Anti-HIV agents

Question 1

What is the name of a drug that inhibits the HIV virus from fusing to the host cell?

Answer 1

Entfuvirtide

Question 2

What are the stages of HIV replication?

Answer 2

• attaches to host cell
• fuses to cell membrane
• RT converts its RNA to DNA
• Integrase is released to integrate viral DNA with DNA of host
• Virus uses host cell machinery to create long protein chains
• proteins cleaved by protease
• new virions are produced and bud off the host cell

Question 3

What are the three major classes of anti-HIV drugs?

Answer 3

nucleoside reverse transcriptase inhibitors (NRTI)
non nucleoside reverse transcriptase inhibitors (NNRTI)
protease inhibitors

Question 4

Give a NRTI and how does it work?

Answer 4

AZT (azidothymidine), prodrug converted to the active triphosphate by thymidine kinase
- For HIV 1 and 2 (given with another NRTI)

Question 5

how do NNRTI act differently from NRTI?

Answer 5

NNRTI act at an allosteric site (remote from AS) so theres no competition for nucleosides and so doesn’t require phosphorylation
-Only for HIV 1

Question 6

Which NNRTI is crushed and used recreationally in Africa?

Answer 6

Efavirenz

Question 7

What drug were HIV protease inhibitors derived from?

Answer 7

ACE inhibitors (for hypertension)

Question 8

What inhibitors do protease inhibitors act as?

Answer 8

transition state inhibitors

Question 9

Give an example of a protease inhibitor?

Answer 9

Saquinavir (Roche) - for HIV 1 and 2

Question 10

What is the difference between ritonavir and saquinavir?

Answer 10

Ritonivir is more hydrophobic but has better bioavailability

Question 11

How is indinavir (another protease inhibitor) administered?

Answer 11

as its sulphate