Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

PHAR 557 > HIV - ARVs > Flashcards

HIV - ARVs Flashcards

(69 cards)

Start Studying
1
Q

T or F: Antiretroviral therapy is essentially a fn’al cure for HIV

A

T

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

T or F: ARVs can be used in any combination to tx HIV

A

F

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Six classes of HIV meds:

A

NRTIs (nucleoside reverse transcriptase inhibitors)

NNRTIs (non-nucleoside…)

Protease inhibitors

Integrase strand transfer inhibitors (INSTIs)

Fusion inhibitors

Chemokine receptor antagonist/entry inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What’re the standard NRTI combinations used in practice?

A
  1. TDF/FTC (tenofovir/emtricitabine)
  2. TAF/FTC (tenofovir/emtricitabine)
  3. ABC/3TC (abacavir/lamivudine)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

MOA of NRTIs

A

phosphorylated to triphosphate form > competitively binds to HIV reverse transcriptase > terminates DNA chain elongation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Which NRTIs are also active against HBV?

A

3TC, FTC, and TDF/TAF (tenofovir)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What’s unique about TDF?

A

It’s a nucleotide, not a nucleoside (i.e. it’s already phosphorylated)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Notable AEs of TDF?

A
  1. Fanconi syndrome (proximal tubule reabsorption problems)
  2. renal failure
  3. decreased BMD
  4. HBV flareup if d/c’ed
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

T or F: TDF is hepatotoxic.

A

F

it’s nephrotoxic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What should be monitored in pts taking TDF?

A

SCr, urine protein, BMD

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Why are TDF and TAF better than classic tenofovir?

A

because TDF and TAF are able to move from the gut into the blood and lymphoid cells, whereas classic tenofovir could not

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are some advantages of TAF over TDF?

A

Higher F and intracellular t1/2 > lower req’d dose and less plasma exposure to tenofovir

less renal tox (no Fanconi syndrome)

less eGFR effects

less BMD reductions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Why isn’t abacavir (ABC) used often

A

Convenience issues > ABC requires HLA-B testing to see if there’s a specific allele present (*5701) that increases risk of hypersensitivity rxn to it

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

ABC - If there is hypersensitivity to it, when would it show up?

A

At week 6 of ABC use

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

T or F: We should rechallenge ABC if hypersensitivity rxn occurs.

A

F > can result it death

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Which two NRTIs are distinguished by a single fluorine atom?

A

3TC and FTC (the “F” is for fluorine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

NNRTIs: MOA?

A

binds to hydrophobic pocket of reverse transcriptase > active site changes shape > disrupts DNA chain elongation (prevents natural nucleosides from being incorporated into viral DNA)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

NRTIs vs NNRTIs: which one is active against HIV-1? HIV-2? Both?

A

NRTIs: active against BOTH HIV-1/2

NNRTIs: active against HIV-1 only

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What’s the issue w/ first gen NNRTIs?

A

low genetic barrier to resistance (single mutation in viral genome confers resistance)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Half life profile of NNRTIs?

A

They’re long (>24h)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Name 3 NNRTIs:

A

RPV (rilpivirine), efavirenz (EFV), doravirine (DOR)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

How should rilpivirine be taken?

A

With foods that contain fat

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What reduces rilpivirine absorption?

A

Protein shakes, higher pH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

CI of rilpivirine?

A

PPIs, H2RAs, antacids (anything that reduces stomach acidity)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Important caution wrt RPV?
It prolongs QT interval > watch out when taking other drugs that do the same
26
Who should NOT receive RPV?
naive pts w/ viral loads >100,000 copies/mL > increased risk of tx failure
27
Major AEs of RPV?
severe rash, depression/mood changes, liver damange
28
How should efavirenz (EFV) be taken?
on an empty stomach
29
How is efavirenz affected by food?
its absorption is increased by high fat meals (hence why it should be taken on an empty stomach)
30
What kind of pts are given doravirine (DOR)?
Naive pts only
31
Name all NRTIs?
3TC, FTC, TAF, TDF, ABC
32
Protease inhibitor (PI) MOA?
inhibits the action of HIV-1/2 protease, an enzyme that cleaves two precursor proteins into smaller fragments.
33
Resistance profile of PI's?
Resistance is RARE (high genetic barrier to resistance)
34
What kinds of pts should use protease inhibitors?
pts who fail other regimens due to resistance, and pts who have poor adherence
35
What do PI's require to be taken concomitantly?
Pharmacokinetic booster
36
Name two PK boosters that may be used w/ PIs
ritonavir (RTV, /r), cobicistat (/c) (note: ritonavir is also a PI)
37
T or F: PIs can cause DM
T
38
RTV (/r, ritonavir) - How is absorption affected by food?
Its absorption is INCREASED by food
39
T or F: Cobicistat is used as a PI booster.
T
40
Cobicistat MOA:
CYP3A4 inhibitor (NOT a PI like ritonavir)
41
T or F: Cobicistat, like ritonavir, is a PI
F (it's a 3A4 inhibitor)
42
What may be observed while taking cobicistat?
Increased serum creatinine by 10-15 µmol/L
43
If an increase of creatinine is observed while taking cobicistat (/c), when should it be this med be stopped?
if SCr rises higher than 10-15 µmol/L
44
Which PI has the highest genetic barrier to resistance?
Darunavir (DRV)
45
Which PI is the most preferred?
Daruavir (DRV)
46
How should DRV be taken?
With food (reduces GI irritation + increases absorption)
47
How should atazanavir (ATV) be taken?
With food (NOT on an empty stomach)
48
What does atazanavir require for it to be absorbed?
acidic envir
49
What is an important AE of ATV (a PI)?
Hyperbilirubinemia (jaundice and scleral icterus)
50
Name the PIs:
darunavir (DRV), atazanavir (ATV), cobicistat (/c) (technically NOT a PI), and ritonavir (RTV, /r)
51
MOA of integrase strand transfer inhibitors (INSTIs)?
Inhibits translated retroviral DNA strand from being inserted into host cell genes
52
Which HIV types are targeted by INSTIs?
HIV-1 and 2
53
T or F: Currently, ALL first-line regimens are INSTI based.
T
54
T or F: INSTIs have few DIs and are better tolerated relative to other ARVs.
T
55
T or F: Despite their better AE profile, INSTIs reduce viral load v. slowly.
F quickly
56
List the INSTIs:
raltegravir (RAL) elvitegravir (EVG) dolutegravir (DTG) bictegravir (BIC)
57
How should RAL be taken?
w/o respect to meals (absorption is higher w/ high fat meal, however)
58
Important DI w/ RAL
Avoid Al and Mg salts > chelation > reduced absorption
59
How should elvitegravir be taken?
with food (increases absorption) and with cobicistat
60
EVG should be separated from _____ by at least 2h
antacids
61
Which INSTI has a lower barrier to resistance?
EVG (elvitegravir)
62
How should dolutegravir (DTG) be taken?
without respect to meals (food increases extent and slows rate of absorption, but not sig)
63
Important DI of DTG
Avoid cations (Al, Ca, Mg, Fe, Zn salts) > take DTG 2h before or 6h after
64
Important AE of DTG?
Increased ALT and AST > may result in acute hepatitis
65
Which population should avoid DTG?
Pregnant women (possible neural tube defects)
66
Which INSTI do we often put pts on?
bictegravir (BIC)
67
How should bictegravir be taken?
w/o regard to meals
68
Important DI involving bictegravir
Interaction w/ cations (Ca, Mg, Al, Fe, sucralfate)
69
Why is bictegravir usually the new standard tx?
Due to it being a small, single tablet

PHAR 557 (36 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions