HIV tx Flashcards

1
Q

initial HIV tx regimen in naive pts

A

2NRTIs + INSTI

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2
Q

why multiple drugs for tx?

A

resistance develops quickly with a single agent so use 2-3

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3
Q

NRTI meaning

A

nucleoside/nucleotide reverse transcriptase inhibitors

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4
Q

NNRTI

A

non-nucleoside reverse transcriptase inhibitors

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5
Q

PIs

A

protease inhibitors

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6
Q

INSTIs

A

integrase strand transfer inhibitors

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7
Q

NRTIs MOA

A

inhibits conversion of HIV RNA to DNA by blocking the function of reverse transcriptase at active site and terminates DNA chain

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8
Q

TDF

A

tenofovir disoproxil fumarate

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9
Q

TAF

A

tenofovir alafenamide

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10
Q

NRTI associated inhibition of mitochondrial DNA function effects

A

lactic acidosis
hepatic steatosis
peripheral neuropathy
lipodystrophy

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11
Q

lamivudine and emtricitabine use

A

interchangeable but never used together

backbone of nearly all current antiretroviral tx regimens

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12
Q

which rx are also active against HBV?

A

lamivudine and emtricitabine (NRTIs)

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13
Q

lamivudine and emtricitabine side effects

A

most well tolerated NRTIs

rare headache, nausea, fatigue

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14
Q

abacavir indication

A

first line in combo with lamivudine and dolutegravir

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15
Q

triumeq

A

combo drug of abacavir, lamivudine and dolutegravir

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16
Q

abacavir side effects

A

hypersensitivity syndrome

  • fever, abdominal pain, rash
  • associated with HLA-B*5701 allele (need genetic testing)

cardio risk

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17
Q

TDF side effects

A

tenofovir disoproxil fumarate
decreased bone mineral density
decreased CrCl
Fanconi syndrome

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18
Q

TAF side effects

A

less than TDF, safer
greater antiviral activity lower dosing needed

adjust for CrCl

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19
Q

what is tenofovir

A

nucleotide adenosine 5imonophosphate derivative

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20
Q

truvada

A

TDF + emtricitabine (2 NRTIs)

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21
Q

Descovy

A

TAF + emtricitabine (2 NRTIs)

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22
Q

higher risk NRTIs used for resistant forms

A

didanosine
stavudine
zidovudine

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23
Q

NNRTIs MOA

A

inhibits conversion of HIV RNA to DNA by blocking the function of reverse transcriptase (binds at different site than NRTIs)

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24
Q

NNRTI downsides and effects

A
low barrier of resistance
drug interactions
hypersensitivity rxns
neuro/psych effects
hepatic clearance
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25
Q

efavirenz

A

NNRTI that is not very common in US

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26
Q

efavirenz side effects

A

neuro: vivid dream, insomnia, hallucinations

teratogenic

hepatotoxic

rash

drug interactions because it is a CYP3A4 inducer/inhibitor

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27
Q

first generation NNRTIs (some tx failure)

A

nevirapine
efavirenz
delaviridine

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28
Q

2nd gen NNRTIs (better)

A

etravirine
doravirine
rilpivirine

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29
Q

should you take efavirenz with food?

A

NO on an empty stomach because high fat meal increases bioavailability

30
Q

rilpivirine indication

A

NNRTI alternative first-line option in select treatment naive patients or as switch therapy for suppressed pts

*also can be used in combo with INSTI

31
Q

rilvipirine side effects

A
drug interactions (CYP3A4)
no PPIs because it needs an acidic environment for absorption
32
Q

NNRTI based regimen

A

2 NRTIs +NNRTI

33
Q

odefsey

A

TAF + emtricitabine + rilpivirine

34
Q

Juluca

A

rilpivirine + dolutegravir (integrase inhibitor)

35
Q

cabenuva

A

injection

rilpivirn + cabotegravir

36
Q

protease inhibitors MOA

A

inhibition of HIV protease enzyme preventing formation and release of mature virions

37
Q

PIs indication

A

high barrier to resistance, very potent
require admin with a booster agent
alternative first-line in combo with 2 NRTIs

38
Q

HIV life cycle basic steps

A
binding
fusion on CD4 cell
reverse transcription 
integration
replication
assembly
budding
39
Q

Protease Inhibitors’ warnings

A
lipodystrophy
nausea/vomiting
diarrhea
cholesterolemia
insulin resistance
cardiovascular risk
drug interactions
40
Q

PI booster agents

A

ritonavir or cobicistat

41
Q

PI that is safe for pregnancy

A

Lopinavir/ritonavir

42
Q

third gen PIs

A

atazanavir

darunavir

43
Q

why use booster agents for PIs

A

less CYP3A4 inhibition

lower dosing frequency required so there are better blood concentrations

44
Q

can you take atazanavir alone?

A

NO needs to be boosted with ritonavir or cobicistat + 2NRTIs

45
Q

atazanavir side effects

A

N/V/D
Hyperbilirubinemia +/- jaundice
nephrolithiasis and cholelithiasis

46
Q

symtuza

A

combo therapy

-darunavir-cobcistat-TAF-emtricitabine (1 tab PO daily)

47
Q

Prezcobix

A

PI + booster
darunavir-cobicistat 1 tab PO
*as part of combination with 2 NRTIs

48
Q

INSTIs MOA

A

prevents the insertion of DNA transcribed from the virus into human cell DNA by inhibiting integrase enzyme

49
Q

INSTI indication

A

part of first-line regimen for treatment naive-patients

INSTI + 2 NRTIs

50
Q

INSTI classwide effects

A
  • drug interactions bc of CYP450 enzymes

- interacts with antacids

51
Q

raltegravir adverse effects

A

rare myalgia, rash, liver toxicity

52
Q

dolutegravir adverse effects

A

neurocognitive effects
weight gain
elevated serum creatinine
neural tube defects

53
Q

less used INSTI

A

raltegravir because it is inferior to dolutegravir and has a lower barrier to resistance

54
Q

2nd gen INSTIs

A

dolutegravir

bictegravir

55
Q

Dolutegravir indication

A

preferred INSTI

more potent and less frequent dosing than raltegravir

56
Q

Bictegravir (Biktaryvy) indication

A

first line recommendation, high barrier to resistance
single small tablet regimen
well-tolerated

57
Q

cabotegravir

A

long acting injectable in combination with rilpivirine

*monthly injection

58
Q

Dovato

A

dolutegravir + lamivudine (NRTI)

59
Q

biktarvy

A

bictegravir + emtricitabine + TAF

60
Q

genvoya

A

TAF-emtricitabine+elvitagravir+cobicistat

61
Q

gp120 and gp41

A

HIV-1 surface glycoproteins gp120 and gp41 mediate viral binding to host target cells

gp120 binds to CD4 cell and causes conformational change

gp41 forms metastable conformation which allows for HIV penetration

62
Q

entry inhibitors’ MOA

A

either inhibition of gp41 and gp120 to stop binding and fusion with target cell

63
Q

maraviroc

A

entry inhibitor

CCR5 blocker that inhibits gp120 blocks HIV attachment to target cells

64
Q

entry inhibitor types

A

fostemsavir
enfuvirtitide
maraviroc
ibalizumab

65
Q

how to monitor ART patients

A

measure HIV RNA
-goal at 16-24 months is undetectable
measure CD4 count
-want an increase by 50-150 within first year

66
Q

Pre-Exposure Prophylaxis

A

prophylactic therapy given to HIV negative patients who are at high risk of developing HIV

67
Q

prophylaxis regimen for prep

A

Entricitabine/TDF (Truvada)

Emtricitabide/TAF (DEscovy-safer)

take daily!

68
Q

Post-Exposure Prophylaxis (PEP)

A

taken within 72 hours of HIV exposure, anti-HIV rx to prevent development of HIV

69
Q

occupational PEP

A

TDF/emtricitabine (Truvada) + raltegravir (INSTI)

70
Q

non-occupational PEP

A

Truvada + Isentress

TDF+emtricitabine+(raltegravir or dolutegravir)