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PHRM 865 > E4 MedChem antivirals I > Flashcards

E4 MedChem antivirals I Flashcards

(84 cards)

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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
T or F: Acyclovir triphos is more stable than Penciclovir triphos in HSV-infected cells
false, other way around
26
short-chain terminator: A) acyclovir B) penciclovir
B
27
obligate DNA chain terminator: A) acyclovir B) penciclovir
A
28
has 3' hydroxyl group on its acyclic side chain A) acyclovir B) penciclovir
B
29
2 clinical uses of oral famciclovir
- primary and recurrent genital herpes - acute herpes zoster
30
1 clinical use of topical penciclovir
recurrent herpes labialis
31
Ganciclovir: structurally very similar to _______. MOA is same as _______
penciclovir for both
32
T or F: Ganciclovir is a better substrate for CMV kinase than acyclovir
true
33
More active against CMV: A) Penciclovir B. Ganciclovir
B, by 100x
34
2 clinical uses for ganciclovir: IV, oral, and intraocular implants: _____ Oral: _______
- CMV retinitis - CMV prophylaxis
35
Toxicity for ganciclovir (more/less) severe than acyclovir. what is the toxicity?
more. myelosuppression (neutropenia and thrombocytopenia)
36
Resistance to ganciclovir is due to mutations in ? or ?
CMV kinase (UL97 gene) or CMV DNA pol (UL54)
37
Valganciclovir is a _______ ester of ganciclovir
monovalyl
38
Valganciclovir is rapidly ________ to ganciclovir by ________ in intestine and liver
hydrolyzed, esterases
39
Valganciclovir is used to treat ________ in _____ pts
CMV retinitis, AIDS
40
Foscarnet inhibits what 3 things
- viral dna polymerase - RNA polymerase - HIV RT
41
T or F: foscarnet requires phosphorylation for activity
false
42
Foscarnet blocks ________ binding site of the viral DNA polymerase
pyrophosphate
43
Foscarnet inhibits ______ of pyrophosphate from dNTPs
cleavage
44
Foscarnet MOA: carboxyl overlaps with binding site of _ ______
Beta phosphate
45
Foscarnet MOA: ___________ occupy position of gamma-phosphate
phosphonates
46
Foscarnet MOA: traps _______ in closed formation
polymerase
47
Foscarnet MOA: DNA is unable to _________
translocate
48
Foscarnet PK: only administered _________
intravenously
49
Foscarnet PK: up to 30% may be ?
deposited in bone
50
foscarnet clinical use
CMV retinitis
51
4 foscarnet toxicitites/AEs
- renal insuff - hypo/hyperphos - hypo/hypercalcemia - headache
52
2 resistance mechs for foscarnet
- mutations in DNA polymerase - mutations in HIV RT
53
T or F: Resistant CMV isolates are cross-resistant to ganciclovir
true
54
Cidofovir is a nucleoside phosphonate analog of ________
cytosine
55
does Cidofovir get phosphorylated?
yes by CELLULAR kinases
56
T or F: Cidofovir requires activation by viral kinases
nope
57
T or F: cidofovir is a chain terminator
yes
58
1 listed AE of Cidofovir
dose-dependent nephrotoxicity NO WAY BRO FR
59
clinical use of Cidofovir
CMV retinitis (weird because its the most broad but whatever)
60
Letermovir MOA
TERMinase complex inhibition by binding to pUL56
61
Influenza virus: (pos/neg) stranded RNA virus
neg
62
what are the 3 types of flu and which ones do vaccines protect against?
A B and C. vaccines protect A and B
63
Flu A viruses are divided into subtypes based on 2 genes. what are they?
Hemagglutinin (H) Neuraminidase (N)
64
flu virus Neuraminidase: essential for ______ ________ Cleaves ? Facilitates virus _________
virus replication glycolytic bonds b/w terminal sialic acids and adjacent sugars Virus dissemination
65
Neuraminidase inhibitors are __________ _______ analogs
transition state
66
Oseltamivir is a prodrug converted to its active form by ?
esterases in liver
67
Oseltamivirs metabolite is an effective inhibitor of?
neuraminidase
68
oseltamivir is active against what and more or less effective against what
A and B Less effective against B
69
when do you need to start oseltamivir therapy?
within 48 hours of first symptoms
70
describe Oseltamivir resistance
associated w/ mutations in active site of neuraaminidase
71
T or F: resistance develops more easily against zanamavir than oseltamivir
false, other way around
72
1 AE w/ zanamavir
bronchospasms
73
what is the last resort tx option for flu?
peramivir, IV drug
74
Peramivir: transition state analog of ______ acid
sialic
75
when would you consider admin of peramivir? (3)
- 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
Baloxavir marboxil MOA
inhibit viral "cap-snatching" (blocks transcription)
77
Baloxavir clinical indication
flu within first 48 hours of sxs (adults 12 yrs+)
78
2 AEs of baloxavir
diarrhea, bronchitis
79
HepC: small, (pos/neg) stranded RNA virus
positive
80
Hep C causes chronic what?
liver infections
81
how is hepC transmitted, what population is most at risk
blood, IV users at risk
82
HepC makes a single ________ that is cleaved by viral and cellular _______.
polyprotein proteases
83
T or F: Ribonuclease - degrades viral RNA but not cellular RNA
true
84
stopping at slide 59 rq

PHRM 865 (40 decks)

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