B3-071B Anti HIV Chemotherapy Flashcards
mechanism: Maraviroc
fusion inhibitor, prevents CCR5 and gp120 binding
before administering Maraviroc, do a ______ to eval for CCR5 or CXCR4
tropism assay
Side effect: maraviroc
severe hepatotoxicity
is maraviroc common?
no
mechanism: enfuvirtide
fusion inhibitor; inhibits gp41 and prevents fusion of membranes
blocks infection of new cells
enfuvirtide
limited to patients who no longer respond to other regimens
enfuvirtide
mechanism: zidovudine
thymidine analog
NRTIs ________ inhibit reverse transcriptase
competitively
Zidovudine exhibits __________, due to specificity for HIV RT
selective toxicity
Zidovudine can reduce
mother-to-newborn transmission
mechanism: abacavir
guanosine analog
abacavir is metabolized
by alcohol dehydrogenase (EtOH interaction)
resistance to abacavir develops _____
slowly
Abacavir can cause a Type _____ hypersensitivity
I
abacavir hypersensitivity is caused by the _______ allele
HLA-B5701
**testing is done on all patients prior to administration, but only 50% react
tenofovir is often combined with
emtricitabine
tenofovir can cause
renal toxicity (disoproxil)
tenofovir and emtricitabine are used for
HIV pre-exposure prophylaxis
post exposure prophylaxis
tenofovir and emtricitabine + integrase inhibitor of protease inhibitor
lamivudine mechanism
cytosine analog
mechanism: emtricitabine
fluorinated analog of lamivudine
NNRTIs ________ inhibit reverse transcriptase
non-competitively (allosteric inhibition)
nevirapine is an ______ of CYP3A
inducer
efavirenz is an ________ of CYP34A
inducer and inhibitor (drug-drug interactions)
side effects: efavirenz
dizziness, drowsiness, nightmares, headaches, confusion, amnesia
why is Efavirenz considered second line?
CNS side effects are severe
Doravirine is metabolized by
CYP34A
intergrase inhibitors provide a ______ viral target
unique
raltegravir is an
intergrase inhibitor
dolutegravir is eleminated by
glucuronidation
minor role for CYP34A
bictegravir is only available in
a fixed combination pill with emtricitabine and tenofovir
bictegravir aka
Biktarvy
cabotegravir must be
dosed with rilpirivine
protease inhibitors inhibit _____ protease
aspartyl
adverse effects of protease inhibitors
diarrhea
nausea
lipodystrophy
insulin resistance
Saquinavir
1st HIV protease inhibitor
indinavir adverse effect
nephrolithiasis
ritonavir
potent CYP34A inhibitor
**boosts concentration of other proteases
darunavir/ritonavir is administered with a
subtherapeutic dose of ritonavir, inhibits CYP34A
cobicistat
no antiviral activity, CYP3A inhibitor
**boosts concentration of other proteases
atazanavir
is not associated with typical protease inhibitor side effects
ART usually consists of
3-4 anti retroviral drugs
2 NRTIs + protease inhibitor
CYP3A4 substrates
delavirdine, efavirenz, nevirapine, all protease inhibitors
CYP34A inducers
efavirenz, nevirapine, amprenavir
CYP34A inhibitors
delavirdine, efavirenz, all protease inhibitors
unique targets of ART
reverse transcriptase
integrase
HIV protease