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D&D Infectious Disease FINAL > Pharm - Antiviral Drugs Part 2 > Flashcards

Pharm - Antiviral Drugs Part 2 Flashcards

1
Q

another name for viral thymidine kinase

A

viral UL97

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2
Q

ganciclovir is a ___ ___ analog

A

acyclic guanosine

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3
Q

does ganiciclovir need the viral enzyme?

A

yes
needed for the initial monophosphorylation

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4
Q

ganciclovir has 100x greater affinity for ___ than acyclovir

A

CMV

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5
Q

2 resistance mechanisms for ganciclovir

A
  1. mutation in UL97 kinase
  2. mutation in UL54 (viral DNA polymerase)
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6
Q

3 main AE of ganciclovir

which 2 are rare

A

rare - CNS and hepatotoxicity

MYELOSUPPRESSION - dose-dependent toxicity

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7
Q

true or false

UL54 mutation gives cross resistance with other drugs

A

TRUE

this affects the viral DNA polymerase

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8
Q

prodrug of ganciclovir

A

valgancyclovir

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9
Q

true or false

foscarnet is a nucleotide

A

FALSE

does not have a base, but DOES have phosphate and bypasses first step with viral thymidine kinase

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10
Q

chemically, foscarnet is…..

A

phosphonoformic acid

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11
Q

structurally, what does foscarnet mimic

A

inorganic pyrophosphate

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12
Q

which viruses can foscarnet inhibit and how

A

BOTH HSV and HIV!!!!

-inhibits herpes DNA and RNA polymerase
-inhibits HIV reverse transcriptase

does so by BLOCKING THE PYROPHOSPHATE BINDING SITE ON THE VIRAL DNA POLYMERASE

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13
Q

true or false

foscarnet is a prodrug

A

true

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14
Q

how is foscarnet administered and why

A

ONLY IV

it is small, but too polar for oral use - not good bioavailability

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15
Q

where is foscarnet deposited?

does it distribute well in CSF?

A

deposits in bones and distributed well in the CSF

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16
Q

name 2 things that foscarnet can be used for

A

-end organ CMV that is ganciclovir resistant

-HSV and VZV when acyclovir resistant

bc both ganciclovir and acyclovir need the 1st step and it’s mutated, but foscarnet does not!!!

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17
Q

resistance mechanism for foscarnet

A

point mutations in viral DNA polymerase
(happens with chronic administration)

if HIV - mutations in reverse transcriptase

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18
Q

true or false

resistance to acyclovir also means resistance to foscarnet, but not vice versa

A

FALSE - other way around

foscarnet CAN be used for acyclovir resistance bc it bypasses 1st step

however, if there is resistance to foscarnet that means there is mutations in DNA polymerase and acyclovir cannot work either

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19
Q

2 AE of foscarnet

A

nephrotoxicity

Ca2+ and K+ alterations

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20
Q

foscarnet is contraindicated with what drugs and why

A

other nephrotixic drugs like amphotericin B and aminoglycosides

too much nephrotoxicity

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21
Q

Cidofovir is a ____ analog

A

cytosine

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22
Q

does cidofovir need viral thymidine kinase?

A

NO

cidoFOvir
has a phosphate group already

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23
Q

true or false

cidofovir IS active against thymidine kinase mutants

A

TRUE

does not need 1st step - already a monophosphate

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24
Q

true or false

cidovofir has broad activity against a lot of viruses

A

true

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25
AE cidoofovir
nephrotoxic
26
major treatment in which cidofovir is used
CMV retinitis
27
when an antiviral is converted into triphosphate, what does this allow the drug to do
competitively inhibit viral DNA polymerase and stop viral DNA synthesis OR incorporate into viral DNA chain and cause chain termination
28
another name for spanish flu
avian flu
29
in flu viruses, where do the periodic mutations occur?
in neuraminidase and hemagglutin ie - H1N1 for spanish flu
30
pandemic vs epidemic vs endemic
endemic - restricted to particular region epidemic - new cases appear in a given population during a given period, at a rate that exceeds what is "expected" based on epidemiology pandemic - outbreak of infectious disease that has spread throughout a very large region or even globally
31
influenza is what kind of virus
orthomyxovirus RNA (negative sense) single strand helical and enveloped
32
the core proteins for influenza can be.....
A B or C
33
what 2 species can influenza be
swine or avian
34
how many H and N subtypes for influenza
16 H 9N
35
2009 swine flu pandemic had what surface proteins
H1N1 (similar to 1918 spanish flu
36
explain antigenic drift for influenza virus
the antibodies to hemagglutinin bind to it and block the virus from binding to the host cell HOWEVER, antigenic drift occurs when mutations ALTER hemagglutinin and the neutralizing antibody can no longer bind to it virus can now bind the host cell and infect it
37
explain anitgenic SHIFT
when an avian and human virus come together, they undergo recombination to produce NEW GENETIC SEGMENTS leads to new viruses and potential pandemic
38
do avian viruses directly infect humans
NO - very rare avians have a2-3 subtypes and humans have a2-6 only swines can infect humans ( havea2-6)
39
what is the function of M2
ion channel that is required for uncoating -- open the envelope and allow the nucleic acid to go into the nucleus of the host cell
40
function HA (hemagglutinin)
allows for viral attachment to host cell membranes and membrane fusion
41
function NA (neuraminidase)
cleaves sialic acid on the surface of host cells, allowing for new viruses to be released prevents aggregation of the new viruses
42
what is PA and what is proposed function
acidic polymerase function is unknown
43
just by looking at the name, how can you tell if something is a neuraminidase inhibitor
"mivir"
44
name 3 neuraminidase inhibitors
oseltamivir zanamivir peramivir
45
all 3 NA inhibitors are analogs of what?
sialic acid
46
explain how viruses are able to leave the host cell and reinfect others (without an NA inhibitor)
mucin forms a barrier for microbes in the respiratory tract. however, mucin is rich in sialic acid, and viral neuraminidase REMOVES THIS SIALIC ACID which helps the virus to penetrate the mucin and leave the cell to reinfect others
47
"the snipper"
neuraminidase -- removes sialic acid
48
true or false oseltamivir is a sialic acid analog
true
49
what does oseltamivir inhibit
neuraminidase
50
HOW does oseltamivir inhibit neuraminidase (ie - irreversible/reversible competitive/noncompetitive)
reversible and competitive (structurally mimics sialic acid)
51
as mentioned, oseltamivir is an NA inhibitor how does this prevent new viral release?
the virus will be trapped on the membrane, and all the new viruses will aggregate and can't get released from the infected cell and reinfect others
52
oseltamivir resistance
mutations in hemagglutinin or neuraminidase
53
true or false oseltamivir is only active vs influenza A
FALSE influenza a and b
54
oseltamivir is active against _____ resistant influenza
amantadine
55
WHEN must oseltamivir be administered and why
within 48 hours of onset will not work if you give too late because the new viruses have already been released and are infecting other cells
56
how long is oseltamivir given and why? how is it good vs the flu
5 days - want to make sure cover the entire viral cycle decreases influenza symptoms, shedding, transmission, and complications
57
**interaction between oseltamivir and probenecid
probenecid will increase the plasma half life of oseltamivir
58
counseling point for oseltamivir
take with food to decrease unwanted GI side effecys
59
any side effects oseltamavir?
not really significant NVD, fatique in japan neuropsych events were reported
60
zanamivir mechanism and route of administration
inhalation same MOA as oseltamavir - NA inhibitor
61
of the 3 NA inhibitors, which is considered the "best" route of administration for treating the flu?
inhalation (zanamivir) because it's a respiratory virus zanamivir has 1000x IC50 values for NA also, gives fast onset and avoids 1st pass
62
what is peramivir and how is it administered
a neuraminidase inhibitor for flu given by IV infusion for min of 15 minutes
63
explain what type of patient would be indicated to receive peramivir
18 years and older who have acute uncomplicated influenza who have been symptomatic for NO MORE THAN 2 days (same as other NA inhibitors)
64
amantadine and rimantidine mechanism
binds and blocks viral M2 channel (which normally is open to allow the influx of H ions into the vesicle with the virus). this prevents the uncoating of the virus. and release from the endosome and into the extracellular matrix to infect other cells
65
true or false amantadine/rimantadine are ONLY active against influenza A
true
66
which is more active - rimantadine or amantadine
rimantadine
67
compare the t1/2 of amantadine/rimantadine with other anti influenza drugs
a lot longer than others like 12-36 hours
68
some major disadvantages of amantadine/rimantadine (not really used anymore)
VERY HIGH RESISTANCE PROFILE lot of AE like GI effects, CNS effects (bc small molecules - nervousness, insomnia, affects dopamine system, deliruym, seizure, etc) also CONTRAINDICATED IN PREGNANT WOMEN
69
true or false amantadine cannot be given to a pregnant person
true
70
name of the anti influenza drug that is not an NA inhibitor or M2 channel blocker
baloxavir
71
true or false baloxavir is not a prodrug
FALSE - it is baloxavir marboxil is converted by hydrolysis to baloxavir
72
how is baloxavir administered and what is its mechanism??
SINGLE DOSE TREATMENT it inhibits the endonuclease activity of the polymerase acidic protein, which is an enzyme that's part of viral RNA polymerase. thus, inhibits viral gene transcription and hence inhibits the replication of new influenza virus
73
baloxavir resistance
amino acid substitutions in the PA (polymerase acidic) protein
74
counseling point for baloxavir
DO NOT GIVE WITH MILK OR ANTACIDS!! absorption prevented bc of diketo acid also, metabolized by CYP3A4 so potentil DDI
75
dosage form baloxavir and what age is it indicated for
oral tablets 12 years or older
76

D&D Infectious Disease FINAL (21 decks)

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