Antivirals Flashcards
Release of Progeny Virus
Neuraminidase inhibitors
Zanamivir and Oseltamivir (Flu A and B)
Nucleic acid synthesis
Guanine nucleotide synthesis: Ribavirin (RSV + HCV)
Viral DNA Polymerase inhibitors: Foscarnet and Cidofovir (HSV and CMV)
Guanosine analogs: Ayclovir, etc (HSV,VZV)
Ganciclovir (CMV)
Uncoating
Amantadine and Rimantadine
No longer used
Protein Synthesis
IFN-a
HBV & HCV
Fusion (HIV)
Attachment: Maraviroc
Penetration: Enfuvirtide
Reverse Transcriptase inhibitors (HIV)
NRTIs Tenofovir (TDF) Emtricitabine (FTC) Abacavir (ABC) Lamivudine (3TC) Zidovudine (ZDV, use to be AZT) Didanosine (ddl) Stavudine (d4T)
NNRTIs
Nevirapine
Efavirenz
Delavirdine
Integrase inhibitors
Raltegravir
Protease inhibitors
Lopinavir Atazanavir Darunavir Fosamprenavir Squinavir Ritonavir Indinavir
Zanamivir/Oseltamivir
Inhibits influenza Neuramidase. Decrease release of progeny
Influenza A and B
Ribavirin
Inhibits gaunaine nulceotides by competitively inhibiting IMP dehydrogenase
RSV, Chronic Hep C
Hemolytic anemia. Severe Teratogen
Acyclovir, Famciclovir, Valacyclovir (Guanosine analogs)
Monophosphylated by HSV/VZV thymidine kinase, but not uninfected cells
Guanosine analogs. Triphosphate formed by cellular enzymes. (incorporated to viral DNA)
Preferentially inhibits viral DNA polymerase by chain termination
HSV, VZV, weak against EBV and nothing in CMV.
Mucocutaneous and genital lesions, encephalitis.
Prophylaxis in immunocompromized.
Only in primary infection, not latent.
Vala is a prodrug to acyclo. increase bio avaialbility
HZ –> Famciclovir, releated
Can cause Obstructive cystalline nephropathy, ARF.
Resistance from mutated viral thymidine kinase
Ganciclovir
Guanosine analog, but different thymidine kinase*
5 monophosphate formed by CMV viral kinase
Guanosine analong
Triphosphate by cellular kinase.
Preferential to viral DNA polymerase
CMV. Especially immunocompromised
Valganciclovir –> prodrug with better oral
Leukopenia, neutropenia, thrombocytopenia, renal toxicity.
More so than acyclovir
Resistance: Mutated CMV DNA polymerase or lack of viral kinase
Foscarnet
Viral DNA polymerase inhibitor that binds to pyrophosphate binding site of the enzyme
Fos = pyroFOSphate analog
Does not require viral kinase activation.
CMV retinitis w/ ganciclovir fail or acyclovir reisstant HSV
Nephrotoxicity, anemia, bad side effects
Resistance from mutated DNA polymerase
Cidofovir
Preferentially inhibits viral DNA polymerase, doesn’t need viral kinase
CMV retintis in immunocompromised patients; acyclovir resistant HSV. long 1/2 life
Nephrotoxicity. Coadminister w/ probenecid and IV saline
HAART
When AIDS defininig illness or
Protease inhibitors
“Navir”
Assembly of virion depends onf HIV-1 (pol) gene. Cleaves polypeptides.
Ritonavir can boost other drug concentrations (inhibits c P450)
Hyperglycemia, hyperlipidemia, GI intolerance, lipidystrophy.
Nephropathy, hematuria w/ Indinavir
Atazanavir –> stones/hyperbili
Indinavir –> stones
Ritonavir –> pancreatitis