Antivirals Flashcards
Acyclovir (zovirax) MOA
Guanosine analogue.Inhibits DNA synthesis by competing with dGTP. Terminates the chain due to lack of 3 prime hydroxyl. Requires phosphorylation by viral thymidine kinase.
Herpes DOC
Acyclovir
Acyclovir resistance
decrease viral thymidine kinase so the drug can’t be activated by phosphorylation.
Acyclovir kinetics
oral/IV/topical. Short half life. Concentrated (trapped) in viral cells. Excreted by the kidney
Valcyclovir
pro-drug with higher bioavailability. Eventually converted into acyclovir.
Acyclovir uses
genital herpes, oral herpes, herpes keratitis, encephalitis, prophylaxis in organ transplants.
Acyclovir toxicity
nephrotoxicity with high IV doses (decreased with hydration), nausea/vomiting, HA. Safe to use during pregnancy.
Docosanol (Abreva) MOA
Inhibits viral fusion
Docosanol (abreva) uses
OTC topical preparation for cold sores
Ganciclovir/valganciclovier MOA
Guanosine analogue activated by viral kinases. inhibits DNA polymerase. Less active and more toxic than Acyclovir.
Ganciclovir kinetics
Ocular implant, IV, Oral.
valganciclovir kinetics
Oral prodrug.
Ganciclovir uses
CMV/Herpes in immunocompromised, CMV retinitis, Life threatening CMV infections.
Ganciclovir toxicity
myelosuppression (neutro, thrombo, leuko) especially when used with zidovudine for HIV. Severe HA, confusion and seizures.
Foscarnet (foscvir) MOA
directly inhibits DNA/RNA polymerase and reverse transcriptase. No need for phosphorylation (good for use in resistant strains).
Foscarnet uses
Back up for HSV/CMV that are resistant to acyclovir or ganciclovir.
Foscarnet toxicity
Renal, adjust the dose and hydration.
Cidofovir (vistide) MOA
Cytosine analogue that inhibits viral DNA polymerase. Phosphorylated independent of viral enzymes.