Antiretrovirals

Question 1

What do highly active antiretroviral therapy do?

Answer 1

Highly active antiretroviral therapy (HAART) shown to suppress HIV indefinitely

Question 2

HIV Factors

Question on this

Answer 2

Check slide
1) Individual Factors
2) Network Factors
3) Community Factors
4) Social and structural Factors
5) Epidemic Stage

Question 3

Antiretroviral Therapy (ART)

Answer 3

Combination therapy to prevent treatment failure, developmentof resistance
- 2 NRTI + 1 active agent from another class = triple therapy
- Dual therapy is also an option = triple therapy in selected setting
- Treatment goal is virologic suppression (HIV RNA <200 copies/mL)

Question 4

Nucleoside Reverse Transcriptase Inhibitors (NRTIs),

FOVIR, VUDINE, CAVIR

Answer 4

Thymidine: Zidovudine
Cytosine: Emtricitabine, Lamivudine
Guanosine: Abacavir
Adenosine: Tenofovir disoproxil fumarate (TDF), Tenofovir alafenamide (TAF)

Question 5

NRTI Pearls

Answer 5

2 of 3 agents in triple therapy NRTIs
- Tenofovir, emtricitabine, lamivudine – have activity vs hepatitis B virus (HBV)
- NRTs are enally eliminated (except abacavir)

PrEP:
- Descovy (emtricitabine and TAF)
- Truvada (emtricitabine and TDF)

Question 6

TDF Vs TAF

Answer 6

• TDF: more renal toxicity and bone risk

Question 7

Zidovudine

Answer 7

Only ARV avaiable for IV administration
- Given during labor when pregnant mother not virologically controlled or complications in pregnancy
- Given to infants as born to persons with HIV as prophylaxis for 4-6 weeks

Question 8

Non-Nucleoside Reverse Transcriptase
Inhibitors (NNRTIs)

VIRINE

Answer 8

• Efavirenz
• Etravirine
• Rilpivirine
• Doravirine

Question 9

NNRTI Pearls

Answer 9

Adverse Effects
- Hepatotoxicity and rash

Low genetic barrier
- Cross resistance to ≥ 1 other NNRTIs common upon treatment failure

Drug interactions
- 3A4 substrates, some NNRTIs can induce metabolism
- Rilpivirine interacts with acid suppressants

Question 10

Rilpivirine is part of?

Answer 10

Rilpivirine part of a long acting injectable regimen with cabotegravir

Question 11

Protease Inhibitors

NAVIR

Answer 11

• Atazanavir
• Darunavir
• Ritonavir

Question 12

Protease Inhibitors Pearls

Answer 12

Historically inconvenient, increased toxicities
- GI and metabolic

Boosting by 3A4 inhibition greatly improved their utility:
- Bioavailability
- Increased toxicities for some Pls
- Reduced risk of resistance

Question 13

Integrase Strand Transfer Inhibitor (INSTIs),

TEGRAVIR

Answer 13

• Raltegravir
• Elvitegravir
• Dolutegravir
• Bictegravir
• Cabotegravir

Question 14

INSTI Pearls

Answer 14

Well Tolerated; Recommended for inital therapy in most situations

Elvitegravir:
- Requires a pharmacokinetic booster
- Prescribed as 4-in 1 combination (with booster; not active against HIV)

Bictegravir:
- Only available as 3-in-1 combination

Cabotegravir
- Part of a long-acting injectable regimen (with rilpivirine)
- Approved for PrEP (Apretude)

Question 15

Entry Inhibitors

Answer 15

• Ibalizumab
• Maraviroc
• Fostemsavir

Question 16

Entry Inhibitor Pearls

Answer 16

Mostly used when options are limited due to resistance
MaraVIRoc
- A test required to determine if would be an option (trophile test)

Ibalizumab
- IV administration every 2 weeks

Fostemsavir

Question 17

Dolutegravir/rilpivirine (Juluca®)

Answer 17

first dual therapy coformulation approved for maintenance therapy

Question 18

Dolutegravir/lamivudine (Dovato®)

Answer 18

First dual therapy coformulation approved for treatment-naïve patients and maintenance therapy