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Pharm > Antivirals > Flashcards

Antivirals Flashcards

1
Q

What is the genetic makeup of Herpesviruses? Enveloped?

A

dsDNA

Enveloped

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2
Q

What is the common MOA of antivirals to treat herpes?

A

Partes the DNA pol in some way

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3
Q

What are the six steps of the viral life cycle?

A
  1. Attachment
  2. entry
  3. mRNA production
  4. Protein and genome synthesis
  5. Virion assembly
  6. Egress
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4
Q

What is the only phase of the viral life cycle in which antivirals are active?

A

Lytic phase

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5
Q

What is the goal of treatment with antivirals?

A

Speed healing and increase time between outbreaks

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6
Q

What are the four herpes viruses that have antiviral therapy available for them?

A

HSV-1
HSV-2
CMV
VZV (HSV-3)

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7
Q

What disease does HSV-1 cause? HSV-2? 3? CMV?

A 
1 = oral herpes
2 = genital herpes
3 = varicella
CMV = pneumonitis, gastroenteritis
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8
Q

What is the MOA of acyclovir?

A

Nucleoside analog that inhibitor of herpesvirus DNA polymerase.
(It is both a competitive inhibitor and substrate for the polymerase)

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9
Q

Does Acyclovir act via competitive or non-competitive inhibition?

A

Competitive inhibition

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10
Q

What happens once Acyclovir is incorporated into the viral DNA chain?

A

Chain terminates

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11
Q

What is the way in which Acyclovir develops resistance?

A

Mutation of thymidine kinase gene

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12
Q

For what two diseases is Acyclovir given PO?

A

Genital herpes

Varicella zoster

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13
Q

What are the four diseases in which Acyclovir is given via IV administration?

A
  1. Severe or disseminated mucocutaneous disease
  2. Neonatal infections
  3. HSV encephalitis
  4. VZV in immunocompromised pts
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14
Q

What are the side effects of Acyclovir?

A

HA
N/v/d
Reversible crystalline nephrotoxicity

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15
Q

What type of drugs should Acyclovir not be given with?

A

Any that damage the kidney

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16
Q

What is valacyclovir?

A

Prodrug of acyclovir (attached to a Valine moiety)

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17
Q

True or false: acyclovir has a high oral bioavailability

A

False–low

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18
Q

What is the MOA of valacyclovir?

A

Inhibitor of herpesvirus DNA

polymerase (same as acyclovir)

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19
Q

What are the diseases that Valacyclovir is given?

A

Primary and recurrent genital herpes
Zoster
Orolabial herpes
Varicella in older children

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20
Q

What is the MOA of Foscarnet?

A

DNA pol inhibitor–Foscarnet binds the site normally occupied by pyrophosphate, thereby blocking pyrophosphate
release and ultimately the catalytic cycle

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21
Q

What is the major difference between acyclovir and Foscarnet?

A

Foscarnet does not require prior phosphorylation by thymidine kinase

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22
Q

What type of molecule is Acyclovir and Valacyclovir?

A

Nucleoside

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23
Q

What type of molecule is foscarnet?

A

Phosphonoformic acid (analog of pyrophosphate)

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24
Q

What is the route of administration of Foscarnet?

A

IV

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25
Q

How is resistance to Foscarnet brought about?

A

Mutation in DNA pol

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26
Q

What is Foscarnet used to treat?

A

HSV and VZV infections that are resistant to acyclovir

CMZ retinitis

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27
Q

What are the adverse effects of Foscarnet?

A

Renal impairment

Changes in Ca, PO3, K, or Mg levels

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28
Q

What drugs should be avoided with Foscarnet?

A

Nephrotoxic

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29
Q

What is the drug used to treat CMV? Why this instead of Acyclovir?

A

Ganciclovir

Is activated more readily by UL97 (CMV gene)

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30
Q

What type of molecule is Ganciclovir?

A

Acyclic guanosine analog

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31
Q

What is the MOA of Ganciclovir?

A

The triphosphate form of ganciclovir is a competitive inhibitor for the viral DNA polymerase and chain terminator when incorporated into the newly synthesized viral DNA genomes

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32
Q

How is Ganciclovir administered?

A

PO or IV

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33
Q

What is the bioavailability of Ganciclovir?

A

Poor

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34
Q

How is resistance to Ganciclovir brought about?

A

Mutations in the UL97 gene

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35
Q

What is Ganciclovir used to treat if given IV?

A

CMV retinitis

CMV colitis, pneumonitis, and esophagitis

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36
Q

What is Ganciclovir used to treat if given IV follow by PO?

A

Reduced the risk of CMV transplant risk

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37
Q

What is Ganciclovir used to treat if given intraocularly?

A

CMV retinitis

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38
Q

What are the adverse effects of Ganciclovir?

A

Myelosuppression

CNS toxicity

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39
Q

What is the MOA of Valganciclovir?

A 
competitive inhibitor for the viral
DNA polymerase (same as Ganciclovir)
40
Q

What is the prodrug form of Ganciclovir? How is this made into a prodrug?

A

Valganciclovir

L-valyl ester of ganciclovir

41
Q

What is the major advantage of Valganciclovir over Ganciclovir?

A

Can be given orally

42
Q

What is valganciclovir used for?

A

CMV retinitis in AIDS

Prevent CMV disease in pts with transplants

43
Q

What type of chemical is Trifluridine?

A

Fluorinated nucleoside

44
Q

What is the MOA of Trifluridine?

A

Competitive inhibitor of thymidine for incorporation into newly synthesized genomes

45
Q

What are the therapeutic indications for Trifluridine?

A

Ocular administration to treat keratoconjunctivitis and recurrent epithelial keratitis d/t HSV-1 and HSV-2

46
Q

Why is Foscarnet used in cases of resistance to Acyclovir?

A

Acts farther down the chain, and does not need to be phosphorylation by viral enzymes, which can mutate

47
Q

What is the MOA of Penciclovir?

A

Inhibits DNA pol for HSV

48
Q

What is the family and genetic makeup of the influenza virus? Enveloped?

A

Orthomyxovirus
-ssRNA
Enveloped

49
Q

What disease does influenza C usually cause?

A

Mild respiratory illness

50
Q

What disease does influenza B usually cause?

A

Mild respiratory illness, but occasionally more severe

51
Q

How soon after initial symptoms must antivirals for the flu be given?

A

48 hours

52
Q

What is the most common complication of influenza?

A

Pneumonia

53
Q

What type of molecule is Oseltamivir? How is it metabolized to its active form?

A

Sialic acid analog that is metabolized to active compound by hepatic esterases

54
Q

What is the MOA of Oseltamivir? What does this cause?

A

Binds to the active side of neuraminidase to inhibit its function

This causes clumping of the progeny virions
on the surface of infected cells

55
Q

How is Oseltamivir administered?

A

Orally

56
Q

How is resistance to Oseltamivir brought about?

A

Point mutations in the hemagglutinin or neuraminidase genes

57
Q

Which influenza strains if Oseltamivir given?

A

A and B strains

58
Q

What are the adverse effects of Oseltamivir?

A

N/v/d
HA
CNS events

59
Q

What type of chemical is Zanamivir? What is this used to treat?

A

Sialic acid used to treat the flu

60
Q

What is the MOA of Zanamivir?

A

Competitively and reversibly binds to the influenza

neuraminidase active site and inhibits its function

61
Q

How is Zanamivir administered?

A

To oropharynx and lungs by inhalation

62
Q

How common is resistance to Zanamivir?

A

Rare

63
Q

What is the difference in the indications for Zanamivir vs Oseltamivir?

A

Zanamivir is only for 7+

64
Q

What are the adverse effects of Zanamivir?

A

Cough, bronchoconstriction

65
Q

What is the MOA of Peramivir? What is it used for? Adverse effects?

A

Neuraminidase inhibitor
Acute, uncomplicated flu
CNS effects

66
Q

How is Peramivir administered?

A

Inhalation

67
Q

What is the chemical structure and MOA of Amantadine?

A

Symmetric tricyclic amines

Inhibits Influenza A M2 protein that is required for nucleocapsid release

68
Q

What is the chemical structure and MOA of Rimantadine?

A

Symmetric tricyclic amines

Inhibits Influenza A M2 protein that is required for nucleocapsid release

69
Q

What are amantadine and rimantadine used to treat?

A

Flu A

70
Q

What is the viral family, genetic makeup, and enveloped status of RSV?

A

Paramyxoviridae
-ssRNA
Enveloped

71
Q

What is RSV?

A

Bronchiolitis and pneumonia in children, ILI in adults

72
Q

What is the drug that is used to treat RSV? How is this administered?

A

Ribavirin–inhalable

73
Q

What type of chemical is Ribavirin? MOA?

A

Guanosine analog that interfere with the synthesis of guanosine triphosphate, and inhibits mRNA capping

74
Q

What is the antiviral for treating Hep C? (not the new curing drug)

A

Ribavirin

75
Q

What are the adverse effects of Ribavirin?

A

Hemolytic anemia

76
Q

What are the contraindications to Ribavirin?

A

Prego
anemic
Renal disease

77
Q

What is the viral family, genetic makeup and enveloped status of HCV?

A

Flaviviridae
+ssRNA
Enveloped

78
Q

Which genotype of HCV is the least responsive to traditional treatment regimes

A

1

79
Q

What is the viral family, genetic makeup and enveloped status of HAV?

A

Picornaviridae
RNA
Non-enveloped

80
Q

What is the viral family, genetic makeup and enveloped status of HBV?

A

Hepadnaviridae
dsDNA
Enveloped

81
Q

What is the viral family, genetic makeup and enveloped status of HEV?

A

Hepeviridae
+ssRNA
Non-enveloped

82
Q

What is the protease that cleaves the viral polyprotein, which is a direct translation of the ssRNA of HCV? Which drugs inhibit this?

A

HCV NS3/4A

Paritaprevir
Simeprevir

83
Q

What are the enzymes that take the +ssRNA of HCV, and turn it into a -ssRNA template for the production of new viral particles? Which drugs inhibit this?

A 
HCV NS5B (RdRp)
HCV NS5A

Sofosbuvir and Dasabuvir

84
Q

What are the two drugs that inhibit the virion assembly?

A

Ledipasvir

Ombitasvir

85
Q

What is the MOA of Paritaprevir? How is it administered?

A

Protease inhibitor for HCV infections

PO administration

86
Q

What are the adverse effects of Paritaprevir?

A

Asthenia

Fatigue

87
Q

How is resistance to Paritaprevir brought about?

A

Specific NS3 gene substitution

88
Q

What is the MOA of Simeprevir? How is it administered?

A

Protease inhibitor in HCV infections

PO administration

89
Q

What are the adverse effects of Simeprevir?

A

Rash/pruitis

90
Q

How is resistance to Simeprevir brought about?

A

Mutations in NS3 gene

91
Q

What is the MOA of Ledipasvir? How is it administered?

A

Nucleotide analog that inhibits HCV NS5A

PO administration

92
Q

What are the adverse effects of Ledipasvir?

A

Diarrhea, HA

93
Q

How does resistance to Ledipasvir come about?

A

NS5A gene substitution

94
Q

What is the MOA of Ombitasvir? How is it administered? Adverse effects?

A

Nucleotide analog that inhibits HCV NS5A
PO administration
Myasthenia

95
Q

What is the MOA of Sofosbuvir? How is it administered? Adverse effects?

A

Nucleotide analog prodrug that is incorporated into HCV’s RNA and breaks it
PO
Anemia, ILI

96
Q

What is the MOA of Dasabuvir? How is it administered? Adverse effects?

A

Non-nucleoside inhibitor of RNA-dependent-RNA pol in HCV
PO administration
Fatigue

Pharm (73 decks)

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