HIV pharmacology Flashcards
Mode of action of Nucleoside Reverse Transcriptase Inhibitors on HIV (NRTIs)
Terminates viral DNA chain elongation via competition with TMP and incorporation in to DNA
What is resistance to Nucleoside Reverse Transcriptase Inhibitors associated with
Via mutations in reverse transcriptase codon
Mode of action of Non-nucleoside Reverse Transcriptase Inhibitors
Diffuses into cell and binds adjacent to active site of reverse transcriptase, leading to conformation change to inhibit
(has a different site from NRTIs)
Mode of action of Protease Inhibitors
[They are a peptidomimetic (mimic peptides)]
–>HIV viral protease is essential for infectivity as it reassembles the HIV particles
–>Cleaves viral polyprotein into
Reverse transcriptase
Integrase
Protease
Structural proteins
Inhibitors bind to active site of HIV protease so there can’t be new viral material assembled
What are resistance to Protease Inhibitors associated with
Mutations in the protease gene
Mode of action of Fusion Inhibitors
Similar to segment of viral glycoprotein gp41
Prevents binding of virus to host cell
Given IV
Mode of action of Integrase Inhibitors
Integrase: HIV enzyme which leads to incorporation of DNA into human chromosome
What does Highly Active AntiRetroviral Therapy consist of
2 Nucleoside transcriptase inhibitors
AND
Either: -Non-nucleoside transcriptase inhibitor or -Protease inhibitor or -Integrase inhibitor
Whats the drawback of Fusion Inhibitors
Fail to respond to other retrovirals
What are the drawbacks of HIV drugs
Significant number of adverse effects
Depends on agent: depression, altered lipid levels, buffalo-hump
What are many of the interactions of HIV drugs part of
Many vi CytP450
What does an ‘Undetectable’ HIV test mean for patient
Undetectable=Untransmittable
If patient is undetectable for 6 months then HIV is untransmittable
