II. Mechanism
- Prevent HIV from being assembled
- Prevent release from infected CD4+ Cells
III. Protocols
IV. Preparations- suffix '/r' added when combined with Ritonavir
- Amprenavir (Agenerase)
- Atazanavir (Reyataz, ATV or ATV/r)
- Unboosted (without Ritonavir) has least adverse effect on lipids
-
Darunavir (DRV or DRV/r)
- Less adverse effects on lipid profile
- Fosamprenavir (Lexiva, FPV or FPV/r)
- Indinavir (Crixivan)
- Lopinavir with Ritonavir (Kaletra, LPV/r)
- Nelfinavir (Viracept)
- Ritonavir (Norvir, /r)
- Saquinavir (Fortovase)
- Saquinavir mesylate (Invirase)
- Tipranavir (Aptivus)
V. Precautions
- Saquinavir and Saquinavir mesylate are not equivalent
VI. Adverse Effects
- See each individual agent for specific adverse effects
- Nephrolithiasis (Indinavir)
- Severe Diarrhea (Nelfinavir)
- Gastrointestinal upset
- Lipodystrophy
-
Insulin Resistance
- Manage with lifestyle changes (diet, Exercise)
- Consider medications
- Severe lipid abnormalities
- Effects
- Hypertriglyceridemia
- Low HDL
- Management
- Consider Atazanavir (unboosted or boosted) or boosted Darunavir (DRV)
- Can be treated with Pravastatin (see below)
- Resolves with discontinuation of Protease Inhibitor
- Effects
- Hepatotoxicity
- Associated with concurrent use of other HIV agents
- Associated with comorbid Hepatitis C
- Osteopenia
VII. Drug Interactions
-
Drug Interactions are common
- Protease Inhibitors cause the most Drug Interactions of all Antiretrovirals
-
Statin drugs (used for PI-induced lipid abnormalities)
- Pravastatin is first choice Statin for use with PI
- Rosuvastatin (Crestor) or Atorvastatin (Lipitor) may also be used with caution
- Do not use Simvastatin or Lovastatin with PI
- Apixiban or Rivaroxaban
- Metabolized by CYP3A4 and P-Glycoprotein
- Protease Inhibitors strongly inhibit CYP3A4 or P-Glycoprotein, with associated bleeding risk