HIV pharmacology Flashcards
What is the brief structure of the HIV? What antigen is present on the surface? What 3 enzymes are present?
Strands of RNA surrounded by capsid (peptide-protein membrane. P24 antigen)
- reverse transcriptase
- integrase
- protease
What are the potential targets that HIV attacks? How does HIV gain entry to the cell?
binds to CD4 plus cytokine receptor
can be macrophage or CD4 T helper cell
What happens to enable the release of the RNA? What does reverse transcriptase do?
- uncoating of capsid
- puts base pairs on RNA to form viral DNA
what does integrase do?
chops up host DNA and inserts viral DNA into host DNA
What happens after integrase step, and what do the proteases do?
host makes new virus particles
after transcription, protease chops up precursor proteins and leads to release
Distinguish between Nucleotide and Nucleoside
Nuceloside – has base and sugar, but no phosphate. Nucleotide has the phosphate
How do NRTIs work?
nucleoside reverse transcriptase inhibitors
Zidovudine phosphorylated by intracellular thymidine kinase to form active zidovudine 5-triphosphate.
Zidovudine 5-triphosphate terminates viral DNA chain elongation via competition with TMP FOR REVERSE TRANSCRIPTASE and incorporation in to DNA.
can become resistant
How do Non-NRTIs work?
binds adjacent to active site of reverse transcriptase, leading to conformation change to inhibit.
act on different site to NRTIs
How do protease inhibitors work?
inhibits proteases (chopping one), allows inactive parts to be made
How do fusion inhibitors work?
prevents binding to host cell
expensive
How do integrase inhibitors work?
prevents integration of viral DNA into host DNA
What is the plan with HAART?
highly active anti-retroviral therapy 2 NRTIs And either Non-NRTI Or Protease inhibitor Or Integrase inhibitor
What kinds of drugs are included in Atripla
2 NRTIs and non-NRTI
