retroantiviral Flashcards
1
Q
Nucleoside reverse transcriptase inhibitors (NRTI’s)
A
- Target = Reverse transcriptase
- mimic nucleotides to inhibt binding to the catalytic site and cause chain termination when incorporated into DNA
- Require cellular kinaes to convert to a triphosphate form
- many also approved for tx of chronic hep B virus
- Adverse effects common to the class:
- Lactic Acidosis, fatty liver disease, lipodystrophy
2
Q
Non-Nucleoside Reverse Transcriptase inhibitors (NNRTIs)
A
- Target = Reverse transcriptase
- Bind to a site on the enzyme distinct from the active site
- Do not require phosphorylation for activation
- Not active against HIV-2
- Adverse Effects
- Rash, Steven Johnson syndrome, Hepatotoxicity
- DRUG-DRUG interactions due to effects on cytochrone P450 enzyme
3
Q
Protease inhibitors
A
- Target = HIV protease
- miic peptide targets for the protease
- block maturation of virion particles after budding
- RESISTANCE = multipe mutations are required for high level of resistance
- ADVERSE
- hyperlipidemia, lipodystrophy, hepatotoxicity, GI intolerance, increased bleeding risk
- DRUG: DRUG INTERACTIONS DUE TO ALTERATION OF CYTOCHROME P450 Enzymes
4
Q
CCR5 REcetpor antagonist
A
- MoA
- gp 120 anchors HIV to target cell by binding to CD4
- CCR5 chemokine receptor binding stabilizes complex and allows gp41-mediated fusion of virus membrane with target cell membrane
- Maraviroc binds to CCR5, preventing gp120 binding, fusion and entry
5
Q
Integrase inhibitor MoA
A
- binds to HIV integrase and prevents DNA strand transfer
