lovastatin with PI
  3. Apixiban or Rivaroxaban
    1. Metabolized by CYP3A4 and P-Glycoprotein
    2. Protease Inhibitors strongly inhibit CYP3A4 or P-Glycoprotein, with associated bleeding risk

VIII. Monitoring

  1. Fasting lipid panel with Glucose every 3-6 months

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Related Studies

Ontology: HIV Protease Inhibitors (C0162714)

Definition (NCI) A protease inhibitor that is designed to target the human immunodeficiency virus (HIV) protease while sparing other host cell proteases. HIV protease mediates the cleavage of viral Gag, Gag-Pol and Nef precursor polypeptides into their mature proteins. Inhibition of HIV protease results in production of noninfectious viral particles.
Definition (MSH) Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly.
Concepts Pharmacologic Substance (T121)
MSH D017320
English Inhibitors, HIV Protease, Protease Inhibitors, HIV, HIV PROTEASE INHIB, HIV Protease Inhibitors, HIV protease inhibitors, HIV protease inhibitor, HIV Protease Inhibitor, Anti-HIV Agents, Protease Inhibitors
French Inhibiteurs de protéase du VIH, Inhibiteurs de la protéinase VIH, Inhibiteurs de la protéinase HTLV-III, Inhibiteurs de la protéase du VIH, Antiprotéases anti-VIH, Anti-protéases anti-VIH
Swedish HIV-proteashämmare
Czech HIV-proteasa - inhibitory
Finnish HIV-proteaasin estäjät
Italian Inibitori della proteasi del HIV, Inibitori della proteasi dell'HIV
Polish Inhibitory proteazy HIV
German HIV-Proteaseinhibitoren, Proteaseinhibitoren, HIV-
Portuguese Inibidores da Protease HIV
Spanish Inhibidores de la Proteasa VIH