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Pharm 446 Final > HIV Part 2: ARVs > Flashcards

HIV Part 2: ARVs Flashcards

1
Q

What are the 5 classes of ANTIRETROVIRALS?

  • what is the suffix associated with each category?
  • describe their Moa.
  • what is the one CCR5 Antagonist?
A

1) Nucleoside Reverse- Transcriptase Inhibiotrs (NRTIs)
- no pattern of suffix. Think: TEAL –> tenofovir, emtricitabine, Abacavir, Lamivudine.
- moa: COMPETITIVELY blocks reverse-transcriptase by MIMICKING nucleosides and integrating into DNA, therebby halting replication process. [recall: RT enzyme converts RNA into DNA]

2) Non Nucleoside Reverse- Transcriptase Inhibiotrs (NNRTIs)
- VIRINES.
- moa: NON-COMPETITIVELY inhibits RTE by binding and causing conformational change.

3) Integrase Inhibiotrs:
- GRAVirs (grase and gravir)
- moa: blocks enzyme that INTEGRATES viral DNA into host genome.

4) Protease inhibitors:
- NAVIRS
- moa: targets protease enzyme, which PRVENTS virus from producing viral proteins.

5) CCR5 Antagonist:
- only one- Maraviroc (MVC)
- blocks the CCR5 receptor on CD4+ T cells to block HIV entry into cells.

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2
Q

What are the 4 main NRTIs?

A

Abacavir (ABC)
Emtricitabine (FTC)*
Lamivudine (3TC)*
Tenofovir (TDF or TAF)***

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3
Q

What are the 2 main NNRTIs?

A

Rilpivirine (RPV)
Doravirine (DOR)

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4
Q

What are the 3 main Integrase INhibitors?

A

Cabotegravir
Dolutegravir (DTG)
Bictegravir (BIC)

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5
Q

BIC is only available in coformulation with what 2 antivirals?

A

TAF/FTC (Tenofovir and Emtricitabine)

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6
Q

What are the 3 Antivirals that also have activity against Hep B?

A

Emtricitabine (FTC)*
Lamivudine (3TC)*
Tenofovir (TDF or TAF)***

**basically all the NRTIs except ABA.

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7
Q

What is the most common FIXED-DOSE COMBINATION Antiviral?

A

BIKTARVY (BIC + TAF + FTC): 1 integrase inhibitor + 2 NRTIs.

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8
Q

What are the 2 LONG-ACTING Antiretrovirals?
- what is the indication?
- Describe the regimen.

A

1) Cabotegravir (Integrase inhibitor) -think: CABS drive a LONG distnace.
2) Rilpivirine (NNRIT) - think: Rilp –> ripped
- indication: must be 12+ and at least 35 kg.
- Regimen: Intragluteal SC injection q 1-2 months.

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9
Q

What are the limitations of the LONG ACTING ARVs?

1) requires what kind of admin?.
2) volume?
3) what’s requried if miss sch. injection by 1 wk or more?

A

1) requires TWO intragluteal SC injectiosn on BOTH sides which requires coordination.
2) Requires LARGE VOLUMES = uncomfortable.
3) oral bridging requried if miss sch. injection by 1 wk or more.

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10
Q

WHEN should pts start ART (ARV therapy)?

A

Start in ALL PTS ASAP or as soon as dx (within days-wk) to dcr disease progression and transmission.

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11
Q

What are the benefits to starting ART ASAP? 3

A
  • pts most motiviated in beginning
  • gives sense of control after dx
  • dcr transmission
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12
Q

Describe the INITIAL ART REGIMEN recommended for MOST ppl with HIV?

  • what are the 4 options? what is the 2 drug regimen?
A

Integrase Inhibiotr based + 1 or 2 NRTs.

1) BIKTARVY ( BIC + TAF + FTC (emtricitabine))** most common.
2) Dolutegravir + Abacavir + Lamivudine
3) Dolutegravir + TDF or TAF + FTC
4) 2 Drug Regimens: Dolutegravir + Lamivudine.

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13
Q

What are the 2 conditions that must be met in order to give the 3 drug regiment with ABACAVIR? (dol + aba+ lam)?

A

1) pt must be HLA-B5701 NEGATIVE
AND
2) Negative for Chronic Hep B

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14
Q

The two drug regimen of Dol + Lam (minus Abacavir) can be just as effective in certain patients. To select the two drug regimen, what are the 3 conditions pts must meet?

A

1) viral load must be BELOW 500,000. NOT preferred if high viral load.
2) pt MUST NOT HAVE HepB (Cuz of incr risk of developing resistance to LAM monotherapy).
3) Genotypic REsistance testing is available (pts with HLA-B5701 allele can’t have ABACAVIR).

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15
Q

What are the 7 factors to consider when choosing an initial ART regimen?

A

– Baseline viral load
– Baseline antiretroviral resistance (if any)
– Food requirements - take w or w/o food.
– Co-infection with hepatitis B
– other comorbidiites: CKD, osteoporosis, cardiac diseases etc which can be worsened by ARV AEs.
– Pregnancy (or individuals of child-bearing
potential) –> less data in some drugs.
– Adverse effects and drug-drug interactions

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16
Q

What are the goals of ART?

1) VL < ?
2) restor eand preserve what?
3) dcr?
4) prevent?

A

1) Suppression and maintenance of VL to < 40 copies/mL
2) restore and preserve immunologic function
3) decrease HIV-related morbidity and mortality
4) prevent HIV transmission

17
Q

What are the 3 relevant labs in HIV? how frequently shoudl pts get them?

A

1) Genotypic Antiretroviral Drug Resistance
Testing (GART)
– @ Baseline and after trx failure

2) HIV viral load
– @ Baseline, q 1-2 months, then q 3-6 months

3) CD4+ cell count
– @ Baseline, then q 3- 6 months
- q yearly in stable pts.

18
Q

What are the 2 best tolerated NRTIs?

A

Lamivudine and Emtricitabine

19
Q
  • Which is the NEWER NRTI formulation? TDF or TAF?
  • What is the advatnage of TAF over TDF? What is the con?
  • What are the 2 big AEs associated with TDF?
  • Food requirements?
A

TAF= newer.
- dcr risk of renal impairment and dcr risk of effects on BMD cuz of dcr systemic exposure.
- con: associated with WEIGHT GAIN.

TDF AEs: incr risk of renal toxicity and associ with dcr BMD.

  • Can take TDF and TAF with or w/o FOOD.
20
Q

What is the biggest AE associated with ABACAVIR (NRTI)?
- what is it linked to?
- freq?
- What must you screen for in order to start abacavir?
- food requirements?

A

HYPERSENSITIVTY RXN –> linked to HLA- B5701 geene.
- freq: 5-6%.
- Sx: same as other HSN rxns.
- B/o starting abacavir, MUST SCREEN PTS FOR HLA-B5701 GENE (can only use if tests negative).
- food: +/-

21
Q

NNRTI AEs:
- What is the biggest issue with EFAVIRENZ?

  • What is the other AE asscoiated with Efavirenz and rilpilvirine?
  • what is the biggest concern with rilpivirine?
  • which is the best tolerated NNRTI?
  • what are the good requriements for efavirenz, rilpivirine, doravirine?
A

Efavirenz:
** causes NEUROPSYCH efffects (viivd dreams, nightmares, can worsen underlyign psych conditions).
- food: NO FOOD.

  • Rash.

–> Rilpivirine: less NS effects than Efavirenz, but depression is an AE.
- Rilpivirine Food: +++ MUST TKAE WITH AT LEAST 400 cal. avoid in food insecure.

–> Doravirine.
- food: +/-

22
Q

Protease Inhibitor AEs:
- What are the 3 biggest AEs assocaited with protease inhibitors?

A

1) GI upset (dairrhea, nauseua)
2) MEtabolic efects (hyperlipidemia and insulin resisntace/diabetes) –> dcr risk with Atanavir and danunavir.
3) Lipodystrophy (beer gut, buffalo hump)
–> also dcr with ataz and daranavir.

23
Q

What are the food requirements for ALL PROTEASE INHIBIOTRS?

A

ALL Protease inhibitors require FOOD admin –> better absorbed and dcr gi effects. -> think: needs PROTEIN

24
Q

How are Integrase inhibitors generally tolerated?
- What is the biggest concern (2)?

  • Weight gain is more pronounced with which 2integrase inhibiotrs?
  • is the incr in Scr an indication of kidney damage?
A

well tolerated.

1) Weight gain (more pronounced with DTG and BIC)
2) may incr Scr, altho thi sis NOT an indicator of kidney damage , it’s due to inhibition of OCT2 cation transporter.

25
Q

What are the 3 biggest mechanisms of ART drug interactions?

A

1) CYP 450 metabolism alterations
2) durgs that affect P-glycoprotein
3) Age related PHYSL changes

26
Q

Order the Antivirals in terms of risk for potential DDIs from HIGHEST to lowest risk.

A

1) Protease Inhibitors and Cobicistat
2) NNRTIs
3) CCR5 Antagonists
–> top 3 all substrates of Cyp3A4.

4) Integrase Inhibitors
–> substrates of UGTa1a and/or cyp3A4
5) NRTIs
–> lowest risk cuz eliminated by Kidney or Non-cyp routes.

27
Q

What is the interaction btwn the integrase inhibitors and co-admin with antacids or cations?
- describe management.

A
  • Chelation.
  • separate AV admin by 2 or more hrs or take with food.
28
Q

Interactions with Protease inhibitors/colbicistat nad CYP3A4 interact with…..

A
  • Fentanyl, oxycodone
  • Anticonvulsants (e.g.
    carbamazepine, phenytoin)
  • Antiplatelet agents
  • Anticoagulants
  • Calcium channel blockers (e.g.
    amlodipine, diltiazem, nifedipine)
  • Corticosteroids (e.g. inhaled
    fluticasone-budesonide,
    triamcinolone by injection)
  • Phosphodiesterase inhibitors
  • Psychotropics (e.g. aripiprazole,
    quetiapine, ziprasidone)
  • Statins (e.g. lovastatin, simvastatin)
    –> Baaasically everything
29
Q

Do protease inhibitors/colbicistat also interact with ADs, oral hypoglycmic meds, and Warfarin?

A

yes! via other cypp450 isoenzymes (2D6, 2c19. 2c9 etc).

30
Q

What booster agent is added to Protease Inhibitors to get better PK and allow for once daily dosing?
- what dose?

A

RITONAVIR 100 mg daily.
– atazanavir 300 mg/ritonavir 100 mg daily
– darunavir 800 mg/ritonavir 100 mg daily
– darunavir 600mg/ritonavir 100 mg twice daily

31
Q

What is the definition of trx failure?

A

Inability to achieve and maintain viral load < 200 copies/mL

32
Q

What are the 3 biggest causes of trx failure?

A

1) Pt adherence
Substance use, mental health disorders, unstable housing,
missed clinic appointments, interruption of access to ART,
cost, adverse effects, pill burden or dosing frequency

2) HIV related –> Drug-resistant virus, prior treatment failure

3) Antiretroviral-regimen Related:
* Suboptimal PK, virologic potency, low genetic barrier to
resistance, food requirements, drug-drug interactions,
prescription error

33
Q

Bcuz AVs work so well, pts will be living longer, so it’s important that they’re also living ________________.

A

healthy lives with good quality of life.

34
Q

What are the potential contributors to higher rates of comorbidities in ppl living with HIV?

A
  • Unconrolled viral replicaiton big risk factors for comordbiities.
    • Food isnecurity, smoking ( Higher rate of smoking in ppl with HIV), alcohol, drugs, lack exerccise etc.
    • Co-infections (HCV for eg) can incr comorbidities
  • chronic inflammation
  • AE effects of meds (Older HIV drugs (older Pis) in particular).
35
Q

HIV pts are more suscpetible to developing what classes of comorbidites?

A
  • cardiovascular disease, bone fractures, diabetes, renal failure, higher rates of cancer, neurological
    impairment, liver disease

Pharm 446 Final (9 decks)

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