Exam 2: Antiretroviral -Part 2- Moniri Flashcards
T/F?
NRTIs are NON-competitive inhibitors of reverse transcriptase and obligate chain terminators.
False
-COMPETITIVE inhibitors
ALL NRTIs must undergo ______ in order to exert drug effects.
mono-, di-, or tri- phosphorylation
Which NRTI only has to undergo di- and tri-phosphorylation and contains 2 formulations?
Tenofovir (Viread, TDF)
Alafenamide (TAF)
Which Tenofovir formulation is associated w/ Less toxicities, increase efficacy, more metabolic AEs?
Tenofovir alafenamide (TAF)
T/F?
TDF concentrates more in the cell in opposed to the blood which increase its’ efficacy.
False
-Tenofovir alafenamide (TAF)
Which 2 NRTIs induce known resistance (M184V)? Why are they still used?
Lamivudine (Epivir, 3TC)
Emtricitabine (Emitriva, FTC)
- they are used b/c the mutation creates a less virulent infection
Which NRTI requires HLA-B*5701 hypersensitivity testing?
Abacavir (Ziagen, ABC)
Which HLA-B is associated w/ slow AIDs progression?
HLA-B27/B57
Which HLA-B is associated w/ fast AIDs progression?
HLA-B35
Which NRTI is associated w/ HIGH toxicities due to high infinity for monophosphate which result in BONE MARROW SUPPRESION, anemia and erythroid?
Zidovudine (Retrovir, AZT)
_____ act at the allosteric site and shifts the enzyme confirmation and a nucleotide can no longer fit and chain extension is inhibited
nNRTIs
What major AEs is associated w/ nNRTIs?
Drug-drug interactions due to being CYP450 effectors
T/F?
nNRTIs are used to effectively treat HIV-1 AND HIV-2.
False
- HIV-1 ONLY
What 3 nNRTIs are CYP inducers?
- Efavirenz (Sustiva) (major ALL 3)
- Nevirapine (Viramune)
- Etravirine (Intelence)
What nNRTI decreases PI levels?
-Efavirenz (Sustiva)
Which nNRTI has QD dosing but should not be taken w/ PPIs?
Rilpivirine (Edurant)
Which nNRTI is used to induce AZT sensitivity?
Delaviradine (Rescriptor)
What 2 nNRTI are CYP Inhibitors ONLY?
- Delaviradine (Rescriptor)
- Rilpivirine (Edurant)
Which nNRTI is associated w/ 103, 108, 181 known gene mutations?
Nevirapine (Viramune)
What nNRTI has QD dosing and is associated w/ teratogenicity and increase CNS SEs?
Efavirenz (Sustiva)
How do PIs inhibit virion maturation?
By mimicking the recognition site. PIs reversibly bind to the site and inhibit polypeptide cleavage (Phe-Pro)
Most PI failure is do to ___?
non-compliance
What ae the 2 major AE effects associated w/ PIs?
- Drug-Drug interactions (Cyp450 isozymes)
- DYSLIPIDEMIA
What is the most potent PI CYP450 inhibitory? What is it commonly used for?
Ritonavir
-boosting agent
What effect dose Ritonavir have on PIs when given in combination?
They increase PIs potency (AUC)
What 3 second generation PIs have an increase in resistance barrier and efficacy?
Darunavir (Prezista)
Atazanavir (Reyataz)
Tipranavir (Aptivus)
Which 2nd generation PI is associated w/ increased SEs (lipids, hepatitis, glucose)
Tipranavir (Aptivus)
Which 2nd generation PI is associated w/ QD doing and less dyslipidemia?
Atazanavir (Reyataz)
Which PI is a prodrug?
Fosamprenavir (Lexiva, Telzir)
_____ is a fusion HIV-1 inhibitor that binds to gp41-inhibits fusion of viral & cell membranes .
Enfuvirtide (Fuzeon)
What medication blocks CCR5? What must be determined prior to this medication being prescribed?
Maraviroc
-tropism
What are the 3 major AEs associated w/ Integrase inhibitors?
- increase in SCr/Cr kinase
- Rhabdomyolysis
- myopathy
What is the major difference between Stribild and Genovoya?
Tenofovir formulation
Genvoya- TAF
Stribild- TDF
- both have the following:
- Emtricitabine
- Elvitegravir
- Cobicistat
What are the 2 agents used for “boosting” purposes?
- Cobicistat
- Ritonavir
Which boosting agent has NO antiretroviral activity?
-Cobicistat
