Antivirals Flashcards
Influenza drugs
Amantadine
Oseltamivir
Zanamivir
Baloxavir marboxil
Herpesvirus drugs
Acyclovir/valacyclovir
Ganciclovir/valganciclovir
Cidofovir (+ probenecid)
Foscarnet
Hemagglutatin
Binds to sialic acid to initiate infection
Neuramidiase
Cleaves/releases virions so other cells can be infected
M2 protein
Influenze protein channel
Incoating and release of viral contents
Chemotherapy
Not a substitute for vaccination
Must be stated within 48 hours for patients with high risk of influenza complications
Amantidine (Adamatases) mechanism
blocks influenza A M2 channel proteins
does not work on influenza B
amantadine resistant
nearly 100% due to mutations in M2 protein
amantidine uses
parkinsons
amantidine adverse effects
mild CNS effects (tremor, diziness, ataxia)
neuramidase inhibitors (oseltamivir, zanamivir) mechanism
competitive inhibitor or viral neuramiinidase
Oseltamivir pharmacokinetics
orally avaliable
zanamivir pharmacokinetics
Given as dry powder for oral inhalation directly to side of infection
Neuramidase inhibitor resistance
Very low
Neuramidase inhibitor uses
Prophylaxis (pre and post exposure to influenza A or B in high-risk or unvaccinated patients)
Given within 48 hours of symptom onset
Oseltamivir adverse effects
Mild nausea and vomiting
Zanamivir adverse effects
Not for use in people with asthma/COPD due to risk of bronchospasm
Cap dependent endonuclease inhibitors (baloxavir marboxil) mechanism
Inhibits cap dependent nucleus
Cap dependent endonuclease inhibitors (baloxavir marboxil) pharmacokinetics
Reduced availability when taken with dairy products
Cap dependent endonuclease inhibitors (baloxavir marboxil) uses
Alternative for oseltamivir for post expoure prophylaxis and treatment of influenza A and B (used within 48 hours)
Cap dependent endonuclease inhibitors (baloxavir marboxil) adverse effects
Mild GI symptoms and headaches
_ herpesvirus is not eradicated by antiviral drugs
Latent
Nucleoside analogues for HSV and VZV (acyclovir, valacyclovir) uses
HSV»VZV
CMV is resistant
Valacyclovir compared to acyclovir
Greater oral bioavaliability
Nucleoside analogues for HSV and VZV (acyclovir, valacyclovir) mechanism
Convirted to acyclo-GMP by viral thymidine kinase in the cytosol of infected cells
Host kinases convert mono to triphosphate which is transported to the nucleus and inhibits viral DNA polymerase or causes DNA chain termination
Resistance to Nucleoside analogues for HSV and VZV
Viral TK defiencu
Nucleoside analogues for HSV and VZV uses
Genital herpes
Primary herpetic gingivostomatitis
Mucocutaneous HSV
HSV encephalitis
VZV infections
Nucleoside analogues for HSV and VZV adverse effects
Occur with IV use
Renal dysfunction from crystalline neuropathy (Minimalized by hydration and slow IV infusion)
Neurotoxicity
Nucleoside analogues for CMV
Ganciclovir
Valganciclovir
Nucleoside analogues for CMV are used for
All herpesviruses but especially CMV
Ganciclovir and calganciclovir mechanism
Same as acyclovir
Converted to monophosphate by CMV UL97 kinase then die and try phosphorylated by host kinases
anti-try phosphates inhibit CMV UL54 DNA polymerase and terminates DNA chain elongation
Nucleoside analogues for CMV reistance
Mutations in UL97 kinase, UL54 DNA polymerase
Valganciclovir compared to ganciclovir
Higher oral bioavaliability
Valganciclovir and ganciclovir uses
Restricted due to toxicity
HSV herpetic keratitis
CMV retinitis
Prophylaxis of CMV infection and organ transplant patients
Valganciclovir and ganciclovir Adverse effects
Lower therapeutic index than acyclovir/valacyclovir
Black box warning for myelosuppression
Renal insufficiency
Nucleotide analogs for CMV
Cidodovir (cytidine nucleotide analogs)
Active against Kinase deficient herpes virus is because they don’t need to be phosphorylated by viral tyrosine kinase
Cidofovir mechanism
Converted to active diphosphate by host kinesis
Inhibits viral DNA polymerase and terminates DNA chain

Cidofovir pharmacokinetics
IV only
Excreted by OAT1
Cidofovir use
Black box warning only for use for CMV retinitis and HIV/AIDS patients
Alternative to ganciclovir, foscarnet
Cidofovir adverse effects
Black box warning for nephrotoxicity
Given with probenecid
Black box warning for neutropenia
Black box warning for carcinogen and teratogen
Non-nucleoside analog for drug resistant HSV and CMV
Foscarnet
Foscarnet uses
All herpesvirures
Hepatitis B
HIV
Foscarnet mechanism
Inhibits DNA polymerase and HIV reverse transcriptase (not used for HIV treatment
Foscarnet use
Black box warning for appropriate use
Ganciclivir-resistane CMV retinitis in HIV/AIDS patients or organ transplant recipients
Acylovar-resistant HSV mucocutaneous infections
Foscarnet adverse effects
Black box warning for nephrotoxicity
Pronounced electrolyte disturbances- Symptomatic hypocalcemia
Blackbox warning for seizures due to electrolyte imbalance