Antivirals Flashcards
what stage of herpes virus is suppressed by antivirals
lytic stage
antiviral treatments are indicated for what members of the herpesvirus family
VZV
HSV-1
HSV-2
CMV
Acyclovir MOA
requires initial phosphorylation by the viral thymidine kinase enzyme
competitive inhibitor of viral DNA polymerase
chain termination upon incorporation into the viral DNA
resistance to acyclovir
mutation of thymidine kinase gene
cross-resistance with other antivirals iwth similar mechanism
oral or IV administration of acyclovir:
- severe/disseminated mucocutaneous disease
- HSV encephalitis
- varicella zoster
- neonate infections
- VZV in immunocompromised
- genital herpes
Oral:
- genital herpes
- varicella zoster
IV:
- severe/disseminated mucocutaneous disease
- neonate infections
- HSV encephalitis
- VZV in immunocompromised patients
prodrug of acyclovir
acyclovir attached to a valine moiety. Metabolised into acyclovir in the liver and intestines
3-5x greater oral bioavailabiilty than acyclovir
Valacyclovir
therapeutic indications for valacyclovir
primary and recurrent genital herpes
varicella in older children and adults
zoster
oralabial herpes
how is foscarnet administered
IV
Analogue of pyrophosphate. Occupries site where pyrophosphate normally resides and blocks pyrophosphate release. Blocks catalytic cycle
**does not require prior phosphorylation by thymidine kinase in order to act
Foscarnet
therapeutic indications of foscarnet
HSV and VZV infections resistant to acyclovir
CMV retinitis, colitis, esophagitis
Ganciclovir requires initial phosphorylation by 1 (viral kinase enzyme). It is phosphorylated much more efficiently than acyclovir, therefore more active for 2 infections. It is also a competitive inhibitor of the viral 3. 4 termination upon incorporation into the viral DNA
- CMV UL97
- CMV
- DNA polymerase
- Chain
how is ganciclovir administered
IV
Oral
Intraocular routes
- poor bioavailability
therapeutic indications for ganciclovir
IV
- CMV retinitis (AIDs)
- CMV colitis, pneumitis, esophagitis (foscarnet does colitis, esophagitis, and retinitis)
Intraocular injection or implant
- CMV retinitis
IV followed by oral
- transplant pts.
how can you reduce the risk of CMV in transplant patients
IV followed by oral ganciclovir
prodrug of ganciclovir with higher bioavailability and serum levels approach IV ganciclovir
valganciclovir