Pharm: Anti-retrovirals Flashcards
Based on Caldwell's objectives
Viral Enzyme that converts viral RNA to DNA:
Reverse transcriptase (aka RNA dependent DNA polymerase)
MOA of NRTI’s
- Inhibit reverse transcriptase by incorporating false nucleic acids into the newly produced proviral DNA
- THESE AGENTS LACKA 3’-HYDROXYL GROUP, thus incorporation into DNA terminates chain elongation
What does NRTI stand for?
Nucleoside reverse transcriptase inhibitors
Which NRTI is part of every regimen recommended by DHHS panel in 2009 guidelines?
Emtricitabine
What does NNRTI stand for?
Non-nucleoside reverse transcriptase inhibitor
MOA of NNRTI’s:
Inhibit RT activity by binding ADJACENT to the enzyme’s active site and inducing conformation changes. Inhibits the RT enzyme itself.
What stage of infection does NRTI’s target?
Early and essential step in HIV replication
Only protects newly infected cells
What stage of infection does NNRTI’s target?
Only protect newly infected cells
What strain does NNRTI’s work against?
HIV-1
Describe the role of protease in viral reproduction:
Viral RNA is converted by viral polyprotiens that are cleaved and activated by protease (RT, integrase, protease)
Binding site of Protease inhibitors:
Reversibly to the active site of the HIV protease
Viral reproduction stage targeted by PIs:
Inhibit the envelope making stage –> so works in ANY currently infected cell
MOA of PIs:
Viral particles become immature and non-infectious
SE of PIs:
Endocrine Disturbances: Hyperglycemia, Fat redistribution, lipid abnormalities (Buffalo hump)
MOA of Fusion inhibitors:
Inhibits fusion of the virus to cellular membranes
-Prevents conformational changes by the virus transmembrane glycoprotein to attach to the CD4+ cells
Enfuvirtide belongs to what drug class?
Fusion Inhibitor
Clinical indications for Enfuvirtide:
Advanced HIV-1 infection patients
-Ongoing viral replication despite antiretroviral therapy
Drug class for Raltegravir Potassium?
Integrase inhibitor
Treatment stage for Raltegravir Potassium?
In treatment naïve patients
Types of drugs given in a PI-based HAART regiment:
One PI + 2 NRTIs
Types of drugs given in an NNRTI based HAART regimen
1 NNRTI + 2 NRTIs
What drug has been associated with Lipodystrophy syndrome?
Stavudine
Treatment of Lipodystrophy syndrome:
Pravastatin and atorvastatin
A side effect specific to indinavir (a protease inhibitor)
alopecia
