Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
18 Cards in this Set
- Front
- Back
|
Antiherpes Nucleoside/ Nucleotide Analoges
|
Acyclovir
Valaciclovir Cidofovir (Does not require viral kinases)(nucleoTide) |
|
|
Acyclovir targets
|
Thymidine Kinase (Intermedate)
DNA-Dependent DNA Pol (Final) |
|
|
Acyclovir Mechanism
|
Prodrug is converted by TK to acyclo-GMP > acyclco-GTP > Inhibits viral DNA Pol, incorporation into nascent DNA results in termination because there is no 3'-OH.
|
|
|
Acyclovir Resistance
|
TK-deficient mutant
TK-low mutant TK mutant incapable of accepting thymidine |
|
|
Anti-HIV Nucleosie analoges
|
Azidothymidine (AZT)
Lamivudine (3TC) Emtricitabine (FTC) |
|
|
Azidothymidine (AZT) Mechanism
|
CELLULAR TK converts AZT > 5'-triphosphate form > Inhibits Reverse Transcriptase (RT), lacks 3'-OH causing chain termination.
|
|
|
Azithrothymidine Toxicity
|
Inhibits cellular TK
Inhibits mito DNA Pol Bone Marrow Suppression |
|
|
Reasons for combination (NRTI + NNRTI) HIV therapy
|
Low efficacy of each drug alone
Resistance mutations to one drug do not effect other Multiple resistance mutations decrease fitness of virus |
|
|
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)
|
Foscarnet
Efavirenz Nevirapine Delavirdine |
|
|
Foscarnet Mechanism
|
Mimics the pyrophosphate product of DNA/RNA polymerization. (Inhibits DNA and RNA pol and does not require activation)
|
|
|
Inhibitor of Viral Attachment
|
Enfuvirtide (T-20)
|
|
|
Enfuvirtide (T-20) Mechanism
|
Mimics HR2, binds HR1, and prevents HR2-HR1 interaction preventing membrane fusion and viral entry.
|
|
|
Inhibitors of Viral Uncoating
|
Amantadine
Rimantadine |
|
|
Amantadine/Rimantadine Mechanism
|
Block M2 channel preventing pH change in endosome
|
|
|
Neuraminidase Inhibitors
|
Zanamivir
Oseltamivir |
|
|
Zanamivir/Oseltamivir Mechanism
|
Binds in Neuraminidase catalytic site preventing release of virions from the cell surface
|
|
|
Action of Interferons
|
Released by lymphocytes in response to pathogens.
Triggers protective defenses of the immune system and activates kinases (PKR) |
|
|
Imiquimod Mechanism
|
Interacts with Toll-like receptors (TLR7 and TLR8) to boost innate immunity including secretion of interferons.
|
