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

B3.071 - HIV Antivirals Flashcards

(85 cards)

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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
what are AEs of zidovudine
common Bone marrow depression CNS - headaches, agitation, insomnia Toxicity enhanced by drugs that compete for glucuronidation
26
what does abacavir do
Guanosine analog and chain terminator
27
resistance to abacavir
develops slowly, requires 2-3 concomitant mutations
28
how is abacavir metabolized
alcohol dehydrogenase
29
AEs of abacavir
skin rash, hypersensitivity, can be fatal
30
what do you need to do before administering abacavir and why
HLA testing | HLA*B5701 allele is predictive marker, but ~50% do no react
31
tenofovir disoproxil and alafenamide what is it and how does it work
after absorption its hydrolized to Acyclic nucleoside phosphonate, a chain terminator. NRTI
32
What is the difference between tenofovir disoproxil and alafenamide
alafenamide has less renal toxicity and bone density loss compared to disoproxil
33
describe the dosing of tenofovir
once daily, renal excretion
34
what are AEs of tenofovir in disoproxil/alafenamide
GI effects - nausea, vomiting, diarrhea | Disoproxil - acute/cumulateive renal toxicity
35
what is tenofovir often combined with
emtricitabine
36
what can be used as HIV prophylaxis
tenofovir
37
what does lamivudine do
cytosine analog, inhibits HIV RT and HBV DNA polymerase
38
how is lamivudine administered/excreted
oral, excreted unchanged in urine
39
half life of lamivudine
serum - 2.5 hr | cellular - 10-15 hr
40
what is the recommended use fo lamivudine (3TC)
pregnant women
41
what is emtricitabine (FTC)
fluorinated analog of lamivudine
42
how is embtricitabine administered
fixed dose combo with tenovir, once daily dosing
43
AEs of emtricitabine
headaches, nausea, rash
44
what does nevirapine do
first generation oral NNRTI | non competitive RT inhibitors, binds near but not in active site
45
what is nevirapine used for
rapid resistance so only approved for combination with nucleoside analogs
46
what is the exception for nevirapine being used only in combination
one dose to mother and neonate
47
what are AEs of nevirapine
skin rash, can be severe hepatotoxicity excellent substrate for CYP3A
48
what does efavirenz do
non competitive RT inhibitors, binds near but not in active site
49
describe the half life of efavirenz
40-60 hr half life; once daily dosing | Bioavailability 45%
50
how should patients take efavirenz
on a empty stomach bc while bioavailability is increased by fat it may increase toxicity
51
AEs of efavirenz
inducer and inhibitor of CYP3A4 so drug drug interactions | CNS effects, dizziness, drowsiness, headache, nightmares
52
why is efavirenz bumped to second line for use
CNS effects can be severe
53
what is raltegravir
INSTI
54
how is raltegravir taken
orally, not with cations or buffered drugs, twice daily
55
how is raltegravir metabolized
by UGT1A1
56
adverse effects of raltegravir
diarrhea, nausea, headache, dizziness, metabolic effects
57
how is dolutegravir administered
oral, not with cations or buffered drugs
58
how does dolutegravir work
integrase inhibitor
59
half life of dolutegravir and how its eliminated
14 hour half life by glucuronidation (UGT1A1)
60
AEs of dolutegravir
insomnia, headache, hypersensitivity
61
how do protease inhibitors work
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
HIV protease is what type of protease
aspartyl protease
63
AEs of protease inhibitors
diarrhea, nausea, lipodystrophy, insulin resistance
64
saquinovir downsides
first HIV protease inhibitor | Extensive first pass effect and many drug drug interactions (CYP3A4)
65
indinavir is metabolized by
CYP3A4
66
AEs of indinavir
hyperbilirubinemia, nephrolthiasis* (crystallizes in urine)
67
ritonavir metabolized by what
CYP3A4 and some 2D6
68
what are AEs of Ritonavir
potent CYP3A4 inhibitor | initial nausea, vomiting, diarrhea, GI, parathesias, headache
69
darunavir is often combined with what
Ritonavir
70
what does the ritonavir do in the darunavir combo
blocks CYP3A protecting darunavir and allowing its effect to persist longer
71
AEs of darunavir
GI, headache, rash
72
what other drug may be combined with darunavir
cobicistat
73
what does atazanavir do
protease inhibitor
74
how is atazanavir dosed and metabolized
once daily dosing, enters CNS, biliary excretion
75
what enzymes does Atazanavir inbibit
UGT1A1, CYP3A4, CYP2C9
76
AEs of atazanavir
diarrhea, nausea, vomiting, headache | hyerbilirubinemia
77
what is atazanavir not associated with AEwise that is important
No dyslipidemia, fat redistribution, metabolic syndrome
78
cobicistat is used for
not an antiviral, used in fixed combinations for boosting of accompanied antiviral drug
79
what does cobicistat inhibit and what does that do
CYP3A, decreases first pass clearance of protease inhibitors, integrase inhibitors
80
when should you not use cobicistat
if creatinine clearance <30
81
what does ART stand for
Anti-retroviral therapy
82
why do all ART regimens include RTIs
to prevent resistance, preventing mutations from sloppy reverse transcriptase
83
which drugs are substrates for CYP3A4
delavirdine, efavirenz, nevirapine, all protease inbhibitors
84
what drugs are inducers of CYP3A4 in other tissues
efavirenz, nevirapine, amprenavir
85
what drugs are inhibitors of CYP3A4
delavirdine, efavirenz, all protease inhibitors especially ritanovir

IBI Test 4 (12 decks)

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