Medchem of Antivirals

Question 1

Fuzeon treats which virus?

Answer 1

HIV

Question 2

Fuzeon moa

Answer 2

blocks entry to CD4+ cell and binds to viral GP41 to inhibit cellular interaction with HIV1

Question 3

Fuzeon dose

Answer 3

subQ 2x daily

Question 4

Why is Fuzeon not used?

Answer 4

Poor compliance and cost

Question 5

Maraviroc

Answer 5

Selzentry

Question 6

Maraviroc moa

Answer 6

binds CCR5 coreceptor needed for entry by only some strains of HIV-1

Question 7

Maraviroc dosing with potent CYP3A inhibitors

Answer 7

150 mg daily

Question 8

Maraviroc dosing with no potent CYP3A inhibitors or CYP3A inducers

Answer 8

300 mg twice daily

Question 9

Maraviroc dosing with potent CYP3A inducers

Answer 9

600 mg twice daily

Question 10

What are 2 different kinds of inhibitors of reverse transcriptase to treat HIV

Answer 10

nucleoside reverse transcriptase

non-nucleoside reverse transcriptase inhibitors

Question 11

What is structurally different for nucleoside reverse transcriptase inhibitors?

Answer 11

Modified deoxyglucose function, with no 3’ OH group

Phosphorylated by cell kinases that are incorporated in viral DNA by the viral enzyme RT

Question 12

Viral proteins made as one long read through protein then cleaved by protease

Answer 12

Viral protease inhibitors

Question 13

Protease inhibitor drugs end in

Answer 13

-vir

Question 14

NRTIs end in

Answer 14

-dine
-bine
pluse didanosine and abicavir

Question 15

HIV inserts copies of its genome as DNA into host cells genome where it hides out
This “latent” HIV can come back out and become active virus again

Answer 15

integrase inhibitors

Question 16

Prevent viral genome insertion into human CD4 cell

Answer 16

integrase inhibitors

Question 17

integrase inhibitors end in

Answer 17

-gravir

Question 18

2 zinc binding portions mean symmetrical or near symmetrical drugs

Answer 18

NS5A inhibitors in HCV

Question 19

NS5A inhibitors end in

Answer 19

-svir

Question 20

RNA polymerase that replicated viral genome (RNA virus)

Answer 20

NS5B

Question 21

RNA dependent RNA polymerase

Answer 21

NS5B

Question 22

NS5B drugs end in

Answer 22

-buvir

Question 23

Sofosbuvir

Answer 23

Sovaldi

Question 24

Sofosbuvir is the active prodrug of

Answer 24

DFMU monophosphate

Question 25

NS3/NS4B protease and HCV protease inhibitors.

ends in

Answer 25

-previr

Question 26

Why do we not see so much resistance development in bacterial therapy (with rare exceptions) yet we have to cover several sites? `

Answer 26

1. time - HIV/HCV longer term therapy
2. Viral loads are higher so more chance of mutant
3. Viral genome replication more error prone

Question 27

drug combos with >1 MOA are usually

Answer 27

more effective and produce less resistance during therapy