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Antivirals Flashcards

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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
Valganciclovir Admin
Oral
26
Ganciclovir & Valganciclovir Tx (3)
Tx or prophylaxis of CMV/Herpes - Immunocomp - Transplant pts - CMV retinitis
27
Ganciclovir & Valganciclovir SE (5)
- 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
28
Other drugs for CMV/Herpes that do NOT req activation (2)
- Cidofovir | - Foscarnet
29
Cidofovir Tx
- Resistant CMV/Herpes
30
Cidofovir SE
- Renal tox (use probenecid/hyrate)
31
Foscarnet MOA
- Inhibits DNA and RNA polymerase, reverse transcriptase
32
Foscarnet Admin
IV
33
Foscarnet Tx
- Resistant CMV/Herpes
34
Foscarnet SE (1)
- Renal toxicity
35
Fomvirsen MOA
- Antisense compound to viral mRNA
36
Fomvirsen Tx
- CMV retinitis (intraocular)
37
Fomviersen SE (2)
- Ocular inflammation | - Visual haze
38
Influenza Drugs (4)
- Oseltamivir - Zanamivir - Amantadine - Rimantadine
39
Neuraminidase Inhibitors (2)
- Oseltamivir | - Zanamivir
40
Oseltamivir & Zanamivir MOA (2)
- Neuraminidase Inhibitors | - Block release of virus
41
Oseltamivir Tx (2)
- Influenza Type A and B | - Bird flu
42
Zanamivir Tx
- Influenza A and B
43
Oseltamivir Admin and SE
- Oral | - NAUSEA/VOMITING (take with food)
44
Zanamivir Admin and SE
- Inhaled or intranasal - May worsen RESPIRATORY fxn in COPD - Bronchospasm in asthmatics
45
Amantadine MOA
- Inhibits uncoating of virus
46
Amantadine Tx
- Influenza A tx and prophylaxis
47
Amantadine Elimination
- Renal
48
Amantadine SE (2)
- CNS HALLUCINATIONS - N/V - Rarely used
49
Rimantidine vs Amantadine SE
- Rimantidine does NOT enter CNS = NO hallucinations
50
RSV Drugs (2)
- Ribavirin | - Palivizumab
51
Ribavirin MOA (4)
- Purine analogue - Becomes phosphorylated - Inhibits viral RNA synthesis - Inhibits RNA polymerase and synthesis of GTP
52
Ribavirin Tx (3)
- Active against many viruses - RSV - Hep C
53
Ribavirin Admin
- Aerosol (RSV) - IV (Lassa, SARS) - Oral
54
Ribavirin SE (4)
- Pulmonary, dyspnea - Hypotension - Anemia - Depression, lethargy - GI
55
Ribavirin CI
- TERATOGENIC (exposure at work)
56
Palivizumab MAO (2)
- Antibody to RSV | - Passive immunity
57
Palivizumab Tx
- Prophylaxis in high risk pts | - Injected 1x per month
58
Drug of Choice for Chronic Hep B
Lamivudine
59
Lamvudine MOA (2)
- Reverse transcriptase inhibitor (also used for HIV) | - Inhibits HBV polymerase
60
Adefovir SE (2)
- Renal toxicity | - Lactic Acidosis
61
Drugs for Hep B (4)
- Lamivudine (DOC) - Adefovir - Entacavir - Telbivudine - --- these drugs replaced interferon a2b for tx HBV
62
Telbivudine MOA
- similar to Lamvudine | - More effective in some pts
63
Drugs of Hep C (6)
- Interferon a2b - Interferon a2a - Boceprevir - Telaprevir - Simeprevir - Sofosbuvir/Ledipasvir (Harvoni) - Viekira
64
Boceprevir, Telaprevir, Simeprevir MOA
- Specific for serine protease needed for replication of HCV
65
Interferon MOA (4)
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
Boceprevir, Telaprevir, Simeprevir increased effectiveness with _____ (2)
- Interferon | - Ribavirin
67
Boceprevir, Telaprevir, Simeprevir SE
- Strong inhibitors of CYP3A4 (drug interactions) | - Exacerbate anemia, neutropenia, fatigue
68
Interferon Toxicity (5)
- Flu-like symptoms - Musculoskeletal aches and pains - GI: nausea, anorexia - CNS: depression, suicide - Hematologic: neutropenia, anemia (worse when combined with Ribavirin, Teleprevir, Boceprevir)
69
Sofosbuvir/Ledipasvir (Harvoni) MOA (3)
- Inhibits NS5B RNA polymerase - Lepidasvir inhibits NS5A - Halts HCV reproduction
70
Sofosbuvir/Ledipasvir (Harvoni) SE (3)
- Irritability - Fatigue - Lethargy
71
Sofosbuvir/Ledipasvir (Harvoni) success with genotype ___
Genotype I
72
Sofosbuvir/Ledipasvir (Harvoni) interesting feature
Possible liver reversal
73
Dasabuvir, Ombitasvir, Paritaprevir, Ritonavir (Viekira) MOA (4)
- Dasabuvir inhibits HCV NS5B polymerase - Ombitasvir inhibits HCV NS5A - Paritaprevir inhibits HCV NS3/4A polymerase - Ritonavir inhibits CYP3A and increases bioavail
74
Dasabuvir, Ombitasvir, Paritaprevir, Ritonavir (Viekira) SE (2)
- Fatigue | - Insomnia
75
Treatments of HIV (5)
- Reverse Transcriptase Inhibitors - Protease Inhibitors - Non-nucleotide Reverse Transcriptase Inhibitors - Fusion Inhibitors - Integrase Inhibitors
76
Nucleotide Reverse Transcriptase Inhibitor (4)
- Zidovudine - Lamivudine - Emtracitabine - Tenofovir - Didanosine - Zalcitabine - Stavudine - Abacavir
77
Zidovudine MOA (2)
- Thymidine analogue - Incorporated into DNA, inhibits reverse transcriptase - Combined with Lamivudine
78
Zidovudine t 1/2 and penetration
- Short t 1/2 | - Gets into CNS
79
Zidovudine Tx (4)
- Maintains CD4 count - Prophylaxis post exposure - Decrease risk of transmission of virus in pregnancy and newborns - AIDS dementia - Psoriasis and T cel leukemia
80
Zidovudine SE (4)
- Anemia, Neutropenia - CNS - GI - Somnolence with ganciclovir
81
Monotherapy for HBV
- Lamivudine
82
Drug for HIV and HBV pts
- Lamivudine
83
Top drug combos for HIV (2)
- Lamivudine & Zidovudine | - Tenofovir & Emtricitabine
84
Tenofovir & Emtricitabine SE (2)
- Mild GI | - Flatulence
85
Didanosine SE (2)
- Peripheral neuropathy | - Combined with Zidovudine
86
Zalcitabine (2)
- Peripheral neuropathy | - Oral ulcers
87
Stavudine SE
- Peripheral neuropathy
88
Abacavir SE
- Hypersensitivity (do not use drug again!)
89
Drugs that cause Peripheral neuropathy
- Didanosine, Stavudine | - Zalcitabine
90
Drugs that cause Lactic Acidosis
- Zidovudine, Zalcitabine | - Didanosine, Stavudine
91
Drugs that cause Anemia/granulocytopenia
- Zidovudine, Didanosine
92
Non-Nucleotide RTIs (3)
- Delavirdine - Nevirapine - Efavirenz
93
Non-Nucleotide RTIs MOA (4)
- Bind directly to inhibit viral reverse transcriptase - Use ONLY with nucleoside analogues - Long-acting, well absorbed - Metabolized by CYP3A/2D6
94
Non-Nucleotide RTIs preferred drug
- Efavirenz
95
Non-Nucleotide RTIs used in pregnancy
- Nevirapine (or just take pt off Efavirenz)
96
"Navir" drugs
Protease Inhibitors
97
Protease Inhibitors MOA
- Inhibited protease prevents cleavage of the polypeptide and subsequent maturation of the viron
98
Protease Inhibitors Features (4)
- 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
Altered body fat distribution - Buffalo hump - Abd fat - THIN face
Protease Inhibitors
100
Protease Inhibitors Other SE (5)
- Cholesterol/TGs increase - Atherosclerosis, cerebrovascular incidents, MI - DM - Depression - Abd pain
101
Protease Inhibitor Drug of First Choice
- Atazanavir
102
Atazanavir (4)
- Well tolerated - Once a day dosing - Less effect lipoproteins - Increase bilirubin (inhibits uridinediphosphate-glucuronosyl transferase A1)
103
Protease Inhibitor Drug of Second Choice
- Darunavir
104
Darunavir Features (2)
- Well tolerated | - Combined with Ritonavir
105
Darunavir SE (2)
- HA | - Nightmares
106
Saquinavir bioavailability (3)
- Increased with high-fat food, Grapefruit juice, Ritonavir - Inducer of CYP3A decreases effectiveness - Inhibition of CYP3A
107
Saquinavir (SE)
- GI common
108
Ritonavir bioavailability (3)
- Inhibit CYP3A4 - Combined with other protease inhibitors to increase their bioavailability - Many drug interactions
109
Ritonavir SE (3)
- GI - Burning, tingling - Liver enzymes elevated
110
Used with Ritonavir to increase availability
Lopinavir
111
Lopinavir/Ritonavir SE (2)
- D/N | - Liver enzymes elevated with hepatic dz
112
Indinavir Features (2)
- Cross resistance with Ritonavir | - Metabolized by CYP3A4, drug reactions
113
Indinavir SE (2)
- Kidney stones | - Hyperbilirubinemia
114
Nefinavir Features
- CYP3A, many drug interactions
115
Nefinavir SE
- Mostly GI
116
Amprenavir/Fosamprenavir (2)
- Good oral absorption | - Inhibits CYP3A4 (many drug interactions/metronidazole)
117
Stevens-Johnson syndrome rash
Amprenavir/Fosamprenavir
118
Tipranavir MOA
- Non-pepiditic protease inhibitor
119
Tipranavir Tx (2)
- May work if resistant to other drugs | - Combined with Ritonavir to increase bioavail (metabolized by CYP3A4)
120
Enfuvirtide MOA (2)
- Binds to viral envelop glycoprotein | - Prevents fusion of virus and entry into cell
121
Enfuvirtide Tx (2)
- No cross resistance with other drugs | - Advanced dz when other drugs fail
122
Enfuvirtide SE (2)
- Injection site/rxn | - Pneumonia
123
Enfuvirtide Admin
SC
124
Drug used only if there is CCR5 receptor on T cell
- Maraviroc
125
Maraviroc SE
- Rash
126
Raltegravir MOA (2)
- Blocks integrase | - Prevents viral replication
127
Raltegravir Tx
- Used when other drugs stop working
128
Raltegravir SE
- N/V | - HA
129
Integrase Inhibitors
Raltegravir
130
Co-receptor inhibitors
Maraviroc
131
Atazanavir + Indinavir =
Bilirubin
132
Didanosine + Stavudine =
Neuropathy
133
Zidovudine + Stavudine =
antagonism
134
Drug that affects Adenosine?
Tenofovir
135
Drugs that affect Guanosine?
Didanosine, Abacavir
136
What drugs affect Thymidine?
Zidovodine, Stavudine
137
What drugs affect Cytosine?
Zalcitabine, Emticitabine, Lamivudine

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