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HIV Pharm Flashcards

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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
What is the mechanism of action of maraviroc?
-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
What are cons to using maraviroc that make it a seldomly-used drug?
- 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
What is the mechanism of action of enfuvirtide?
-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
True or False: enfuvirtide is active against both HIV-1 and HIV-2.
False; enfuvirtide is NOT active against HIV-2
29
What is the required method of administration of enfuvirtide and why?
-parenteral, because it's a 36aa peptide, so if it were administered orally, it would be digested
30
What NRTI is the only guanine analog?
abacavir
31
What should be ruled out on a patient before you prescribe any ART including abacavir?
--HLA-B*5701 genotype, due to the risk of a potentially fatal hypersensitivity syndrome
32
True or False: abacavir is effective against HBV
False
33
To what class of anti-retroviral drug is HIV-2 intrinsically resistant?
--non-nucleoside reverse transcriptase inhibitors (NNRTI) --NNRTI's are only active against HIV-1
34
What is the preferred sequence of the "+1" drugs in ART?
1) INSTI 2) protease inhibitor 3) NNRTI
35
Which CYP is most commonly involved in HIV pharmacology?
CYP3A4
36
What condition should you watch out for when administering tenofovir disoproxil fumarate (TDF) in patients with renal insufficiency?
Fanconi Syndrome --avoid tenofovir disoproxil fumarate (TDF) in patients with a GFR < 60
37
What are some NRTI's and their analogous nucleoside?
-zidovudine (AZT) and stavudine are thymidine analogs - emtricitabine and lamivudine are cytidine analogs - abacavir is a guanosine analog - tenofovir is an adenosine analog
38
True or False: NRTI's must be phosphorylated to provide substrate for the enzymes.
True
39
True or False: ART drugs eradicate the virus from cells that are already infected.
False; they only prevent the infection of susceptible cells
40
What are common toxicities associated with NRTI's?
- lactic acidosis syndrome due to mitochondrial toxicity - peripheral neuropathy due to mitochondrial toxicity - pancreatitis due to mitochondrial toxicity - anemia - myopathy
41
What was the first antiretroviral drug discovered?
zidovudine (AZT)
42
What are toxicities associated with zidovudine (AZT)?
- bone marrow suppression - skeletal muscle myopathy - hepatic steatosis
43
What toxicities are associated with stavudine?
- peripheral neuropathy - lipodystrophy and fat wasting!!! - lactic acidosis - hepatic steatosis
44
For a treatment-naive patient with low HIV copy number, which dual drug combination is approved?
lamivudine and dolutegravir | an NRTI and an INSTI
45
What is the mechanism of action of NRTI's?
-inhibits native nucleotides from being incorporated into viral DNA and thus terminates elongation
46
Between tenofovir disoproxil fumarate (TDF) and tenofovir alafenamide (TAF), which has lower renal and bone toxicity? Why?
-tenofovir alafenamide (TAF) because its plasma concentration is lower
47
What are some non-nucleoside reverse transcriptase inhibitors (NNRTI's) used in ART?
- doravirine ("best in class") - efavirenz - etravirine - rilpivirine - nevirapine
48
What is the most significant side effect of efavirenz?
-CNS toxicity | used to be considered teratogenic
49
Which NNRTI has a unique ability in that it still works after mutations have occurred that disrupt the activity of other NNRTI's?
-etravirine
50
True or False: substance abuse disorders are prevalent among HIV patients and are a contraindication for ART.
False
51
What is the maximum threshold for HIV RNA copies in the plasma for sexual transmission to remain unlikely?
<200 copies/mL >200 copies/mL requires extra methods to prevent transmission
52
True or False: adding a single antiretroviral agent to a failing regimen is recommended.
False, because you risk a resistance to ALL drugs in the regimen if you do that.
53
If HIV develops a resistance to doravirine, which other NNRTI's will still work?
rilpivirine and etravirine
54
Doravirine is a useful NNRTI after resistance to which other two NNRTI's has developed?
rilpivirine or efavirenz
55
The presence of which HIV co-receptor renders the virus resistance to maraviroc?
CXCR4
56
What type of Phase II metabolism of antiretroviral drugs tends to result in less drug-drug interations?
glucuronidation
57
What is the side effect of prolonged use of emtricitabine?
-hyperpigmentation of palms and soles (particularly in African Americans)
58
What are some side effects of tenofovir disoproxil fumarate (TDF)?
- nephrotoxicity w/ acute tubular necrosis | - decreased bone density that stabilizes
59
True or False: NNRTI's (efavirenz, etravirine, rilpivirine, doravirine, nevirapine) need to be phosphorylated to be active.
False
60
What is the mechanism of action of NNRTI's?
-bind to hydrophobic pocket of HIV reverse transcriptase as a non-competitive antagonist
61
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?
enfuvirtide
62
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.
True

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