Anti-viral agents Flashcards
What is the selectivity of action of aciclovir
only activated in infected cells, then becomes concentrated
has a higher affinity for viral DNA polymerase than cellular enzymes`
What enzyme activates aciclovir?
thymidine kinase
What is aciclovir competitive with, what does it do?
Competes with GTP
Inhibits viral DNA polymerase, DNA chain terminator
has a narrow spectrum of activity
There is resistance to aciclovir, but these are non-pathogenic. How are they resistant?
Also appears in less harmful viruses, how?
Also appears in harmful viruses, how?
Absence of thymidine kinase
Mutant form of thymidine kinase
Altered DNA polymerase
What is the prophylaxis treatment for genital herpes
aciclovir
patient can titrate dose
cessation leads to pre-therapy state
leads to long term therapy
An anti-cytomegalovirus drug example is ganciclovir
what does it require
what does it do
what is it active against
disadvantages
requires phosphorylation by UL97
ganciclovir triphosphate acts as DNA pol inhibitor
active against all herpesviruses
poor oral absorption - valganciclovir
toxic to bone marrow.
Another example of an anti-cytomegalovirus is cidofovir
what does it require
what does it do
what is it active against
disadvantages
Non-viral dependent phosphorylation
Inhibits viral DNA polymerase
Broad spectrum
given by IV
nephrotoxic
The last example of an anti-cytomegalovirus drug is foscarnet
what does it do
disadvantages
viral DNA polymerase inhibitor
poor oral availability
nephrotoxic
Ribavirin may interfere with mRNA processing and acts a mutagen. It is broad spectrum; both DNA and RNA viruses, but it is only useful in what scenarios
Severe RSV infection - inhale drug
Lassa fever
Chronic hep C virus infection
Amantadine inhibits uncoating of influenza A virus, but is no longer recommended, why?
Poorly tolerated bc of CNS stimulation
resistance rapidly emerges
Neuraminidase inhibitors, work against all known influenza NA (for severe/high risk). name the two examples
zanamavir and
oseltamivir (resistance reported)