Nucleoside Reverse Transcriptase Inhibitors and Non-Nucleoside REverse Transcriptase inhibitors (NRTIs + NNRTIs) Flashcards
What are the NRTIs nucleoside analogs
Tenofovir alafenamide, tenofovir disoproxil, abacavir, lamivudine, emtricitabine
What are the combination NRTIs
Descovy, Truvada, Epzicom
What is the MOA of NRTIs
Competitive inhibitor of HIV reverse transcriptase and terminator of viral DNA synthesis
How doe viral RNA become DNA, how does the ds viral dna get into the cell, how does the virus enzymes become active
Reverse transcritpase, Viral intergrase, Viral protease
Which NtRTI is already phosphorylated and is active against HIV and Hep B, what is it an analog of
Tenofovir disoproxil, Adenosine
What are the serious side effects of Tenofovir, what is monitored
Nephrotoxicity and Decrease in BMD/ Scr, glucosuria, proteinuria
T/F: Tenofovir alafenamide fumarate is a produrg converted intracelluralarly with the goal of having high metabolite concentration in target cells and low plasma tenofovir exposure along with no renal or bone toxicity
True
What enzyme converts TAF to Tenofovir D
Cathepsin A
T/F: TAF is worth than TDF
False: TAF is safer, just as efficacious, has activity against Hep B as well
When are the only times TDF would be preffered over TAF
Pre-exposure prophylaxis or if a patient is taking rifabutin
What is the NRTI that is hepatically metabolized and has a risk of causing Hypersensitivity REaction
Abacavir (ABC)
T/F: Patients that hav an abacavir allergy should never be rechallenged because they could potentially die
True
What is the Genetic screening that should be done to see if Abacavir is safe in an HIV patient
HLA-B*5701
What NRTi has little to no side effect while having activity against HIV and HBV but HBV has built up resistance/ what is the sister analog with better activity against Hep B and is renally eliminated
Lamivudine, Emtricitabine
What is a class side effect of NRTI, why
Mitochondrial toxicity, inhibition of mitochondrial DNA
What is the ranking for the combination NRTIs
Descovy, Epzicom, Truvada
What are the NNRTIs, MOA
Efavirenz, Etravirine, Rilpivirine, Doravirine/ directly bind RT causing a conformation change preventing viral DNA synthesis
Which NNRTI was an early potent and daily dosing single tablet, what is a key drug interaction, adverse effect unique to the drug
Efavirenz, CYP3A4, Central Nervous system such as dizziness, vivid dreams
What NNRTI was developed to treat EFV-resitant virus and NOT used in treatment for NAIVE patients
Etravine (intelience)
What NNRT is approved for Tx naive and people who have taken drugs before and has no hepatic drug metabolism, smallest antiretroviral tablet, and is ok in preganancy
Rilprivirine
What are disadvantages of using Rilprivirine
Must take with food (preferably the largest meal of the day), contraindicated with PPIs (separate 12 hours. Not the most potent ART (shouldn’t be used in patients with Viral load higher than 100000 or CD4 less than 200)
What is the newest NNRTs that is used in resistance profiles, hepatically eliminated and will have to double the dose to 100 mg BID who are taking Rifabutin
Doravirine
What is the only FDA approved drug used for patients at high risk for HIV contraction
Truvada
2NRTIs plus another agent from another class is a three active drug that is recommended for HIV treatment naive patients
True
