Antivirals Flashcards

1
Q

Most viruses are composed of what?

A

proteins and nucleic acids

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2
Q

What virus is not composed of proteins and nucleic acids?

A

prions

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3
Q

What do viruses require to replicate?

A

host cellular machinery

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4
Q

Viruses are obligate _________ parasites.

A

intracellular

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5
Q

Where do almost all DNA viruses replicate?

A

nucleus

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6
Q

All viral RNA is single stranded. (T/F)

A

False: single or double stranded

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7
Q

Describe the general replication cycle

A
  • attachment
  • penetration/entry
  • un-coating
  • transcription
  • translation
  • replication
  • assembly
  • release
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8
Q

Viruses are more difficult to treat than bacterial infections. (T/F)

A

True

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9
Q

What is the main reason viruses are more difficult to treat than bacterial infections?

A

intracellular nature

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10
Q

Antivirals are generally (more/less) toxic when compared to anti-infectives.

A

more

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11
Q

What are the 3 main concerns with antiviral medications?

A
  1. drug delivery
  2. drug concentrations
  3. resistance
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12
Q

Most antiviral agents have (robust/sparse) effect on latent viruses.

A

sparse

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13
Q

What are the main reasons why we cannot cure HIV? (5)

A
high genetic 
- variability
- functionality
- turnover
memory cells
reservoir seeding
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14
Q

What are the 7 antiretroviral drug classes?

A
  1. nucleoSide reverse transcriptase inhibitor
  2. nucleoTide reverse transcriptase inhibitor
  3. non-nucleoside reverse transcriptase inhibitor
  4. protease inhibitor
  5. integrase inhibitor
  6. fusion inhibitor
  7. co-receptor inhibitor
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15
Q

What class does AZT belong to?

A

nucleoSide reverse transcriptase inhibitor

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16
Q

What class does Tenofovir belong to?

A

nucleoTide reverse transcriptase inhibitor

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17
Q

What class does Efavirenz belong to?

A

non-nucleoside reverse transcriptase inhibitor

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18
Q

What class does Tipranavir belong to?

A

protease inhibitor

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19
Q

What class does Raltegravir belong to?

A

integrase inhibitor

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20
Q

What class does Enfurvitide belong to?

A

Fusion inhibitor

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21
Q

What class does Maraviroc belong to?

A

Co-receptor inhibitor

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22
Q

What is the minimum number of medications to treat HIV?

A

3

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23
Q

Do ARVs eradicate virus or retard viral replication?

A

retard viral replication

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24
Q

Which ARVs have efficacy against Hep B?

A
  • lamivudine
  • emtricitabine
  • adefovir
  • tenofovir
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25
Q

What are some proposed curative techniques for HIV?

A
  • vaccine
  • viral coaxing and intesification
  • gene therapy
  • BMT
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26
Q

What is acyclovir used to treat?

A
  • HSV-1
  • HSV-2
  • VZ
  • some efficacy against CMV and EBV
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27
Q

What is the MOA of acyclovir?

A

Acyclovir triphosphate competes with endogenous substrates for binding to viral DNA polymerase. Once incorporated into the growing DNA chain, further synthesis is halted.

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28
Q

Acyclovir is a ________ analog converted by viral _______ ______ in infected cells to acyclovir ____phosphate which is converted to acyclovir ____phosphate.

A
  • guanosine
  • thymidine kinase
  • mono
  • tri
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29
Q

Acyclovir is commonly used for (suppression/treatment) of genital herpes.

A

both suppression and treatment

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30
Q

Resistance is (common/rare) for acyclovir.

A

common

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31
Q

What are the most common ADRs with acyclovir?

A

CNS related and rare

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32
Q

Acyclovir is available in what dosage forms?

A

PO, IV, topical

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33
Q

How are acyclovir and valacyclovir related to each other?

A

Valacyclovir is the prodrug form of acyclovir

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34
Q

What is the goal of using a prodrug of acyclovir (valacyclovir)?

A

to enhance drug delivery

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35
Q

Valacyclovir serum levels approach those of what?

A

IV acyclovir

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36
Q

How is the spectrum of activity of valacyclovir different from acyclovir?

A

it is identical to acyclovir spectrum

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37
Q

Valacyclovir has a (more complex/simpler) dosing regimen than acyclovir.

A

simpler

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38
Q

In what dosage form is penciclovir available?

A

topical

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39
Q

What is the oral bioavailability of penciclovir?

A

poor

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40
Q

Penciclovir should be administered q__ for what condition?

A
  • q 2 hours

- herpes labialis

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41
Q

Famciclovir is the prodrug of what?

A

penciclovir

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42
Q

What is the benefit of formulating penciclovir in a prodrug form?

A

famciclovir has good oral absorption

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43
Q

For what conditions is famciclovir indicated?

A
  • recurrent HSV

- HZ

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44
Q

What is the MOA of ganciclovir?

A

nucleoside analog of guanine that eventually results in DNA chain termination within infected cells

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45
Q

What is the primary indication of ganciclovir?

A

control/treatment of CMV

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46
Q

What are less common indications of ganciclovir?

A
  • HIV

- solid organ transplant

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47
Q

What is PO ganciclovir indicated for?

A

suppression of CMV

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48
Q

What is IV ganciclovir indicated for?

A

treatment of CMV

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49
Q

What antiviral has 10 times more potency against CMV?

A

ganciclovir

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50
Q

What is the prodrug of ganciclovir?

A

valganciclovir

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51
Q

When might valganciclovir be indicated?

A

PO treatment of CMV

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52
Q

What is the main ADR of ganciclovir?

A

neutropenia

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53
Q

What medication is an inorganic pyrophosphate?

A

Foscarnet

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54
Q

Foscarnet has a (wide/specific) spectrum of activity.

A

wide

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55
Q

What is the MOA of foscarnet?

A

Binds and inactivates DNA polymerase without any requirement for phosphorylation by TK

56
Q

What is a proposed place in therapy for foscarnet?

A

potential in resistant cases

57
Q

What is the spectrum of activity for foscarnet?

A
  • HSV 1
  • HSV 2
  • CMV
  • Influenza A and B
  • HIV
  • Hep B
58
Q

When is foscarnet most commonly used?

A

treatment of resistant CMV and HSV

59
Q

Why is foscarnet not used more often?

A

highly intolerable with significant dose-limiting renal toxicity

60
Q

Foscarnet is available in what dosage form?

A

IV

61
Q

What is the administration method of foscarnet that helps to prevent renal toxicity?

A

pre-hydration with NS

62
Q

What is the chemical class of cidofovir?

A

acyclic nucleoside phosphate derivative

63
Q

What is the spectrum of activity for cidofovir?

A
  • HSV 1
  • HSV 2
  • VZ
  • EBV
  • CMV
64
Q

What specific mechanism allows cidofovir to be useful in resistant cases?

A

Does not require TK phosphorylation for activation

65
Q

In what patients is cidofovir indicated?

A

CMV-infected AIDS patients with foscarnet/ganciclovir intolerance or resistance

66
Q

Cidofovir is available in what dosage form?

A

IV only

67
Q

What is the main ADR of cidofovir?

A

nephrotoxicity

68
Q

What is the administration method of cidofovir that helps to prevent renal toxicity?

A

pre-hydratewith NS and consider addition of oral doses of probenecid

69
Q

What is the purpose of co-administering probenecid with cidofovir?

A

probenecid prevents secretion of cidofovir

70
Q

What are the first generation Hep C drugs?

A
  • ribavirin

- interferons

71
Q

What is the MOA of ribavirin?

A

interference with several key viral replication steps, primarily at the transcription level

72
Q

What is the spectrum of activity for ribavirin?

A
  • Influenza A and B
  • mumps
  • measles
  • parainfluenza
  • HSV
  • Hep B
  • Hep C
  • RSV
73
Q

What is the most common use of ribavirin?

A

heptidic disease

74
Q

In patients with hepatitis, ribavirin is commonly combined with what?

A

interferons

75
Q

Ribavirin is available in what dosage forms?

A

PO

76
Q

What is the pregnancy category for ribavirin?

A

X - teratogenic

77
Q

Contraception is required for _________ post-treatment with ribavirin.

A

6 months

78
Q

What are the ADRs of ribavirin?

A
  • nausea
  • headache
  • lethargy
79
Q

Exact MOA of interferons varies with what?

A

concentrations and presence or absence of other interferons/interleukins

80
Q

Interferon-α is believed to induce what antiviral changes in exposed and infected cells?

A
  • induction of proteins that inhibit DNA synthesis
  • promotion of enzymes that cleave both cellular RNA and DNA
  • alteration of cell membranes to block viral release from infected cells
81
Q

What is the typical route of administration of interferons?

A
  • Sub Q

- IM

82
Q

Interferons are combined with ribavirin when treating what?

A

Hep B and C

83
Q

What are ADRs of interferons?

A
  • serious, dose and treatment limiting effects
  • “flu-like”
  • depression
  • suicidal ideations
84
Q

What is the purpose of pegylating interferons?

A
  • reduce daily dosing requirements

- reduce ADRs

85
Q

What are the second generation Hep C agents?

A
  • Telaprevir
  • Boceprevir
  • Sofosbuvir
  • Simeprevir
  • Ledipasvir & Sofosbuvir
  • Ombitasvir & Paritaorevir & Ritonavir + Dasabuvir
86
Q

What class does telaprevir belong to?

A

protease inhibitor

87
Q

Telaprevir targets Hep C genotype __.

A

1

88
Q

Which is the most difficult Hep C genotype to treat?

A

1

89
Q

Telaprevir is intended to be used with what other medications?

A
  • peg-interferon α

- ribavirin

90
Q

What is the dosage of telaprevir?

A
  • 375 mg (3 tabs) BID with food ( ≥ 20 g of fat)
91
Q

What are ADRs of telaprevir?

A
  • rash (SJS?)
  • anemia
  • NV
  • dysphagia
  • anal irritation
92
Q

What class does boceprevir belong to?

A

protease inhibitor

93
Q

Boceprevir targets Hep C genotype __.

A

1

94
Q

What is the dosage of Boceprevir?

A

800 mg PO TID

95
Q

Boceprevir is intended to be used with what other medications?

A
  • peg-interferon α

- ribavirin

96
Q

What are the ADRs of boceprevir?

A
  • fatigue
  • anemia
  • headache
  • dysphagia
  • alopecia
97
Q

What class does Sofosbuvir belong to?

A

polymerase inhibitor

98
Q

Sofosbuvir is effective against Hep C genotypes __ - __.

A

1 - 6

99
Q

What is the dosage of sofosbuvir?

A

400 mg PO QD with or without food

100
Q

What is the regimen for Hep C G1 and G4?

A

12 weeks of triple therapy : sofosbuvir + interferon + ribavirin

101
Q

What is the regimen for Hep C G2?

A

12 weeks of dual therapy : sofosbuvir + ribavirin

102
Q

What is the regimen for Hep C G3?

A

24 weeks of dual therapy : sofosbuvir + ribavirin

103
Q

What are the common ADRs of sofosbuvir?

A
  • fatigue

- headache

104
Q

What class does simeprevir belong to?

A

Hep C specific protease inhibitor

105
Q

What Hep C genotype is simeprevir effective against?

A

genotype 1

106
Q

What is the dose of simeprevir?

A

150 mg PO QD with food

107
Q

What medications must simeprevir be used with?

A

interferon + ribavirin

108
Q

What are common ADRs of simeprevir?

A
  • rash
  • photosensitivity
  • nausea
  • pruritus
  • myalgia
109
Q

What medications make up Harvoni?

A
  • ledipasvir

- sofosbuvir

110
Q

What is the MOA of ledipasvir?

A

inhibits viral phosphoprotein NS5A

111
Q

What is the MOA of sofosbuvir?

A

polymerase inhibitor (mimics uridine analogs)

112
Q

What is the dose of Harvoni?

A

1 tablet PO QD on empty stomach

113
Q

What Hep C genotype does Harvoni target?

A

genotype 1

114
Q

What is the range of duration of therapy of Harvoni?

A

8 - 24 weeks

115
Q

What category of medication should be avoided with Harvoni?

A

stomach acid reducers

116
Q

What is the MOA of ombitasvir?

A

inhibits HCV NS5A protein

117
Q

What is the MOA of paritaprevir?

A

inhibits HCV NS#/4A protease

118
Q

What is the MOA of ritonavir?

A

inhibits CYP3a (favorable drug interaction)

119
Q

Ritonavir has no Hep C activity. (T/F)

A

True

120
Q

What is the MOA of Dasabuvir?

A

inhibits NS5B RNA-dependent polymerase

121
Q

What Hep C genotype does Viekira Pak target?

A

G1

122
Q

What antivirals are used to treat influenza?

A
  • Amantidine

- Rimantidine

123
Q

What is the MOA of Amantidine?

A

inhibits viral M2 protein with resultant blockage of viral replication

124
Q

What is the relationship of rimantidine to amantidine?

A

hydrophilic analog of amantidine with reduced CNS ADRs

125
Q

Amantidine is used for what other condition?

A

dopamine agonist used to manage Parkinson’s disease

126
Q

There is high incidence of resistance to amantidine. (T/F)

A

True

127
Q

In what patient population are amantidine and rimantidine indicated in?

A

high-risk individuals who are not candidates for vaccinations

128
Q

Neuraminidase inhibitors are derivatives of what?

A

amantidine

129
Q

What is the MOA of neuraminidase inhibitors?

A

inhibits viral neuraminidase: enzyme critical in the maturation and infectivity of newly produced viral particles

130
Q

What strains of influenza is neuraminidase inhibitor effective against?

A

A and B

131
Q

Neuraminidase inhibitors are most effective when administered within ____ of symptom onset and no more than ___.

A
  • 30 hours

- 48 hours

132
Q

What are the neuraminidase inhibitor agents?

A
  • Zanamivir
  • Oseltamivir
  • Peramivir
133
Q

What is the route of administration of zanamivir?

A

inhaled powder

134
Q

What is the route of administration of oseltamivir?

A

oral

135
Q

What is the route of administration of peramivir?

A

parenteral