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SBL > HIV Pharm > Flashcards

HIV Pharm Flashcards

1
Q

What are some Integrase Strand Transfer Inhibitors used to treat HIV?

A
  • raltegravir
  • dolutegravir
  • bictegravir
  • elvitegravir
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2
Q

What is the mechanism of action of INSTI’s?

A

-prevent the formation of covalent bonds between viral DNA and host DNA

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3
Q

Which two INSTI’s have a high genetic barrier to resistance?

A
  • dolutegravir

- bictegravir

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4
Q

Which INSTI is contraindicated in pregnancy and why?

A
  • dolutegravir

- -evidence of increased neural tube defects

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5
Q

Which characteristic of the retrovirus life cycle allows it to remain in the host for long periods of time?

A

-its ability to transfer its DNA into the host DNA (strand transfer)

–this is what’s blocked by Integrase Strand Transfer Inhibitors (INSTI’s)

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6
Q

Which INSTI needs to be boosted, with what, and why?

A

-elvitegravir needs to be boosted with cobicistat (a CYP inhibitor) because its metabolized by CYP3A4

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7
Q

What class of HIV drug is the primary “+1” active agent for treatment-naive patients?

A

Integrase Strand Transfer Inhibitors (INSTI’s)

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8
Q

Which population of HIV patients can be particularly challenging to treat and why?

A
  • elderly
  • -more comorbidities means more medications
  • -cognitive decline
  • -heightened risk of mood disorders
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9
Q

What is the usual regiment of antiretroviral therapy?

A

-a backbone of 2 NRTI’s (each targeting a different base) and one other active agent from a different drug class

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10
Q

What is the most commonly used NRTI backbone because of its superiority?

A
  • emtricitabine (cytidine analog)

- tenofovir (adenosine analog)

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11
Q

What happens when an HIV drug that is also effective against HBV is discontinued?

A

-rebound viremia of HBV

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12
Q

Which HIV drugs are also effective against HBV?

A
  • emtricitabine and lamivudine (cytidine analogs)

- tenofovir (adenosine analog)

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13
Q

What are some protease inhibitors used to treat HIV?

A
  • saquinavir
  • indinavir
  • darunavir
  • atazanavir
  • lopinavir
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14
Q

What is the mechanism of action of protease inhibitors?

A
  • competitive inhibition of viral aspartyl protease (homodimer) so that the virus can’t cleave (at the N-terminal side of proline residues) the ‘gag’ and ‘pol’ precursor peptides
  • HIV then can’t generate its reverse transcriptase, protease, or integrase, etc.
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15
Q

What metabolizes protease inhibitors and what is the consequence?

A

CYP3A4, which means that they inhibit the metabolism of other drugs

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16
Q

True or False: protease inhibitors are also substrates for P-glycoprotein (MDR1).

A

True. This means that they can influence and BE influenced by other drugs that are also transported by this mechanism.

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17
Q

What two drugs are used to “boost” levels of other protease inhibitors because of their role as CYP3A4 inhibitors?

A
  • ritonavir (more potent)

- cobicistat

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18
Q

What was the first protease inhibitor used to treat HIV and why is it no longer used?

A

–saquinavir, because of its pill burden

it only had a half life of 1-2 hrs

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19
Q

What is a unique side effect of indinavir?

A

-crystaluria and renal stones

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20
Q

What is a side effect of darunavir and why?

A
  • rash/hypersensitivity

- it’s a sulfa drug

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21
Q

Which protease inhibitor has the longest half-life and which has the second longest half-life when boosted by cobicistat?

A
  • darunavir (15 hrs)

- atazanavir (8 hrs)

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22
Q

What is a side effect of atazanavir?

A

-unconjugated hyperbilirubinemia (not associated w/ hepatitis)

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23
Q

Which protease inhibitor is not used much anymore, but did have a role in use after other protease inhibitors had failed?

A

lopinavir

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24
Q

What are entry inhibitors used to treat HIV?

A
  • enfurvatide (aka T20)

- maraviroc

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25
Q

What is the mechanism of action of maraviroc?

A

-blocks the binding of viral gp120 to CCR5 co-receptor on CD4 cell

–only active against CCR5-trophic viruses, not CXRCR4 or mixed-trophic viruses

26
Q

What are cons to using maraviroc that make it a seldomly-used drug?

A
  • the test to determine viral tropism is essential to determine if maraviroc will work, but the test is expensive
  • renal elimination, so if GFR is <60, the dosage needs to be adjusted
27
Q

What is the mechanism of action of enfuvirtide?

A

-T20 peptides prevent the conformational change of HIV that would normally allow it to form the hairpin structure necessary to enter the CD4 cell

28
Q

True or False: enfuvirtide is active against both HIV-1 and HIV-2.

A

False; enfuvirtide is NOT active against HIV-2

29
Q

What is the required method of administration of enfuvirtide and why?

A

-parenteral, because it’s a 36aa peptide, so if it were administered orally, it would be digested

30
Q

What NRTI is the only guanine analog?

A

abacavir

31
Q

What should be ruled out on a patient before you prescribe any ART including abacavir?

A

–HLA-B*5701 genotype, due to the risk of a potentially fatal hypersensitivity syndrome

32
Q

True or False: abacavir is effective against HBV

A

False

33
Q

To what class of anti-retroviral drug is HIV-2 intrinsically resistant?

A

–non-nucleoside reverse transcriptase inhibitors (NNRTI)

–NNRTI’s are only active against HIV-1

34
Q

What is the preferred sequence of the “+1” drugs in ART?

A

1) INSTI
2) protease inhibitor
3) NNRTI

35
Q

Which CYP is most commonly involved in HIV pharmacology?

A

CYP3A4

36
Q

What condition should you watch out for when administering tenofovir disoproxil fumarate (TDF) in patients with renal insufficiency?

A

Fanconi Syndrome

–avoid tenofovir disoproxil fumarate (TDF) in patients with a GFR < 60

37
Q

What are some NRTI’s and their analogous nucleoside?

A

-zidovudine (AZT) and stavudine are thymidine analogs

  • emtricitabine and lamivudine are cytidine analogs
  • abacavir is a guanosine analog
  • tenofovir is an adenosine analog
38
Q

True or False: NRTI’s must be phosphorylated to provide substrate for the enzymes.

A

True

39
Q

True or False: ART drugs eradicate the virus from cells that are already infected.

A

False; they only prevent the infection of susceptible cells

40
Q

What are common toxicities associated with NRTI’s?

A
  • lactic acidosis syndrome due to mitochondrial toxicity
  • peripheral neuropathy due to mitochondrial toxicity
  • pancreatitis due to mitochondrial toxicity
  • anemia
  • myopathy
41
Q

What was the first antiretroviral drug discovered?

A

zidovudine (AZT)

42
Q

What are toxicities associated with zidovudine (AZT)?

A
  • bone marrow suppression
  • skeletal muscle myopathy
  • hepatic steatosis
43
Q

What toxicities are associated with stavudine?

A
  • peripheral neuropathy
  • lipodystrophy and fat wasting!!!
  • lactic acidosis
  • hepatic steatosis
44
Q

For a treatment-naive patient with low HIV copy number, which dual drug combination is approved?

A

lamivudine and dolutegravir

an NRTI and an INSTI

45
Q

What is the mechanism of action of NRTI’s?

A

-inhibits native nucleotides from being incorporated into viral DNA and thus terminates elongation

46
Q

Between tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide (TAF), which has lower renal and bone toxicity? Why?

A

-tenofovir alafenamide (TAF) because its plasma concentration is lower

47
Q

What are some non-nucleoside reverse transcriptase inhibitors (NNRTI’s) used in ART?

A
  • doravirine (“best in class”)
  • efavirenz
  • etravirine
  • rilpivirine
  • nevirapine
48
Q

What is the most significant side effect of efavirenz?

A

-CNS toxicity

used to be considered teratogenic

49
Q

Which NNRTI has a unique ability in that it still works after mutations have occurred that disrupt the activity of other NNRTI’s?

A

-etravirine

50
Q

True or False: substance abuse disorders are prevalent among HIV patients and are a contraindication for ART.

A

False

51
Q

What is the maximum threshold for HIV RNA copies in the plasma for sexual transmission to remain unlikely?

A

<200 copies/mL

> 200 copies/mL requires extra methods to prevent transmission

52
Q

True or False: adding a single antiretroviral agent to a failing regimen is recommended.

A

False, because you risk a resistance to ALL drugs in the regimen if you do that.

53
Q

If HIV develops a resistance to doravirine, which other NNRTI’s will still work?

A

rilpivirine and etravirine

54
Q

Doravirine is a useful NNRTI after resistance to which other two NNRTI’s has developed?

A

rilpivirine or efavirenz

55
Q

The presence of which HIV co-receptor renders the virus resistance to maraviroc?

A

CXCR4

56
Q

What type of Phase II metabolism of antiretroviral drugs tends to result in less drug-drug interations?

A

glucuronidation

57
Q

What is the side effect of prolonged use of emtricitabine?

A

-hyperpigmentation of palms and soles (particularly in African Americans)

58
Q

What are some side effects of tenofovir disoproxil fumarate (TDF)?

A
  • nephrotoxicity w/ acute tubular necrosis

- decreased bone density that stabilizes

59
Q

True or False: NNRTI’s (efavirenz, etravirine, rilpivirine, doravirine, nevirapine) need to be phosphorylated to be active.

A

False

60
Q

What is the mechanism of action of NNRTI’s?

A

-bind to hydrophobic pocket of HIV reverse transcriptase as a non-competitive antagonist

61
Q

What is the last resort antiretroviral therapy that is approved for use only in treatment-experienced patient when the virus is replicating despite being on ART?

A

enfuvirtide

62
Q

True or False: a single exposure to nevirapine (an NNRTI) as monotherapy can cause HIV to become resistant to it in one-third of patients.

A

True

SBL (4 decks)

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