HIV Flashcards
What are the stages of HIV replication and how is this useful?
Stage 1+2: Binding of virus to CD4 receptors and CCR5/CXCR4 co-receptors on the surface of CD4 host cell and fusion of HIV to CD4 cell membrane. CCR5 antagonists and fusion inhibitors work here
Stage 3: HIV RNA is converted to HIV DNA by reverse transcriptase. It can then enter the CD4 cell nucleus. Reverse transcriptase inhibitors work here (NRTIs and NNRTIs)
Stage 4: integration - integrate i s release and used to insert HIV DNA into the host cell. Integrase inhibitors used here.
Stage 5: Host cell machinery is used to transcribe and translate HIV DNA into HIV RNA. No meds for this stage
Stage 6:new HIV RNA, proteins and enzymes (including protease) move to cell surface and assemble into immature HIV. No meds for this stage
Stage 7 - immature HIV pushes out of the CD4 cell and protease breaks up the long viral protein chains, creating a mature virus that can then infect other cells. Protease inhibitors used here.
Enfuvirtide, maraviroc and vicriviroc are what type of ARTs?
Fusion/Penetration blockers/CCR5 antagonists.
What are 2 NNRTIs? What stage do they work at?
Efavirenz, Rilpivirine
Stage 3 - reverse transcriptase inhibitors.
What are some common NRTIs?
Abacavir, emtricitabine, lamivudine, TDF, TAF, zidovudine.
What are some examples of INSTIs and where do they act?
Bictegravir, dolutegravir, elvitegravir and raltegravir
Stage 4 - Integrase strand transfer inhibitor
What are some common Protease inhibitors (PIs) and where do they work?
Atazanavir, Darunavir, Fosamprenavir, lopinavir, tipranavir.
Stage 7 - where the protease cuts the long viral strands to create a mature virus.
What is an ART naive regimen?
2NRTIs (stage 3) and 1 INSTI (stage 4)
What is an alternative ART regimen?
One “base” (either PI, NNRTIS or INSTI) and 2 NRTIs.
What is Z LATTE?
Acronym for the NRTIs:
Zidovudine, Lamivudine, Abacavir, TDF, TAF and Etravirine
T/F: NRTIs have a high barrier to resistance.
False - low. Barrier to resistance. Resistance develops easily. That’s what ART regimens usually include 2 NRTIs AND a base (PI/INSTI or NNRTI)
Abacavir - what is key prior to prescribing this medication?
“A for allergies”
Patients must be screened for the HLA-B*5701 allele due to extreme risk for hypersensitivity.
What class of antiretrovirals ends in “-tegravir”
INSTIs - stage 4 Integrase inhibitors
What are some DI examples for INSTIs? Some SEs?
“-tegravir”
Polyvalent cations (Mg, MVI, Iron, Ca) need to be separated by 2hrs.
depression and SI.
which has a higher barrier for resistance, INSTIs or NRTIs?
INSTIs.
What is the preferred drug for treatment of HIV during pregnancy?
Dolutegravir (INSTI) and darunavir. (PI)
What are some trends of AEs in INSTIs?
Increased SCr through inhibition of tubular secretion
Increased r/o rhabdo
Hepatotoxic.
What is REDEN?
NNRITs
Rilpivirine, Efavirenz, Doravirine, Etravirine and Nevirapine.
What class of ARTs non- competitively inhibit the conversion of HIV RNA to HIV DNA?
NNRTIs.
What are some DIs with NNRITs?
CYP3A4 inducers like phenytoin, rifampin, carbamazepine, oxcarbazepine, phenobarbital
Acid suppressants.
Which NNRTI has a high fail rate and should not be used with viral load > 100,000 copies or cD4 count < 200?
Rilpivirine.
What are some AEs with Efavirenz?
NNRTI
CNS SEs like depression, SI
Increased cholesterol and triglycerides.
When you see PIs, think:
DIs! PIs = DIs!
Major CYP3A4 substrate/strong inhibitors
Warnings for: Hyperglycemia, dyslipidemia, increased r/o CVD, hepatic dysfunction.
what class of ARTs end in “-Navir”?
PIs (except for Atazanair and Bevirimat
What are Ritonavir and Cobicistat?
ART boosters/enhancers they have many DIs!
If the HIV strain binds to CXCR4 or is a mixed binder, will Maraviroc be effective?
No. Miraviroc is a CCR5 antagonist (fusion inhibitor)
What is Fostemsavir? When is it used?
Attachment inhibitor. Used in combination with other ARTs in patients who are failing current therapy.
What is a common ART regimen for treatment-naive patients?
2NRTI backbone
- TDF, TAF OR Abacavir
plus
-Lamivudine or Emtricitabine
And 1 INSTI
-Dolutegravir, Elvitegravir or Raltegravir
What is the preferred medication used in the tx regimen for PEP?
What is the timeline?
2 NRTIs - Truvada (TDF and emtricitabine)
1 INSTI - dolutegravir or raltegravir.
Started w/in 72hrs and continue for 28 days
Test at baseline, 4-6ths, 3 mo and 6mo post exposure.
T/F: a ART tx regimen of 2 NRTIs and 1 NNRTI is appropriate.
True. As long as there is a 2 NRTI combo, the “base” can be either a PI, NNRTI, or INSTI.
