7. Antivirals Flashcards
Amantadine / Rimantadine - MOA
Block viral penetration / uncoating (M2 ion channel protein)
- Also causes Dopamine release from intact nerve terminals.
“A MAN 2 DINE takes off his COAT”
Amantadine / Rimantadine - Clinical Use
Prophylaxis and treatment of Influenza A –> Recent CDC report that 100% of all influenza A now resistant –> no longer used.
- PARKINSON’S
“Amantadine blocks influenza A and causes problems with the cerebellA”
Amantadine / Rimantadine - Toxicities
Ataxia, dizziness, slurred speech
“Amantadine blocks influenza A and causes problems with the cerebellA”
- Rimantadine does not cross BBB - Less CNS side effects.
Amantadine / Rimantadine - Resistance
Mutated M2 protein
Zanamivir / Oseltamivir - MOA
Inhibit Influenza neuraminadase –> prevent release of progeny virus.
Zanamivir / Oseltamivir - Clinical Use
INFLUENZA A and B
Ribavirin - MOA
Inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase
Inhibit RNA genome replication
Ribavirin - Clinical Use
RSV
- CHRONIC HEPATITIS C
Ribavirin - Toxicities
Hemolytic anemia
-Severe teratogen
Acyclovir - MOA
Monophosphorylated by HSV/VZV thymidine kinase –> Guanisine analog –> preferentially inhibits viral DNA via chain termination (Cellular enzymes make a triphosphate).
Acyclovir - Clinical Use
HSV (mucocutaneous, genital, and encephalitis), VZV, EBV
- Prophylaxis in immunocompromised
- No effect on latent forms of HSV and VZV
- Valacyclovir is prodrug of Acyclovir with better bioavailability
- For Herpes Zoster use Famciclovir
Acyclovir - Toxicities
Few serious side effects, possible nephrotoxicity
Acyclovir - Resistance
Lack of viral thymidine kinase
Ganciclovir - MOA
5’-Monophosphate formed by CMV viral kinase –> Guanosine analog –> preferentially inhibits viral DNA via chain termination (Cellular enzymes make a triphosphate).
Ganciclovir - Clinical Use
CMV especially in immunocompromised
- Valganciclovir is prodrug of Ganciclovir with better bioavailability
Ganciclovir - Toxicities
Leukopenia, Neutropenia, Thrombocytopenia, renal toxicity
- More toxic to host enzymes than Acyclovir