Lecture 9: Anti-Viral Agents II (for HIV Infection) Flashcards
True or False: The currently available anti-retroviral agents that can treat HIV infections have been designed to target the HIV-2 life cycle
False - HIV-1
Which three enzymes are found within the nuclear capsid of the HIV molecule?
- Protease
- Integrase
- Reverse Transcriptase
True or False: Infection by HIV is treated with combination of anti-retroviral drugs
True
True or False: Nucleoside monophosphate, nucleoside diphosphate, and nucleoside triphosphate are all nucleotides
True
____ 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
C. Zidovudine
True or False: Zidovudine has significant Synovial Fluid penetration
False - it has significant CSF penetration
What are the three main AE associated with Zidovudine?
- GI
- CNS
- Hematologic
___ 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
D. Lamivudine
True or False: Lamivudine is also active against Hep B virus
True
True or False: Both Lamivudine and Zidovudine have GI, CNS, and hematological adverse effects
True
____ 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
E. Tenofovir
True or False: The AE’s associated with Tenofovir, a nucleotide reverse transcriptase inhibitor, include: CNS, GI, and Renal
True
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
D. Reverse Transcription
____ 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
A. Efavirenz
Both Efavirenz and protease inhibitors have AE, which include: CNS, GI, and ____
Endocrine/metabolic (lipid metabolism)
All protease inhibitors are metabolized and inhibitors of hepatic ___
P450
____ is an inhibitor of HIV protease, exclusively metabolized by liver cytochrome P450 and has AE that include: CNS, GI, and ___
Atazanavir Sulfate; endocrine/metabolic (increased serum cholesterol; lipodystrophy)
____ 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
Atazanavir Sulfate
____ 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
B. Enfuvirtide
True or False: AE’s associated with entry and fusion inhibitors (like Enfuvirtide) include: CNS, GI, and Derm
True
____ 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
D. Maraviroc
True or False: CCR5 antagonism prevents interactions between human CC45 coreceptor and GP120 subunit of the viral envelope glycoprotein
True
True or False: Maraviroc, a chemokine receptor CCR5 antagonist, is metabolized by CYP P450 and has AE that include: GI, Derm, Infections, and Endocrine
False - Maraviroc, a chemokine receptor CCR5 antagonist, is metabolized by CYP P450 and has AE that include: GI, Derm, Infections, and RESPIRATORY!!
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
E. Raltegravir
True or False: Raltegravir has CNS, Endocrine/Metabolic, as well as Hepatic AE’s associated with it
True
