Anti-Virals Flashcards
Mechanism of action of Ion Channel Blockers (Adamantane Drugs)
Block the viral M2 proton channel, prevent uncoating of influenza virus (early endosome)
<p>Names of Adamantane drugs </p>
<p>Rimantadine, Amantadine </p>
Enfuvirtide and Maraviroc act on what type of virus
HIV
Enfuvirtide MOA
Mimics HR2, binds to HR1 and prevents HR1-HR2 interaction, thus preventing fusion of HIV with CD4 T cell
Maraviroc MOA
small molecule antagonist that binds to CCR5. Only blocks strains of HIV that use CCR5 receptor (HIV-1)
Name the 2 antivirals that act as nucleic acid synthesis inhibitors
Acyclovir (valacyclovir), Ganciclovir (valganciclovir)
Acyclovir & Ganciclover act on what viruses
Herpes simples viruses 1 & 2, Varicella zoster virus, & cytomegalovirus
First step needed prior to acyclovir & ganciclover activity
Require metabolic activation to a triphosphate form
MOA of Acyclovir & ganciclover
After being metabolically activated to a triphosphate form, acyclovir or ganciclover compete with dGTP for terminal end of growing DNA chain within viral DNA polymerase. After binding to terminal end, traps the polymerase at that location, preventing further chain elongation.
Does acyclovir/ganciclover use host or viral kinase for activation?
Viral kinase used for addition of first phosphate group
Route of administration for acyclovir/ganciclover?
As a orally absorbed pro drug (valacyclovir/valganciclover)
Name NRTI’s used to treat HIV
ABACAVIR LAMIVUDINE TENOFOVIR DISOPROXIL ZIDOVUDINE (AZT) EMTRICITABINE didanosine (ddl) stavudine
Metabolic activation of nucleoside reverse transcriptase inhibitors (NRTIs) occurs by host or viral kinase?
Host kinase used for addition of first phosphate group.
NRTI inhibition type (competitive or noncompetitive)?
NRTI’s competitively inhibit reverse transcriptase.
Indirect inhibition of polymerase by NRTI has what consequence?
NRTIs also inhibit host cell mitochondrial DNA polymerase, causing depletion of mitochondrial DNA and subsequently mitochondrial RNA and peptides involves in ox phos. This ultimately leads to mitochondrial dysfunction, and leads to several toxicities associated with NRTIs.