Flashcards in Antivirals Deck (24):
Block neuraminidase. Decreases release of progeny. Used to treat influenza A and B
Inhibits synthesis of guanine nucleotides by inhibiting inosine monophosphate dehydrogenase.
Used for RSV, hepatitis C (chronic)
Severe teratogen, hemolytic anemia.
Acyclovir, famciclovir, valacyclovir
Must be phosphorylated to be active. Phosphorylated in HSV/VZV by thymidine kinase. Guanosine analog. Preferentially inhibits DNA polymerase via chain termination.
Few adverse effects.
Resistance if thymidine kinase mutated.
Used in HSV and VZV. Weak activity against EBV.
Valacyclovir is a prodrug and has better oral bioavailability
Toxicity of acyclovir, famciclovir, valacyclovir?
Obstructive crystalline nephropathy and acute renal failure if not hydrated.
5'monophosphate formed by CMV viral kinase. Guanosine analog. Triphosphate formed by cellular kinases. Inhibits DNA polymerase.
Use in CMV.
Leukopenia, neutropenia, thrombocytopenia, renal toxicity. Much more toxic to host enzymes than acyclovir.
Viral DNA polymerase inhibitor that binds to the pyrophosphate binding site of the enzyme. Does not require activation by viral kinase.
Used in CMV retinitis or when CMV has UL97 mutation.
Preferentially inhibits viral DNA polymerase. Does not require phosphorylation by viral kinases.
Used in CMV retinitis in immunocompromised or in acyclovir resistant HSV.
Severely nephrotoxic so administer with saline and probenecid.
Initiated when patients present with AIDS defining illness or low CD4
End in -navir (atazanavir, darunavir, indinavir, etc).
Assembly of virions depends on HIV protease (pol), which cleaves polypeptide into functional parts).
Inhibits CYP450 so can boost drug concentrations
Abacavir, didanosine, emtracitabine, lamivudine, stavudine, zidovudine, tenofovir.
Mostly nucleosides and must be phosphorylated to be active
Which NRTI is a nucleotide and doesn't need to be phosphorylated to be active?
NRTIs side effects
Bone marrow suppression, peripheral neuropathy, pancreatitis
Efavirinz, nevirapine, delavirdine
Bind to reverse transcriptase at different site than NRTIs, do not require phosphorylation.
Integrase inhibitor, prevents integration of HIV genome into host cell chromosomes. Can cause hypercholesterolemia.
Enfuviritide blocks GP41, inhibiting entry
Maraviroc binds CCR-5 on t-cell/monocytes and inhibits interaction with GP120.
Glycoproteins normally synthesized by virus infected cells.
IFN a use
used in chronic hepatitis B and C, KS, hairy cell leukemia, condyloma accuminatum, renal cell carcinoma, malignant melanoma
IFN b use