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(J2) HIV/AIDS > HIV Pharm > Flashcards

HIV Pharm Flashcards

1
Q

What are the main classes of HIV drugs?

A
  1. NRTI, nucleoside reverse transcriptase inhibitors
  2. NNRTI, non-nucleoside reverese transcriptase inhibitors
  3. INSTI, integrase strand transfer inhibitors
  4. protease inhibitors
  5. fusion inhibitors
  6. entry blockers
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2
Q

What does a normal ART regimen look like?

What classes are first, second, and thrid line?

A

combination regimen of 3 drugs from at least 2 different classes

“2 +1”

First line:

  • “2” -> NRTI
  • “+1” -> INSTI

Second line:

-“+1” -> protease inhibitors

Thrid line:

-“+1” -> NNRTI

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3
Q

What changes should be made when an HIV patient does not respond to their ART therapy?

A

2 or more of the drugs should be changed to prevent formation of drug resistance

new drugs should have a different mechanism of resistance from original drugs

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4
Q

What are NRTIs?

A

Nucleoside reverse transcriptase inhibitors:

-mimic nucleotides but lack 3’ -OH, incorperated into HIV DNA during synthesis by reverse transcriptase -> chain termination

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5
Q

What black box warning is associated with NRTIs and why?

A

-NRTIs are not recognized by human DNA polyerase, however, they are partially recognized by mitochondrial DNA polymerase -> mitochondrial toxicity

-lactic acidosis

  • peripheral neuropathy
  • anemia
  • myopathy
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6
Q

What is a common suffix in NTRIs?

A

“-vudine”

not found in all NTRIs

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7
Q

What is zidovudine (AZT)?

What if any toxicities are associated with it?

A

NRTI (“-vudine”)

-thymidine analog, needs phosphorylation

Toxicities:

  • myelosupression -> cytopenias
  • lipodystrophy (common to thymidine analogs)
  • mitochondrial toxicity (common to all NTRIs)
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8
Q

What is stavudine (d4T)?

What if any toxicities are associated with it?

A

NRTI (“-vudine”)

-thymidine analog, needs phosphorylation

Toxicities:

  • peripheral neuropathy
  • lipodystrophy (*most prominent in stavuidne*)
  • mitochondrial toxicity (common to all NTRIs)
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9
Q

What is emtricitabine (FTC)?

What if any toxicities are associated with it?

A

NRTI

-cytosine analog, needs phosphorylation

Toxicities:

  • hyperpigmentation of palms and soles (common in AAs)
  • one of the least toxic
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10
Q

What is lamivudine (3TC)?

What if any toxicities are associated with it?

A

NRTI (“-vudine”)

-cytidine analog, needs phosphorylation

Toxicities:

  • peripheral neuropathy
  • one of the least toxic
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11
Q

What is abacavir (ABC)?

What if any toxicities are associated with it?

A

NRTI

-guanosine analog (only one), needs phosphorylation

Toxicities:

-fatal hypersensitivity with HLA-B*5701 -> rash

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12
Q

What is tenofovir disoproxil fumarate (TDF)?

What if any toxicities are associated with it?

A

NRTI

-adenosine analog, already phosphorylated

Toxicities:

-nephrotoxicity -> (Fanconi syndrome)

-decreased bone density

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13
Q

What is tenofovir alafenamide (TAF)?

What if any toxicities are associated with it?

A

NRTI

-adenosine analog, already phosphorylated

Toxicities:

  • well tolerated
  • lower plasma concentrations that TDF -> less risk of renal and bone s/x
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14
Q

What NRTI is most commonly used in children and pregnant women?

A

-zidovudine

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15
Q

What NRTI(s) is also effective against HTLV?

A

-zidovudine

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16
Q

What NRTI(s) is also effective against HBV?

A
  • emtricitabine (both C)
  • lamivudine (both C)
  • tenofovir
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17
Q

What NRTIs are often co-formulated?

A
  • emtricitabine / lamivudine (cytosine)
  • tenofovir (adenosine)
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18
Q

What are INSTIs?

A

Integrase strand transfer inhibitors:

-blocks integration of HIV DNA into cell DNA -> no viral DNA replication

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19
Q

What is a common suffix in INSTIs?

A

“-tegravir”

inteGRAse

20
Q

What is raltegravir?

What if any toxicities are associated with it?

A

INSTI (“-gravir”)

Toxicities:

  • generally well tolerated
  • immune reconstitution syndrome
  • rhabdomyolysis
  • hypersensitivity reaction
21
Q

What is dolutegravir?

What if any toxicities are associated with it?

A

INSTI (“-gravir”)

Toxicities:

-generally well tolerated

-possible neural tube defects w/ pregnancy

  • immune reconstitution syndrome
  • rhabdomyolysis
  • hypersensitivity reaction
22
Q

What is bictegravir?

What if any toxicities are associated with it?

A

INSTI (“-gravir”)

comes only in combination with other drugs

Toxicities:

-generally well tolerated

23
Q

What makes INSTIs first line “+1” ART drugs?

A
  • will often still be effective when other drugs are resisted (unique mechanism of resistance)
  • development of resistance is actually genetically resisted

-generally well tolerated

24
Q

What are protease inhibitors?

A

inhibit cleavage of HIV precursor proteins into active proteins

target:

  • homodimer asrpartyl protease (cleaves proline)
  • human aspartyl proteases are monomers and not affected
25
Q

What is a common suffix in protease inhibitors?

A

“-navir”

26
Q

What is darunavir?

What is special about it?

A

Protease inhibitor (“-navir”)

-current first choice PI

-sulfa drug -> possible hypersensitivity

27
Q

What is atazanavir?

What is special about it?

A

Protease inhibitor (“-navir”)

-elevated unconjugated bilirubin w/o hepatitis

28
Q

What is lopinavir?

What is special about it?

A

Protease inhibitor

-often works after failure of other PIs

29
Q

What is indinavir?

Whats special about it?

A

protease inhibitor (“-navir”)

-not used any more due to crystaluria/renal stone

30
Q

What are common toxicities of protease inhibitors?

A
  • dyslipidemia
  • immune reconstitution syndrome
  • GI symptoms
31
Q

What drugs are almost always given along with protease inhibitors?

A

CYP3A4 inhibitors

  • ritonavir
  • cobicistat
  • most protease inhibitors are metabolized by CYP3A4 so inhibitors increase the concentration of PIs
32
Q

What is ritonavir?

A

CYP3A4 inhibitor

33
Q

What is cobicistat?

A

CYP3A4 inhibitor

-used w/ azatanavir and darunavir

34
Q

What are NNRTIs?

A

Non-nucleoside reverse transcriptase inhibitors:

-non-competitive reverse transcriptase inhibitor

35
Q

What is a common feature in the name of NNTRIs?

A

“-vir-“ is in the middle of the name, not the end

(Don’t rely on this outside of HIV medications, its literally just something I found helpful. Enfuvirtide and maraviroc break this rule so I’m sure there are non-HIV antivirals that do as well)

36
Q

nevirapine

A

NNTRI

37
Q

efavirenz

A

NNTRI

38
Q

etravirine

A

NNTRI

39
Q

rilpivrine

A

NNTRI

40
Q

doravirine

A

NNTRI

41
Q

What makes NNRSTIs third line “+1” ART drugs?

A
  • only effective against HIV-1; HIV-2 naturally resistant
  • easily develop resistance
42
Q

What are fusion inhibitors?

A

targets gp41 which is involved in viral membrane fusion with host cell -> virus can’t fuse, cells not infected

43
Q

What is enfuvirtide?

A

Fusion inhibitor (enfuvirtide)

-must be administered parenerally

44
Q

What are the benefits/disadvantages of enfuvirtide?

A

Benefits:

-unique mechanism; remains active following resistance to other drugs

Disadvantages:

  • not effective against HIV-2
  • VERY expensive
45
Q

What are entry blockers?

A

blocks GP120 (HIV molecule that recognizes CXCR4 and CCR5) from binding CCR5

46
Q

What is maraviroc?

A

entry blocker

maraviroc

47
Q

What are the benefits/disadvantages of maraviroc?

A

Benefits:

-unique mechanism; remains active following resistance to other drugs

Disadvantages:

  • only effective against HIV that is tropic to CCR5 only; ineffective against CXCR4 only tropic and mixed tropic
  • requires expensive testing to determine tropism

(J2) HIV/AIDS (2 decks)

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