Antivirals Flashcards
NRTI’s
Abacavir, Lamivudine, Emtricitibine
NNRTI’s
Efavirenz
Nucleotide
Tenofovir
HIV Protease inhibitors
Ritonavir, Darunavir, Atazanavir
Fusion/Entry/Integration inhibitors
Enfuvirtide, Maraviroc, Dolutegravir
Genotype for resistance?
RT and Protease
Zidovudine (AZT) - analog
Thymidine
NRTI’s - TOX
mitochondrial DNA polymerase gamma TOX
Hyperlipidemia/insulin resistance (aidovudine, stavudine)
Lactic acidosis with hepatic steatosis (life threatening, monitor aminotransferase levels)
Abacavir - analog
Guanosine
Abacavir - metabolism
Deactivated in liver
Abacavir - combo
+Lamivudine
Abacavir - TOX
MI (caution in CV, platelet adhesion)
HLA-B*5701 hypersensitivty
skin rash
Lamivudine/Emtricitabine - analog
L = cytosine analog (Em is fluorinated analog of L, longer half life)
Lamivudine/Emtricitabine - used in?
HBV treatment
Truvada
Emtricitabine + Tenofovir DF
Tenofovir - analog
acyclic nucleotide of adenosine
Tenofovir - drug or prodrug?
Prodrug
Truvada - use?
First line backbone + chronic hepatitis
Truvada - excrete?
Renal
Truvada - TOX
fatigue weakness flatulence renal accumulation (ATN, renal failure, Fanconi's) osteopenia
Efavirenz - mechanism
Allosteric binding to RT, inhibits RNA/DNA polymerase, doesn’t need phosphorylation, not competitive inhibition, not against HIV-2
Efavirenz - in pregnancy?
NO
Which HIV drug NOT in pregnancy?
Efavirenz
Efavirenz - drug drug rx
metabolized by/induces CYP3A4
Efavirenz - TOX
nightmares/psych (at start - resolves)
GI, skin, SJS
Protease inhibitors - mechanism
peptidomimetics, inhibit proteolytic cleavage of gag and gag-pol, no activation, resistsance common