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IBI Test 4 > B3.071 - HIV Antivirals > Flashcards

B3.071 - HIV Antivirals Flashcards

1
Q

what are HIV life cycle drug targets for intervention

A

Binding and fusion
Reverse transcriptase
Integrase
HIV protease

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2
Q

what does integrase do

A

clips host cell DNA strand and inserts viral genome

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3
Q

what do early stage targets do

A

prevent infection of new cells

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4
Q

what is a limitation of early stage targets

A

they are “one time” targets

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5
Q

what do late target drugs do

A

prevent production of mature infectious virus, spread of infection in pt and transmission

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6
Q

what drug inhibits binding

A

maraviroc

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7
Q

what drug inhibits fusion

A

Enfuvirtide

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8
Q

what drugs inhibit integrase

A

Raltegravir
Dolutegravir
Elvitegravir

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9
Q

what drugs are nucleoside RT inhibitors

A 
Zidovudine (AZT)
Abacavir
Tenofovir disoproxil
Tenofovir alafenamide
Lamivudine
Emtricitabine
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10
Q

what are the NNRTIs

A 
Nevirapine
Efavirenz
Rilpivirine
Etravirine
Delavirdine
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11
Q

what are metabolism inhbititors

A

Cobicistat

Ritonavir (also a PI, not clinically used alone)

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12
Q

what are the protease inhibitors

A 
Darunavir
Atazanavir
Lopinavir
Nelfinavir
Fosamprenavir
Tipranivir
Indinavir
Saquinavir
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13
Q

what does maraviroc do

A

chemokine receptor CCR5 antagonist, prevents CCR5:gp120 interaction

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14
Q

what is a tropism assay

A

test to see if virus uses CCR5 or CXCR4, need to know before giving drug

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15
Q

how is maraviroc given and how is it metabolized

A

oral;CYP3A4 and MDR1 (pgp) substrate

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16
Q

AEs of maraviroc

A

cough, muscle pain, diarrhea

Possible severe hepatotoxicity may be preceded by systemic allergic response (black box warning)

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17
Q

what is Enfuvirtide and what does it do

A

Fusion Inhibitor

Binds to gp41 of HIV-1 envelope, prevents fusion of viral and host cell membranes

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18
Q

what are AEs of Enfuvirtide

A

most have injection site rxns, nodules and cysts are really common >80%

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19
Q

how is Enfuvirtide given and what is the half life

A

Subcutaneous, 4 hours

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20
Q

How does Zidovudine work

A

Thymidine analog that is a competitive substrate for/inhibitor of IHV reverse trancriptase
Inhibits initial replicaiton, stable infection of new cells

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21
Q

Zidovudine pharmacokinetics

A

well absorbed from GI, widely distributed including CNS (~60% of serum level), rapidly metabolized and excreted

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22
Q

half life of zidovudine

A

1-3 hours in plasma, intracellularly 3-7 hours

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23
Q

what is zidovudine used for

A

reduce mother to newborn transmission

Fixed dose combination with lamivudine

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24
Q

how does resistance to zidovudine arise

A

mutations in RT

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25
Q

what are AEs of zidovudine

A

common
Bone marrow depression
CNS - headaches, agitation, insomnia
Toxicity enhanced by drugs that compete for glucuronidation

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26
Q

what does abacavir do

A

Guanosine analog and chain terminator

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27
Q

resistance to abacavir

A

develops slowly, requires 2-3 concomitant mutations

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28
Q

how is abacavir metabolized

A

alcohol dehydrogenase

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29
Q

AEs of abacavir

A

skin rash, hypersensitivity, can be fatal

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30
Q

what do you need to do before administering abacavir and why

A

HLA testing

HLA*B5701 allele is predictive marker, but ~50% do no react

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31
Q

tenofovir disoproxil and alafenamide what is it and how does it work

A

after absorption its hydrolized to Acyclic nucleoside phosphonate, a chain terminator. NRTI

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32
Q

What is the difference between tenofovir disoproxil and alafenamide

A

alafenamide has less renal toxicity and bone density loss compared to disoproxil

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33
Q

describe the dosing of tenofovir

A

once daily, renal excretion

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34
Q

what are AEs of tenofovir in disoproxil/alafenamide

A

GI effects - nausea, vomiting, diarrhea

Disoproxil - acute/cumulateive renal toxicity

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35
Q

what is tenofovir often combined with

A

emtricitabine

36
Q

what can be used as HIV prophylaxis

A

tenofovir

37
Q

what does lamivudine do

A

cytosine analog, inhibits HIV RT and HBV DNA polymerase

38
Q

how is lamivudine administered/excreted

A

oral, excreted unchanged in urine

39
Q

half life of lamivudine

A

serum - 2.5 hr

cellular - 10-15 hr

40
Q

what is the recommended use fo lamivudine (3TC)

A

pregnant women

41
Q

what is emtricitabine (FTC)

A

fluorinated analog of lamivudine

42
Q

how is embtricitabine administered

A

fixed dose combo with tenovir, once daily dosing

43
Q

AEs of emtricitabine

A

headaches, nausea, rash

44
Q

what does nevirapine do

A

first generation oral NNRTI

non competitive RT inhibitors, binds near but not in active site

45
Q

what is nevirapine used for

A

rapid resistance so only approved for combination with nucleoside analogs

46
Q

what is the exception for nevirapine being used only in combination

A

one dose to mother and neonate

47
Q

what are AEs of nevirapine

A

skin rash, can be severe
hepatotoxicity
excellent substrate for CYP3A

48
Q

what does efavirenz do

A

non competitive RT inhibitors, binds near but not in active site

49
Q

describe the half life of efavirenz

A

40-60 hr half life; once daily dosing

Bioavailability 45%

50
Q

how should patients take efavirenz

A

on a empty stomach bc while bioavailability is increased by fat it may increase toxicity

51
Q

AEs of efavirenz

A

inducer and inhibitor of CYP3A4 so drug drug interactions

CNS effects, dizziness, drowsiness, headache, nightmares

52
Q

why is efavirenz bumped to second line for use

A

CNS effects can be severe

53
Q

what is raltegravir

A

INSTI

54
Q

how is raltegravir taken

A

orally, not with cations or buffered drugs, twice daily

55
Q

how is raltegravir metabolized

A

by UGT1A1

56
Q

adverse effects of raltegravir

A

diarrhea, nausea, headache, dizziness, metabolic effects

57
Q

how is dolutegravir administered

A

oral, not with cations or buffered drugs

58
Q

how does dolutegravir work

A

integrase inhibitor

59
Q

half life of dolutegravir and how its eliminated

A

14 hour half life by glucuronidation (UGT1A1)

60
Q

AEs of dolutegravir

A

insomnia, headache, hypersensitivity

61
Q

how do protease inhibitors work

A

HIV proteins must be translated as polyproteins, they have to be cleaved to yield active individual proteins. These drugs prevent mature viral particle production

62
Q

HIV protease is what type of protease

A

aspartyl protease

63
Q

AEs of protease inhibitors

A

diarrhea, nausea, lipodystrophy, insulin resistance

64
Q

saquinovir downsides

A

first HIV protease inhibitor

Extensive first pass effect and many drug drug interactions (CYP3A4)

65
Q

indinavir is metabolized by

A

CYP3A4

66
Q

AEs of indinavir

A

hyperbilirubinemia, nephrolthiasis* (crystallizes in urine)

67
Q

ritonavir metabolized by what

A

CYP3A4 and some 2D6

68
Q

what are AEs of Ritonavir

A

potent CYP3A4 inhibitor

initial nausea, vomiting, diarrhea, GI, parathesias, headache

69
Q

darunavir is often combined with what

A

Ritonavir

70
Q

what does the ritonavir do in the darunavir combo

A

blocks CYP3A protecting darunavir and allowing its effect to persist longer

71
Q

AEs of darunavir

A

GI, headache, rash

72
Q

what other drug may be combined with darunavir

A

cobicistat

73
Q

what does atazanavir do

A

protease inhibitor

74
Q

how is atazanavir dosed and metabolized

A

once daily dosing, enters CNS, biliary excretion

75
Q

what enzymes does Atazanavir inbibit

A

UGT1A1, CYP3A4, CYP2C9

76
Q

AEs of atazanavir

A

diarrhea, nausea, vomiting, headache

hyerbilirubinemia

77
Q

what is atazanavir not associated with AEwise that is important

A

No dyslipidemia, fat redistribution, metabolic syndrome

78
Q

cobicistat is used for

A

not an antiviral, used in fixed combinations for boosting of accompanied antiviral drug

79
Q

what does cobicistat inhibit and what does that do

A

CYP3A, decreases first pass clearance of protease inhibitors, integrase inhibitors

80
Q

when should you not use cobicistat

A

if creatinine clearance <30

81
Q

what does ART stand for

A

Anti-retroviral therapy

82
Q

why do all ART regimens include RTIs

A

to prevent resistance, preventing mutations from sloppy reverse transcriptase

83
Q

which drugs are substrates for CYP3A4

A

delavirdine, efavirenz, nevirapine, all protease inbhibitors

84
Q

what drugs are inducers of CYP3A4 in other tissues

A

efavirenz, nevirapine, amprenavir

85
Q

what drugs are inhibitors of CYP3A4

A

delavirdine, efavirenz, all protease inhibitors especially ritanovir

IBI Test 4 (12 decks)

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