HIV ART Treatment Flashcards
(48 cards)
What is the structure of a typical ART regimen
2 NRTIs
+
either
- INSTI
- PI + PK enhancer
- NonNRTI
What are the 6 NRTIs
- Tenofovir disoproxil fumarate (TDF)
- Tenofovir alafenamide (TAF)
- Emtricitabine (FTC)
- Lamivudine (3TC)
- Abacavir (ABC)
- Zidovudine (ZDV)
TT ELAZ
What are the 5 NNRTIs
- Doravirine (DOR)
- Rilpivirine (RPV)
- Efavirenz (EFV)
- Nevirapine (NVP)
- Etravirine (ETR)
DRE NE
What are the 3 Protease inhibitors
Darunavir/r or /c (DRV)
Atazanavir (ATV)
Lopinavir (LPV)
-vir
LAD
What are the 5 INSTI (integrase strand transfer inhibitor)
-gravir
- Raltegravir (RAL)
- Elvitegravir (EVG)
- Cabotegravir (CAB)
- Dolutegravir (DTG)
- Bictegravir (BIC)
What are the 4 attachment and entry inhibitors
- Enfuvirtide (T-20)
- Maraviroc (MVC)
- Fostemsavir (FTR)
- Ibalizumab (IBA)
What drug is a Capsid inhibitor
- Lenacapavir
(LEN)
Differentiate between the 2 PK boosters Ritonavir and Cobicistat
Availability/usage
Enzyme inhibition/induction
ADR
anti-HIV activity?
Ritonavir
Availability
- used with many PIs
- single entity drug
Enzyme
- Potent CYP3A4
- has induction effects
ADR
- GI effects
- insulin resistance
- hyperlipidemia
HIV activity?
- Anti-HIV activity at higher doses
Cobicistat
Availability
- Used with PIs atazanavir, darunavir & elvitegravir (INSTI)
Enzyme inhibition
- CYP 3A4
- no induction effects
ADR
- GI effects
- inc Screatinine without affecting GFR
HIV activity?
- None
What are the 3 options for triple drug regimens in Newly diagnosed HIV patients who are treatment naive
TAF / FTC / Bictegravir
TAF / FTC + Dolutegravir
TDF / FTC + Dolutegravir
FTC = emtricitabine
When can you give double therapy in newly diagnosed patients (3)
Which ones to give
- No HBV co-infection
- No resistance
- HIV RNA < 500,000 copies/mL
Lamivudine 3TC + Dolutegravir
What options of treatment are for HIV patients if they used
Cabotegravir for prep
+ no resistance test results are back (4)
Add Protease inhibitor + Booster
TAF / FTC / Darunavir / cobicistat
TDF / FTC + Darunavir / cobicistat
TAF/ FTC + Darunvair + Ritonavir
TDF / FTC + Darunavir + Ritonavir
Which drugs/classes cause weight gain
INSTI
+
TAF
NRTI
TDF vs TAF
Advantages
Disadvantages
Dose + renal dose
TDF
Adv
- favourable lipid effects
Disadv
- Decline in kidney function
- BMD reduction
Dose
- 300mg
- CrCl <50 = less frequent dosing intervals
TAF
Adv
- Favourable effects on renal markers & BMD
Dose
- 10mg daily with PI & booster
- 25mg daily with non-booster
- TAF not recommended CrCl <30
Wha is the dosing for other NRTIs such as Embtricitabine (FTC) and Lamivudine (3TC)
Embtricitabine (FTC)
- 200mg
- available only as combo product
Lamivudine (3TC)
- not really used
- 300mg
- Flexible renal dosing
What are important things to note when treating HIV with HBV co-infection
If Hep B co-infection, need 2 drugs that are active against Hep B
- TAF/TDF + FTC/3TC
**Cannot discontinue those therapies as it may cause serious hepatocellular damage which can reactivate Hep B
Why is abacavir not recommended as first line anymore (3)
HLA B*5701 testing required (takes >7 days and we want to start ARV within 7 days of diagnosis)
Risk of abacavir hypersensitivity syndrome
*NO association with CV disease – meta-analysis proved this association is wrong
What is the abacavir hypersensitivity syndrome
Symptoms
- Potentially life-threatening, multi-system reaction
- Non-specific sx: fever, rash, GI, malaise, respiratory issues
- Median onset: 9 days
- Symptoms worsen with continuation of abacavir
- Stopping abacavir will prompty reverse HSR
HLA-B* 5701 testing:
* Positive result has a strong association (40-50% chance) to abacavir HSR
Screening for patients is required ONCE in their lifetime
What is the dosing for the 2 main INSTI we use
Bictegravir (BIC)
- 50mg
Doulegravir
- Tx naive: 50mg daily
- INSTI resistance or INSTI naive w/ booster: 50mg BID
ADRs with bictegravir
WEIGHT GAIN
Headache
Diarrhea
Nausea
ADRs with Dolutegravir
WEIGHT GAIN
Headache
Insomnia
Depression & suicidal ideation (rare)
What is the main reaction that occurs with Bictegravir and dolutegravir
False CrCl elevation
Follow up on CrCl at 1 month: this becomes new baseline
Due to inhibitor of renal proximal tubule secretion of creatinine
When can raltegravir + 2 NRTIs be preferably used (3)
- Pregnancy
- Chemotherapy
- TB treatment
What is the main alternate treatment if a patient cannot use an INSTI (usually due to weight gain)?
Dose?
Use a PI + booster: Darunavir
- Treatment naive/Pi naive
- 800mg daily
- w/ ritonavir 100mg daily or cobicistat 150mg - Treatment with 1 of 11 darunavir resistance associated mutations (RAMs)
- 600mg BID
- w/ ritonavir 100mg BID
Why is the PI Atazanavir not used anymore as an alternate for INSTI? (3)
- Moderate barrier to resistance
- Low gastric pH required (PPI interaction)
- Bilirubin elevates (surrogate marker for adherence)