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DEN 7108 Micro and Immuno Concepts Part II > Exam 3 Anti-retroviral therapy > Flashcards

Exam 3 Anti-retroviral therapy Flashcards

1
Q

What are some therapeutic implications of HAART?

A
  • Inhibit RTase (cytoplasmic)
  • Inhibit integrase (nuclear)
  • Inhibit protease (cytoplasmic)
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2
Q

Anti-retroviral therapy drugs approved by FDA (5)

A
  • Reverse transcriptase inhibitors (RTI)
  • Protease inhibitors
  • Fusion and entry inhibitors
  • Integrase inhibitors
  • Pharmacokinetic enhancers
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3
Q

What is a NRTI?

A

Nucleoside reverse transcriptase inhibitor

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4
Q

NRTI’s are _____ analogs

A

Nucleoside

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5
Q

First generation NRTI’s are not ____ specific

A

Viral DNA polymerase (RT)

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6
Q

First NRTI’s introduced

A
  • Azidothymidine (AZT)
  • Zidovudine (ZDV)
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7
Q

Functions of NRTI’s

A
  • chain terminators
  • block RTase
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8
Q

What are NNRTI’s?

A

Non-nucleoside reverse transcriptase inhibitors

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9
Q

What do NNRTI’s do?

A
  • Allosteric “non-competitive” inhibition
  • Bind to binding site, not enzyme active site
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10
Q

NNRTI’s are synergistic with ____

A

NRTI’s

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11
Q

Characteristics of protease inhibitors

A
  • Synthetic peptide
  • Non-hydrolysable
  • stable
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12
Q

What is the function of protease inhibitors?

A

Block HIV protease (polyprotein cleavage)

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13
Q

What does integrase inhibitor do?

A

Inhibits irreversible strand transfer step of DNA integration

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14
Q

Raltegravir is an example of:

A

Integrase inhibitor

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15
Q

Integrase inhibitors are metabolized by:

A

Cellular glucuronidation

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16
Q

Dolutegravir is an example of:

A

Integrase inhibitor

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17
Q

____ (integrase inhibitor) was approved in August 2013. It has a prolonged intracellular half life

A

Dolutegravir

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18
Q

Elvitegravir (EVG) is an example of:

A

Integrase inhibitor

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19
Q

Elvitegravir is also called:

A

Vitekta

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20
Q

____ (integrase inhibitor) was approved in September 24, 2014

A

Elvitegravir

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21
Q

______ is the newest integrase inhibitor (Jan 22, 2021)

A

Cabotegravir

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22
Q

Examples of pharmacokinetic enhancers

A
  • Cobicistat (COBI); Tyboost
  • P450 CYP3A4 enzyme inhibitor
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23
Q

A new attachment inhibitor called _____ binds to ____

A

Fostemsavir; gp120

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24
Q

Enfuviritide is an example of:

A

Fusion inhibitor

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25
Q

Enfuviritide binds to ____

A

gp41

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26
Q

Maraviroc is a _____ inhibitor which acts as a _____

A

Entry; CCR5 receptor agonist

27
Q

Which drug has a black box warning?

A

Maraviroc (hepatotoxicity)

28
Q

What does it mean if a drug has a black box warning?

A

Can kill a patient

29
Q

Ibalizumab is a ____ inhibitor that binds to ____

A

Entry; CD4

30
Q

____ is for restricted use only with multidrug-resistant HIV-1

A

Ibalizumab

31
Q

____ is always used in combination

A

Cobicistat (Tyboost)

32
Q

HAART stands for:

A

Highly active anti-retroviral therapy

33
Q

HAART consists of:

A

Combinations of antiretroviral drugs that block different stages of viral replication

34
Q

What are the US FDA approved HAART combination products?

A
  • Stribild
  • Triumeq
  • Evotaz
  • Prezcobix
  • Genvoya
35
Q

Stribild (HAART) consists of what antivirals?

A
  • Elvitegravir (II)
  • Cobicistat (PE)
36
Q

Evotaz (HAART) consists of what antivirals?

A
  • Atazanavir
  • Cobicistat
37
Q

Prezcobix (HAART) consists of what antivirals?

A
  • Darunavir
  • Cobicistat
38
Q

Genvoya (HAART) consists of what antivirals?

A
  • Elvitegravir (II)
  • Cobicistat (PE)
39
Q

Stribild was introduced in what year?

A

2012

40
Q

In what year was Evotaz, Prezcobix, and Genvoya introduced?

A

2015

41
Q

What are the DHSS recommendations for current standard of care?

A
  • All HIV+ patients with an AIDS-defining illness or CD4 count of < 350/microliter
  • All pregnant HIV+ patients regardless of CD4 count
  • HIV post-exposure prophylaxis (PEP)
42
Q

If one has CD4+ 350-500/microliter, what is the indication for HAART therapy?

A

Strong/moderate recommendation

43
Q

If one has CD4+ >500/microliter, what is the indication for HAART therapy?

A

Recommended/optional

44
Q

If one has HBV or HCV co-infection, what is the indication for HAART therapy?

A

Recommended

45
Q

If one has HIV-associated nephropathy, what is the indication for HAART therapy?

A

Recommended

46
Q

If one has acute HIV infection, what is the indication for HAART therapy?

A

Optional

47
Q

Those who undergo HAART therapy have increased _____ and decreased _____

A

CD4 count; risk of opportunistic infection of death

48
Q

Vertical transmission of HIV can occur through what ways?

A
  • Ante-partum
  • During delivery
  • During breastfeeding
49
Q

Risk of perinatal transmission is significantly reduced with:

A

Effective antiretroviral (ART/HAART) therapy

50
Q

____ is needed to reduce perinatal transmission for all pregnant women with HIV infection, regardless of ____

A

3 part regimen; Viral load or CD4 cell count

51
Q

HAART therapy and pregnancy: include ____ in ARV regimen, and for newborns Rx is _____

A

Zidovudine (AZT); AZT first six weeks of life

52
Q

HIV post-exposure prophylaxis

A
  • 2 drug PEP (NNRTI + NRTI) for 4 weeks
  • 3+ drug PEP for 4 weeks
53
Q

What is PrEP?

A

Pre-exposure prophylaxis

54
Q

Success of PrEP in ____ recently reported

A

MSM

55
Q

HAART therapy may induce:

A

Immune restoration disease (IRD)

56
Q

What is immune restoration disease?

A

Diseases properly recognized –> larger immune response after immune system restored

57
Q

In immune reconstitution syndrome, flares of _____ are particularly common

A

Mycobacterial disease

58
Q

Co-infection of HIV and TB causes:

A
  • 800x greater risk for developing active TB
  • increases transmission of TB
  • Increases overall % with latent TB
59
Q

Side effects of NRTI’s

A
  • Pancreatitis
  • Neuropathy
  • GI
  • Marrow suppression
60
Q

Side effects of NNRTI’s

A
  • Rash
  • Hypersensitivity reactions
61
Q

Side effects of protease inhibitors (PI’s)

A
  • glucose intolerance
  • hyperlipidemia
  • lipodystrophy
  • breast hypertrophy
  • GI
  • paresthesia
  • Rashes
62
Q

Side effects of fusion inhibitors

A
  • hypersensitivity
  • increased risk of bacterial pneumonia
63
Q

Lipodystrophy caused by protease inhibitors can cause:

A
  • fat buildup
  • fat loss
  • increased fat levels in the blood
  • increase in blood sugar
64
Q

On 1/21/21, the US FDA approved ______ as a complete regimen for the treatment of HIV-1 infection in adults. This is the first FDA-approved ____ complete regimen for HIV-infected adults that is administered ____

A

Cabenuva; injectable; once a month

DEN 7108 Micro and Immuno Concepts Part II (27 decks)

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