Antiretrovirals

Question 1

What is a CD4 cell?

Answer 1

T4 cell = Helper cell

Mission control of immune system, tells the other cells what to do

Question 2

HIV infects what?

Answer 2

Destroys CD4 cells so no immune response, the WBC is normal

Question 3

What do cells release to communicate with other cells?

Answer 3

Cytokines and interleukins

Question 4

HIV must go through what receptors?

Answer 4

• CD4 receprot
• R5 or X4 coreceptor

Depends on strain, 99% in USA use R5

Question 5

HIV baseline genetic material is

Answer 5

RNA (opposite of humans)

Question 6

Viruses replicate ____

Answer 6

intracellularly because it needs it to convert DNA to proteins

Question 7

How does a virus replicate?

Answer 7

viral DNA integrates into our DNA (point of no return)

Question 8

CD4 cell dies through what?

Answer 8

apoptosis

CD4 cell counts go down, patient gets infection and dies

Question 9

What is Pre-Exposure Prophylaxis

Answer 9

start patient on anti-retrovirals, about 79% stopped

Question 10

What is the PREP mitigating factor?

Answer 10

TIME, must have drugs on board within 48 – 72 hours

Question 11

What is PREP DOC?

Answer 11

Truvada

Question 12

What enzymes are involved in HIV replication?

Answer 12

• Reverse transcriptase (RNA –> DNA)
• Integrase (DNA into CD4 nucleus)
• Protease (pro-proteins –> activated proteins)

Question 13

What are the nucleoside reverse transcriptase inhibitors?

Answer 13

• Zidovudine
• Lamivudine / Emtricitabine (QD version)
• Abacavir
• Tenovir (nucleotide RTI)

Question 14

What was the first HIV drug?

Answer 14

Zidovudine (1987 originally for chemo)

Question 15

Zidovudine adverse effect?

Answer 15

Severe anemia due to marrow suppression, malaise, tachycardia

Question 16

Lamivudine a/e?

Answer 16

None, benign

Question 17

Abacavir a/e?

Answer 17

risk of anaphylaxis so must draw assay before prescribing (must be HLA-5701 negative)

Hypersensitivity

Question 18

Tenofovir a/e

Answer 18

Renal toxic so monitor serum Cr

Question 19

What are the non-nucleoside reverse transcriptase inhibitors? A/E?

Answer 19

Nevirapine (rash)

Efavirenz (nightmares but gives you buzz so give HS)

Question 20

What are the 4 main protease inhibitors?

Answer 20

• Lopinavir / Ritonavir
• Atazanavir * Cobi
• Tipranavir
• Darunavir * Cobi

Question 21

Protease inhibitors are associated with what?

Answer 21

Hyperglycemia and hyperlipidemia

Question 22

Lopinavir / Ritonavir is _____

Answer 22

BOOSTED (also called Kaletra)

Question 23

Atazanavir a/e?

Answer 23

increases bilirubin and turns patient yellow but NOT nephrotoxic

Question 24

What is special about atazanavir?

Answer 24

Acid requiring drug (no PPIs, H2RAs and antacids require spacing)

Question 25

What drugs are always boosted?

Answer 25

Tipranavir

Darunavir

Question 26

What drug is the fusion inhibitor? how does it work?

Answer 26

Enfuvirtide

CD4 receptor blocker

Injectable so LAST LINE (needles = bad)

Question 27

What is the R5 coreceptor blocker?

Answer 27

Maraviroc

Risk of selecting for X4 so last effort

Question 28

How are the integrase inhibitors as a class?

Answer 28

Clean, few drug interactions

EXPENSIVE!

Question 29

What are the integrates inhibitors/

Answer 29

• Raltegravir

- Elvitegravir

Question 30

What is Cobicistat?

Answer 30

CP450 inhibitor

Question 31

What are the 3 antiretroviral combinations?

Answer 31

1) 2 NRTI + 1 NNRTI
2) 2 NRTI + 1 Protease Inhibitor
3) 2 NRTI + 1 Integrase Inhibitor

Question 32

What is boosting? what are the examples?

Answer 32

add CP450 inhibitor (goes from TID to QD)

• Low dose ritonavir
• Cobicistat (preferred agent, does not contribute to resistance)

Question 33

What HIV drugs cover Hep C?

Answer 33

NONE

Question 34

What HIV drugs cover Hep B?

Answer 34

• Lamivudine
• Emtricitabine
• Tenofovir (and TAF)

Question 35

Finish the STR drugs

Answer 35

rr