Study your flashcards anywhere!

Download the official Cram app for free >

  • Shuffle
    Toggle On
    Toggle Off
  • Alphabetize
    Toggle On
    Toggle Off
  • Front First
    Toggle On
    Toggle Off
  • Both Sides
    Toggle On
    Toggle Off
  • Read
    Toggle On
    Toggle Off
Reading...
Front

How to study your flashcards.

Right/Left arrow keys: Navigate between flashcards.right arrow keyleft arrow key

Up/Down arrow keys: Flip the card between the front and back.down keyup key

H key: Show hint (3rd side).h key

A key: Read text to speech.a key

image

Play button

image

Play button

image

Progress

1/88

Click to flip

88 Cards in this Set

  • Front
  • Back
viral replication could be inhibited at which four levels
1. adhesion, penetration or uncoating
2. nucleic acid synthesis
3. protein synthesis
4. assembly and release
4 antivirals that inhibit penetration and/or uncoating
rimantadine
enfuvirtide
amantadine
docosanol
(READ)
at therapeuticallly safe doses, amantadine's and rimantadine's utility is limited to the prophylactic treatment of ___
influenza A
amantadine MOA
inhibits viral uncoating by blocking viral membrane protein M2 proton channel
amantadines method of selectivity
no comparable process in host cells
amantadine, oral admin?
yes- rapidly absorbed
three toxicity sx of amantadine
dizziness
anxiety
insomnia
a saturated fatty alcohol that inhibits fusion of viral envelope to cell membrane
docosanol
effective for treatment of HSV-1
docosanol
36 residue synthetic peptide based on sequence of HIV gp41 that blocks fusion of the HIV virion to lymphocytes
enfuvirtide
two principal adverse effects of enfuvirtide
hypersensitivity reactions and pneumonia
two drugs that block viral assembly and release
zanamivir (Relenza)
oseltamivir (Tamaflu)
Zanamivir and oseltamivir are approved for tx of ___ infections; if initiated during the first __ hours they can reduce severity of sx and shorten duration
influenza A and B

48 hours
zanamivir and oseltamivir MOA
inhibit viral neuramidase ->
inhibits cleavage of sialic acid from glycoproteins, glycolipids, oligosaccharides
-> blocks budding of new virus
-> slow spread through respiratory tract
which, oseltamivir or zanamivir, causes nausea and vomitting?
oseltamivir

zanamivir is relatively free of side effects
___ is directed against the F protein of RSV and is approved for prophylactic treatment of RSV infections in high risk infants
palivizumab
(a humanized monoclonal antibody)
two side effects of palivizumab
fever
pneumonia
9 drugs that inhibit viral nucleic acid synthesis
trifluridine
vidarabine
ribavirin
acyclovir
valacyclovir
penciclovir
famciclovir
ganciclovir
valganciclovir
(3 + 6 ciclovir's)
a thymidine analogue in which the three hydrogens in the 5-methyl group of thymidine have been replaced by fluorines
trifluridine
drug of choice for the treatment of herpetic conjunctival keratitis
trifluridine
trifluridine MOA
inhibits thymidylate synthetase
and feedback inhibits other steps in pyrimidine biosynthesis
trifluridine method of selectivity
differential rate of viral and cellular DNA synthesis
why is trifluridine only useful in metabolically inactive sites like the eye
it is rapidly metabolized by nucleotideases
trifluridine adverse effects
mild temporary burning and tingling
hypersensitivity in 3% of patients
an adenosine analogue in which the ribose has been replaced with arabinose
vidarabine (adenine arabinoside)
active against herpes simplex and herpes zoster infection and used for tx of ocular herpes simplex infections
vidarabine
a synthetic nucleoside containing 1,2,4 triazole carboxamide fused to a ribose moiety
ribavirin
ribavirin is approved for the tx of ___ infections and in combination with interferon alpha for the treatment of ___
RSV infections in kids

hepatitis C
ribavirin MOA
phosphorylated forms perturb intracellular nucleotide pools (?)
monophosphate *inhibits inosine monophosphate dehydrogenase*, an enzyme essential for syntheis of GMP
ribavirin admin?
inhalation for tx of RSV
a quanosine analogue having an acyclic side chain in place of the ribose moiety
acyclovir
effective against HSV1 and HSV2 and varicella zoster
drug of choice for herpes encephalitis, and tx of chicken pox
acyclovir
acyclovir MOA
phosphorylated by thymidine kinase -> becomes a triphosphate -> potent inhibition of viral DNA polymerase
why would acyclovir incorporation into nascent DNA result in chain termination
has no 3'-OH
acyclovir method of selectivity
it is more readily phosphorylated by viral TK than the cellular enzyme --> only infected cells accumulate the triphosphate
a prodrug form of acyclovir that is converted to acyclovir during first-pass hepatic metabolism
valacyclovir
oral administration of valacyclovir yields serum concentrations of acyclovir ___ compared to those after oral acyclovir
3-5x greater
valacyclovir reduces transmission of HSV-2 by __%
50%
an acyclovir analogue effective for the topical treatment of herpes labialis (cold sores)
penciclovir
penciclovir prodrug
famciclovir
ganciclovir, also an acyclic guanine nucleoside analog, inhibits which enzyme
CMV-encoded DNA polymerase
what phosphorylates ganciclovir
CMV encoded UL97 phosphotransferase
(and to a limited extent by cellular kinase)
the immunosuppressive side effects of ganciclovir (granulocytopenia, thrombocytopenia) limit its use to ___ and ___
severe CMV in immunocompromised
and
CMV retinitis
ganciclovir admin for CMV retinitis
ocular implant
ganciclovir prodrug
valganciclovir
name 7 nucleoSIDE reverse transcriptase inhibitors (NRTIs)
zidovudine
lamivudine
stavudine
emtricitabine
zalcitabine
didanosine
abacavir
(3 vudines + 2 citabines + didanosine + abacavir)
a synthetic thymidine analogue in which the 3'-OH of thymidine has been replaced with an azido group
zidovudine (AZT)
___ prolongs the lives of patients with AIDS and decreases transmission of the virus from mother to fetus
AZT (zidovudine)
zidovudine (AZT) MOA
competes w/ dTTP for binding to reverse transcriptase
when incorporated into viral DNA, nascent chains are terminated due to the absence of a 3'-OH
AZT method of selectivity
HIV encoded reverse transcriptase is 100x more likely to use AZT instead of thymidine than is DNA polymerase
method of HIV resistance to AZT
mutations in HIV RT gene
all NRTIs have the potential to induce ______ as a result of their _____
lactic acidosis

mitochondrial toxicity
a deoxyadensoine analog whose major dose limiting toxicities are peripheral neuropathy and fatal pancreatitis
didanosine (ddI)
NRTI approved for treatment of HBV
lamivudine
a guanosine analog with less hepatotoxicity than AZT
abacavir
lamivudine + zidovudine
combivir
(COMBIne things when you're LA-Zy)
abacavir + lamivudine
epzicom
abacavir + lamivudine + zidovudine
trizivir
name three nucleotide reverse transcriptase inhibitors (these aren't NRTIs - NRTIS are nucleoSIDE reverse transcriptase inhibitors)
tenofovir disoproxil
cidofovir
adefovir

(the "fovir's")
which nucleotide reverse transcriptase inhibitor inhibits HIV reverse transcriptase by being converted to the diphosphate form
tenofovir disoproxil
which nucleotide reverse transcriptase inhibitor is used for the treatement of ganciclovir or foscarnet resistant CMV retinitis
cidofovir
which nucleotide reverse transcriptase inhibitor is used for the treatment of HBV
adefovir
name three non-neucleoside reverse transcriptase inhibitors
delaviridine
nevirapine
efavirenz

*they should all be used in combo therapy
what does foscarnet inhibit
HSV and CMV encoded DNA polymerase
drug of choice for acyclovir-resistant herpes simplex in AIDS patients
foscarnet
is hydroxyurea FDA approved
no
how does hydroxyurea work?
it inhibits ribonucleoTIDE reductase ->
reducing endogenous deoxyribonucleotide pools and increasing the ratio of nucleoside RT inhibitors to endogenous nucleotides
amprenavir/fosamprenavir
atazanavir
indinavir
lopinavir
nelfinavir
ritonavir
saquinavir
HIV protease inhibitors (PIs)
HIV protease inhibitors MOA
bind to the catalytic site of HIV encoded protease ->
blocks cleavage of multiprotein gag-pol precursor into mature viral protein products
HIV protease inhibitors should only be used as part of a combo therapy that includes one or more _____
nucleoside analogs
if all PIs share the same target, would you use two different ones at the same time?
yes- they work better that way
ritonavir + liponavir
Kaletra
(Rita got Lipo and changed her name to Kaletra)
a soft gelatin version of saquinavir provides greater...
bioavailability
do inducers or inhibitors of CYP3A4 decrease serum concentration of PIs
inducers (rifampin)
HIV method of resistance to PIs
mutation in protease gene
low molecular weight glycoproteins with a broad in vitro spectrum of antiviral activity
interferon's
2a,
n1
alfacon-1
...
what can they tx?
HCV and variety of malignancies
which two interferons can be used to treat condyloma acuminata
interferon alpha 2b and n3
effective for tx of HBV and in combination with ribavirin is effective for tx of chronic HCV
interferon alpha 2-b
if administered during acute infection, ___ reduces frequency of chronic infection
interferon alpha 2-b
interferon MOA
two interferon induced enzymes inhibit viral protein synthesis:
1. dsRNA-dependent protein kinase -> phosphorylates protein synthesis factor eIF-2
2. RNA-dep 2'-5' oligoadenylate synthetase -> activates RNase that degrades viral message
how are interferons administered
IM or IV
___ interferon alphas have longer half lives and requires less frequent admin
pegylated
___ is an antisense oligonucleotide complementary to the immediate early transcriptional unit (IE2) of CMV
fomivirsen
how is fomivirsen administered
IV
what can fomivirsen tx
CMV retinitis in AIDS patients
imiquimod is effective for the tx of...
condyloma accuminata
(via induction of cytokines)
this mitotic inhibitor is also effective for tx of condyloma accuminata but doesn't work as well
podofilox