Anti-Retrovirals Part II Flashcards
Describe the mechanism of action of NNRTIs?
They are not nucleosides or nucleotides. They bind to the reverse transcriptase enzyme and deactivate it.
Name 2 NNRTIs to which HIV rapidly develops resistance.
Nevirapine
Efavirenz
Name 3 NNRTIs, known as second generation NNRTIs, to which HIV doesn’t develop resistance as quickly.
Doravirine
Rilpivirine
Etravirine
What is the mechanism of action of fusion inhibitors?
Blocks the CD4 receptor
Name a fusion inhibitor that is not used often and state how it is administered.
Enfuvirtide - Injected BID. Used as a drug of last resort.
What is the mechanism of action of Maraviroc?
R5 receptor blocker - no effects on X4
What lab is drawn before administering maraviroc and why?
Trophic Assay that tells you which co-receptor the patient’s HIV primarily uses.
What is the mechanism of action of integrase inhibitors?
Block integrase preventing entry of viral DNA into the cell nucleus and thus preventing integration of viral DNA with host cell DNA
What is the hottest class of HIV drugs in 2021?
Integrase inhibitors
List 3 integrase inhibitors.
Raltegravir
Elvitegravir
Dolutegravir
What is unique about the drug Fostemsavir?
- It blocks the CD4 receptor but at a different attachment point than enfuvirtide
- It is administered PO (enfuvitride is injected)
Name a pure potent CP450 inhibitor that can be used as a booster and list its advantages.
Cobicistat. No GI side effects. Doesn’t contribute to resistance as you would when using ritonavir
What are the three standard recipes used when administering drugs to treat HIV?
2 NRTIs and 1 NNRTI
2 NRTIs and 1 Protease Inhibitor
2 NRTIs and 1 Integrase Inhibitor –> hottest
What is a hot method for administration of HIV drug cocktails?
STR –> single tablet regimen, IE, all three drugs in one pill.
T/F: There is no way to test a patient’s resistance to HIV medications.
False –> resistance testing exists
What percent of new HIV patients are resistant to at least 1 medication at baseline?
15% have resistance at baseline
Describe when resistance testing is repeated in HIV patients?
When treatment fails with failure defined as detectable viral load.
What are the primary and secondary goals in HIV treatment?
Primary: undetectable viral load
Secondary: CD4 count increase
List the 4 anti-retrovirals that also cover Hepatitis B.
Lamivudine, Emtricitabine, Tenofovir (TDF), and Tenofovir Alfenamide (TAF)
List the anti-retrovirals that also cover Hepatitis C.
No HIV drugs cover Hep C
What other diseases are HIV patients screened for?
Hep A, B, and C, chlamydia, gonorrhea, syphilis
Describe and differentiate between PEP, NPEP, PREP, and TasP.
- PEP: post exposure prohylaxis –> 3 drugs x 30 days within 48-72 hours
- NPEP: non-occupational PEP –> same as PEP if high risk exposure
- PREP: Pre-Exposure Prophylaxis –> people at high risk for HIV get 2 drugs QD
- TasP: Treatment as Prevention –> undetectable = untransmittable
What are two drug combinations given for PREP?
Truvada: Tenofovir (TDF) and Emtricitabine
Descovy: Tenofovir Alfenamide (TAF) and Emtricitabine
T/F: Oral sex is considered high risk exposure for HIV.
F: almost impossible to transmit HIV orally
What new HIV drug regimen was just approved by the FDA?
Once a month injectable antiretroviral combination
