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PHRM 865 > E4 MedChem antivirals I > Flashcards

E4 MedChem antivirals I Flashcards

1
Q

HSV-1
A. oral
B. genital

A

A

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2
Q

HSV-2
A. oral
B. genital

A

B

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3
Q

when can severe disease occur from CMV?

A

if infection occurs during fetal development

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4
Q

Acyclovir:
______ _______ derivative

A

acyclic guanosine

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5
Q

Acyclovir:
lacks _ _____

A

3’ hydroxyl

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6
Q

Acyclovir selectively accumulates in ________ cells.
this results in (higher/lower) conc.

A

infected, higher

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7
Q

Acyclovir requires _ phosphorylation events

A

3

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8
Q

Acyclovir MOA

A

competitive inhibitor of viral DNA polymerase

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9
Q

Acyclovir competes with _____

A

dGTP

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10
Q

T or F:
acyclovir is incorporated into DNA

A

true

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11
Q

Acyclovir acts as a _____ terminator

A

chain

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12
Q

Acyclovir is active against what 3 things

A

HSV-1, HSV-2, VZV

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13
Q

2 resistance mechanisms against acyclovir

A

mutations in viral thymidine kinase
mutations in viral DNA polymerase

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14
Q

Valacyclovir is an _______ ester of acyclovir

A

L-valyl (whatever tf this means)

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15
Q

Valacyclovir is rapidly converted to _________ by _________ in the intestine and liver

A

acyclovir, esterases

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16
Q

T or F:
Valacyclovir has improved efficacy compared to acyclovir for all indications

A

true frfr

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17
Q

valacyclovir is transported by ________ ________ ____ transporters

A

intestinal amino acid

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18
Q

Famciclovir is a prodrug of ______

A

penciclovir

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19
Q

How is famciclovir converted to penciclovir?

A

first pass metabolism in intestine and liver

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20
Q

MOA of famciclovir and penciclovir:
1. activated by ____ and cellular _________
2. competitive inhibitor of viral ____ _________
3. Does NOT cause immediate _______ __________

A
  1. viral, kinases
  2. dna polymerase
  3. chain termination
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21
Q

T or F:
Viral kinase mutants confer cross-resistance to penciclovir and acyclovir

A

true

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22
Q

T or F:
acyclovir has a higher affinity for HSV TK than penciclovir

A

false, other way around

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23
Q

T or F:
levels of penciclovir triphos in infected cells are higher than the levels of acyclovir triphos

A

true

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24
Q

T or F:
HSV DNA polymerases have a higher affinity for acyclovir triphos than for penciclovir

A

true

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25
Q

T or F:
Acyclovir triphos is more stable than Penciclovir triphos in HSV-infected cells

A

false, other way around

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26
Q

short-chain terminator:
A) acyclovir
B) penciclovir

A

B

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27
Q

obligate DNA chain terminator:
A) acyclovir
B) penciclovir

A

A

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28
Q

has 3’ hydroxyl group on its acyclic side chain
A) acyclovir
B) penciclovir

A

B

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29
Q

2 clinical uses of oral famciclovir

A
  • primary and recurrent genital herpes
  • acute herpes zoster
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30
Q

1 clinical use of topical penciclovir

A

recurrent herpes labialis

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31
Q

Ganciclovir:
structurally very similar to _______. MOA is same as _______

A

penciclovir for both

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32
Q

T or F:
Ganciclovir is a better substrate for CMV kinase than acyclovir

A

true

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33
Q

More active against CMV:
A) Penciclovir
B. Ganciclovir

A

B, by 100x

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34
Q

2 clinical uses for ganciclovir:
IV, oral, and intraocular implants: _____
Oral: _______

A
  • CMV retinitis
  • CMV prophylaxis
35
Q

Toxicity for ganciclovir (more/less) severe than acyclovir. what is the toxicity?

A

more. myelosuppression (neutropenia and thrombocytopenia)

36
Q

Resistance to ganciclovir is due to mutations in ? or ?

A

CMV kinase (UL97 gene)
or
CMV DNA pol (UL54)

37
Q

Valganciclovir is a _______ ester of ganciclovir

38
Q

Valganciclovir is rapidly ________ to ganciclovir by ________ in intestine and liver

A

hydrolyzed, esterases

39
Q

Valganciclovir is used to treat ________ in _____ pts

A

CMV retinitis, AIDS

40
Q

Foscarnet inhibits what 3 things

A
  • viral dna polymerase
  • RNA polymerase
  • HIV RT
41
Q

T or F:
foscarnet requires phosphorylation for activity

42
Q

Foscarnet blocks ________ binding site of the viral DNA polymerase

A

pyrophosphate

43
Q

Foscarnet inhibits ______ of pyrophosphate from dNTPs

44
Q

Foscarnet MOA:
carboxyl overlaps with binding site of _ ______

A

Beta phosphate

45
Q

Foscarnet MOA:
___________ occupy position of gamma-phosphate

A

phosphonates

46
Q

Foscarnet MOA:
traps _______ in closed formation

A

polymerase

47
Q

Foscarnet MOA:
DNA is unable to _________

A

translocate

48
Q

Foscarnet PK:
only administered _________

A

intravenously

49
Q

Foscarnet PK:
up to 30% may be ?

A

deposited in bone

50
Q

foscarnet clinical use

A

CMV retinitis

51
Q

4 foscarnet toxicitites/AEs

A
  • renal insuff
  • hypo/hyperphos
  • hypo/hypercalcemia
  • headache
52
Q

2 resistance mechs for foscarnet

A
  • mutations in DNA polymerase
  • mutations in HIV RT
53
Q

T or F:
Resistant CMV isolates are cross-resistant to ganciclovir

54
Q

Cidofovir is a nucleoside phosphonate analog of ________

55
Q

does Cidofovir get phosphorylated?

A

yes by CELLULAR kinases

56
Q

T or F:
Cidofovir requires activation by viral kinases

57
Q

T or F:
cidofovir is a chain terminator

58
Q

1 listed AE of Cidofovir

A

dose-dependent nephrotoxicity NO WAY BRO FR

59
Q

clinical use of Cidofovir

A

CMV retinitis (weird because its the most broad but whatever)

60
Q

Letermovir MOA

A

TERMinase complex inhibition by binding to pUL56

61
Q

Influenza virus:
(pos/neg) stranded RNA virus

62
Q

what are the 3 types of flu and which ones do vaccines protect against?

A

A B and C. vaccines protect A and B

63
Q

Flu A viruses are divided into subtypes based on 2 genes. what are they?

A

Hemagglutinin (H)
Neuraminidase (N)

64
Q

flu virus Neuraminidase:
essential for ______ ________
Cleaves ?
Facilitates virus _________

A

virus replication
glycolytic bonds b/w terminal sialic acids and adjacent sugars
Virus dissemination

65
Q

Neuraminidase inhibitors are __________ _______ analogs

A

transition state

66
Q

Oseltamivir is a prodrug converted to its active form by ?

A

esterases in liver

67
Q

Oseltamivirs metabolite is an effective inhibitor of?

A

neuraminidase

68
Q

oseltamivir is active against what and more or less effective against what

A

A and B
Less effective against B

69
Q

when do you need to start oseltamivir therapy?

A

within 48 hours of first symptoms

70
Q

describe Oseltamivir resistance

A

associated w/ mutations in active site of neuraaminidase

71
Q

T or F:
resistance develops more easily against zanamavir than oseltamivir

A

false, other way around

72
Q

1 AE w/ zanamavir

A

bronchospasms

73
Q

what is the last resort tx option for flu?

A

peramivir, IV drug

74
Q

Peramivir: transition state analog of ______ acid

75
Q

when would you consider admin of peramivir? (3)

A
  • pt not responsive to oral/inhaled tx
  • drug delivery by a route other than IV is not feasible
  • clinician judges IV tx is appropriate due to other circumstances
76
Q

Baloxavir marboxil MOA

A

inhibit viral “cap-snatching” (blocks transcription)

77
Q

Baloxavir clinical indication

A

flu within first 48 hours of sxs (adults 12 yrs+)

78
Q

2 AEs of baloxavir

A

diarrhea, bronchitis

79
Q

HepC: small, (pos/neg) stranded RNA virus

80
Q

Hep C causes chronic what?

A

liver infections

81
Q

how is hepC transmitted, what population is most at risk

A

blood, IV users at risk

82
Q

HepC makes a single ________ that is cleaved by viral and cellular _______.

A

polyprotein
proteases

83
Q

T or F:
Ribonuclease - degrades viral RNA but not cellular RNA

84
Q

stopping at slide 59 rq

PHRM 865 (34 decks)

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