Antiretroviral drugs Flashcards

1
Q

what are the NTRIs?

A
zidovudine 
lamivudine 
abacavir 
tenofovir disoproxil 
emtricitabine
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2
Q

what are the NNTRIs?

A

nevirapine

efavirenz

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3
Q

what is the fusion inhibitor agent?

A

enfuvirtide

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4
Q

what are the protease inhibitor agents?

A

ritonavir
atazanavir
darunavir

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5
Q

what is the coreceptor antagonist agent?

A

maraviroc

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6
Q

what are the integrase inhibitor agents?

A

raltegravir
elvitegravir
dolutegravir

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7
Q

what is the target of NRTIs?

A

reverse transcriptase

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8
Q

what are the adverse effects common to the NTRIs?

A

lactic acidosis
fatty liver
lipodystrophy

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9
Q

what is the MOA of the NTRIs?

A

mimic nucleotides to inhibit nt binding to catalytic site and cause chain termination when incorporated into DNA

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10
Q

abacavir is what class of drug?

A

NTRI

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11
Q

which drug should be avoided in HIV patients with opiate substance abuse? why?

A

abacavir

lowers effectiveness of methadone

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12
Q

abacavir is an analogue of what compound?

A

guanosine

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13
Q

lamivudine is an analogue of what compound?

A

cytosine

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14
Q

what are the therapeutic indications for lamivudine?

A

naive and experienced HIV patients
HBV
safe for pregnant women and neonates

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15
Q

what are the therapeutic indications for abacavir?

A

naive and experienced HIV patients

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16
Q

emtricitabine is an analogue of what compound?

A

fluorinated analogue of lamivudine

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17
Q

lamivudine is what class of drug?

A

NTRI

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18
Q

emtricitabine is what class of drug?

A

NTRI

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19
Q

emtricitabine is contraindicated in what populations?

A

pregnant women
young children
renal or hepatic failure

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20
Q

tenofovir is what class of drug?

A

NTRI

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21
Q

tenofovir is an analogue of what compound?

A

adenosine

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22
Q

which NTRI is suggested to reduce transmission?

A

tenofovir

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23
Q

zidovudine is what class of drug?

A

NTRI

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24
Q

zidovudine is an analogue of what compound?

A

deoxythymidine

25
what are the adverse effects of zidovudine?
myelosuppression | fatigue, malaise, nausea
26
what is the main therapeutic indication for zidovudine?
post exposure prophylaxis
27
what is the target for the NNTRIs?
reverse transcriptase (does not bind to active site)
28
do NNTRIs require phosphorylation for activation?
no
29
what is the important adverse effect of NNTRIs?
drug-drug interactions due to effects on cyp450 enzymes
30
efavirenz is what class of drug?
NNTRI
31
nevirapine is what class of drug?
NNTRI
32
cross resistance can occur between nevirapine and what other drug?
efavirenz
33
what NNTRI can be used to prevent vertical transmission?
nevirapine
34
what is the MOA for the protease inhibitors?
mimic peptide targets for protease
35
what is the important adverse effect for the protease inhibitors?
drug interactions due to alteration of cyp450 enzymes
36
which antiretroviral drug classes alter activity of cyp450 enzymes?
NNTRIs | PIs
37
atazanavir is what class of drug?
PI
38
what drugs should be avoided with atazanavir use?
PPIs
39
ritonavir is what class of drug?
PI
40
what is the main adverse effect of ritonavir?
potent inhibitor of cyp enzymes
41
which antiretroviral drug is used as a low dose booster? why? which class of drug is this?
ritonavir - increased half life of ARV due to cyp effect PI
42
what class of drug is darunavir?
PI
43
which drug is useful in HIV strains that are resistant to multiple PIs?
darunavir
44
coreceptor antagonists bind what protein?
CCR5
45
maraviroc is what class of drug?
coreceptor antagonist
46
what is the therapeutic indication for maraviroc?
therapy experienced patients with predominantly CCR5 tropic virus
47
what must be screened for prior to using coreceptor antagonists?
CCR5 tropism
48
enfuvirtide is what class of drug?
FI
49
which ARV drugs is injected?
enfuvirtide
50
what are the adverse effects of enfuvirtide?
painful nodule at injection site | insomnia, eosinophilia, allergy
51
which situation is indicated for enfuvirtide?
treatment experienced patients with evidence of HIV replication even with ARV treatment
52
raltegravir is what class of drug?
integrase inhibitor
53
elvitegravir is what class of drug?
integrase inhibitor
54
what drugs must be administered with elvitegravir? why?
cobicistat ritonavir inhibit cyp enzymes to increase afficacy
55
dolutegravir is what class of drug?
integrase inhibitor
56
which integrase inhibitor retains activity against strains that are resistance to both raltegravir and elvitegravir?
dolutegravir
57
who is ARV therapy recommended for?
all HIV patients regardless of CD4 count perinatal and heterosexual most important
58
what is the preferred combination ARV therapy?
1 PI (ritonavir boosted) plus 2 NTRIs -OR- 1 II plus 2 NTRIs