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Flashcards in HIV Pharm Deck (47)
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1

What are the main classes of HIV drugs?

  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

2

What does a normal ART regimen look like?

What classes are first, second, and thrid line?

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

 

3

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

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

4

What are NRTIs?

Nucleoside reverse transcriptase inhibitors:

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

5

What black box warning is associated with NRTIs and why?

-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

6

What is a common suffix in NTRIs?

"-vudine"

 

not found in all NTRIs

7

What is zidovudine (AZT)?

What if any toxicities are associated with it?

NRTI ("-vudine")

 

-thymidine analog, needs phosphorylation

 

Toxicities:

-myelosupression -> cytopenias

-lipodystrophy (common to thymidine analogs)

-mitochondrial toxicity (common to all NTRIs)

8

What is stavudine (d4T)?

What if any toxicities are associated with it?

NRTI ("-vudine")

 

-thymidine analog, needs phosphorylation

 

Toxicities:

-peripheral neuropathy

-lipodystrophy (*most prominent in stavuidne*)

-mitochondrial toxicity  (common to all NTRIs)

9

What is emtricitabine (FTC)?

What if any toxicities are associated with it?

NRTI 

 

-cytosine analog, needs phosphorylation

 

Toxicities:

-hyperpigmentation of palms and soles (common in AAs)

-one of the least toxic

10

What is lamivudine (3TC)?

What if any toxicities are associated with it?

NRTI  ("-vudine")

 

-cytidine analog, needs phosphorylation

 

Toxicities:

-peripheral neuropathy

-one of the least toxic

11

What is abacavir (ABC)?

What if any toxicities are associated with it?

NRTI

 

-guanosine analog (only one), needs phosphorylation

 

Toxicities:

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

12

What is tenofovir disoproxil fumarate (TDF)?

What if any toxicities are associated with it?

NRTI

 

-adenosine analog, already phosphorylated

 

Toxicities:

-nephrotoxicity -> (Fanconi syndrome)

-decreased bone density

13

What is tenofovir alafenamide (TAF)?

What if any toxicities are associated with it?

NRTI

 

-adenosine analog, already phosphorylated

 

Toxicities:

-well tolerated

-lower plasma concentrations that TDF -> less risk of renal and bone s/x

14

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

-zidovudine

15

What NRTI(s) is also effective against HTLV?

-zidovudine

16

What NRTI(s) is also effective against HBV?

-emtricitabine (both C)

-lamivudine (both C)

-tenofovir

17

What NRTIs are often co-formulated?

-emtricitabine / lamivudine (cytosine)

-tenofovir (adenosine)

18

What are INSTIs?

Integrase strand transfer inhibitors:

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

19

What is a common suffix in INSTIs?

"-tegravir"

 

inteGRAse

20

What is raltegravir?

What if any toxicities are associated with it?

INSTI ("-gravir")

 

Toxicities:

-generally well tolerated

-immune reconstitution syndrome

-rhabdomyolysis

-hypersensitivity reaction

21

What is dolutegravir?

What if any toxicities are associated with it?

INSTI ("-gravir")

 

Toxicities:

-generally well tolerated

-possible neural tube defects w/ pregnancy

-immune reconstitution syndrome

-rhabdomyolysis

-hypersensitivity reaction

22

What is bictegravir?

What if any toxicities are associated with it?

INSTI ("-gravir")

 

comes only in combination with other drugs

 

Toxicities:

-generally well tolerated

23

What makes INSTIs first line "+1" ART drugs?

-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

What are protease inhibitors?

inhibit cleavage of HIV precursor proteins into active proteins

 

target:

-homodimer asrpartyl protease (cleaves proline)

-human aspartyl proteases are monomers and not affected

25

What is a common suffix in protease inhibitors?

"-navir"

26

What is darunavir?

What is special about it?

Protease inhibitor ("-navir")

 

-current first choice PI

-sulfa drug -> possible hypersensitivity

27

What is atazanavir?

What is special about it?

Protease inhibitor ("-navir")

 

-elevated unconjugated bilirubin w/o hepatitis

28

What is lopinavir?

What is special about it?

Protease inhibitor

 

-often works after failure of other PIs

29

What is indinavir?

Whats special about it?

protease inhibitor ("-navir")

 

-not used any more due to crystaluria/renal stone

30

What are common toxicities of protease inhibitors?

-dyslipidemia

-immune reconstitution syndrome

-GI symptoms