W06_05 HIV Therapeutics Flashcards
when to start HIV ART?
for sure if CD4 < 350;
sometimes is CD4 < 500
why initiate ART earlier for HIV?
morbidity/mortality benefit;
decrease risk of transmission;
decrease HIV-associated inflammation
what are some absolute indications to start HIV ART?
opportunistic infection (e.g. thrush); malignancy; pregnancy; HIV-associated nephropathy; HIV-associated thrombocytopenia; HepB patients
what’s an “undetectable” viral load in HIV?
<40 copies/mL
what’s the mutation rate of the HIV?
~1 per day (1/2000 bp error, in a 9749 nucleoside genome)
what are nucleoside reverse transcriptase inhibitors?
nucleoside analogues that lack a 3’ terminal hydroxy group
what is abacavir?
nucleoside analogue for HIV
what is tenofovir disoproxil fumarate (TDF)?
nucleoside analogue for HIV and HepB
what’s TDF/FTC?
a combination NRTI
what’s ABC/3TC
a combination NRTI
MoA for non-nucleoside reverse transcriptase inhibitors?
bind at non-active side and induce conformational changes to prevent the enzyme function (noncompetitive)
what’s efavirenz (EFV)?
NNRTI for HIV
MoA for HIV protease inhibitors?
inhibit the HIV protease from splitting up the gag and pol proteins
what’s ritonavir (RTV)?
protease inhibitor. note this is a “half drug” whose effects are better suited towards blocked CYP3A4
what’s atazanavir (ATV)?
protease inhibitor
what’s darunavir (DRV)?
protease inhibitor
what’s maraviroc?
CCR5 antagonist that prevents HIV viral entry
why aren’t fusion inhibitors used any longer?
they have injection site reactions
what’s elvitegravir?
integrase inhibitor. often given as combination (TDF/FTC/ELV/c)
what’s dolutegravir?
integrase inhibitor
what’s colbicistat?
pharmacologic booster that inhibits 3A4 and is given with integrase inhibitor elvitegravir
what do we have to test for before giving abacavir?
hypersensitivity; HLA*B5701 must be negative
