Hepatitis Antivirals Flashcards
What is the treatment for HBV?
Lamivudine with Pegylated Interferon-alpha
Other antivirals - Entecavir, tenofovir, adefovir dipivoxil, telbivudine
M.O.A of Pegylated Interferon Alpha
- What does “pegylated” mean?
IFN-a
- cytokine protein
- inhibits viral replication by inducing host cell enzymes which inhibit viral RNA translation leading to degradation of viral mRNA and tRNA
- activates NKCs and macrophages
- increases antigen presentation to lymphocytes
- induces resistance of host cells to virus - seroconversion of HbeAg to HbeAb
Pegylated = conjugated to polyethylene glycol - makes it last 7x longer in serum
What is the treatment for HCV?
Pegylated IFN-a + Ribavirin
Both teratogenic
M.O.A of Nucleoside Analogs;
- Lamivudine (cytosine analogue)
- Adefovir Dipivoxil (adenosine analogue)
- Entecavir (guanosine analogue)
- Tenofovir (adenosine analogue)
- Telbivudine (thymidine analogue)
All have to be phosphorylated intracellularly to their active analog forms.
They inhibit HBV DNA poly (reverse transcriptase) by:
- competing with the endogenous nucleoside for incorp into DNA (Lamivudine, Entecavir)
- are incorp into the DNA where they terminate further elongation of DNA chain (adefovir, telbivudine, tenofovir)
M.O.A of Ribavirin
Pro-drug for synthetic guanosine nucleoside analog
Converted to 5’ phosphate derivatives, the main product being ribavirin-triphosphate, which inhibits guanosine triphosphate formation, preventing viral mRNA capping and blocking RNA-dep RNA poly