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12 Cards in this Set
- Front
- Back
Protease Inhibitors (PIs) includes:
a. b. c. d. e. f. g. |
Protease Inhibitors (PIs) includes:
a. Indinavir (Crixivan) b. Ritonavir (Norvir) c. Saquinavir (Fortovase or Invirase) d. Nelfinavir (Viracept) e. Amprenavir (Agenerase) and Fosamprenavir (Lexiva) f. Kaletra (Lopinavir/Ritonavir) g. Revataz (Atazanavir) *MOA for all is "protease inhibitor" *Pharmacotherapy for all is "Combination therapy for the management of HIV infection" |
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Indinavir (Crixivan)
method of action: |
Indinavir (Crixivan)
method of action: Protease inhibitor- inhibits HIV protease which is necessary for cleaving HIV proteins to form infectious new virions *same MOA for all other PIs |
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Indinavir (Crixivan)
pharmacokinetics: |
Indinavir (Crixivan)
pharmacokinetics: a. Presence of food reduces oral absorption by 80% (!) b. Hepatically metabolized by CYP3A4 enzyme |
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Ritonavir
pharmacokinetics: |
Ritonavir
pharmacokinetics: a. Hepatically metabolized b. EXTREMELY POTENT INHIBITOR OF CYTOCHRONE P450 ENZYME SYSTEMS; many drug interactions |
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Sawuinavir (fortovase or Invirase)
pharmacokinetics: |
Sawuinavir (fortovase or Invirase)
pharmacokinetics: a. Hepatically metabolized b. Oral bioavailability extremely low; must be taken with meals to maximize absorption |
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Nelfinavir (Viracept)
pharmacokinetics: |
Nelfinavir (Viracept)
pharmacokinetics: a. metabolized primarily in the liver b. absorption enchanced 2-3 fold WITH FOOD |
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Nelfinavir (Viracept)
safety profile: |
Nelfinavir (Viracept)
safety profile: a. major adverse effect: diarrhea (prevent with IMODIUM) b. drug interactions: INHIBITOR of CYP3A(4) |
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Amprenavir (Agenerase) and Fosamprenavir (Lexiva)
pharmacokinetics: |
Amprenavir (Agenerase) and Fosamprenavir (Lexiva)
pharmacokinetics: metabolized in liver by CYP3A4 enzymes |
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Amprenavir (Agenerase) and Fosamprenavir (Lexiva)
safety profile: |
Amprenavir (Agenerase) and Fosamprenavir (Lexiva)
safety profile: a. MAJOR adverse effects: -GI events (n/v/d) -Rash: mild/moderate; rarely severe -Parasthesias (perioral/peripheral) b. Patient Warnings -Allergy potential: amprenavir is a sulfonamide compound -Vitamin E use: the Vitamin E in the amprenavir dose exceeds RDA -Drug interactions c. Protease Inhibitor-induced syndromes -Hyperglycemia -Lipid abnormalities (increased triglycerides, cholesterol) -Fat redistribution |
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Kaletra (Lopinavir/Ritonavir)
pharmacokinetics: |
Kaletra (Lopinavir/Ritonavir)
pharmacokinetics: metabolized in liver, CYTOCHROME P450 INHIBITOR |
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Kaletra (Lopinavir/Ritonavir)
major adverse effects: |
Kaletra (Lopinavir/Ritonavir)
major adverse effects: -GI Intolerance -Increased liver enzymes -hyperglycemia and fat re-distribution syndrome |
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Revataz (Atazanavir)
info: |
Revataz (Atazanavir)
info: *Acidic environment needed for absorption *Contraindicated with Proton Pump inhibitors *Space administration from antacids |