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PPOM1 Block 4 > Lecture 184 > Flashcards

Lecture 184 Flashcards

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1
Q

Binding and fusion of HIV to the host cell requires binding of what viral protein to CD4?

A

Gp120

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2
Q

What viral protein is exposed and forms a hairpin structure to facilitate fusion of HIV to the host cell?

A

Gp41

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3
Q

What HIV gene encodes structural proteins?

A

Gag

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4
Q

What HIV gene encodes for 3 enzymes including reverse transcriptase?

A

Pol

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5
Q

What HIV gene encodes for a large envelope protein?

A

Env

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6
Q

What stage of the HIV life cycle does maraviroc target?

A

Entry (chemokine and CD4 receptors)

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7
Q

What stage of the HIV life cycle does fostemsavir target?

A

Entry (attachment and fusion)

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8
Q

What stage of the HIV life cycle does ibalizumab target?

A

Entry (attachment and fusion)

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9
Q

What stage of the HIV life cycle does enfuvirtide target?

A

Entry (attachment and fusion)

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10
Q

What stage of the HIV life cycle does lenacapavir target?

A

Capsid (penetration and uncoating)

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11
Q

What stage of the HIV life cycle do NRTIs target?

A

Reverse transcription

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12
Q

What stage of the HIV life cycle do NNRTIs target?

A

Reverse transcription

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13
Q

What stage of the HIV life cycle do INSTIs target?

A

Integration

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14
Q

What stage of the HIV life cycle do protease inhibitors target?

A

Maturation (assembly, budding, and release)

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15
Q

What is the expected increase in CD count within the first year of ART?

A

50-150 cells/mm3

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16
Q

What is the typical make up of the recommended initial ART regimen?

A

2 NRTIs and an INSTI

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17
Q

An inflammatory reaction to overt or subclinical opportunistic infections or malignancies occurring after initiation of ART

A

Immune reconstitution inflammatory syndrome (IRIS)

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18
Q

What class of ARTs does abacavir belong to?

A

Nucleoside reverse transcriptase inhibitors (NRTIs)

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19
Q

What class of ARTs does lamivudine belong to?

A

Nucleoside reverse transcriptase inhibitors (NRTIs)

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20
Q

What class of ARTs does emtricitabine belong to?

A

Nucleoside reverse transcriptase inhibitors (NRTIs)

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21
Q

What class of ARTs does tenofovir belong to?

A

Nucleotide reverse transcriptase inhibitors (NRTIs)

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22
Q

What class of ARTs does zidovudine belong to?

A

Nucleoside reverse transcriptase inhibitors (NRTIs)

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23
Q

ZDV

A

Zidovudine

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24
Q

3TC

A

Lamivudine

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25
FTC
Emtricitabine
26
ABC
Abacavir
27
TFV
Tenofovir
28
What type of analog is zidovudine (ZDV)?
Thymidine
29
What type of analog is lamivudine (3TC)?
Cytidine
30
What type of analog is emtricitabine (FTC)?
Cytidine
31
What type of analog is abacavir (ABC)?
Guanosine
32
What type of analog is Tenofovir (TFV)?
Adenosine
33
What class of ARTs competitively inhibits the incorporation of native deoxynucleotides into the nascent viral DNA chain?
NRTIs
34
NRTIs act as chain inhibitors because they lack what functional group in their structure?
3'-OH group
35
What is the activity of NRTIs?
HIV-1 and HIV-2
36
M184V/I amino acid substitution confers high level resistance to what NRTIs?
Lamivudine (3TC) and emtricitabine (FTC)
37
M184V/I amino acid substitution confers low level resistance to what NRTI?
Abacavir (ABC)
38
M184V/I amino acid substitution restores susceptibility to what NRTIs?
Tenofovir (TFV) and zidovudine (ZDV)
39
What primary cause of toxicity in NRTI ARTs is due to inhibition of what host enzyme?
DNA polymerase-gamma (mitochondrial enzyme)
40
Lactic acidosis and hepatic steatosis are potentially fatal adverse effects associated with what ART class?
NRTIs
41
What NRTI has the highest potential for mitochondrial toxicity?
Zidovudine (ZDV)
42
What modification must be made to activate NRTIs?
Tri phosphorylation by host cellular kinases
43
TDF
Tenofovir disoproxil fumarate
44
TAF
Tenofovir alafenamide
45
What tenofovir prodrug is administered at a lower dose due to higher intracellular concentrations of active TFV-DP?
TAF
46
What tenofovir prodrug is recommended for use in children >2 years old?
TDF
47
What tenofovir prodrug is recommended for use in children/adolescents >12 years old?
TAF
48
Tenofovir is safe for treatment in what special population?
Pregnant people (all trimesters)
49
What non-HIV infection can tenofovir be used to treat?
Chronic HBV treatment
50
What US boxed warning accompanies tenofovir?
Can cause acute exacerbation of HBV infection in co-infected patients if tenofovir is discontinued
51
Which tenofovir prodrug is associated with less long-term kidney and bone toxicity?
TAF
52
What are the most common non-mitochondrial toxicities of tenofovir?
Renal impairment, kidney injury, bone loss
53
What other NRTI should tenofovir not be combined with?
Abacavir (ABC)
54
What group of drugs can increase tenofovir levels?
P-gp inhibitors
55
P-gp inducers are contraindicated during treatment with which tenofovir prodrug?
TAF
56
Lamivudine (3TC) should not be administered with what other NRTI?
Emtricitabine (FTC)
57
Emtricitabine (FTC) should not be administered with what other NRTI?
Lamivudine (3TC)
58
What US boxed warning accompanies Emtricitabine (FTC)?
Can cause acute exacerbation of HBV infection in co-infected patients if tenofovir is discontinued
59
What US boxed warning accompanies lamivudine (3TC)?
Can cause acute exacerbation of HBV infection in co-infected patients if tenofovir is discontinued
60
What NRTI is associated with hyperpigmentation, usually on the hands/soles of the feet?
Emtricitabine (FTC)
61
Which NRTI is metabolized by alcohol dehydrogenase and glucuronyl transferase?
Abacavir (ABC)
62
All patients starting abacavir (ABC) should be screened for what HLA allele?
HLA-B*5701
63
What contraindication is associated with abacavir?
Previous hypersensitivity reactions
64
Abacavir should not be paired with which of NRTI?
Tenofovir
65
What other NRTI is abacavir usually paired with?
Lamivudine (3TC)
66
Alcohol may interact with which NRTI?
Abacavir
67
Which NRTI is used as perinatal IV infusion to prevent vertical HIV transmission?
Zidovudine (ZDV)
68
What NRTI is recommended for use in neonates?
Zidovudine (ZDV)
69
What NRTI requires twice daily oral dosing?
Zidovudine (ZDV)
70
What class of ARTs does bictegravir (BIC) belong to?
Integrase strand transfer inhibitors (INSTIs)
71
What class of ARTs does dolutegravir (DTG) belong to?
Integrase strand transfer inhibitors (INSTIs)
72
What class of ARTs does elvitegravir (EVG) belong to?
Integrase strand transfer inhibitors (INSTIs)
73
What class of ARTs does raltegravir (RAL) belong to?
Integrase strand transfer inhibitors (INSTIs)
74
What class of ARTs does cabotegravir (CAB) belong to?
Integrase strand transfer inhibitors (INSTIs)
75
BIC
Bictegravir
76
DTG
Dolutegravir
77
EVG
Elvitegravir
78
RAL
Raltegravir
79
CAB
Cabotegravir
80
What class of ARTs blocks the catalytic activity of integrase, preventing the strand transfer step?
Integrase strand transfer inhibitors (INSTIs)
81
What class of ARTs is recommended first-line combined with 2 NRTIs for initial ART in treatment-naive patients?
INSTIs
82
What is the activity of INSTIs?
HIV-1 and HIV-2
83
Oral absorption of all INSTIs is impaired by ____
Polyvalent cations (antacids and supplements)
84
BIC is a substrate of ____, _____, and _____
CYP3A4, p-GP and UGT1A1
85
DTG is a substrate of ____ (minor), ____, and ____
CYP3A4, P-gp, and UGT1A1
86
EVG is a substrate of ____
CYP3A4
87
RAL is a substrate of _____
UGT1A1
88
CAB is a substrate of ____
UGT1A1
89
Which INSTI requires boosting with cobicistat?
Elvitegravir (EVG)
90
Cobicistat is an inhibitor of ____ and ____
CYP3A4 and P-gp
91
Which two INSTIs have a high barrier to resistance?
Dolutegravir (DTG) and bictegravir (BIC)
92
Which two INSTIs have a low barrier to resistance?
Raltegravir (RAL) and elvitegravir (EVG)
93
Bictegravir (BIC) is available as a fixed dose combination containing:
Bictegravir (BIC)-tenofovir (TAF)-emtricitabine (FTC)
94
What forms is dolutegravir available in?
Single drug tablet and fixed-dose combinations
95
What two fixed dose combinations is dolutegravir found in?
Dolutegravir (DTG)-abatacept (ABC)-emtricitabine (FTC) & dolutegravir (DTG)-lamivudine (3TC)
96
Depression/SI, hypersensitivity reactions, and hepatotoxicity are AEs of what INSTI?
Dolutegravir (DTG)
97
Elvitegravir (EVG) is available in what two fixed dose combinations?
Elvitegravir (plus cobicistat)(EVG)-tenofovir (TDF)-emtricitabine (FTC) & Elvitegravir (plus cobicistat)(EVG)-tenofovir (TAF)-emtricitabine (FTC)
98
Increased triglycerides and LDL cholesterol are AEs of what INSTI?
Elvitegravir (EVG)
99
What form is raltegravir (RAL) available in?
Single drug tablet
100
Increase CK, myopathy, and hypersensitivity reactions are AEs of what INSTI?
Raltegravir (RAL)
101
What forms is cabotegravir (CAB) available in?
Oral form, IM suspension, and fixed dose cabotegravir (CAB)-rilpivirine IM suspension
102
What is a contraindication for use of IM cabotegravir?
Gluteal implants or fillers
103
How is tolerability of cabotegravir and rilpivirine determined?
1 month oral dosing of both
104
How often is IM cabotegravir-rilpivirine administered?
4-8 weeks
105
What are the required criteria for use of cabotegravir-rilpivirine treatment?
No baseline resistance to either medication, no prior virologic failures, no active HBV, no pregnancy, and no medications with drug interactions
106
Which INSTI is used for PrEP?
Cabotegravir (IM)
107
What are the most frequently reported side effects of the INSTI class?
Headache and GI effects

PPOM1 Block 4 (44 decks)

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