antivirals Flashcards
HIV fusion inhibition
attachment: maravirocpenetration: enfuvirtide
HIV inTEGRAse inhibition
doluTEGRAvir, elviTEGRAvir, ralTEGRAvir
HIV protease inhibition
atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, ritonavir, saquinavir
HIV reverse transcriptase inhibition
NRTIS, NNRTI
NRTIs
abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, zidovudine
NNRTIs
delaviridine, efavirenz, nevirapine
HBV, HCV protein synthesis inhibition
INF-a (binds via PKR)
uncoating (influenza)
amantadine, rimantadine(no longer used, high resistance)
Guanosine analogs
acyclovir (HSV, VZV)Ganciclovir (CMV)
viral DNA polymerase inhibitors
cidofovir (HSV)foscarnet (CMV)
guanine nucleoside synthesis inhibitor
ribavirin (RSV, HCV)
release of progeny inhibitors
neuraminidase inhibitors (Oseltamivir, Zanamivir) in flu A,B
Ganciclovir MOA
5’-monophosphate formed by CMV viral kinase. Guanosine analog. Triphosphate formed by cellular kinases. preferentially inhibits viral DNA polymerase
Ganciclovir use
CMV, esp. in IC pts.
Valganciclovir, prodrug of ganciclovir, has better oral bioavailability
Ganciclovir ADR
bone marrow suppression (leukopenia, neutropenia, thrombocytopenia); renal toxicity
more toxic to host than acyclovir
Ganciclovir resistance
mutated viral kinase
Foscarnet MOA
Viral DNA/RNA polymerase inhibitor and HIV reverse transcriptase inhibitor.
Binds to pyrophosphate-binding site of enzyme.
*Does not require any kinase activation
Foscarnet use
CMV retinitis in IC patients when ganciclovir fails; acyclovir-resistant HSV
Foscarnet ADR
nephrotoxicity, electrolyte abnormalities lead to seizures
Foscarnet Mech of resistance
mutated DNA polymerase
Cidofovir MOA
preferentially inhibits viral DNA polymerase. Does not require phosphorylation by viral kinase
Cidofovir use
CMV retinitis in IC patients;
acyclovir-resistant HSV.
Long-half life
Cidofovir ADR
nephrotoxicity (coadmin w/ probenecid and IV saline to dec)
HIV triple therapy
2 NRTIs and preferably an integrase inhibitor