Antivirals Flashcards
Anti-Influenza drugs
Oseltamivir, Zanamivir, Rimantadine
mechanism: oseltamivir, zanamivir
inhibit neuraminidase; inhibit viral progeny release
sialic acid analogs
oseltamivir, zanamivir
adverse effects: oseltamivir, zanamivir
GI upset
**zanamivir may exacerbate COPD/asthma
flu strain treated by oseltamivir and zanamivir
A and B
inhibitors of viral genome replication: HSV and VZV
acyclovir, valacyclovir
inhibitors of viral genome replication: CMV
ganciclovir, valganciclovir
Inhibitors of viral genome replication: HSV, VZV, CMV
cidofovir, foscarnet
Antihepatitis Virus
ribavirin
INF a
hepatitis B
lamivudine
tenofovir
adefovir
entecavir
telbivudine
hepatitis C
simeprevir
sofosbuvir
ledepasvir
daclatasvir
dasabuvir
Does acyclovir cure HSV/VZV infections?
no, mangement
mechanism: acyclovir, valacyclovir
nucleoside analog
guanine attached to acyclic moiety
acyclovir is activated by
thymidine kinase
ACV monophosphate is converted to
ACV triphosphate
resistance to acyclovir
mutation/loss of thymidine kinase
mechanism: ribavirin
inhibits guanine synthesis, mutates viral DNA
ribavirin is activated by
host kinases
ribavirin inhibits
RNA polymerase
Clinical Use: Ribavirin
Hep C, RSV (aerosol)
adverse effects: ribavirin
hemolytic anemia
teratogen
pruritis
resistance: ribavirin
genotype 1 HCV
administration: ribavirin
oral, inhalation
excretion: ribavirin
urine
adverse effects: acyclovir
crystalline nephropathy
renal failure with poor hydration
administration: acyclovir
oral, IV, topical
excretion: acyclovir
urine
prodrugs have higher
oral bioavailability
mechanism: ganciclovir
guanosine analog
initial phosphorylation of ganciclovir is done by
UL97
clinical use: ganciclovir
CMV first line
adverse effects: ganciclovir
bone marrow suppression
nephrotoxicity
CNS toxicity
teratogen
resistance: ganciclovir
mutated tyrosine kinase
administration: ganciclovir
IV, opthalmic
excretion: ganciclovir
urine
why is ganciclovir more toxic?
better substrate for kinases= higher toxicity, less selectivity
mechanism: foscarnet
nucleoside analog, viral DNA/RNA inhibitor
foscarnet inhibits
HIV RT
clinical use: foscarnet
CMV 2nd line
acyclocvir resistant HSV
broad spectrum for viral illnesses
adverse effects: foscarnet
nephrotoxicity
electrolyte imbalance
seizures
resistance: foscarnet
mutated DNA polymerase
administration: foscarnet
IV
excretion: foscarnet
urine
mechanism: cidofovir
nucleotide analog, inhibits viral DNA polymerase
clinical use: cidofovir
CMV, HSV (3rd line)
adverse effects: cidofovir
nephrotoxicity
administation: cidofovir
IV
excretion: cidofovir
urine
what can reduce the toxicity of cidofovir?
probencid
mechanism: trifluridine
thymidine analogue, requires host kinases
clinical use: trifluridine
HSV 1/2 Keratitis, CMV
adverse effects: trifluridine
hypersensitivity
administation: trifluridine
opthalmic, topical
INF-a mechanism
cytokine, anti-viral state activates JAK/STAT
clinical use: INF-a
chronic HBV/HCV, condyloma acuminatum, HHV-8, hairy cell leukemia, renal cell carcinoma, malignant melanoma
INF-a adverse effects
neutropenia, myopathy, depression, flu-like symptoms
administration INF-a
IM, IV
excretion INF-a
urine
mechanism: lamivudine
cytosine analog, inhibits HIV RT and HBV polymerase
clinical use: lamivudine
HBV, HIV
adverse effects: lamivudine
headache, fever, nausea
resistance: lamivudine
mutated polymerase
mechanism: sofosbuvir
HCV RNA dependent RNA polymerase
clinical use: sofosbuvir
HCV w/ ledipasvir
adverse effects: sofosbuvir
headache, fever, nausea
telaprevir mechanism
HCV protease inhibitor
clinical use: telaprevir
HCV w/ peg-interferon, ribavirin
adverse effects: telaprevir
rash, pruritis, fatigue, GI, anemia, CYP3A inhibition
resistance: telaprevir
develops rapidly
mechanism: simeprevir
HCV protease inhibitor
clinical use: simeprevir
HCV w/ ribavirin, simeprevir, ledipasvir
adverse effects: simeprevir
photosensitivity, rash
rimantidine/amantadine mechanism
inhibits M2 protein, inhibits viral uncoating
clinical use: rimantidine
Flu A PPX or treatment
adverse effects: rimantadine
severe CNS, GI
mechanism of resistance: rimantadine
mutated M2 protein, widespread resistance
Ozeltamivir/zanamavir mechanism
NA inhibitor
Ozeltamivir/zanamavir clinical use
flu A and B
adverse effects oseltamivir
headache, GI
zanamivir adverse effects
headache, sore throat, asthma ex.
Ozeltamivir/zanamavir resistance
NA mutation
administration Ozeltamivir
oral
administation zanamivir
inhaled