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Pharm 321 HIV > Therapeutics Slide Deck 2 > Flashcards

Therapeutics Slide Deck 2 Flashcards

1
Q

Antiretroviral classes

Antiretroviral classes

A

NRTI, NNRTI, PI, INSTI, Attachment & Entry Inhbiitors, Capsid Inhibitor

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2
Q

What are the drugs for NRTI?

A

TDF, TAF, FTC, 3TC, ABC, ZDV

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3
Q

What drugs belong to NNRTI?

A

DOR, RPV, EFV, NVP, ETR

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4
Q

What drugs belong to PI?

A

DRV/r or DRV/c, ATV/r, LPV/r

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5
Q

What are the drugs for INSTI?

What are the drugs for INSTI?

A

CAB, BIC, DTG, EVG/c, RAL

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6
Q

Attachment and Entry Inhibitors?

A

T-20, MVC, FTR, IBA

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7
Q

Capsid Inhibitor ?

A

LEN

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8
Q

TDF stands for?

A

Tenofovir** d**isoproxil fumarate (TDF)

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9
Q

TAF stands for?

A

Tenofovir** alaf**enamide

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10
Q

FTC stands for?

A

Emtricitabine

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11
Q

3TC stands for?

A

Lami-vudine

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12
Q

ABC stands for?

A

ABA-cavir

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13
Q

ZDV stands for?

A

Zido-vudine

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14
Q

What does DOR stand for?

A

DORAVIRINE

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15
Q

What does RPV stand for?

A

Rilpivirine

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16
Q

What does EFV stand for?

A

Efavirenz

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17
Q

What does NVP stand for?

A

Nevirapine

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18
Q

What does ETR stand for?

A

Etravirine

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19
Q

PIs: DRV is what and given with what?

A

DRV: Darunavir
can be given with (r) or (c)

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20
Q

PIs: What is ATV and what is it given with?

A

Atazanavir and given with (r)

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21
Q

PIs: What does LPV stand for and what is it given with?

A

LPV= Lopinavir and given with r

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22
Q

CAB stands for what?

A

Cabotegravir

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23
Q

BIC stands for what?

A

Bictegravir

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24
Q

DTG stands for what?

A

Dolutegravir

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25
Q

EVG stands for what? anything unusual for this?

A

Elvitegravir and given with booster (c)

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26
Q

RAL stands for what?

A

Raltegravir

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27
Q

T-20 stands for what?

A

Enfuvirtide

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28
Q

MVC stands for what?

A

Maraviroc

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29
Q

FTR stands for what?

A

Fostemsavir

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30
Q

IBA stands for what?

A

Ibalizumab

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31
Q

LEN stands for what?

A

LENA-capavir

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32
Q

HIV Drug Therapy Key Points:

What are the possible combinations of typical ART regimens?

A

2 NRTIs + INSTI
2 NRTIs + PI+PK enhancer
2 NRTIs + NNRTI

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33
Q

When to take PK boosters ?

A

At the same time as ARV drug being boosted

34
Q

Ritonavir:

A

Protease inhibitor, causes adverse GI evenrs, taste disturbances, hyperlipidemia, insulin resistance.

35
Q

Cobicistat

A

only as part of combo, adverse GI events, inhibits CrCl via MATE1 inhibition, but eGFR is not affected/

36
Q

The (5) 1st Line ARV regimens for most HIV Tx Naive Patients

A

1). BIC/FTC/TAF
2). DTG + FTC/TAF
3). DTIG+ FTC/TDF
4). DTG/ABC/3TC
5). DTG/3TC

37
Q

Selecting Initial ART: Pt characteristics

A

Pre-Tx HIV-1 RNA
Pre-Tx CD4 count
HIV genotype results
HLA-B*5701 status
Individual preferences Anticipated adherence
ART timing post-diagnosis

38
Q

Selecting Initial ART: Regimen-specific considerations

A

1) Barrier to resistance
2) Potential AEs and drug toxicities, including risk of development of comorbid diseases
3) Known/potential DDIs
4) Convenience
5) Cost and access

39
Q

Selecting Initial ART: Presence of specific conditions/factors

A

1) Comorbid conditions
2) Pregnancy or wish to become pregnant
3) Coinfections: HVC, HCV, TB

40
Q

Step #1 The _ _ _ _ backbone . Identify the drugs that belong to this class

A

The Nucleoside Reverse Transcriptase Inhbitors
- TDF (Tenofovir disoproxil fumarate)
**- TAF **(Tenofovir AlaFenamide)
- **ABC (Abacavir)
- FTC **(Emtricitabine)
- **3TC **( Lamivudine)

41
Q

HSR is a reaction to what?

A

Abacavir Hypersensitivity Reaction (HSR)

42
Q

AHS reactions can cause what symptoms and median onset? Aggrevating/Remitting factors?

A
  • Non-specific symptoms:
    fever, rash, GI, malaise, respiratory issues
  • median onset is 9 days
  • sx worsen if continuation fo drug, will reverse if stopped
43
Q

HLA-B*5701 test is what for?

A

If positive= Do not initiate abacavir.
* Very strong association between HLA-B5701 presence and abacavir HSR
If positive, 40-50% chance of abacavir HSR
* Should screen for HLA-B5701 before starting on abacavir- screen once in lifetime
* White pts have higher risk
* A negative HLA-B*5701 result doesn’t absolutely rule out the possibility of some form of ABC HSR

44
Q

Is ABC still recommended as initial therapy in most people with HIV/ concerns?

A

NO! Hard to start ARVs w/in 7 days when it takes > 7days to get HLA*B5701 result back in developed world.
NO large advantage over DTG/3TC alone

45
Q

TDF vs TAF
What are both their advantages compared to ABC?

A
  • They are both active against HBV
  • They both dont require HLAB5701 testing
  • TDF is associated with favorable lipid effects
46
Q

TDF vs TAF. What are each others advantages?

A
  • TDF= better lipid profile
  • TAF= better on renal markers and BMD
47
Q

What is the advantage of ABC compared to TAF/TDF? What pts could we use it in?

A

No dose adjustment in Renal pts, no nephrotoxicity and less BMD effects than either of them
**Use in pts with renal dysfunction or BMD issues? **

48
Q

Disadvantages of TDF?

A
  • decline in kidney function
  • proximal renal tubulopathy= proteinuria, phosphate wasting
  • BMD reductions due to phosphate wasting
49
Q

Disadvantages of TAF?

A
  • bad bad for lipids
  • more weight gain than TDF
50
Q

Disadvantages of ABC?

A
  • Requires HLA*B5701
  • unsolved MI risk
51
Q

What are the doses of TDF, TAF, and ABC?

A

TDF= 300 mg OD
TAF= 10 mg OD when given with boosted PI/Cobicistat boosted elvitegravir
or 25 mg OD when given with non boosted ARVs
ABC= 600 mg OD

52
Q

Renal adjustment in HIV Tx for TDF and TAF

A

TDF= Recommended for CrCl < 50mL/min

TAF=Not required if CrCl > 15 mL/min
*Cavet: TAF is co-formulated with FTC when used to treat HIV infection; b/c FTC has renal dose adjustment recommendations for CrCl < 30mL/min, TAF containing regimens aren’t recommended if CrCl < 30mL/min and patient not on hemodialysis.

53
Q

FTC (Emtrici-tabine). What is the dose, and active against what?

A

200 mg daily and active against HBV as well

54
Q

3TC (Lamivudine)

A

Standard dose 300 mg daily , commonly used with ABC
Active against HBV as well
Product monograph will tell you to dose reduce if renal function is < 50 mL/min…… but in practice this varies due to available only in 300 mg or 150 mg tablets, as a study showed that pts with renal function issues can tolerate normal doses of lamivudine

55
Q

All patients with coinfection of HIV & HBV should receive ARV regimen that……

A

Includes 2 drugs with activity against HBV:

TAF or TDF + FTC or 3TC

56
Q

INSTI (integrase strand inhibitor). What are the two players and their doses?

A

Bictegravir (BIC) - 50 mg
Dolutegravir (DTG)- 50 mg OD (Tx/INSTI naive) or 50 mg BID (INSTI resistance or in Tx/INSTI naive when given with enzyme inducers)

57
Q

Bictegravir side effects?

A

Diarrhea
Nausea
Headache
Weight gain

58
Q

Dolutegravir side effects?

A

Insomnia
Headache
Depression and suicidal ideation
(rare; usually in patients with pre- existing psychiatric conditions)
Weight gain

59
Q

What are the benefits of the INSTIs?

A

High efficacy, tolerability, safety, high barrier to resistance, few DI, low pill burden

60
Q

Explain the SCr change we see with bictegravir and dolutegravir or elvitegravir/c ?

A

SCr INCREASES by approx. 8 to 13 umol/L occurs within the first 4 weeks of bictegravir and dolutegravir (and elvitegravir/c)- eGFR decreases (but does not mean kidneys are worsening). Tx due to inhibition of renal proximal tubule secretion of creatinine but remains stable thereafter.

61
Q

THIRD STEP: add Step 1 & Step 2 together (2 NRTI + 1 INSTI approach)

A

BIC/FTC/TAF= Biktarvy
DTG+ FTC/TAF= Tivicay + Descovy
DTG+ FTC/TDF= Tivicay+ Truvada
DTG/ABC/3TC= Triumeq

62
Q

What are the advantages of single tablet regimens?

A

Simplicity, convenience, fewer copays, reduces selective nonadherence to components of regimen

63
Q

What are the disadvantages of single tablet regimens?

A

inability to adjust dosages of components if needed to drug-drug interactions or tolerability issues (renal insufficiency), not available for all ART regimens, and not available for all NRTI pairings

64
Q

When can we use 2 ARV drug regimen? (i.e., Dovato (DTG+3TC) Dolutegravir/lamivudine

A

Tx-Naive PLWH, contains 50 mg DTG, 1 pill once a day. Who is this NOT for?
* HIV Viral Load > 500,000 copies/mL,
* HBV co-infection
* ART being started before the results of HIV genotype resistance testing or HBV testing are available
* MAYBE if CD4 count < 200 cells/mm3 ????????

65
Q

What drug can we use in pregnancy and in situations where more long-term clinical experience is needed? (i.e., chemo or TB Tx)

A

Tenofovir prodrug (TDF or TAF) + emtricitabine + raltegravir

66
Q

side effects of raltegravir ??

A

WEIGHT gain, insomnia, uncommon CK elevation, muscle weakness, and rhabdomyolysis, Rare (TEN or SJS, rashes)

67
Q

Raltegravir (RAL) - old INSTI

A

either 400 mg BID or 1200 mg PO OD. Benefits: low resistance barrier, higher pill burden, less convenient BID dosing

68
Q

Elvitegravir- old INSTI

A

low barrier to resistance, PK booster needed (cobicistat), required which means +++ drug interactions

69
Q

When would we use Stribild, Genvoya (Tenofovir prodrug, emtricitabine, + elvitegravir/cobicistat)

A

This player isn’t going to get any field time anymore….

70
Q

What if we can’t/don’t go with an INSTI containing regimen?

A

Could prop up the PI or revive the NNRTI as the 3rd wheel for the NRTI backbone

71
Q

Protease Inhibitor (PI)s . What is a current drug example and a benched one?

A

Darunavir (DRV) Dosing: 1) 800 mg PO daily with Food for Tx/PI naive- boost with ritonavir 100 mg PO daily or Cobicistat 150 mg PO daily
2) 600 mg PO BID for Tx experienced with at least 1 of 11 darunavir reisstance assoicated mutations (RAMs) - boost with ritonavir 100 mg PO BID

72
Q

Atazanavir (ATV) is a benched player

A

-Has moderate barrier to resistance, low gastric pH required for absorption so PPI contraindicated, bilirubin is a surrogate marker for checking adherence
- atazanavir inhibits UGT1A1 to cause unconjugated hyperbilirubinemia (benign), but unless jaundice or scleral icterus happens, we dont have to stop

73
Q

What is the benfit of darunavir? In what patients would we use this?

A

Benefit is that darunavir (DRV) has a HIGH barrier to resistance so we can use it in people who have been HIV+ for a long time, since the 90’s, as they probably have complex resistance profiles

74
Q

What are the common protease inhbiitor side effects?

A

1) Nausea
2) GI intolerance
3) Diarrhea
& can also have increase in lipids, triglycerides, can have some CVD risks

75
Q

NNTRIs. What are these? Who could we use it for?

A

Non-nucleoside reverse transcriptase inhibitors (NNRTIs). Potential niche area for those experiencing s/e with INSTIs use like extreme weight gain

76
Q

What are the two key players that are NNRTIs? Whats a retired player?

A

Dora-VIRINE (DOR)
Rilpi-VIRINE (RPV)
retired- Efavirenz (EFV)

77
Q

DORAvirine

A

-Resistance to both DOR and NRTIs at virologic failure
-Combo product is with TDF rather than TAF (only tenofovir combo product with 3TC)
**TDF/DOR/3TC **

78
Q

Rilpivirine (RPV)

A
  • Higher rates of virologic failure in patients with HIV VL > 100,000 copies/mL, CD4 counts < 200 cells/mm³
  • Requires an acidic environment for absorption
    PPI contraindicated
79
Q

Counselling for Doravirine?

A

100 mg PO once daily, with or without food

80
Q

Counselling for rilpivirine?

A

25 mg PO once daily with a MEAL containing at least 390 calories

81
Q

Efavirenz counselling and when would we see efavirenz?

A

600 mg PO HS
OR 400mg daily studied in ENCORE-1 and found to be non-inferior for viral suppression with fewer efavirenz related s/e vs. 600 mg daily.
A STR with efavirenz 400mg/ TDF/ lamivudine is available in some countries (400mg daily dose not studied in pregnant women or TB/HIV co-infx)
Empty stomach to reduce CNS s/e (high fat foods increases absorption by 50%)

82
Q
A

Pharm 321 HIV (1 decks)

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