HIV Pharm - NRTIs Flashcards
General MOA for NRTIs
(-) incorporation of native nucleotides and terminate DNA elongation
General MOA for NRTIs
(-) incorporation of native nucleotides and terminate DNA elongation
NRTIs must enter the cell and become _______
Phosphorylated
NRTIs (-)
Reverse transcriptase
– Takes RNA to DNA
NRTIs must (-) Reverse Transcriptase without (-) DNA?
Polymerase of the host cell
Some NRTIs (-) _____ DNA polymerase ___
Mitochondrial DNA Polymerase Gamma
The widely used NRTIs that (-) Mitochondrial DNA Polymerase Gamma have ____ affinity for gamma
LOW affinity
Zidovudine interferes with?
Thymidine incorporation
Adverse side effects of Zidovudine?
Bone marrow suppression
Myopathy
Hepatic Steatosis
What was the first ART drug discovered?
Zidovudine
Stavudine interferes with?
Thymidine incorporation
Adverse side effects of Stavudine?
Peripheral neuropathy and fat wasting
What NRTIs interfere with Thymidine incorporation?
Zidovudine
Stavudine
Zidovudine and Stavudine and ____ used now
Less used now
Emtricitabine inteferes with?
Cytosine incorporation
Emtricitabine has a ____ barrier to resistance if monotherapy
LOW
Emtricitabine half life and metabolism?
Long half life and excreted UNCHANGED in urine
Emtricitabine is one of the least toxic agents! What is one possible side effect?
Hyperpigmentation of the palms/soles with prolonged use
Iamivudine interferes with?
Cytosine incorporation
Iamivudine has a ___ barrier to resistance if monotherapy
LOW
Iamivudine half life and metabolism?
Long half life and excreted UNCHANGED in urine
Iamivudine is one of the least toxic agents! What is it similar to?
Emtricitabine
Emtricitabine is similar to?
Iamivudine
What NRTIs interfere with Cytosine incorporation?
Emtricitabine
Iamivudine
What agent is often used with Iamivudine to treat naive patients?
Dolutegravir
What agent is often used with Iamivudine to treat naive patients?
Dolutegravir
What NRTI interferes with Guanine incorporation?
Abacavir
Abacavir interferes with?
Guanine incorporation
Abacavir should not be used with patients with what locus?
HLA-B*5701
In patients with HLA-B*5701 locus, what does Abacavir cause?
Aberrant TNF release
= Potentially fatal hypersensitivity syndrome
Adverse effects of Abacavir?
Potentially fatal hypersensitivity syndrome
Avoided in CAD patients
Tenofovir Disoproxil Fumarate interferes with?
Adenosine incorporation
Adverse effects of Tenofovir Disoproxil Fumarate?
Nephrotoxicity that can cause Fanconi Syndrome
Decreased bone mineral density
Tenofovir Alafenamide interferes with?
Adenosine incorporation
Adverse effects of Tenofovir Alafenamide?
LESS renal and bone toxicity than Tenofovir Disoproxil Fumarate
– Can cause slight weight gain
What NRTIs interfere with Adenosine incorporation?
Tenofovir Disoproxil Fumarate
Tenofovir Alafenamide
What NRTI that interferes with Adenosine incorporation causes slight weight gain but less renal and bone toxicity?
Tenofovir Alafenamide
What NRTI that interferes with Adenosine incorporation causes nephrotoxicity and decreased bone mineral density?
Tenofovir Disproxil Fumarate
What NRTI that interferes with Guanine incorporation causes aberrant TNF release in some patients?
Abacavir
What NRTI that interferes with Cytosine incorporation can cause sole/palm hyperpigmentation with prolonged use?
Emtricitabine
ART involves 2 NRTIs that each target?
A different base
ART involves 2 NRTIs that each target?
A different base
What is the best combo of NRTIs?
Emtricitabine + Tenofovir
What is the best combo of NRTIs?
Emtricitabine + Tenofovir
What is the best combo of NRTIs?
Emtricitabine + Tenofovir