Lecture 9: Anti-Viral Agents II (for HIV Infection)

Question 1

True or False: The currently available anti-retroviral agents that can treat HIV infections have been designed to target the HIV-2 life cycle

Answer 1

False - HIV-1

Question 2

Which three enzymes are found within the nuclear capsid of the HIV molecule?

Answer 2

1. Protease
2. Integrase
3. Reverse Transcriptase

Question 3

True or False: Infection by HIV is treated with combination of anti-retroviral drugs

Answer 3

True

Question 4

True or False: Nucleoside monophosphate, nucleoside diphosphate, and nucleoside triphosphate are all nucleotides

Answer 4

True

Question 5

____ is a nucleoside that inhibits reverse transcriptase. Because it lacks a 3’ OH group, incorporation into viral DNA leads to chain termination + inhibition of viral replication

A. Emtricitabine
B. Abacavir
C. Zidovudine

Answer 5

C. Zidovudine

Question 6

True or False: Zidovudine has significant Synovial Fluid penetration

Answer 6

False - it has significant CSF penetration

Question 7

What are the three main AE associated with Zidovudine?

Answer 7

1. GI
2. CNS
3. Hematologic

Question 8

___ is a nucleoside that contains sulfur and inhibits reverse transcriptase. Incorporation into viral DNA leads to chain termination + inhibition of viral replication.
A. Emtricitabine
B. Abacavir
C. Zidovudine
D. Lamivudine

Answer 8

D. Lamivudine

Question 9

True or False: Lamivudine is also active against Hep B virus

Answer 9

True

Question 10

True or False: Both Lamivudine and Zidovudine have GI, CNS, and hematological adverse effects

Answer 10

True

Question 11

____ is a nucleoTIDE (phosphorylated nucleoside) reverse transcriptase inhibitor that inhibits HIV replication and is active against the Hep B virus
A. Emtricitabine
B. Abacavir
C. Zidovudine
D. Lamivudine
E. Tenofovir

Answer 11

E. Tenofovir

Question 12

True or False: The AE’s associated with Tenofovir, a nucleotide reverse transcriptase inhibitor, include: CNS, GI, and Renal

Answer 12

True

Question 13

Both nucleoside RT inhibitors and nonnucleoside RT inhibitors target which phase of the HIV-1 cell cycle?
A. Integration
B. Budding and Release
C. Attachment and Fusion
D. Reverse Transcription

Answer 13

D. Reverse Transcription

Question 14

____ is a non-nucleoside reverse transcriptase inhibitor that is a substrate for cytochrome P450 isoforms and can treat HIV-1 infections
A. Efavirenz
B. Emtricitabine
C. Abacavir
D. Zidovudine
E. Lamivudine
F. Tenofovir

Answer 14

A. Efavirenz

Question 15

Both Efavirenz and protease inhibitors have AE, which include: CNS, GI, and ____

Answer 15

Endocrine/metabolic (lipid metabolism)

Question 16

All protease inhibitors are metabolized and inhibitors of hepatic ___

Answer 16

P450

Question 17

____ is an inhibitor of HIV protease, exclusively metabolized by liver cytochrome P450 and has AE that include: CNS, GI, and ___

Answer 17

Atazanavir Sulfate; endocrine/metabolic (increased serum cholesterol; lipodystrophy)

Question 18

____ binds to site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors to individual functional proteins required for infectious HIV

Answer 18

Atazanavir Sulfate

Question 19

____ is a entry and fusion inhibitor of HIV that binds to the GP41 subunit of the viral envelop glycoprotein and inhibits the fusion of HIV-1 virus with CD4 cells
A. Atazanavir Sulfate
B. Enfuvirtide
C. Darunavir

Answer 19

B. Enfuvirtide

Question 20

True or False: AE’s associated with entry and fusion inhibitors (like Enfuvirtide) include: CNS, GI, and Derm

Answer 20

True

Question 21

____ is a chemokine receptor CCR5 antagonist of HIV that selectively and reversibly binds to the CCR5 co-receptors located on human CD4 cells
A. Atazanavir Sulfate
B. Enfuvirtide
C. Darunavir
D. Maraviroc

Answer 21

D. Maraviroc

Question 22

True or False: CCR5 antagonism prevents interactions between human CC45 coreceptor and GP120 subunit of the viral envelope glycoprotein

Answer 22

True

Question 23

True or False: Maraviroc, a chemokine receptor CCR5 antagonist, is metabolized by CYP P450 and has AE that include: GI, Derm, Infections, and Endocrine

Answer 23

False - Maraviroc, a chemokine receptor CCR5 antagonist, is metabolized by CYP P450 and has AE that include: GI, Derm, Infections, and RESPIRATORY!!

Question 24

The viral cDNA strand made by RT enzyme is processed and inserted into the human genome by HIV-1 Integrase enzyme. _____ inhibits activity of integrase enzyme.
A. Atazanavir Sulfate
B. Enfuvirtide
C. Darunavir
D. Maraviroc
E. Raltegravir

Answer 24

E. Raltegravir

Question 25

True or False: Raltegravir has CNS, Endocrine/Metabolic, as well as Hepatic AE’s associated with it

Answer 25

True