Antiretrovirals Flashcards

1
Q

which antivirals alter cytochrome p450 and are often used to increase concentrations of ARV drugs that are metabolized through those pathways

A

Ritonavir - CYP3A4 and 2D6cytochrome; results in large increases in plasma concentrations of drugs

Atazanavir - CYP3A4 and CYP2C9

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2
Q

what are the nucleoside reverse transcriptase inhibitors (NRTI)

A
  • Abacavir
  • Lamivudine
  • Tenofovir disoproxil fumarate
  • Tenofovir alafenamide
  • Emtricitabine
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3
Q

what are the protease inhibtiors

A

“-navir”

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4
Q

what are the non-nucleoside reverse trasncriptase inhibitors (NNRTI)

A

Efavirenz

Rilpivirine

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5
Q

what are the integrade strand transfer inhibtiros?

A

“-gravir”

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6
Q

fusion inhibitor

A

enfuvirtide

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7
Q

co-receptor antagonists

A

maraviroc

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8
Q

MOA of NRTIs

A

target = reverse transcriptase

mimic nucleotides to inhibit nucleotide binding to the catalytic site and cause chain termination when incorporated into DNA

require cellular kinases to convert to triphosphate form

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9
Q

Lamivudine:

  1. class?
  2. administration?
  3. therapeutic indications
A
  1. NRTI
  2. oral
  3. initial tx for HIV, chronic HBV (w/ interferon)
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10
Q

Emtricitabine

  1. class?
  2. administration?
  3. how does it differ from lamivudine
  4. therapeutic indications?
A
  1. NRTI
  2. oral
  3. longer T1/2; doesn’t treat HBV
  4. initial tx of HIV
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11
Q

All antiretrovirals are administered orally besides what drug? how is it administered?

A

Enfuvirtide

  • 2x daily - subQ injection
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12
Q

what drug should be geneitcally screened for HLA-B5701 due to hypersensitivity reactions (fever, rash, fatigue, GI; re-challenge = fatal)

A

Abacavir

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13
Q

Abacavir:

  1. class?
  2. therapeutic indication
A
  1. NRTI

2. initial tx of HIV

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14
Q

Tenofovir disoproxil fumarate:

  1. class?
  2. therapeutic indications?
A
  1. NRTI

2. inital tx HIV, chronic HBV (w/ interferon)

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15
Q

who is tenofovir disoproxil fumarate contraindicated for

A

pts with renal impairment

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16
Q

MOA of integrase strand transfer inhibitors (INSTI)

A

binds to HIV integrase and inhibits DNA strand transfer

17
Q

Raltegravir

  1. class
  2. therapeutic indication
A
  1. INSTI

2. initial tx HIV

18
Q

Elvitegravir

  1. class?
  2. therapeutic indications?
  3. creatine clearance?
A
  1. INSTI
  2. initial HIV tx
  3. <70 ml/min
19
Q

Dolutegravir

  1. class?
  2. therapeutic indications?
A
  1. INSTI

2. initial HIV tx

20
Q

MOA of protease inhibtiors

A

target = HIV protease

mimic peptide targets for the protease

block the maturation of virion particles after budding

21
Q

Ritonavir

  1. class?
  2. therapeutic indications?
A
  1. protease inhibitor

2. booster - increase T1/2 of coadministered ARV drug due to CYP3A4 effect

22
Q

what are NNRTIs not active against

A

HIV-2

23
Q

NNRTIs MOA

A

Target = reverse transcriptase

bind to a site on enzyme distinct from the active site

do not require phospohrylation for activation

24
Q

what class is efavirenz and rilpivirine

A

NNRTI

25
Q

what classes of drugs are reserved for tx experienced HIV patients

A

CCR5 receptor antagonists

Fusion inhibitor

26
Q

what drug must you screen for tropism before use?

A

Maraviroc

27
Q

what are the CCR5 coreceptor antagonists

A

Maraviroc

28
Q

theraputic indication for maraviroc

A

tx expereinced pts with CCR5 tropic virus

29
Q

what drug is a fusion inhibitor

A

enfuvirtide

30
Q

therapeutic indication for enfuvirtide

A

tx experience pt with evidence of HIV replication even with ARV tx

31
Q

pre-exposre prohphylaxis

A

Tenofovir disproxil fumerate and emtricitibine

32
Q

what drug is not advised for post exposure prophylaxis

A

Abacavir - b/c need screening for HLA-B5701