Antiretrovirals

Question 1

What are the 3 receptors on the CD4 cell that can bind to HIV and which one is more prevalent?

Answer 1

CD4 and 2 co-receptors: R5 and X4

R5 is the most common

Question 2

Why is HIV considered a retrovirus?

Answer 2

RNA –> DNA via reverse transcriptase

Question 3

How does HIV DNA get into the nucleus? What enzyme cleaves the new DNA to activate it?

Answer 3

Integrase

Protease

Question 4

What is the “point of no return” when HIV infects a cell?

Answer 4

Once it becomes integrated into the host cell nucleus

Can give drugs to people BEFORE integration and prevent PONR.

Question 5

Which part of the host cell do we NOT have an antiretroviral for?

Answer 5

X4 receptor blocker

Question 6

Can drugs cure HIV? How many drugs are used to treat HIV?

Answer 6

No, only suppress it. Can only eliminate the cells that have the HIV within in via chemo/radiation, therapeutic BMT.
3 drugs

Question 7

What are the combos for the 3 drugs that are used to treat HIV? Why would someone NOT be on one of these recipes?

Answer 7

2 NRTIs + 1 NNRTI
2 NRTIs + 1 PI
2NRTIs + 1 II
There is probably history of resistance.

Question 8

How many drugs are used for prep? What is the brand name for the combination drug?

Answer 8

2

Truvada

Question 9

What three drugs cover Hep B?

Answer 9

1. Lamivudine
2. Emtricitabine
3. Tenofovir

Question 10

What are the 5 main groups of HIV drugs?

Answer 10

1. CD4 Receptor blocker
2. R5 receptor blocker
3. Nucleoside Reverse Transcriptase Inhibitor
4. Integrase Inhibitors
5. Protease Inhibitors

Question 11

Zidovudine AZT is an example of an ________. What are the 4 AEs?

Answer 11

NRTI
Anemia (severe bone suppresion), tachy, malaise, GI upset
A in AZT is for Anemia

Question 12

Lamivudine 3TC is an example of an __________. It is known to be realtively _________.

Answer 12

NRTI

benign

Question 13

Emtricitabine FTC an QD analogue of _______.

Answer 13

Lamivudine 3TC

Question 14

Abacavir is an ________. What is the major AE with this drug? What should you do before you administer this drug?

Answer 14

NRTI
Anaphylaxis (hypersensitivity).
Do a HLA5701 test- (+) means patient is highly likely to react with Abacavir.

Question 15

What other group of ARVs is grouped with NucelosideRTIs? Name one.

Answer 15

Nucleotide RTIs.

Tenofovir.

Question 16

Which patients should take Tenofovir cautiously? how can you monitor this risk?

Answer 16

Nephrotoxicity patients

SrCr

Question 17

What are HIV boosters?

Answer 17

They increase the effectiveness of various ARVs by enhancing or “boosting” their levels in the body.
They allow another med in the ARV cocktail to be given at a lower dose or less often, thereby reducing the number of pills you have to take each day.

Question 18

Name the two boosters. How do they work?

Answer 18

Cobicistat - pure
Ritonavir - Protease Inhibitor
POTENT CP450 inhibitor.

Question 19

What is an AE Of Ritonavir?

Answer 19

multiple drug interactions

Question 20

Atazanavir is a ______. Name its 2 disadvantages.

Answer 20

PI

1. Cosmetic yellowing of skin
2. Acid-requiring drug - no H2RAs, PPIs, antacids

Question 21

Tipranavir and Darunavir are ___. What is required when you take them?

Answer 21

PIs

Boosters are required in all instances.

Question 22

Efavirenz is an _______. What is its claim to fame?

Answer 22

NNRTI

QHS dosing

Question 23

Which 2 groups of people would it be risky for to take Efavirenz considering its AEs?

Answer 23

People w/ mental illness and drug users

AEs: CNS disengagement and vidid nightmares

Question 24

What kind of drug is Enfuvirtide? What is the brand name?

Answer 24

CD4 receptor antagonist (receptor blocker)

Fuzeon

Question 25

Name the AE for Enfuvirtide. Why is it last line therapy?

Answer 25

It is an injection, so giving needles to HIV patients seems dangerous.

Question 26

Maraviroc falls in the _______ ARV category. What is the brand name? How does it work? Why don’t people use it very often?

Answer 26

Co-receptor antagonist
Selzentry
Blocks R5 with no effects on X4.
We are afraid it could select for X4 and increase the prevalence for X4 type HIV. Last stitch effort here.

Question 27

Which category of ARV is most recent, $$$ and has the fewest AEs? What are they?

Answer 27

Integrase Inhibitors

Raltegravir & Elvitegravir

Question 28

Name the 5 STRs.

Answer 28

1. Genvoya
2. Complere
3. Atripla
4. Triumeq
5. Stribild

Question 29

Name the components of Genvoya.

Answer 29

TAF + FTC + II + Cobi

Question 30

What is TAF? What are the 2 benefits of TAF?

Answer 30

Son of Tenofavir

1. Accumulates intracellularly (very potent)
2. Less side effects (less toxicity)

Question 31

What is Cobicistat? What are the advantages?

Answer 31

Its the other booster. Its a potent CP450 inhibitor

Not an ARV (like Ritonavir), no effects on lipids

Question 32

Which would you prefer, Ritonavir or Cobicistat?

Answer 32

Cobicistat b/c it does not contribute to resistance as Ritonavir can.

Question 33

What is the most important mitigating factor in deciding whether or not PREP/drugs will prevent seeding?

Answer 33

Time

you can PREVENT an exposure if

Question 34

Why are there 3 different RTI?

Answer 34

Resistance

Question 35

1 ARV drug - resistance in ___ days.

2 ARV drugs - resistance in ___ days.

Answer 35

1-2 days

2 weeks

Question 36

What is a generalization about PIs?

Answer 36

They all can be boosted - meaning they are all CP450 substrates.

Question 37

What is another NNRTI other than Efavirenz? What is the most important AE?

Answer 37

Nevirapine.

Rash - SJS