Antiviral Agents Flashcards
What is acyclovir effective against?
herpes simplex 1,2 and herpes zoster virus
What does acyclovir convert?
To monophosphate acyclo-GMP by viral thymidine kinase, then to triphosphate by a cellular enzyme
How does acyclovir work?
The triphosphate formed inhibits DNA polymerase through chain terminations
How is acyclovir administered?
Topically
Orally
IV
How are some adverse effects of acyclovir?
psychiatric = Cotards
Toxicity if overdose = lethargy, confusion, myoclonus
What is the difference between valacyclovir and acyclovir?
Vala is acyclovir esterified to valine
greater oral bioavilability
How does resistance to acyclovir and valaciclovir occur?
Mutation of viral thymidine kinase and/or DNA polymerase
What is idoxuridine used for?
Topically only = herpes keratitis
- too toxic for systemic use
What are ganciclovir and valganciclovir against?
Active CMV
What is acyclovir an analogue of?
Guanosine
What is ganciclovir an analogue of?
Deoxyguanosine
What does ganciclovir do?
Phosphorylated to monophosphate by CMB thymidine kinase then to triphosphate by cellular kinases
How does ganciclovir work?
Inhibits viral DNA polymerase by acting as a chain terminator
What is the difference between valganciclovir and ganciclovir?
Valine ester of it
Greater oral bioavailability
What are the adverse effects of valganciclovir and ganciclovir?
Adverse effects such as bone marrow suppression
Which drugs are effective against herpes?
foscarnet acyclovir valacyclovir ganciclovir valgancyclovir
Which drugs are reverse transcriptase inhibitors?
Nuceloside and nucleotide analgoues (NRTIs)
- nuceloside analogues = zidovudine, lamivudine
- nucleotide analogues = tenofovir
What do NRTIs do?
inhibit reverse transcriptase by incorporating into growing DNA chain and not linking subsequent base
Adverse effects of zidovudine?
GI, haem, headache, hepatotoxic, cardiomyopathy
Adverse effects of lamivudine?
nausea, fatigue, headache, diarrhoeaa, cough, pro-inflamm response, autoimmunity