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obgyn > HIV > Flashcards

HIV Flashcards

1
Q

Tenofovir Disoproxil (TDF) + emtricitabine (FTC)

A

Truvada
PrEP - preventative

Bone and kidney toxicity

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2
Q

Tenofovir Alafenamide (TAF + emtricitabine (FTC)

A

Descovy
PrEP - preventative
New in 2019, less toxicity

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3
Q

Cabotegravir for PrEP

A

Apretude
PrEP - preventative

1st long-acting injectable integrase inhibitor (q8 weeks)

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4
Q

Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) MOA

A

Inhibit conversion of HIV RNA to DNA by blocking the function of reverse transcriptase

Inhibits RT at active site and terminates DNA chain

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5
Q

Second generation NRTI

A

Abacavir (ABC)
Emtricitabine (FTC)
Tenofovir disoproxil fumarate (TDF)

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6
Q

Third generation NRTI

A

Tenofovir alafenamide (TAF)

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7
Q

NRTI side effects

A

Inhibition of mitochondrial DNA functon and replication can lead to:

  • Lactic acidosis (rare, can occur at any time)
  • Hepatic steatosis
  • 1st gen associated with: peripheral neuropathy, lipodystrophy - may never resolve
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8
Q

Emtricitabine and Lamivudine general

A

Current backbone of recommended ART

Interchangable but NEVER use in conjunction

Active against hepB - when discontinuing in HIV + HepB patient, HBV rebound and worsening hepatitis can occur

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9
Q

Emtricitabine and lamivudine adverse effects

A

Most well tolerated NRTI
Rare: headache, nausea, fatigue

  • Require dosing adjustment with CrCl < 50mL/min
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10
Q

Triumeq

A

Abacavir + lamivudine + dolutegravir

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11
Q

Abacavir AE

A

Hypersensitivity syndrome: typically w/in 2-6 weeks initiation… fever, abdominal pain, and rash, fatal when re-challenged

Associated with HLA-B*5701 allele (test before starting abacavir)

Other: increased CVD risk in patients with underlying disease

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12
Q

Tenofovir formulations

A

Nucleotide adenosine 5i-monophosphate derivative

Tenofovir disoproxil fumarate (TDF): decreases bone mineral density, decrease CrCl over time, fanconi syndrome (rare)

Tenofovir alafenamide (TAF): greater antiviral activity, lower dosing allowing for decrease in AE

TAF > TDF (rather have an A, than a D)

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13
Q

Truvada

A

TDF + emtricitabine

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14
Q

Descovy

A

TAF + emtricitabine

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15
Q

Non-Nucleoside reverse transcriptase inhibitors (NNRTIs) MOA

A

Inhibit conversion of HIV RNA to DNA by blocking function of reverse transcriptase

Binds RT at non-active site

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16
Q

Describe resistance in NNRTI

A

low barrier of resistance - single point mutation in RT can inactivate all members of class (some exceptions)

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17
Q

NNRTI drug interactions

A

CYP450 substrates, some also inducers/inhibitors

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18
Q

NNRTI adverse effects

A

Hypersensitivity reactions (rash), increased liver enzymes, diarrhea, pruritis

neurological/psychiatric (efavirenz&raquo_space;> etravirine&raquo_space; rilpivirine > doravirine)

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19
Q

first generation NNRTIs

A

Nevirapine
Efavirenz*
Delavirdine

Mod-high potentcy, some treatment failure, most common. resistance mutation: K103N

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20
Q

second generation NNRTIs

A

Etravirine
Rilpivirine*
Doravirine

higher potency, rarely associated with treatment failure, no effect of K103N

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21
Q

Efavirenz

A

Neuropsychiatric AE: vivid dreams, insomnia, hallucinations, dizziness, difficult concentrating, suicidal ideation
Teratogenic
Hepatotoxicity
Rash - maculopapular to SJS and TEN

Not used as much anymore

22
Q

Efavirenz drug interactions

A

CYP3A4 substrates (carbamazepine, posaconazole)

23
Q

Rilpivirine general

A

Well tolerated (fewer AE than efavirenz) but not as potent

More failures when Vl > 100,000 or CD4+ <200

24
Q

Rilpivirine drug interactions + other

A

Plasma concentrations influenced by various CYP enzymes - protease inhibitors and azole antifungals increase plasma RPV levels

CI with strong CYP3A4 inducers

Needs ACIDIC environment for absorption (PPI are CI; can do H2 receptor antagonist at least 12 hours before)

25
Q

Odefesy

A

TAF + emtricitabine + rilpivirine

26
Q

Juluca

A

Rilpivirine + dolutegravir

27
Q

Cabenuva

A

Rilpivirine + cabotegravir

28
Q

Protease inhibitors MOA

A

Inhibition of HIV protease enzyme, preventing formation and release of mature virons

High barrier to resistance, potent viral efficacy

Need pharmacokinetic booster

29
Q

Third generation PI

A

Atazanavir
Darunavir

As go from first –> 3rd, decrease in AE: lipodystrophy, N/V, diarrhea, cholesterolemia, insulin resistance

30
Q

Protease Inhibitors AE

A

Most common with 1st gen (ritonavir, indinavir, saquinavir, nelfinavir)

GI intolerance: N/V, diarrhea
Lipodystrophy: long term complications resulting from metabolic and morphologic abnormalities (fat atrophy and deposition)
Lipid abnormalities (hypertriglyceridemia, cholesterolemia, lipoaccumulation - lopinvair/ritonavir highest risk)
31
Q

Protease inhibitors class effects

A

Cardiovascular risk: dyslipidemia, insulin resistance, atherosclerosis, myocardial infarction

Major drug interactions due to booster (CYP3A4, CYP2D6)

Food effects bioavailability

32
Q

boosted protease inhibitor regimens

A

addition of booster –> inhibition of CYP34A –> reduced metabolism of PI –> lower dosing frequency/better blood concentrations

boosters: ritonavir or cobicistat

33
Q

Atazanavir

A

Don’t use with hepatic impairment
take with food
needs acidic environment
CI with CYP34A

usually active in patients who have failed other PI

34
Q

Atazanavir adverse effects

A

N/V/D
hyperbilirubinemia +/- jaundice or scleral icterus
nephrolithiasis + cholelithiasis
lower cardio risk vs other PI

35
Q

Darunavir

A

Can be considered alternative first line treatment in some treatment naive

AE: well tolerated, favorable lipid profile compared to other PI, possible higher CVD risk vs atazanavir

drug-drug: CYP34A

36
Q

Symtuza

A

darunavir-cobicistat-TAF-emtricitabine

37
Q

Prezcobix

A

darunivir-cobicistat

38
Q

Integrase strand transfer inhibitors (INSTIs) MOA

A

prevents the insertion of DNA (transcribed from the virus) into human cell DNA by inhibiting integrase enzyme

39
Q

first gen INSTI

A

Raltegravir

Elvitegravir

40
Q

second gen INSTI

A

Dolutegravir

Bictegravir

41
Q

third gen INSTI

A

cabotegravir

42
Q

Raltegravir

A

twice day dosing (use declining)

found to be inferior to dolutegravair

43
Q

elvitegravir

A

can only get in combo pills: stribild, genvoya
some nausea, diarrhea

MAJOR 34A inhibitor
resistance may infer cross resistance w/ raltegravir

44
Q

Dolutegravir

A

Preferred INSTI

AE: decreases tubular secretion of creatinine, weight gain, neuropsychiatric effects (depression, anxiety, sleep disturbances), neural tube defects?

45
Q

Bictegravir

A

First-line recommendation! high barrier to resistance, small single tablet, well-tolerated

Biktarvy: bictegravir + emtricitabine + TAF

46
Q

cabotegravir

A

long-acting injectable in combo with injectable rilpivirine (Cabenuva) - monthly injection

extended release injectable (apretude) - q8 week injection for PrEP

47
Q

entry inhibitors

A

Subclasses
CD4 post-attachment inhibitor
CCR5 coreceptor antagonist
Fusion inhibitors

48
Q

Fusion inhibitors

A

Enfuviritide (Fuzeon) - binds to gp41 and prevents attachment of HIV virus to T-cell

AE: injection site reactions, sclerotic lesions

49
Q

monitoring ART

A

measure HIV RNA (viral load): prior to start, 4-6 weeks after initiation, every 1-2 months, every 3-6 months, etc.. as viral load decreases
GOAL: undetectable at 16-24 weeks.

measuure CD4 count: monitor every 3-6 months
GOAL: increase by 50-150 in 1st year

50
Q

PEP

A

3 drug regimen preferred
- TDF/FTC + RAL (occupational)
- Truvada + Isentress or Tivicay (nonoccupational)
Reasonable to substitute TAF or other INSTI

Duration: 4 weeks

obgyn (14 decks)

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