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PDAT6 ID > 37/38 - Antiretrovirals > Flashcards

37/38 - Antiretrovirals Flashcards

1
Q

Protease Inhibitors = PIs
Symtuza / Prezista / Prezcobix
Prezista = Darunavir

CLASS ADR / Considerations

A

FAT MALDISTRUBUTION
+
GI ISSUES
NVD > INSTIs

CI w/ SIMVASTATIN** + **LOVASTATIN

  • *Metabolic Disorders** –> HYPERLipidemia
  • *PI’s have MOST effect on LIPIDS**
  • *Liver Toxicity**
  • not recommended in SEVERE hepatic impairment*
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2
Q

Which Antiretroviral are we worried
most about WEIGHT GAIN?

A

INSTIs
Bictarvy / Triumeq / Genvoya
Dolutegravir(Tivicay)/ Raltegravir (Isentress)

Dolutegravir > elvitegravir

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3
Q

TRIUMEQ

Class / Contents / Restrictions

A
  • *INSTI**
  • *dolutegravir + abacavir + lamivudine**

Abacavir requires a:
HLA-B*5701 test

HYPERSENSITIVITY RXN
1st 6 weeks

INSOMNIA

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4
Q

RALTEGRAVIR
Isentress

Drug Class / Metabolism / ADR

A

INSTI
Seperate from Antacids / Ca+ Vitamins
BIDor2T qd

All INSTI = Hepatic metabolism
NO P450 METABOLISM
just a substrate of:
UGT1A1

RHABDOMYOLYSIS
only INSTI with this ADR

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5
Q

SYMTUZA
Darunavir + Cobicistat / TAF-FTC

Metabolism

A

PIs are LIVER metabolism

DRV:
CYP3A4 Inhibitor & Substrate + 2C9 INDUCER

COBI:
CYP3A4 Inhibitor & Sub** + **2D6 Inhibitor
LOTS OF DRUG INTERACTIONS
↑SCr

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6
Q

IBALIZUMAB
Trogarzo

Class / ADR / Considerations

A

Entry Inhibitor –> Binds CD4
only for MDR HIV infection

  • *2k IV Loading Dose** –> 800mg q2weeks
  • if DOSE is missed –> RESTART w/ loading dose*
  • *NO DRUG INTRACTIONS**
  • does NOT suppress IMMUNE system*
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7
Q
  • *ENFUVIRTIDE**
  • *Fuzeon**

Class / ADR / Considerations

A

Entry Inhibitor –> Prevents Membrane Contact + Fusion pore

90mg 1ml
SUBQ BID
needs to be stored in fridge + reconstituted

INJECTION SITE REACTIONS
98% of patients

no drug interactions = injected

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8
Q

BIKTARVY

Class / Contents / Restrictions

A
  • *INSTI**
  • *bictegravir** + TAF + emtricitabine

only if CrCl > 30 mL/min
+
NOT recommended in SEVERE HEPATIC impairment

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9
Q

ENTRY INHIBITORS

Drugs / Targets

A
  • *IBALIZUMAB**
  • *CD4** Binding, IV loading dose –> IV q2weeks
  • *MARAVIROC**
  • *CCR5 Coreceptor**, BID dosing adjusted by CYP3A4

ENFUVIRTIDE
prevents Membrane contact / fusion pore
90mg 1ml SC - BID

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10
Q
  • *INSTIs**
  • *Integrase Inhibitors**

Drugs + Drug Combos

A
  • *Bictarvy**
  • *bictagravir** / TAF + emtricitibine
  • *Triumeq**
  • *dolutegravir** / ABC + lamivudine
  • *Genvoya**
  • *eletegravir** + cobicistat / TAF + emtricitibine
  • Stribild#2*
  • *Dolutegravir** = Tivicay
  • can be BID*
  • *Raltegravir** = Isentress
  • *BID** or HD 2T qd
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11
Q

Which Antiretroviral do we have to
AVOID in PREGNANCY?

A

INSTIs
Bictarvy / Triumeq / Genvoya
Dolutegravir(Tivicay)/ Raltegravir (Isentress)

  • *AVOID IN PREGNANCY_ due to _NEURAL TUBE DEFECTS**
  • but if you have to / already on…*
  • *Raltegravir > Dolutegravir**
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12
Q

TRIUMEQ
dolutegravir + abacavir + lamivudine

Metabolism Considerations
+ Contraindications?

A

NOT recommended in SEVERE HEPATIC impairment

All INSTI have hepatic metabolism:
Dolutegravir is a Substrate of:
UGT1A1
= DOFETILIDE is CONTRAINDICATED

only a MINOR CYP3A4 Substrate

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13
Q
  • *Which Antiretroviral do we need to**
  • *seperate from ANTACIDS?**
A

INSTIs
Bictarvy / Triumeq / Genvoya
Dolutegravir (Tivicay) / Raltegravir (Isentress)

Antacids/Vitamins containing polyvalent cations:
Al / Mg / Ca
need to be taken:
>2 hours before or >2*/6 hours AFTER
2* is only for BICTARVY

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14
Q

Which Antiviral has the ADR of:
RHABDOMYOLYSIS

A

RALTEGRAVIR = Isentress

INSTI

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15
Q

BIKTARVY
bictegravir+TAF+emtricitabine

Metabolism Considerations
+ Contraindications?

A

NOT recommended in SEVERE HEPATIC impairment

All INSTI have hepatic metabolism:
Bic is a Substrate of:
CYP3A4 + UGT1A1

Bic is a INHIBITOR of:
OCT2** + **MATE1
= DOFETILIDE is CONTRAINDICATED

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16
Q

SYMTUZA

Drug Class / Contents / ADR

A

Protease Inhibitor
Darunavir + Cobicistat / TAF-FTC
Class ADR:
NVD GI issues / Fat maldistrubution

DRV = RASH - Sulfonamide Moiety

  • NOT RECOMMENDED FOR:*
  • *CrCl < 30 ml/min**
  • *Severe Hepatic Impairment**
17
Q

When would we use:
DOLUTEGRAVIR(Tivicay)on its OWN ?
Combo is Triumeq
dolutegravir / abc / lamivudine

A
  • *IF HLA-B*5701 test is POSITIVE**
  • since they can NOT take*
  • *ABACAVIR**

would INSTEAD use:
DOLUTEGRAVIR (Tivicay)
PLUS
Descovy OR Truvada
TAF/FTC or TDF/FTC

18
Q

Which antiretroviral requires:
TROPISM TESTING?

A

MARAVIROC
SELZENTRY

Tropism Testing tells us which CoReceptor it binds to
needs to be:
CCR5
NOT 4 or BOTH
in order to use for the patient

19
Q

MARAVIROC
Selzentry

Class / ADR / Considerations

A

Entry Inhibitor –> CCR5 Coreceptor

TROPISM TESTING
required

  • *CYP3A4 SUBSTRATE**
  • *300mg BID**
  • *3A4 Inhibitors** –> 150mg BID // INDUCERS –> 600mg BID

ADRS:
HEPATOXICITY** + **DIZZINESS/Postural Hypotension

20
Q
  • *Protease Inhibitors**
  • *DARUNAVIR Combinations + Considerations**
A
  • *DRV_ requires a _BOOSTER**
  • *COBI** or RITONAVIR

PREZCOBIX = DRV + Cobi

  • *Prezista + Norvir** = DRV + Ritonavir
  • *WITH FOOD**

Symtuza = DRV/Cobi + TAF/FTC

21
Q

ENTRY INHIBITORS
Ibalizumab / Maraviroc / Enfuvirtide

Indications?

A

MULTI-DRUG RESISTANT
HIV Infection
after failing their current antiviral
almost ALWAYS requires a PA

Heavily Treatment-Experienced Adults

22
Q

Which antiretroviral has the issue of:
INSOMNIA

A

DOLUTEGRAVIR
TIVICAY

Also BICTARVY

Triumeq (Dolutegravir + ABC/3TC)

23
Q

Which antiretroviral is
Contraindicated with
SIMVASTATIN**+**LOVASTATIN

A

PROTEASE INHIBITORS
Symtuza / Prezista / Prezcobix
Prezista = Darunavir

24
Q
  • *Elivitegravir**
  • *Special Considerations**
A

Found in Genvoya:
Elvitegravir+Cobi / TAF+FTC

Only if CrCL > 30 ml/min
1 tab daily WITH food
Separate EVG/c/TDF/FTC and antacid administration by >2 hours

25
Q

Which AntiRetrovirals require
TWICE A DAY DOSING?
BID

A

NNRTI:

  • *Etravirine** = Intelence
  • *Doravarine** if coadmin w/ rifabutin

INSTI:
Raltegravir

Entry Inhibitors:

  • *Maravoric**
  • *Enfuvirtide** - 90mg (1m) SC BID
26
Q

Which antiretrovirals have a

CrCl Restriction?

A

Need CrCl > 30 ml/min:

BIKTARVY
bictegravir / TAF/FTC

  • *GENVOYA**
  • *elivite**gravir/cobi + TAF/FTC

SYMTUZA
darunavir/cobi + TAF/FTC

PDAT6 ID (31 decks)

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