Antiviral Drug List Flashcards
What are the viruses targeted by Acyclovir?
Herpes Simplex Virus and VZV (varicella-zoster)
What is the mechanism of action of Acyclovir?
structural analog of deoxyguanosine
phosphorylated by viral thymidine kinase (TK)
preferential incorporation by viral DNA polymerase
causes chain termination
What is the bioavailability of Acyclovir?
~20% oral bioavailability (valacyclovir is 3-5X better (taken up by transporters in intestine + kidney)
penetrates CSF
What is the toxicity of Acyclovir?
generally well-tolerated
What is the type of resistance to Acyclovir?
mutations in TK or viral polymerase
What is the mechanism of action of Foscarnet?
binds to pyrophosphate site of viral polymerase (also RTase)
100-fold greater selective inhibitor of viral versus human polymerase
What is the virus targeted by Foscarnet?
HSV or CMV (especially if it is resistant to Acyclovir)
What is the bioavailability of Foscarnet?
IV administration
penetrates CNS
What is the type of resistance to Foscarnet?
mutations in polymerases
What is the toxicity of Foscarnet?
nephrotoxicity is high (~30%) but reversible
hypocalcemia and CNS toxicity is also significant (25% pts)