HAART

Question 1

MOA of NTRI’s?

Answer 1

Reverse transcriptase inhibitors
Get converted into dNTP by host kinases-> get used for HIV DNA strand synthesis-> cause termination of elongation (no 3’ OH group)

Question 2

What is the black box warning of NRTI’s?

Answer 2

Lactic acidosis syndrome

Question 3

When would Tenofovir be contraindicated? What would you use instead?

Answer 3

In patients with renal insufficiency

Use Abacavir instead (both are purine NRTI’s)

Question 4

What patients cannot take Abacavir? Why?

Answer 4

People with HLA-B*5701 polymorphisms

Causes a multisystem inflammatory reaction

Question 5

How do NRTI’s cause lactic acidosis?

Answer 5

Inactivate mitochondrial polymerase gamma, which causes mitochondria to use glycolysis instead of OxPhos
Convert pyruvate-> Lactate

Question 6

What is the preferred NRTI combo?

Answer 6

Tenofivir (Purine) and Emtricitabine (Pyrimidine)

Question 7

What is the preferred NRTI combo in pregnancy?

Answer 7

Zidovudine and Lamivudine

Question 8

What is the preferred NNRTI? Who can’t take it?

Answer 8

Efavirenz

C/I in pregnancy

Question 9

What is the MOA of NNRTI’s?

Answer 9

Directly bind to HIV reverse transcriptase and distort it–> cannot make viral DNA

Question 10

What is the alternative NNRTI that is ok for pregnant patients?

Answer 10

Nevirapine

Question 11

What are the most common side effects of NNRTI’s?

Answer 11

Drug hypersensitivity, rash, and Stevens-Johnson syndrome
Hepatotoxicity- may be severe and life-threatening
Drug-Drug interactions from CYP450 induction

Question 12

What is responsible for NNRTI resistance? What is the exception?

Answer 12

Single mutation in reverse transcriptase- K103N

Etravirine is exception (alternative tx)

Question 13

What is the standard combo of 3 reverse transcriptase inhibitors?

Answer 13

Tenofovir/Emtricitabine and Efavirenz

Question 14

What is the preferred combo of reverse transcriptase inhibitors in pregnancy?

Answer 14

Zidovudine/Lamividine and Nevirapine

Question 15

What is the protease inhibitor suffix?

Answer 15

-navir

Question 16

What is the MOA of protease inhibitors?

Answer 16

Mimic HIV protease target and inhibit function, preventing production of HIV proteins

Question 17

What is the use of Ritanavir?

Answer 17

Used as a “booster” to make other protease inhibitors more effective- inhibits CYP3A4

Question 18

What side effects are associated with Protease inhibitors?

Answer 18

Potential Sulfa drug hypersensitivity reaction

Lipodystrophy, especially since in combo with NRTI’s

Question 19

What is the preferred NRTI + PI therapy?

Answer 19

Tenofivir/Emtricitabine + Atazanavir/Ritonavir

Question 20

What is the overall treatment regimen preferred for pregnant women?

Answer 20

Zidovudine/Lamivudine + Lopinavir/Ritonavir

Question 21

What is the MOA and use for Maraviroc?

Answer 21

CCR5 antagonist-> blocks gp120 binding

Useful for MDR viruses that have become resistant to other classes