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SBL exam II > HIV Pharm > Flashcards

HIV Pharm Flashcards

1
Q

What does HIV bind to in order to enter cells?

A

CD4 and then either CXCR4 or CCR5

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2
Q

Maraviroc MOA

A
  • binds specifically to CCR5 to prevent viral entry into the host cell
  • should test co-receptor tropism prior to initiating (if virus has tropism for CXCR4 then this drug will not work well)
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3
Q

Maraviroc is used only in

A

those infected with virus with tropism for CCR5

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4
Q

Maraviroc adverse effects

A
  • generally well tolerated

- systemic allergic rxn then hepatotoxicity has been reported

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5
Q

Enfuvirtide MOA

A
  • fusion inhibitor
  • binds to gp41 preventing conformational and structural changes needed to allow fusion of viral envelope with host membrane
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6
Q

How is enfuvirtide administered?

A

subQ injection

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7
Q

enfuvirtide AE

A
  • local injection site rxns
  • insomnia, HA, dizziness, nausea
  • hypersensitivity is rare
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8
Q

How are nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs) used in tx of pts with HIV?

A
  • included in nearly all tx regimens when beginning antiretroviral therapy
  • Mostly provide protection to susceptible cells because if viral DNA is already integrated it will not do anything for those cells
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9
Q

MOA of NRTIs

A
  • competitive inhibition of HIV reverse transcriptase
  • incorporates into growing viral DNA chain
  • leads to premature chain termination due to inhibition of binding with the incoming nucleotide
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10
Q

List the nucleoSIDE reverse transcriptase inhibitors

A 
abacavir
didanosine
lamivudine
emtricitabine
stavudine
zidovudine
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11
Q

List the nucleoTIDE reverse transcriptase inhibitors

A

tenofovir

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12
Q

What is unique about abacavir?

A
  • metabolized by alcohol dehydrogenase
  • serum levels increase with concurrent ethanol ingestion
  • guanosine
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13
Q

AE of abacavir

A
  • hypersensitivity (within 1st 6 wks of therapy)
  • fever, fatigue, nausea, vomiting, diarrhea
  • resp sym: dyspnea, cough
  • skin rash (50%)
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14
Q

AE of didanosine

A
  • dose dependent pancreatitis (conditions or drugs that may cause pancreatitis are contraindicated)
  • retinal changes with optic neuritis (mandated periodic retinal exams)
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15
Q

What is unique about lamivudine

A
  • active against both HIV and HBV
  • cytosine analog
  • AE are uncommon (HA, dizziness, insomnia, fatigue)
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16
Q

What is unique about emtricitabine

A
  • active against HIV & HBV (so I guess it’s not unique idk)
  • long half-life (once daily dosing)
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17
Q

AE of emtricitabine

A
  • HA, diarrhea, nausea, rash

- hyperpigmentation of palms & soles, esp in african americans

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18
Q

AE of stavudine

A
  • dose dependent peripheral sensory neuropathy

- dyslipidemia

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19
Q

Which was the first antiretroviral drug to be approved?

A

zidovudine

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20
Q

AE of zidovudine

A
  • macrocytic anemia
  • neutropenia
  • GI intolerance, HA, insomnia
21
Q

which 3 NRTIs are active against HIV and HBV

A

lamivudine(side), emtricitabine(side), tenofovir (nucleotide)

22
Q

AE of tenofovir (only nucleotide reverse transcriptase inhibitor)

A
  • generally well tolerated

- flatulence

23
Q

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) MOA

A
  • binds directly to HIV reverse transcriptase in site distant from active site
  • binding induces conformation change
24
Q

NNRTIs resistance

A
  • develops rapidly with monotherapy
  • HIV transcriptase point mutations that alter binding
  • no cross resistance between NNRTIs and the NRTIs
25
Q

AE of NNRTIs

A

-GI intolerance, skin rash

Metabolized by CYP450

26
Q

First generation of NNRTIs

A

delavirdine
efavirenz
nevirapine

27
Q

Second generation of NNRTIs

A

etravirine

rilpivirine

28
Q

What is the difference between 1st and 2nd gen NNRTIs

A

2nd gen are most potent, have longer 1/2 lives, and decreased side effects

29
Q

AE of delavirdine

A
  • skin rash

- HA, fatigue, nausea, diarrhea

30
Q

AE of efavirenz

A
  • CNS (50%): dizziness, drowsiness, insomnia, nightmares

- skin rash

31
Q

What is unique about nevirapine

A
  • first NNRTI to be approved for HIV

- used in preventing transmission of HIV from mother to child

32
Q

AE of nevirapine

A
  • rash

- liver toxicity

33
Q

AE of etravirine

A

rash, nausea, diarrhea

34
Q

AE of rilpivirine

A
  • rash, depressiom HA, insomnia, increased serum aminotransferases
  • high doses asssoc. with QT prolongation
35
Q

MOA of integrase strand transfer inhibitors (INSTIs)

A
  • binds HIV integrase

- inhibits strand transfer & prevents ligation of reverse-transcribed HIV DNA int the chromosome of host cell

36
Q

AE of INSTIs

A

well tolerated, HA & GI effects more common

37
Q

List of INSTIs

A

all drugs end in “-gravir”
dolutegravir
elvitegravir
raltegravir

38
Q

What does elvitegravir need to be combined with

A

cobicistat as a booster

39
Q

Which drugs are preferred for tx naive pts?

A
  • dolutegravir in combo with others

- raltegravir

40
Q

MOA of protease inhibitors

A
  • block the HIV protease and prevent the maturation of the final structural proteins that make up the mature virion core
  • specifically inhibits the action of HIV aspartyl protease
41
Q

Protease inhibitors: resistance & AE

A

-resistance develops quickly with monotherapy
AE:
-GI intolerance
-hyperglycemia, hyperlipidemia, lipoatrophy, fat deposition
-redistribution & accumulation of fat

42
Q

Protease inhibitors: metabolism

A

metabolized by CYP3A4

-enormous potential for drug-drug interactions

43
Q

List of protease inhibitors

A 
atazanavir
darunavir
fosamprenavir
indinavir
lopinavir
nelfinavir
ritonavir
saquinavir
tipranavir
44
Q

Darunavir must be co-administered with what?

A

ritonavir or cobicistat

45
Q

AE of indinavir

A

unconjugated hyperbilirubinemia & nephrolithiasis

–consumption of 48 ounces (1.5L) of water daily helps to prevent formation of kidney stones

46
Q

Ritonavir is primarily used as?

A

a booster

  • -very potent CYP450 inhibitor
  • -high rate of GI SE at standard doses
47
Q

When is tipranavir indicated?

A

in pts resistant to other protease inhibitors

-combined with ritonavir

48
Q

Highly active antiretroviral therapy (HAART)

A

2 NRTIs plus either:

  • 1 protease inhibitor (sometimes 2 for boosting)
  • 1NNRTI
  • 1 INSTI

SBL exam II (1 decks)

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