Human Immunodeficiency Virus Book

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Protease Inhibitor

Aka: Protease Inhibitor
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  1. See Also
    1. Anti-Retroviral Therapy
  2. Mechanism
    1. Prevent HIV from being assembled
    2. Prevent release from infected CD4 cells
  3. Protocols
    1. Most Protease Inhibitors are "boosted" with concurrent use of Ritonavir (Norvir)
      1. Limited by adverse gastrointestinal effects
  4. 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)
  5. Precautions
    1. Saquinavir and Saquinavir mesylate are not equivalent
  6. 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
  7. 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
  8. Monitoring
    1. Fasting lipid panel with Glucose every 3-6 months
  9. References
    1. (1998) Med Lett Drugs Ther 40(1041):115
    2. (2009) Treat Guidel Med Lett 7(78): 11-22
    3. Reust (2011) Am Fam Physician 83(12): 1443-51

HIV Protease Inhibitors (C0162714)

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 Inhibitor, Human Immunodeficiency Virus Protease Inhibitor [EPC], HIV PI, HIV Protease Inhibitor (HIV PI), Human Immunodeficiency Virus Protease Inhibitor, HIV protease inhibitors, 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
Russian VICH-PROTEAZY INGIBITORY, ВИЧ-ПРОТЕАЗЫ ИНГИБИТОРЫ
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
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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