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PR3151 Finals > HIV > Flashcards

HIV Flashcards

1
Q

RTI

A

1) Nucleoside (NRTI)
Pyrimidine (Cytidine) Analogues
- Lamivudine
- Emtricitabine
Pyrimidine (Thymidine) Analogues
- Zidovudine
Purine (Guanosine) Analogues
- Abacavir
Purine (Adenosine) Analogues
- Tenofovir Disoproxil Fumarate

2) Non-Nucleoside (NNRTI)
- Efavirenz
- Rilpivirine

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2
Q

INSTI

A

Dolutegravir
Bictegravir
Raltegravir
Elvitegravir

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3
Q

Fusion Inhibitors

A

Enfuvirtide

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4
Q

PIs

A

Ritonavir
Lopinavir
Atazanavir
Darunavir
Fosamprenavir

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5
Q

PK Enhancers

A

Ritonavir (PI)
Cobicistat

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6
Q

CCR5 Antagonist

A

Maraviroc

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7
Q

ART Combinations

A

2 NRTI + 1 INSTI
- Tenofovir + Emtricitabine + Bictegravir
- Tenofovir + Emtricitabine + Dolutegravir
- Abacavir + Lamivudine + Dolutegravir

1 NRTI + 1 INSTI = Emtricitabine + Dolutegravir
- Not for HIV RNA > 500 000 copies/mL
- Not for HBV coinfection
- Not for those whose genotypic resistance testing of HIV or HBV testing are unavailable yet and you already want to start ART

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8
Q

NRTI advantages

A

ART Dual Backbone
Renal elimination
DDI not concerned

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9
Q

NRTI disadvantages

A

1) Mitochondrial toxicity (Rare, serious, More in Zidovudine)
- Lactic acidosis
- Hepatic Steatosis (Fat Infiltrate)
- Lipoatrophy (Fat loss)

2) Renal dose adjustments (Except abacavir)

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10
Q

NRTI ADRs (Specific to each)

A

Minimal toxicities
- Lamivudine – N/V/D
- Emtricitabine – N/D, hyperpigmentation

Tenofovir – N/V/D, Renal impairment, BMD decrease (TAF < TDF)

Abacavir – N/V/D, Hypersensitivity (HLA-B5701 – Rash, fever, malaise, fatigue, appetite loss, sore throat, cough, SOB, fatal ⇒ Discontinue, no rechallenge ⇒ Test for absence of HLA-B5701 before initiation), MI risk (Not used in CV risk patients)

Zidovudine – N/V/D, myopathy, bone marrow suppression (anemia, neutropenia)

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11
Q

INSTI Advantages

A

Good virologic effectiveness
Genetic barrier to resistance
Generally Well tolerated

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12
Q

INSTI disadvantages (Generally)

A

ADR:
- Weight gain
- N/D
- Headache
- Depression, suicidality (Rare, only in preexisting psychiatric)

DDI:
- Polyvalent cation coadministration
- CYP3A4 inducers/inhibitors

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13
Q

INSTI ADR (Specific)

A

Bictegravir / Dolutegravir – Inhibit SCr tubular secretion, no impact on GFR, resulting in increased SCr

Raltegravir – Pyrexia, Rhabdomyolysis (CK)

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14
Q

NNRTI Advantages

A

Long half life

Less metabolic toxicity than PIs (e.g. HLD, insulin resistance)

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15
Q

NNRTI Disadvantages

A

Genetic barrier to resistance is low
Cross resistance
Skin rash (Rilpivirine < Efavirenz)
CYP450 DDI
QTc prolongation

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16
Q

NNRTI ADRs

A

Efavirenz
- Rash
- HLD, LDL-C, TG
- Neuropsychiatric SE (Insomnia, depression, hallucination)
- Hepatotoxicity

Rilpivirine
- Depression
- Headache

17
Q

NNRTI DDI

A

Efavirenz
- Substrate – CYP3A4
- Inducer – CYP2B6, CYP2C19

Rilpivirine
- Substrate – CYP3A4
- PPIs ⇒ Gastric pH increase ⇒ Reduced oral absorption

18
Q

Protease Inhibitors Advantages

A

Genetic barrier to resistance
PI resistance is less common

19
Q

Protease Inhibitors Disadvantages

A
  • Metabolic complications (Dyslipidemia, Insulin resistance)
  • GI side effects (N/V/D)
  • Hepatotoxicity (esp HepB and HepC)
  • CYP3A4 inhibitors and substrates ⇒ DDI
  • Morphologic complication (Fat maldistribution, lipohypertrophy)
  • Osteopenia / Osteoporosis
20
Q

Protease Inhibitors ADRs

A

Ritonavir – Paresthesia (Numb extremities), taste perversion

Darunavir – Good GI tolerability, less lipid effects, Skin rash, SJS

Atazanavir – Good GI tolerability, less lipid effect, hyperbilirubinemia, QTc prolongation, skin rash

21
Q

Protease Inhibitors DDI

A

Ritonavir – Potent CYP3A4, 2D6 inhibitor (Usually in combi with other PIs to boost levels)

Atazanavir – PPIs ⇒ Decrease absorption

22
Q

Fusion Inhibitors Advantages

A

No DDI, Injection by SC BD

23
Q

Fusion Inhibitors Disadvantages

A

Disadvantages – ADRs

Adverse Effects
- Injection site reaction (Erythema, induration, nodules, cyst, pruritus, ecchymosis
- Hypersensitivity, fever, rash, chills, BP drops (Rare)
- Bacterial pneumonia

24
Q

CCR5 Antagonist Disadvantages and ADRs

A

Needs co-receptor tropism assay before initiation

Must be CCR5 predominant to use

Not to use if CXCR4 or dual/mixed tropism
CYP3A4 substrate

List of ADRs
- Abdominal pain
- Cough
- Dizziness
- Musculoskeletal symptoms
- Pyrexia
- Rash
- URTI
- Hepatotoxicity
- Orthostatic hypotension

PR3151 Finals (10 decks)

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