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