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PPOM1 Block 4 > Lecture 185 > Flashcards

Lecture 185 Flashcards

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1
Q

What class of ARTs does doravirine (DOR) belong to?

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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2
Q

What class of ARTs does rilpivirine (RPV) belong to?

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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3
Q

What class of ARTs does efavirenz (EFV) belong to?

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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4
Q

What class of ARTs does nevirapine (NVP) belong to?

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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5
Q

What class of ARTs does etravirine (ETR) belong to?

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

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6
Q

What class of ARTs are allosteric, noncompetitive inhibitors of HIV-1 reverse transcriptase that bind to a hydrophobic binding pocket near the active site of RT?

A

Non-nucleoside reverse transcriptase inhibitors

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7
Q

How do NNRTIs differ from NRTIs in terms of activation?

A

NNRTIs do not need to be intracellularly phosphorylated

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8
Q

What is the barrier to resistance for NNRTIs?

A

Generally low barrier to resistance

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9
Q

What is the likely consequence of resistance forming to one NNRTI?

A

Cross-resistance between NNRTIs is common

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10
Q

What type of testing should be done in all patients before initiating NNRTI therapy?

A

Resistance testing

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11
Q

Rashes, GI disturbances, and neuropsychiatric side effects are adverse effects associated with what ART class?

A

NNRTIs

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12
Q

What fixed dose combination is Doravirine (DOR) available in?

A

Doravirine-tenofovir-emtricitabine (DOR-TDF-FTC)

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13
Q

Doravirine (DOR) is a substrate of ____

A

CYP3A4

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14
Q

Under what special conditions should oral efavirenz be taken?

A

Empty stomach (food increases absorption and AEs)

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15
Q

What fixed dose combination is efavirenz (EFV) available in?

A

Efavirenz/tenofovir/emtricitabine (EFV/TDF/FTC)

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16
Q

Neuropsychiatric side effects, skin rash, and QTc prolongation are AEs of what NNRTI?

A

Efavirenz (EFV)

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17
Q

Efavirenz is a substrate of ____

A

CYP3A4

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18
Q

Efavirenz is a mixed inducer/inhibitor of ____

A

CYP3A4

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19
Q

Efavirenz is an inducer of ____ and ____

A

CYP2B6 and CYP2C19

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20
Q

Under what special conditions should oral rilpivirine be taken?

A

With a meal, requires acid for absorption

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21
Q

What fixed dose combinations is rilpivirine (RPV) available in?

A

RPV/TDF/FTC & RPV/TAF/FTC

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22
Q

Which NNRTI should only be prescribed to adults with HIV RNA <100,000 copies/mL and CD4 count >200?

A

Rilpivirine (RPV)

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23
Q

Depression, headache, and QTc prolongation are AEs of which NNRTI?

A

Rilpivirine (RPV)

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24
Q

Rilpivirine (RPV) is a substrate of ____

A

CYP3A4

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25
Which NNRTI should not be combined with proton pump inhibitors (PPIs)?
Rilpivirine (RPV)
26
What is the main therapeutic use for nevirapine (NVP)?
Presumptive therapy in neonates at high-risk of perinatal HIV transmission (ZDV/FTC/NVP)
27
What NNRTI carries a significant risk for hepatotoxicity?
Nevirapine
28
Which NNRTI should not be initiated in women with CD4 >250 or men with CD4 >400 due to increased risk of hepatotoxicity?
Nevirapine (NVP)
29
Which NNRTI has the highest barrier to resistance?
Etravirine (ETR)
30
Etravirine is a substrate of ____
CYP3A4
31
Etravirine (ETR) induces ____
CYP3A4
32
Etravirine (ETR) inhibits ____ and ____
CYP2C9 and CYP2C19
33
What class of ARTs does atazanavir (ATV) belong to?
Protease inhibitors
34
What class of ARTs does darunavir (DRV) belong to?
Protease inhibitors
35
What is the activity of protease inhibitors?
Mainly HIV-1, DRV has some activity against HIV-2
36
What class of ARTs are reversible inhibitors that bind to the active site of HIV protease and prevent cleavage of polyproteins?
Protease inhibitors
37
What level of resistance do protease inhibitors typically possess?
High genetic barrier to resistance
38
Which ART class is always administered with a booster?
Protease inhibitors
39
What boosters are combined with protease inhibitors?
Ritonavir and cobicistat
40
Ritonavir and cobicistat are potent inhibitors of ____ and ____
CYP3A4 and P-gp
41
GI symptoms and metabolic effects are AEs associated with what class of ARTs?
Protease inhibitors
42
UGT induction by ritonavir may decrease the efficacy of ____
Hormonal contraceptives
43
Which class of ARTs interacts with methadone, potentially inducing withdrawal?
Protease inhibitors
44
How should atazanavir (ATV) be taken?
With food
45
Jaundice, cholelithiasis, and nephrolithiasis are AEs of what protease inhibitor?
Atazanavir (ATV)
46
What drug interaction with atazanavir (ATV) decreases absorption?
Drugs that increase gastric pH
47
What special population are protease inhibitors preferred for initial therapy?
Pregnancy, boosted doses twice daily
48
How should darunavir (DRV) be dosed?
Once daily for treatment naïve, twice daily for treatment experienced
49
How should darunavir (DRV) be taken?
With food
50
Which protease inhibitor is contraindicated in severe liver disease?
Darunavir (DRV)
51
Darunavir administration should be cautioned in people with a history of what allergy?
Sulfonamides
52
Conformational change in gp120 exposes a binding site for what co-receptors on the T-cell surface?
CCR5 or CXCR4
53
Binding to the co-receptor triggers further conformational changes in HIV's ____ protein, leading to fusion of the membranes
Gp41
54
What class of ARTs does maraviroc (MVC) belong to?
CCR5 inhibitor (entry inhibitors)
55
What ART selectively binds to the human CCR5 co-receptor on the host cell, preventing the viral gp120 from interacting with CCR5?
Maraviroc (MVC)
56
What is the activity of maraviroc (MVC)?
CCR5-tropic HIV-1
57
Tropism testing must be done before starting what ART?
Maraviroc (MVC)
58
Maraviroc can be used in patients >____ years old
>16 years old
59
Which entry inhibitor ART is associated with concerns for hepatotoxicity?
Maraviroc (MVC)
60
What class of ARTs does enfuvirtide (T-20) belong to?
Fusion inhibitor (Entry inhibitor)
61
What ART binds to the first heptad repeat (HR1) region of HIV gp41, preventing conformational changes required for fusion of membranes?
Enfuvirtide (T-20)
62
What is the activity of enfuvirtide (T-20)?
HIV-1
63
What is the indicated use of enfuvirtide (T-20)?
Treatment experienced adults and children (>6 years) with ongoing HIV replication despite ART
64
Injection site reactions making long-term use challenging is an adverse effect of what ART?
Enfuvirtide
65
How is Enfuvirtide (T-20) administered?
SubQ injections
66
What class of ARTs does fostemsavir belong to?
Fusion inhibitor (entry inhibitor)
67
What ART is a prodrug of temsavir?
Fostemsavir
68
What ART binds directly to HIV-1 gp120 near the CD4 binding site, preventing the initial attachment to the CD4 receptor?
Fostemsavir
69
Temsavir is a substrate of ____ and ____
CYP3A4 and P-gp
70
What is the activity of fostemsavir?
HIV-1
71
What is the indicated use for fostemsavir?
Heavily treatment-experienced adults with multidrug resistant HIV-1 failing current ART
72
Nausea, hepatic enzyme elevation, and QT interval prolongation are adverse effects of what entry inhibitor?
Fostemsavir
73
What class of ARTs does ibalizumab belong to?
Post-attachment inhibitor (entry inhibitor)
74
What ART binds to domain 2 of human CD4 receptor and interferes with post-attachment conformational changes required for gp120 to interact with co-receptors?
Ibalizumab
75
How is ibalizumab administered?
IV infusion every 14 days
76
What is the indicated use of ibalizumab?
Heavily treatment-experienced adults with multidrug-resistant HIV-1
77
Dizziness, diarrhea, nausea, and rash are associated with what entry inhibitor ART?
Ibalizumab
78
What class of ARTs does lenacapavir (LEM) belong to?
Capsid inhibitor
79
What ART directly binds to the interface between capsid protein subunits?
Lenacapavir (LEM)
80
How is lenacapavir (LEM) administered?
Oral initiation, SubQ maintenance every 6 months
81
Lenacapavir (LEM) is a substrate of ____
CYP3A4
82
What is the indicated use of lenacapavir?
Heavily treatment-experienced adults with multidrug-resistant HIV-1 failing current therapy
83
What is a common AE of lenacapavir?
Injection site reactions
84
What are two common NRTI backbones?
Tenofovir (TDF or TAF)/emtricitabine (FTC) & abacavir (ABC)/lamivudine (3TC)
85
What two-drug regimen can be used as initial therapy for adults with HIV-1?
Dolutegravir (DTG)-lamivudine (3TC) AKA Dovato
86
TDF-emtricitabine (FTC), TAF-emtricitabine (FTC), and IM cabotegravir are options for ____
PrEP
87
TDF-emtricitabine with dolutegravir or raltegravir is the preferred regimen for ____
PEP
88
How long is PEP?
4 weeks
89
What is the preferred treatment for pregnant people with HIV?
2 NRTI backbone with dolutegravir

PPOM1 Block 4 (44 decks)

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