Antivirals Flashcards

1
Q

Drugs that affect (3):

Attachment and penetration

A
  • Enfuviritide (HIV)
  • Docosanol (HSV)
  • Palivizumab (RSV)
  • Maraviroc
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2
Q

Drugs that affect (2):

Uncoating

A
  • Amantadine

- Rimantadine (Influenza)

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3
Q

Drugs that affect (5):

Synthesis of viral components

A
  • NRTIs (HIV)
  • NNRTIs (HIV)
  • Acyclovir (HSV)
  • Foscarnet (CMV)
  • Entecavir (HBV)
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4
Q

Drug that affects (1):

Packaging and assembly of virus particle

A
  • Protease inhibitors (HIV)
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5
Q

Drug that affects (1):

Release of virus

A
  • Neuraminidase inhibitors (Influenza)
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6
Q

Virus attaches to specific receptors on host cell and becomes internalized

A

Attachment and penetration

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7
Q

Protein coat of the virus is dissolved by viral enzymes to liberate viral RNA or DNA

A

Uncoating

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8
Q

Virus takes over host cell nucleus and replicates its DNA or RNA, then makes proteins

A

Synthesis of viral components

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9
Q

Viral genome may be encapsulated by viral protein, multiple membranes, or no protein

A

Packaging and assembly of virus particle

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10
Q

Some viruses are released rapidly and kill the host cell; others are released slowly and allow the cell to survive

A

Release of virus

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11
Q

Herpes Drugs (4)

A
  • Acyclovir (Zovirax)
  • Valacyclovir (Valtrex)
  • Famciclovir (Famvir)
  • Docosanol (Abreva)
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12
Q

Acyclovir MOA (3)

A
  • Guanosine analoge
  • Activated by viral thymidine kinase
  • Inhibits DNA synthesis by competing with dGTP
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13
Q

Acyclovir Admin and t 1/2

A
  • Oral
  • Topical
  • IV
  • Short half life, dose 3-4qd
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14
Q

Acyclovir Elimination

A

Kidney

- Decreased renal fxn will affect drug significantly

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15
Q

Prodrug of Acyclovir

A

Valacyclovir

  • Higher biavail
  • Food does NOT affect absorption
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16
Q

DOC Herpes

A

Acyclovir

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17
Q

Acyclovir Tx (3)

A
  • Genital herpes, herpes keratitis, herpes zoster, herpes encephalitis, varicella zoster
  • Prophylaxis in organ transplant
  • Chronically to immunocomp
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18
Q

Acyclovir SE (3)

A

Well tolerated

  • N/V, HA
  • Nephrotoxic with high IV dose (hydrate)
  • Somnolence/lethargy with Zidovudine in HIV pts
  • Safe in pregnancy
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19
Q

Famciclovir (Famvir) / Penciclovir MOA and features

t 1/2, elimination

A
  • Phosphorylated by viral thymidine kinase
  • Similar to acyclovir
  • Longer t 1/2
  • Renal elimination
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20
Q

Docosanol MOA

A
  • Inhibits viral fusion to cell membrane
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21
Q

Docosanol Tx

A
  • OTC cold sores
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22
Q

CMV/Herpes Drugs (5)

A
  • Ganciclovir
  • Valganciclovir
  • Cidofovir
  • Foscarnet
  • Fomvirsen
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23
Q

Ganciclovir & Valganciclovir MOA (3)

A
  • Inhibits CMV DNA replication
  • Activated by viral kinase in cells infected with herpes or CMV
  • Less selective than acyclovir (more toxic)
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24
Q

Ganciclovir Admin

A

IV

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25
Q

Valganciclovir Admin

A

Oral

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26
Q

Ganciclovir & Valganciclovir Tx (3)

A

Tx or prophylaxis of CMV/Herpes

  • Immunocomp
  • Transplant pts
  • CMV retinitis
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27
Q

Ganciclovir & Valganciclovir SE (5)

A
  • Neutropenia, thrombocytopenia (mainly when high doses given IV, especially when combined with Zidovudine)
  • Nausea, fever (most common)
  • Rash
  • Phlebitis
  • Confusion, headache, seizures
  • Abnormal liver function tests
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28
Q

Other drugs for CMV/Herpes that do NOT req activation (2)

A
  • Cidofovir

- Foscarnet

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29
Q

Cidofovir Tx

A
  • Resistant CMV/Herpes
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30
Q

Cidofovir SE

A
  • Renal tox (use probenecid/hyrate)
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31
Q

Foscarnet MOA

A
  • Inhibits DNA and RNA polymerase, reverse transcriptase
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32
Q

Foscarnet Admin

A

IV

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33
Q

Foscarnet Tx

A
  • Resistant CMV/Herpes
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34
Q

Foscarnet SE (1)

A
  • Renal toxicity
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35
Q

Fomvirsen MOA

A
  • Antisense compound to viral mRNA
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36
Q

Fomvirsen Tx

A
  • CMV retinitis (intraocular)
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37
Q

Fomviersen SE (2)

A
  • Ocular inflammation

- Visual haze

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38
Q

Influenza Drugs (4)

A
  • Oseltamivir
  • Zanamivir
  • Amantadine
  • Rimantadine
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39
Q

Neuraminidase Inhibitors (2)

A
  • Oseltamivir

- Zanamivir

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40
Q

Oseltamivir & Zanamivir MOA (2)

A
  • Neuraminidase Inhibitors

- Block release of virus

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41
Q

Oseltamivir Tx (2)

A
  • Influenza Type A and B

- Bird flu

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42
Q

Zanamivir Tx

A
  • Influenza A and B
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43
Q

Oseltamivir Admin and SE

A
  • Oral

- NAUSEA/VOMITING (take with food)

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44
Q

Zanamivir Admin and SE

A
  • Inhaled or intranasal
  • May worsen RESPIRATORY fxn in COPD
  • Bronchospasm in asthmatics
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45
Q

Amantadine MOA

A
  • Inhibits uncoating of virus
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46
Q

Amantadine Tx

A
  • Influenza A tx and prophylaxis
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47
Q

Amantadine Elimination

A
  • Renal
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48
Q

Amantadine SE (2)

A
  • CNS HALLUCINATIONS
  • N/V
  • Rarely used
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49
Q

Rimantidine vs Amantadine SE

A
  • Rimantidine does NOT enter CNS = NO hallucinations
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50
Q

RSV Drugs (2)

A
  • Ribavirin

- Palivizumab

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51
Q

Ribavirin MOA (4)

A
  • Purine analogue
  • Becomes phosphorylated
  • Inhibits viral RNA synthesis
  • Inhibits RNA polymerase and synthesis of GTP
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52
Q

Ribavirin Tx (3)

A
  • Active against many viruses
  • RSV
  • Hep C
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53
Q

Ribavirin Admin

A
  • Aerosol (RSV)
  • IV (Lassa, SARS)
  • Oral
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54
Q

Ribavirin SE (4)

A
  • Pulmonary, dyspnea
  • Hypotension
  • Anemia
  • Depression, lethargy
  • GI
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55
Q

Ribavirin CI

A
  • TERATOGENIC (exposure at work)
56
Q

Palivizumab MAO (2)

A
  • Antibody to RSV

- Passive immunity

57
Q

Palivizumab Tx

A
  • Prophylaxis in high risk pts

- Injected 1x per month

58
Q

Drug of Choice for Chronic Hep B

A

Lamivudine

59
Q

Lamvudine MOA (2)

A
  • Reverse transcriptase inhibitor (also used for HIV)

- Inhibits HBV polymerase

60
Q

Adefovir SE (2)

A
  • Renal toxicity

- Lactic Acidosis

61
Q

Drugs for Hep B (4)

A
  • Lamivudine (DOC)
  • Adefovir
  • Entacavir
  • Telbivudine
  • — these drugs replaced interferon a2b for tx HBV
62
Q

Telbivudine MOA

A
  • similar to Lamvudine

- More effective in some pts

63
Q

Drugs of Hep C (6)

A
  • Interferon a2b
  • Interferon a2a
  • Boceprevir
  • Telaprevir
  • Simeprevir
  • Sofosbuvir/Ledipasvir (Harvoni)
  • Viekira
64
Q

Boceprevir, Telaprevir, Simeprevir MOA

A
  • Specific for serine protease needed for replication of HCV
65
Q

Interferon MOA (4)

A

Blocks viral entry

  1. Blocks transcription and translation of mRNA
  2. Blocks viral replication
  3. Blocks viral processing
  4. Blocks viral assembly and release
66
Q

Boceprevir, Telaprevir, Simeprevir increased effectiveness with _____ (2)

A
  • Interferon

- Ribavirin

67
Q

Boceprevir, Telaprevir, Simeprevir SE

A
  • Strong inhibitors of CYP3A4 (drug interactions)

- Exacerbate anemia, neutropenia, fatigue

68
Q

Interferon Toxicity (5)

A
  • Flu-like symptoms
  • Musculoskeletal aches and pains
  • GI: nausea, anorexia
  • CNS: depression, suicide
  • Hematologic: neutropenia, anemia (worse when combined with Ribavirin, Teleprevir, Boceprevir)
69
Q

Sofosbuvir/Ledipasvir (Harvoni) MOA (3)

A
  • Inhibits NS5B RNA polymerase
  • Lepidasvir inhibits NS5A
  • Halts HCV reproduction
70
Q

Sofosbuvir/Ledipasvir (Harvoni) SE (3)

A
  • Irritability
  • Fatigue
  • Lethargy
71
Q

Sofosbuvir/Ledipasvir (Harvoni) success with genotype ___

A

Genotype I

72
Q

Sofosbuvir/Ledipasvir (Harvoni) interesting feature

A

Possible liver reversal

73
Q

Dasabuvir, Ombitasvir, Paritaprevir, Ritonavir (Viekira) MOA (4)

A
  • Dasabuvir inhibits HCV NS5B polymerase
  • Ombitasvir inhibits HCV NS5A
  • Paritaprevir inhibits HCV NS3/4A polymerase
  • Ritonavir inhibits CYP3A and increases bioavail
74
Q

Dasabuvir, Ombitasvir, Paritaprevir, Ritonavir (Viekira) SE (2)

A
  • Fatigue

- Insomnia

75
Q

Treatments of HIV (5)

A
  • Reverse Transcriptase Inhibitors
  • Protease Inhibitors
  • Non-nucleotide Reverse Transcriptase Inhibitors
  • Fusion Inhibitors
  • Integrase Inhibitors
76
Q

Nucleotide Reverse Transcriptase Inhibitor (4)

A
  • Zidovudine
  • Lamivudine
  • Emtracitabine
  • Tenofovir
  • Didanosine
  • Zalcitabine
  • Stavudine
  • Abacavir
77
Q

Zidovudine MOA (2)

A
  • Thymidine analogue
  • Incorporated into DNA, inhibits reverse transcriptase
  • Combined with Lamivudine
78
Q

Zidovudine t 1/2 and penetration

A
  • Short t 1/2

- Gets into CNS

79
Q

Zidovudine Tx (4)

A
  • Maintains CD4 count
  • Prophylaxis post exposure
  • Decrease risk of transmission of virus in pregnancy and newborns
  • AIDS dementia
  • Psoriasis and T cel leukemia
80
Q

Zidovudine SE (4)

A
  • Anemia, Neutropenia
  • CNS
  • GI
  • Somnolence with ganciclovir
81
Q

Monotherapy for HBV

A
  • Lamivudine
82
Q

Drug for HIV and HBV pts

A
  • Lamivudine
83
Q

Top drug combos for HIV (2)

A
  • Lamivudine & Zidovudine

- Tenofovir & Emtricitabine

84
Q

Tenofovir & Emtricitabine SE (2)

A
  • Mild GI

- Flatulence

85
Q

Didanosine SE (2)

A
  • Peripheral neuropathy

- Combined with Zidovudine

86
Q

Zalcitabine (2)

A
  • Peripheral neuropathy

- Oral ulcers

87
Q

Stavudine SE

A
  • Peripheral neuropathy
88
Q

Abacavir SE

A
  • Hypersensitivity (do not use drug again!)
89
Q

Drugs that cause Peripheral neuropathy

A
  • Didanosine, Stavudine

- Zalcitabine

90
Q

Drugs that cause Lactic Acidosis

A
  • Zidovudine, Zalcitabine

- Didanosine, Stavudine

91
Q

Drugs that cause Anemia/granulocytopenia

A
  • Zidovudine, Didanosine
92
Q

Non-Nucleotide RTIs (3)

A
  • Delavirdine
  • Nevirapine
  • Efavirenz
93
Q

Non-Nucleotide RTIs MOA (4)

A
  • Bind directly to inhibit viral reverse transcriptase
  • Use ONLY with nucleoside analogues
  • Long-acting, well absorbed
  • Metabolized by CYP3A/2D6
94
Q

Non-Nucleotide RTIs preferred drug

95
Q

Non-Nucleotide RTIs used in pregnancy

A
  • Nevirapine (or just take pt off Efavirenz)
96
Q

“Navir” drugs

A

Protease Inhibitors

97
Q

Protease Inhibitors MOA

A
  • Inhibited protease prevents cleavage of the polypeptide and subsequent maturation of the viron
98
Q

Protease Inhibitors Features (4)

A
  • Mutations and resistance common when used alone (COMBINE with NRTIs)
  • Do not interrupt therapy
  • Metabolized by CYP3A4
  • Drug interactions: St. John’s Wort (always find out about OTC drug use)
99
Q

Altered body fat distribution

  • Buffalo hump
  • Abd fat
  • THIN face
A

Protease Inhibitors

100
Q

Protease Inhibitors Other SE (5)

A
  • Cholesterol/TGs increase
  • Atherosclerosis, cerebrovascular incidents, MI
  • DM
  • Depression
  • Abd pain
101
Q

Protease Inhibitor Drug of First Choice

A
  • Atazanavir
102
Q

Atazanavir (4)

A
  • Well tolerated
  • Once a day dosing
  • Less effect lipoproteins
  • Increase bilirubin (inhibits uridinediphosphate-glucuronosyl transferase A1)
103
Q

Protease Inhibitor Drug of Second Choice

104
Q

Darunavir Features (2)

A
  • Well tolerated

- Combined with Ritonavir

105
Q

Darunavir SE (2)

A
  • HA

- Nightmares

106
Q

Saquinavir bioavailability (3)

A
  • Increased with high-fat food, Grapefruit juice, Ritonavir
  • Inducer of CYP3A decreases effectiveness
  • Inhibition of CYP3A
107
Q

Saquinavir (SE)

108
Q

Ritonavir bioavailability (3)

A
  • Inhibit CYP3A4
  • Combined with other protease inhibitors to increase their bioavailability
  • Many drug interactions
109
Q

Ritonavir SE (3)

A
  • GI
  • Burning, tingling
  • Liver enzymes elevated
110
Q

Used with Ritonavir to increase availability

111
Q

Lopinavir/Ritonavir SE (2)

A
  • D/N

- Liver enzymes elevated with hepatic dz

112
Q

Indinavir Features (2)

A
  • Cross resistance with Ritonavir

- Metabolized by CYP3A4, drug reactions

113
Q

Indinavir SE (2)

A
  • Kidney stones

- Hyperbilirubinemia

114
Q

Nefinavir Features

A
  • CYP3A, many drug interactions
115
Q

Nefinavir SE

116
Q

Amprenavir/Fosamprenavir (2)

A
  • Good oral absorption

- Inhibits CYP3A4 (many drug interactions/metronidazole)

117
Q

Stevens-Johnson syndrome rash

A

Amprenavir/Fosamprenavir

118
Q

Tipranavir MOA

A
  • Non-pepiditic protease inhibitor
119
Q

Tipranavir Tx (2)

A
  • May work if resistant to other drugs

- Combined with Ritonavir to increase bioavail (metabolized by CYP3A4)

120
Q

Enfuvirtide MOA (2)

A
  • Binds to viral envelop glycoprotein

- Prevents fusion of virus and entry into cell

121
Q

Enfuvirtide Tx (2)

A
  • No cross resistance with other drugs

- Advanced dz when other drugs fail

122
Q

Enfuvirtide SE (2)

A
  • Injection site/rxn

- Pneumonia

123
Q

Enfuvirtide Admin

124
Q

Drug used only if there is CCR5 receptor on T cell

125
Q

Maraviroc SE

126
Q

Raltegravir MOA (2)

A
  • Blocks integrase

- Prevents viral replication

127
Q

Raltegravir Tx

A
  • Used when other drugs stop working
128
Q

Raltegravir SE

129
Q

Integrase Inhibitors

A

Raltegravir

130
Q

Co-receptor inhibitors

131
Q

Atazanavir + Indinavir =

132
Q

Didanosine + Stavudine =

A

Neuropathy

133
Q

Zidovudine + Stavudine =

A

antagonism

134
Q

Drug that affects Adenosine?

135
Q

Drugs that affect Guanosine?

A

Didanosine, Abacavir

136
Q

What drugs affect Thymidine?

A

Zidovodine, Stavudine

137
Q

What drugs affect Cytosine?

A

Zalcitabine, Emticitabine, Lamivudine