antiviral pharmacology/medchem Flashcards

1
Q

immune globulin use

A

acute, serious infections
post exposure prophylaxis
used with nucleoside antiviral

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2
Q

herpes genome

A

dsDNA

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3
Q

influenza genome

A

(-) ssRNA

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4
Q

viruses that use host polymerase

A
DNA viruses
herpes (human and simplex)
varicella
epstein-barr
CMV
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5
Q

acyclovir MoA

A

guanosine analog prodrug

terminates DNA chain synthesis

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6
Q

what converts acyclovir to active drug

A
  • viral thymidine kinase does first phosphorylation

- guanosine monophosphate kinase does rest

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7
Q

resistance mechanisms to acyclovir and valacyclovir

A
  • deficient thymidine kinase
  • altered thymidine kinase
  • altered DNA polymerase
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8
Q

gancyclovir activity against

A

CMV
HSV
VZV
HHV

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9
Q

ganciclovir toxicity

A

high because its less specific to viral thymidine kinase

-potential for bone marrow toxicity

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10
Q

famciclovir features

A
  • prodrug of penciclovir which increases bioavailability

- similar to acyclovir but longer duration

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11
Q

cidofovir MoA

A

cytosine analog that inhibits DNA synthesis

No viral TK needed

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12
Q

cidofovir dose limiting toxicity

A

nephrotoxicity

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13
Q

cidofovir route

A

IV only due to poor bioavailability

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14
Q

foscarnet MoA

A

inhibits DNA polymerase by blocking nucleotide binding, with no need of triphosphate (thus TK) like acyclovir and others

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15
Q

foscarnet side effects

A
headache
tremor
seizures
hallucinations
*all due to chelation of calcium*
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16
Q

foscarnet dose limiting toxicity

A

nephrotoxicity

hypocalcemia

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17
Q

foscarnet route

A

IV only

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18
Q

idoxuridine and trifluridine (thymidine analogs) MoA

A

is phosphorylated then inhibits DNA synthesis by inhibiting thymidylic phosphorylase

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19
Q

fomivirsen use

A

CMV retinitis

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20
Q

fomivirsen MoA

A

inhibits replication through specific and nonspecific mechanisms like virus binding

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21
Q

fomivirsen route

A

eye injection (intravitreal)

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22
Q

docosanol use

A

cold sores

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23
Q

imiquimod use

A

HPV infections

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24
Q

imiquimod MoA

A

not fully understood, does induce secretion of pro-inflammatory cytokines

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25
Q

influenza strain that causes pandemics

A

A only

26
Q

influenza nomenclature

A

H (hemagglutinin - 16 subtypes)

N (neuraminidase - 9 subtypes)

27
Q

neuraminidase inhibitor drugs

A

zanamivir

oseltamivir (prodrug)

28
Q

neuraminidase inhibitor MoA

A

inhibits cleavage of sialic acid and the release of virus from the infected cell

29
Q

neuraminidase inhibitor adverse effects

A

bronchospasm
unusual psychiatric behavior
d/n
Uncommon though

30
Q

viral uncoating inhibitor use

A

influenza A

31
Q

viral uncoating inhibitor drugs

A

amantadine

rimantadine

32
Q

viral uncoating inhibitor MoA

A

inhibits M2 ion channel in flu virus and uncoating of virus in endosome

33
Q

viral uncoating inhibitors adverse effects

A

GI and CNS

34
Q

hepatitis C genome

A

(+) ssRNA

35
Q

hepatitis B genome

A

dsDNA-RT

36
Q

hepatitis strain with no vaccine

A

C

37
Q

hep A transmission

A

fecal-oral

38
Q

hep C transmission

A

injection drug use

blood exposure

39
Q

interferon use

A

in combination with ribavirin for hep C

not very useful however

40
Q

ribavirin use

A

combo therapy for hep C

41
Q

ribavirin MoA

A
  • inhibits capping of 5’ end of mRNA

- inhibits inosine monophosphate deyhdrogenase in DNA production

42
Q

ribavirin adverse effects

A
  • hemolytic anemia
  • bone marrow suppression
  • possibly teratogenic
43
Q

NS5A inhibitor MoA

A

inhibits the scaffolding protein that allows for the building of complex protein structures for use in the hep C virus

44
Q

NS5A (replication complex) inhibitor drugs

A
daclatasvir
velpastasvir
pibrentasvir
elbasvir
ledipasvir
45
Q

NS5A inhibitor adverse effects

A

headache
fatigue
nausea

46
Q

HCV protease (NS3/A4) inhibitor drugs

A

glecaprevir
paritaprevir
grazoprevir

47
Q

HCV protease inhibitor adverse effects

A

anemia

skin rashes

48
Q

HCV polymerase (NS5B) inhibitors

A

sofosbuvir

49
Q

HCV polymerase inhibitor drug interaction

A

serious bradycardia with amiodarone

50
Q

hep B transmission

A

contact with blood or body fluids of infected person

51
Q

unique DNA construct for hep B

A

covalently closed circular DNA (cccDNA)

52
Q

HIV drugs used for hepatitis (NI inhibitors)

A

tenofovir

entecavir

53
Q

valacyclovir features

A
  • great oral bioavailability

- cleaved to active drug by valacyclovirase before portal circulation

54
Q

idoxuridine and trifluridine toxicity

A

bone marrow toxicity

-not very specific for virus so we get a lot into our DNA

55
Q

which drugs have the phosphonate group

A

cytidine analogs
cidofovir
deoxycytidine

56
Q

why aren’t adamantanse used much

A

near universal resistance

57
Q

hemagglutinin

A

influenza component that binds to human glycoprotein containing sialic acid

58
Q

NI inhibitors MoA

A
  • compete with adenosine to cause chain termination

- prodrug

59
Q

HCV polymerase inhibitor (NS5B) MoA

A

inhibit nucleoside biosynthesis and mRNA capping

60
Q

HCV protease inhibitors MoA

A

bind non-covalently to serine in the active site