HIV antivirals Flashcards
List the 6 types of HIV antiviral drugs
- CCR5 antagonist
- Fusion Inhibitors
- Reverse transcriptase Inhibitors (NARTIs)
- Reverse Transcriptase Inhibitors (NNRTIs)
- Integrase Inhibitors
- Protease Inhibitors
Which 2 drugs block viral entry into the cell?
- CCR5 antagonist
2. Fusion Inhibitors
Which 4 drugs Inhibit enzymes required for HIV replication?
- NARTI’s (reverse transcriptase inhibitor)
- NNRTIs (reverse transcriptase inhibitor)
- Integrase Inhibitor
- Protease Inhibitor
CCR5 Antagonist MOA
Block ability for CCR5 co-receptor to bind with gp120 on HIV virion blocking entry of HIV into CD4 cell
Why do you need to test pt first for CCR5 drug?
to see if pt’s HIV strain is CCR5-tropic
CCR5 Antagonist Prototype:
Maraviroc (Selzentry)
Fusion Inhibitor MOA
Blocks entry of HIV into CD4 cells, binding gp41 on HIV envelope, preventing HIV molecule and CD4 cell binding by fusing two lipid bilayer membranes
Fusion Inhibitor Prototype
Enfuvirtide (Fuzeon, T-20)
Cost and AE of Enfuvirtide
$52,000/year
Injection site reaction
^less med adherence
When is Enfuvirtide used?
When resistance to other drugs occurs
Nucleotide/nucleoside Reverse Transcriptase Inhibitor (NARTI) MOA
-Inhibit creation of viral DNA by substituting useless nucleotide in strand of base pairs (Dummy pair)
NARTIs Prototype:
Zidovudine (AZT)
Abacavir (ABC, Ziagen)
Key SE and considerations for NARITs
Zidovudine (AZT)- SE: anemia, neutropenia
Abacavir (Ziagen, ABC)- Test for HLA-B*5701. if positive, do not give drug
When would you use NARTIs? (Zidovudine, AZT or Abacavir, Ziagen)
1st line of treatment regimens
Non-Nucleotide reverse transcriptase inhibitors (NNRTIs) MOA
bind to the active center of reverse transcriptase and cause direct inhibition (Pie)
NNRTI Prototype:
Efavirenz (Sustiva)
AE of NNRTIs
Rash, hypersensitivity. If these are sever, discontinue use
Key consideration for NNRTIs
Many drug-drug interactions CYP450
Key points for Efavirenz (Sustiva)
Crosses the blood brain barrier
Teratogenic (NOT for pregnancy)
InTEGRase Inhibitors MOA
Prevent HIV genetic material from being integrated into DNA of CD4 cell (CD4 being guarded by the tiger)
Integrase Inhibitor Prototype:
RalTEGRavir
AE of Raltegravir
well tolerated, can cause increased liver enzymes and rarely cause hypersensitivity reaction
Protease Inhibitors MOA
Prevent protease enzyme from cutting HIV polyprotein. Leaves cell inactive and useless. (He’s a proTEASE, leaving HIV homeboy lip and useless)
PI effectiveness
Most effective antiretroviral drug available. Can reduce viral load to undetectable levels.
