37/38 - Antiretrovirals Flashcards
Protease Inhibitors = PIs
Symtuza / Prezista / Prezcobix
Prezista = Darunavir
CLASS ADR / Considerations
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*
Which Antiretroviral are we worried
most about WEIGHT GAIN?
INSTIs
Bictarvy / Triumeq / Genvoya
Dolutegravir(Tivicay)/ Raltegravir (Isentress)
Dolutegravir > elvitegravir
TRIUMEQ
Class / Contents / Restrictions
- *INSTI**
- *dolutegravir + abacavir + lamivudine**
Abacavir requires a:
HLA-B*5701 test
HYPERSENSITIVITY RXN
1st 6 weeks
INSOMNIA
RALTEGRAVIR
Isentress
Drug Class / Metabolism / ADR
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
SYMTUZA
Darunavir + Cobicistat / TAF-FTC
Metabolism
PIs are LIVER metabolism
DRV:
CYP3A4 Inhibitor & Substrate + 2C9 INDUCER
COBI:
CYP3A4 Inhibitor & Sub** + **2D6 Inhibitor
LOTS OF DRUG INTERACTIONS
↑SCr
IBALIZUMAB
Trogarzo
Class / ADR / Considerations
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*
- *ENFUVIRTIDE**
- *Fuzeon**
Class / ADR / Considerations
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
BIKTARVY
Class / Contents / Restrictions
- *INSTI**
- *bictegravir** + TAF + emtricitabine
only if CrCl > 30 mL/min
+
NOT recommended in SEVERE HEPATIC impairment
ENTRY INHIBITORS
Drugs / Targets
- *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
- *INSTIs**
- *Integrase Inhibitors**
Drugs + Drug Combos
- *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
Which Antiretroviral do we have to
AVOID in PREGNANCY?
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**
TRIUMEQ
dolutegravir + abacavir + lamivudine
Metabolism Considerations
+ Contraindications?
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
- *Which Antiretroviral do we need to**
- *seperate from ANTACIDS?**
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
Which Antiviral has the ADR of:
RHABDOMYOLYSIS
RALTEGRAVIR = Isentress
INSTI
BIKTARVY
bictegravir+TAF+emtricitabine
Metabolism Considerations
+ Contraindications?
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
SYMTUZA
Drug Class / Contents / ADR
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**
When would we use:
DOLUTEGRAVIR(Tivicay)on its OWN ?
Combo is Triumeq
dolutegravir / abc / lamivudine
- *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
Which antiretroviral requires:
TROPISM TESTING?
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
MARAVIROC
Selzentry
Class / ADR / Considerations
Entry Inhibitor –> CCR5 Coreceptor
TROPISM TESTING
required
- *CYP3A4 SUBSTRATE**
- *300mg BID**
- *3A4 Inhibitors** –> 150mg BID // INDUCERS –> 600mg BID
ADRS:
HEPATOXICITY** + **DIZZINESS/Postural Hypotension
- *Protease Inhibitors**
- *DARUNAVIR Combinations + Considerations**
- *DRV_ requires a _BOOSTER**
- *COBI** or RITONAVIR
PREZCOBIX = DRV + Cobi
- *Prezista + Norvir** = DRV + Ritonavir
- *WITH FOOD**
Symtuza = DRV/Cobi + TAF/FTC
ENTRY INHIBITORS
Ibalizumab / Maraviroc / Enfuvirtide
Indications?
MULTI-DRUG RESISTANT
HIV Infection
after failing their current antiviral
almost ALWAYS requires a PA
Heavily Treatment-Experienced Adults
Which antiretroviral has the issue of:
INSOMNIA
DOLUTEGRAVIR
TIVICAY
Also BICTARVY
Triumeq (Dolutegravir + ABC/3TC)
Which antiretroviral is
Contraindicated with
SIMVASTATIN**+**LOVASTATIN
PROTEASE INHIBITORS
Symtuza / Prezista / Prezcobix
Prezista = Darunavir
- *Elivitegravir**
- *Special Considerations**
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
Which AntiRetrovirals require
TWICE A DAY DOSING?
BID
NNRTI:
- *Etravirine** = Intelence
- *Doravarine** if coadmin w/ rifabutin
INSTI:
Raltegravir
Entry Inhibitors:
- *Maravoric**
- *Enfuvirtide** - 90mg (1m) SC BID
Which antiretrovirals have a
CrCl Restriction?
Need CrCl > 30 ml/min:
BIKTARVY
bictegravir / TAF/FTC
- *GENVOYA**
- *elivite**gravir/cobi + TAF/FTC
SYMTUZA
darunavir/cobi + TAF/FTC
