Antifungal and Antiviral Agents: Antiretroviral Agents III
Terms
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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" -
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 -
Indinavir (Crixivan)
pharmacokinetics: -
Indinavir (Crixivan)
pharmacokinetics:
a. Presence of food reduces oral absorption by 80% (!)
b. Hepatically metabolized by CYP3A4 enzyme -
Ritonavir
pharmacokinetics: -
Ritonavir
pharmacokinetics:
a. Hepatically metabolized
b. EXTREMELY POTENT INHIBITOR OF CYTOCHRONE P450 ENZYME SYSTEMS; many drug interactions -
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 -
Nelfinavir (Viracept)
pharmacokinetics: -
Nelfinavir (Viracept)
pharmacokinetics: a. metabolized primarily in the liver
b. absorption enchanced 2-3 fold WITH FOOD -
Nelfinavir (Viracept)
safety profile: -
Nelfinavir (Viracept)
safety profile:
a. major adverse effect: diarrhea (prevent with IMODIUM)
b. drug interactions: INHIBITOR of CYP3A(4) -
Amprenavir (Agenerase) and Fosamprenavir (Lexiva)
pharmacokinetics: -
Amprenavir (Agenerase) and Fosamprenavir (Lexiva)
pharmacokinetics: metabolized in liver by CYP3A4 enzymes -
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 -
Kaletra (Lopinavir/Ritonavir)
pharmacokinetics: -
Kaletra (Lopinavir/Ritonavir)
pharmacokinetics: metabolized in liver, CYTOCHROME P450 INHIBITOR -
Kaletra (Lopinavir/Ritonavir)
major adverse effects: -
Kaletra (Lopinavir/Ritonavir)
major adverse effects:
-GI Intolerance
-Increased liver enzymes
-hyperglycemia and fat re-distribution syndrome -
Revataz (Atazanavir)
info: -
Revataz (Atazanavir)
info:
*Acidic environment needed for absorption
*Contraindicated with Proton Pump inhibitors
*Space administration from antacids