Antivirals EC Flashcards
Zanamivir, Oseltamivir (MOA, Use, Tox)
Inhibit influenza NEURAMINIDASE and block release of progeny
Treats influenza A and B
Ribavirin (MOA, Use, Tox)
Inhibits IMP DEHYDROGENASE and therefore guanine nucleotide synthesis
RSV, Chronic hep. B
Hemolytic anemia, Teratogenic
Acyclovir (MOA, Use, Tox)
Inhibits VIRAL DNA POLYMERASE
Monophosphated by thymidine kinase - Guanosine analog
Treat HSV and VZV
Ganciclovir (MOA, Use, Tox)
Inhibits VIRAL DNA POLYMERASE
5’-monophosphate formed by thymidine kinase- Guanoside analog
Treat CMV
Leukopenia, Neutropenia, Thrombocytopenia
Renal toxicity
Foscarnet (MOA, Use, Tox)
Inhibits VIRAL DNA POLYMERASE
Binds to PYROPHOSPHATE BINDING SITE
“FOScarnet=pyroFOSphate analog”
Acyclovir resistant HSV
Failure of gancyclovir in CMV retinitis
Nephrotoxic
Cidofovir (MOA, Use, Tox)
Inhibits VIRAL DNA POLYMERASE
CMV retinitis
Acyclovir resistant HSV
What does HAART therapy consist of?
3 drugs to prevent resistance:
2 NRTIs (nucleoside reverse transcriptase inhibitors)
+
1 Protease inhibitor
or
1 NNRTI (non-nucleoside reverse transcriptase inhibitor)
or
1 Integrase inhibitor
Lopinavir, Atazanavir, Darunavir, Fosamprenavir, Saquinavir, Ritonavir, Indinavir (MOA, Use, Tox)
HIV PROTEASE INHIBITORS prevent maturation of new virus
“NAVIR tease a PROTEASE”
Hyperglycemia GI Lipodystrophy Nephropathy Hematuria (Indinavir)
Why is Ritonavir often given?
To BOOST concentrations of other drugs by inhibiting P450s
Tenofovir, Emtricitabine, Abacavir, Lamivudine, Zidovudine, Didanosine, Stavudine (MOA, Use, Tox)
NRTIs (Nucleoside reverse transcriptase inhibitors)
Competitively inhibit HIV reverse transcriptase Chain termination (lack 3'OH)
Bone marrow suppression (reversible)
Peripheral neuropathy
Lactic acidosis
Anemia (Zidovudine)
What NRTI does not have to be activated?
Tenofovir is a nucleotide analog and does not have to be activated
All other NRTIs must be phosphorylated to be active
What NRTI is used for prophylaxis in pregnancy with a HIV+ woman?
Zidovudine
Nevirapine, Efavirenz, Delavirdine (MOA, Use, Tox)
Bind reverse transcriptase at a different spot
Do not need to be activated
Bone marrow suppression (reversible)
Peripheral neuropathy
Rash
Raltegravir (MOA, Use, Tox)
Inhibits HIV integrase (integration into genome)
Hypercholesterolemia
Interferons (MOA, Use, Tox)
Glycoproteins synthesized by virus infected cells; block viral replication
IFN-alpha: Hep. B and C, Kaposi’s sarcoma
IFN-beta: MS
IFN-gamma: NADPH oxidase deficiency
Neutropenia
Myopathy