Wk 32: HIV 4 Flashcards
What are the classes of ARV drugs?
- NRTI backbones
- Protease inhibitors
- Integrase inhibitors
- NNRTIs
- CCR5 inhibitors
What would you use for treatment?
2 NRTIs plus 1 drug from another class
How do NRTIs work?
- Block addition of nucleotide to DNA chain during retrotranscription
- Structure resembles nucleotide but terminate DNA chain building
What are the 3 types of NRTI backbone?
- Truvada: TDF + emtricitabine: caution stage 3-5 CKD
- Descovy: TAF + emtricitabine
- Kivexa: abacavir + lamivudine
How do the tenofovir salts work?
- TDF + TAF: prodrugs
- TDF activated in plasma
- TAF activated intracellularly
- TAF lower plasma conc + fewer s/e
- TDF: red bone density + impaired renal function
When would you avoid abacavir?
- Fatal hypersensitivity reactions: avoid HLA-B 5701 gene positive
- Caution: CVD risk + VL >1000,000
What is the mechanism of action of protease inhibitors?
- Bind catalytic site of HIV protease
- Prevent processing of viral enzymes
- Incomplete + non-infectious virions released
What are the pros + cons of protease inhibitors?
+ No resistance
- S/e: peripheral neuropathy, headache, n+v
What is the MOA of integrase inhibitors?
- Incorporates HIV genome into host cell genome
- Integrase inhibitors block access to integrase
What are the pros + cons of integrase inhibitors?
+ Fewer s/e
- Low barrier to resistance
What is the MOA of NNRTI?
- Bid to reverse transcriptase + impair function
- Viral DNA formation terminated
When would you not use NNRTIs?
- Psychiatric illness
- VL >100,000
What is an example of a protease inhibitor?
NAVIR
- Atazanavir
- Darunavir
What is an example of a integrase inhibitor?
GRAVIR
- Dolutegravir
- Elvitegravir
- Raltegravir
What is an example of a NNRTI?
Rilpivirine
How do you monitor for treatment failure?
Sustained VL rebound: >4-6 wks