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P3 Infectious Disease II > Exam 2: Antiretroviral -Part 2- Moniri > Flashcards

Exam 2: Antiretroviral -Part 2- Moniri Flashcards

1
Q

T/F?

NRTIs are NON-competitive inhibitors of reverse transcriptase and obligate chain terminators.

A

False

-COMPETITIVE inhibitors

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2
Q

ALL NRTIs must undergo ______ in order to exert drug effects.

A

mono-, di-, or tri- phosphorylation

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3
Q

Which NRTI only has to undergo di- and tri-phosphorylation and contains 2 formulations?

A

Tenofovir (Viread, TDF)

Alafenamide (TAF)

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4
Q

Which Tenofovir formulation is associated w/ Less toxicities, increase efficacy, more metabolic AEs?

A

Tenofovir alafenamide (TAF)

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5
Q

T/F?

TDF concentrates more in the cell in opposed to the blood which increase its’ efficacy.

A

False

-Tenofovir alafenamide (TAF)

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6
Q

Which 2 NRTIs induce known resistance (M184V)? Why are they still used?

A

Lamivudine (Epivir, 3TC)
Emtricitabine (Emitriva, FTC)
- they are used b/c the mutation creates a less virulent infection

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7
Q

Which NRTI requires HLA-B*5701 hypersensitivity testing?

A

Abacavir (Ziagen, ABC)

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8
Q

Which HLA-B is associated w/ slow AIDs progression?

A

HLA-B27/B57

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9
Q

Which HLA-B is associated w/ fast AIDs progression?

A

HLA-B35

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10
Q

Which NRTI is associated w/ HIGH toxicities due to high infinity for monophosphate which result in BONE MARROW SUPPRESION, anemia and erythroid?

A

Zidovudine (Retrovir, AZT)

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11
Q

_____ act at the allosteric site and shifts the enzyme confirmation and a nucleotide can no longer fit and chain extension is inhibited

A

nNRTIs

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12
Q

What major AEs is associated w/ nNRTIs?

A

Drug-drug interactions due to being CYP450 effectors

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13
Q

T/F?

nNRTIs are used to effectively treat HIV-1 AND HIV-2.

A

False

- HIV-1 ONLY

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14
Q

What 3 nNRTIs are CYP inducers?

A
  • Efavirenz (Sustiva) (major ALL 3)
  • Nevirapine (Viramune)
  • Etravirine (Intelence)
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15
Q

What nNRTI decreases PI levels?

A

-Efavirenz (Sustiva)

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16
Q

Which nNRTI has QD dosing but should not be taken w/ PPIs?

A

Rilpivirine (Edurant)

17
Q

Which nNRTI is used to induce AZT sensitivity?

A

Delaviradine (Rescriptor)

18
Q

What 2 nNRTI are CYP Inhibitors ONLY?

A
  • Delaviradine (Rescriptor)

- Rilpivirine (Edurant)

19
Q

Which nNRTI is associated w/ 103, 108, 181 known gene mutations?

A

Nevirapine (Viramune)

20
Q

What nNRTI has QD dosing and is associated w/ teratogenicity and increase CNS SEs?

A

Efavirenz (Sustiva)

21
Q

How do PIs inhibit virion maturation?

A

By mimicking the recognition site. PIs reversibly bind to the site and inhibit polypeptide cleavage (Phe-Pro)

22
Q

Most PI failure is do to ___?

A

non-compliance

23
Q

What ae the 2 major AE effects associated w/ PIs?

A
  • Drug-Drug interactions (Cyp450 isozymes)

- DYSLIPIDEMIA

24
Q

What is the most potent PI CYP450 inhibitory? What is it commonly used for?

A

Ritonavir

-boosting agent

25
Q

What effect dose Ritonavir have on PIs when given in combination?

A

They increase PIs potency (AUC)

26
Q

What 3 second generation PIs have an increase in resistance barrier and efficacy?

A

Darunavir (Prezista)
Atazanavir (Reyataz)
Tipranavir (Aptivus)

27
Q

Which 2nd generation PI is associated w/ increased SEs (lipids, hepatitis, glucose)

A

Tipranavir (Aptivus)

28
Q

Which 2nd generation PI is associated w/ QD doing and less dyslipidemia?

A

Atazanavir (Reyataz)

29
Q

Which PI is a prodrug?

A

Fosamprenavir (Lexiva, Telzir)

30
Q

_____ is a fusion HIV-1 inhibitor that binds to gp41-inhibits fusion of viral & cell membranes .

A

Enfuvirtide (Fuzeon)

31
Q

What medication blocks CCR5? What must be determined prior to this medication being prescribed?

A

Maraviroc

-tropism

32
Q

What are the 3 major AEs associated w/ Integrase inhibitors?

A
  • increase in SCr/Cr kinase
  • Rhabdomyolysis
  • myopathy
33
Q

What is the major difference between Stribild and Genovoya?

A

Tenofovir formulation
Genvoya- TAF
Stribild- TDF

  • both have the following:
  • Emtricitabine
  • Elvitegravir
  • Cobicistat
34
Q

What are the 2 agents used for “boosting” purposes?

A
  • Cobicistat

- Ritonavir

35
Q

Which boosting agent has NO antiretroviral activity?

A

-Cobicistat

P3 Infectious Disease II (5 decks)

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