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Year 2 Pharmacology > Antiretroviral drugs > Flashcards

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
Q

what are the adverse effects of zidovudine?

A

myelosuppression

fatigue, malaise, nausea

26
Q

what is the main therapeutic indication for zidovudine?

A

post exposure prophylaxis

27
Q

what is the target for the NNTRIs?

A

reverse transcriptase (does not bind to active site)

28
Q

do NNTRIs require phosphorylation for activation?

A

no

29
Q

what is the important adverse effect of NNTRIs?

A

drug-drug interactions due to effects on cyp450 enzymes

30
Q

efavirenz is what class of drug?

A

NNTRI

31
Q

nevirapine is what class of drug?

A

NNTRI

32
Q

cross resistance can occur between nevirapine and what other drug?

A

efavirenz

33
Q

what NNTRI can be used to prevent vertical transmission?

A

nevirapine

34
Q

what is the MOA for the protease inhibitors?

A

mimic peptide targets for protease

35
Q

what is the important adverse effect for the protease inhibitors?

A

drug interactions due to alteration of cyp450 enzymes

36
Q

which antiretroviral drug classes alter activity of cyp450 enzymes?

A

NNTRIs

PIs

37
Q

atazanavir is what class of drug?

A

PI

38
Q

what drugs should be avoided with atazanavir use?

A

PPIs

39
Q

ritonavir is what class of drug?

A

PI

40
Q

what is the main adverse effect of ritonavir?

A

potent inhibitor of cyp enzymes

41
Q

which antiretroviral drug is used as a low dose booster? why? which class of drug is this?

A

ritonavir - increased half life of ARV due to cyp effect

PI

42
Q

what class of drug is darunavir?

A

PI

43
Q

which drug is useful in HIV strains that are resistant to multiple PIs?

A

darunavir

44
Q

coreceptor antagonists bind what protein?

A

CCR5

45
Q

maraviroc is what class of drug?

A

coreceptor antagonist

46
Q

what is the therapeutic indication for maraviroc?

A

therapy experienced patients with predominantly CCR5 tropic virus

47
Q

what must be screened for prior to using coreceptor antagonists?

A

CCR5 tropism

48
Q

enfuvirtide is what class of drug?

A

FI

49
Q

which ARV drugs is injected?

A

enfuvirtide

50
Q

what are the adverse effects of enfuvirtide?

A

painful nodule at injection site

insomnia, eosinophilia, allergy

51
Q

which situation is indicated for enfuvirtide?

A

treatment experienced patients with evidence of HIV replication even with ARV treatment

52
Q

raltegravir is what class of drug?

A

integrase inhibitor

53
Q

elvitegravir is what class of drug?

A

integrase inhibitor

54
Q

what drugs must be administered with elvitegravir? why?

A

cobicistat
ritonavir

inhibit cyp enzymes to increase afficacy

55
Q

dolutegravir is what class of drug?

A

integrase inhibitor

56
Q

which integrase inhibitor retains activity against strains that are resistance to both raltegravir and elvitegravir?

A

dolutegravir

57
Q

who is ARV therapy recommended for?

A

all HIV patients regardless of CD4 count

perinatal and heterosexual most important

58
Q

what is the preferred combination ARV therapy?

A

1 PI (ritonavir boosted) plus 2 NTRIs

-OR-

1 II plus 2 NTRIs

Year 2 Pharmacology (70 decks)

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