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Infectious Diseases > Exam 4 - antivirals MCMP part 1 > Flashcards

Exam 4 - antivirals MCMP part 1 Flashcards

1
Q

acyclovir MOA

A

competitive inhibitor of viral DNA polymerase
incorporated into the DNA
acts as chain terminator

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2
Q

acyclovir resistance

A

mutations in viral thymidine kinase
mutations in viral DNA polymerase

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3
Q

acyclovir spectrum

A

HSV1, HSV2, and VZV

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4
Q

valacyclovir moa

A

same as acyclovir

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5
Q

valacyclovir resistance

A

same as acyclovir

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6
Q

valacyclovir spectrum

A

HSV 1/2, VZV

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7
Q

how does valacyclovir compare to acyclovir

A

improved bioavailability and efficacy

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8
Q

penciclovir and famciclovir moa

A

activated by viral and cellular kinases via phos
competitive inhibitor of viral DNA polymerase
NO chain termination

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9
Q

penciclovir and famciclovir resistance

A

viral kinase mutations

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10
Q

penciclovir vs acyclovir

A

higher affinity for HSV TKs
more stable
but very similar potencies

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11
Q

ganciclovir moa

A

same as penciclovir

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12
Q

ganciclovir resistance

A

mutations in CMV kinase UL97 gen or UL54
not cross resistant

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13
Q

valganciclovir moa

A

same as penciclovir

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14
Q

valganciclovir resistance

A

same as ganciclovir

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15
Q

valganciclovir and ganciclovir spectrum

A

CMV retinitis

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16
Q

famciclovir and penciclovir spectrum

A

herpes and herpes zoster

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17
Q

foscarnet moa

A

carboxyl overlaps with binding site
phos occupies position
traps polymerase in closed formation
DNA cannot translocate

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18
Q

foscarnet spectrum

A

CMV retinitis

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19
Q

foscarnet resistance

A

mutations in DNA pol or HIV RT
cross resistant to ganciclovir

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20
Q

cidofovir moa

A

only phos x2
competitive inhibitor and chain terminator

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21
Q

cidofovir spectrum

A

CMV, HSV1, HSV2, VZV

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22
Q

letermovir moa

A

inhibits terminase complex (rolling) and prevents cleavage and packaging

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23
Q

letermovir resistance

A

no cross resistance

24
Q

what are the chain terminators of herpes drugs

A

acyclovir and valacyclovir
penciclovir and famciclovir
ganciclovir and valganciclovir
cidofovir

25
Q

which herpes drugs can be incorporated in the viral DNA

A

acyclovir and val
penciclovir and fam
gan and valgan
cidofovir

26
Q

what are prodrugs of the herpes drug

A

valacyclovir
famciclovir
valganciclovir

27
Q

how is valacyclovir and famciclovir activated

A

activated by viral thymidine kinase which is more active in infected cells

28
Q

how is valganciclovir activated

A

activated by cellular kinases but accumulates in CMV cells due to higher activity in those cells

29
Q

what herpes drugs show cross resistance with eachother

A

-acyclovir, valacyclovir, penciclovir and famciclovir
-ganciclovir and valganciclovir

30
Q

what drugs are similar to NRTIs

A

acyclovir, valacyclovir, penciclovir, famciclovir, and valganciclovir

31
Q

why are valacyclovir and valganciclovir more bioaviable

A

they are rapidly converted in the liver and intestine by esterases

32
Q

describe the influenza life cycle

A

enveloped into new cell
broken down for mRNA synthesis
RNA replicated
sent off to be exported out

33
Q

what steps in the life cycle of influenza are targeted by drugs

A

the exportation step
neuraminidase

34
Q

what is the MOA for neuraminidase inhibitors

A

bind to the active site of neuraminidase enzymes and prevent the cleavage of sialic acid residues on viral envelopes. This stops the spread of the virus

35
Q

neuraminidase inhibitor resistance

A

mutations in the active site of neuraminidase

36
Q

baloxavir moa

A

inhibits viral “cap snatching” aka blocks transcription

37
Q

life cycle of hep c

A

receptor binding and endocytosis
release of viral DNA
translation of viral rna
proteolytic processing
rna replication
virion assembly
transport and release of particle

38
Q

ribavirin moa

A

inhibition of IMPDH to reduce GTP levels
direct inhibition of rna polymerase
incorporation into viral RNA

39
Q

ribavirin specrum

A

flu a & b
hep abc
herpes
VZV
measles
hantavirus
lassa fever virus

40
Q

protease inhibitor moa

A

block cleavage of the HCV polyprotein

41
Q

p1-p3 substrates

A

simeprevir
paritaprevir

42
Q

p2-p4 substrates

A

grazoprevir
voxilaprevir
glecaprevir

43
Q

resistance of protease inhibitors

A

mutations in the NS3 active site

44
Q

sofosbuvir moa

A

NS5B inhibitor
rna polymerase inhibitor
incorporated into rna chain and causes termination

45
Q

resistance to sofosbuvir

A

S288T mutation

46
Q

dasabuvir moa

A

NS5B inhibitor
binds to palm I site of HCV rna polymerase
prevents conformational changes and blocks incorporation into viral RNA

47
Q

what are the NS5A inhibitors

A

ledipasivir
elbasvir
daclatasvir
velpatasvir (2nd gen)
pibrentasvir (2nd gen)

48
Q

how to NS5A inhibitors work

A

bind tightly to NS5A and inhibit both viral RNA replication and assembly/release of viral particles

49
Q

resistance to NS5A inhibitors

A

occur in first 100 amino acids
first gen: single mutation
second gen: retain activity against common resistants

50
Q

what is the black box warning for HCV antivirals

A

hep B can get reactivated

51
Q

describe the life cycle of hep b

A

partially double stranded DNA virus. viral genome replication includes an RNA intermediate that is converted to DNA by reverse transcriptase

52
Q

anti HBV drug moa

A

incorporated into viral DNA
causes DNA chain termination

53
Q

remdisivir moa

A

inhibits viral RNA polymerase

54
Q

nirmatrelvir moa

A

peptidomimetic that inhibits active site cysteine residue in 3CLpro

55
Q

molnupiravir moa

A

polymerase inhibitor and chain terminator

Infectious Diseases (28 decks)

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