Anti-Hepatitis and HIV

Question 1

Lamivudine

Answer 1

Characteristics:
- Cellular Kinase phosphorylates x3
- Treats HBV, HIV

MOA:
- Lamivudine Triphosphate inhibits reverse transcription of HBV
–> Inhibits Viral DNA Polymerase

Question 2

Adefovir

Answer 2

Characteristics:
- Adefovir Dipivoxil is converted into Adefovir
- Cellular Kinase phosphorylates x2
- Treats HBV (HIV, HSV, CMV)

MOA:
- Adefovir-PPP inhibits RT HBV
–> Inhibits vDNA polymerase

Question 3

Tenofovir

Answer 3

Characteristics:
- dAMP analogue
- Cellular Kinase phosphorylates x2
- Treats Chronic HBV (and HIV)
- Good for Lamivudine Resistant HBV

MOA:
- Inhibits protein priming
- Inhibits DNA synthesis

Question 4

Entecavir

Answer 4

Characteristics:
- dGMP analogue
- Cellular Kinase phosphorylates 32
- Treats Chronic HBV

MOA:
- Inhibits HBV DNA Polymerase (RT, +Strand Synthesis, Base Priming)

Question 5

Interferons

Answer 5

1. Inhibit Transcription
2. Inhibit Translation
3. Inhibit Post-Translational Processing
4. Inhibit Virus Maturation
5. Inhibit Virus Release

Chronic HBV or Acute HCV
- IFN

Chronic HCV:
IFN + Ribavirin

Question 6

Ribavirin

Answer 6

Characteristics
- Phosphorylated by Host Cell

MOA:
- Triphosphate: Inhibits RNA Polymerase
–> Interferes with viral mRNA elongation
- Monophosphate: Inhibits IMP Dehydrogenase
–> No conversion IMP to XMP which is needed for GTP synthesis

Question 7

Grazoprevir

Answer 7

HIV

S3/4A Protease Inhibitor
- Prevents cleavage of virus

Question 8

Simeprevir

Answer 8

HIV

NS3/4A Protease Inhibitor
- Prevents cleavage of virus

Question 9

Sofosbuvir

Answer 9

HIV

RNA Polymerase Inhibitor
- Phosphorylate x3
- Acts as chain terminator when incorporated into HCV RNA by NS5B

Question 10

Maraviroc

Answer 10

HIV

Entry Inhibitor

Binds to hosts C-C Chemokine Receptor 5 (CCR5) preventing HIV from binding
- Targets CCR5-Torpic-HIV-1

Question 11

Enfuvirtide

Answer 11

HIV

Entry Inhibitor (Fusion Inhibitor)
- Binds to gp41 glycoprotein preventing HIV from binding and fusing with cellular membrane

Question 12

Abacavir

Answer 12

HIV

MOA:
- Nucleoside Reverse Transcriptase Inhibitor
1. Intracellular Phosphorylation by cellular kinase to triphosphate
2. NRTi get incorporated into vDNA chain leading to Chain Termination

Question 13

Delaviridine

Answer 13

HIV

MOA:
- Non-Nucleoside Reverse Transcriptase Inhibitor (No Phosphorylation)
–> Allosteric Modulator of RT

Question 14

Atazanavir

Answer 14

HIV

MOA:
- Protease Inhibitor (No Phosphorylation)
–> Inhibit HIV protease preventing maturation of HIV

Question 15

Dolutegravir

Answer 15

HIV

MOA:
- Integrase strand transfer inhibitor
–> Prevent integration of virus into host chromosomes (Nucleus)