Pharm Anti-virals Flashcards

1
Q

Acyclovir (Spectrum)

A

Anti-viral (15-21% bioavailability)

Herpes simplex (HSV) 1 and 2
Varicella-zoster (VZV)
EBV

Not CMV

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2
Q

Famciclovir (Spectrum)

A

Anti-viral (77% bioavailability)

Herpes simplex (HSV) 1 and 2
Varicella-zoster (VZV)
EBV

Not CMV

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3
Q

Ganciclovir (Spectrum)

A

Active against cytomegalovirus (CMV)

Poor bioavailability (5-9%)

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4
Q

Foscarnet (Spectrum)

A

Anti-viral

GCV resistant CMV,
ACV-resistant HSV 1&2, VZV
Intolerable myelosuppression with GCV

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5
Q

Valacyclovir

A

Prodrug of Acyclovir combined with valine

Improved bioavailability to 54% but 5x more expensive

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6
Q

Famciclovir

A

Prodrug of penciclovir

Improved oral bioavailability over ACV of 77%

Oral treatment of VZV

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7
Q

Valaganciclovir

A

Prodrug, valine ester of Ganciclovir

Improved bioavailability to 60%

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8
Q

Foscarnet (MOA)

A

Inorganic pyrophosphate analog

Directly inhibits viral DNA polymerase (Reversibly blocks pyrophosphate binding site of viral DNA polymerase)

Renal metabolism

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9
Q

Acyclovir (MOA)

A

Deoxyguanosine nucleotide analog that inhibits transcription by viral DNA polymerase

Renal metabolism

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10
Q

Ganciclovir (MOA)

A

Deoxyguanosine nucleotide analog that inhibits transcription by viral DNA polymerase

Renal metabolism

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11
Q

Acyclovir (Toxicity)

A

Rare, not significant
Nephrotoxicity: can crystallize in renal tubules
Neurotoxicity: lethargy, confusion, delirium

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12
Q

ACV Resistance

A

Due to loss of viral thymidine kinase, altered TK activity, or DNA polymerase mutants

ACV-R HSV or VSV will be cross-resistant to famciclovir and ganciclovir

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13
Q

Ganciclovir (Toxicity)

A
Myelosuppression (Neutropenia and thrombocytopenia)
CNS toxicity (Headache, change in mental status)
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14
Q

Ganciclovir Resistance

A

Reduced intracellular phosphorylation due to point mutations/deletions in the UL97 gene

Point mutations in the viral DNA polymerase

Cross resistance to Foscarnet

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15
Q

Foscarnet (Toxicity)

A

Very significant

Nephrotoxicity (usually 2nd week of therapy)
- Reversible

Metabolic abnormalities

  • Hypocalcemia
  • Hypomagnesemia
  • Hypokalemia

CNS abnormalities
- Headache, irritability, seizures

Painful genital ulcerations

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16
Q

Hep B Therapy Drugs

A

Lamivudine/emtricitabine (Least potent)
Entecavir
Tenofovir (Most potent)

17
Q

Hep B Drugs (MOA)

A

Nuceloside analogs: inhibits hepatitis B DNA polymerase via chain termination

Suppresses replication, not a cure

18
Q

Interferon alpha 2a or 2b (MOA)

A

Hep C

Induce interferon-stimulated genes which establish an antiviral state within cells, though the response is not virus specific; inhibit viral protein synthesis

19
Q

Interferon alpha 2a or 2b (Side effects)

A
  • Fever, myalgia
  • Neutropenia, thrombocytopenia
  • Hypothyroidism
  • Depression
20
Q

Ribavirin (MOA)

A

Hep C

Nuceloside analog

21
Q

Ribavirin (Side effects)

A
  • Hemolytic anemia
  • Teratogenic
  • Flu-like symptoms
  • Depression/irritability
  • Rash
  • Nausea/diarrhea
22
Q

Interferon + ribavirin (response rates)

A
Most responsive to least:
2 and 3
4
5
6
1
23
Q

Interferon + ribavirin (Limitations)

A

Not well tolerated
Poor response rates
Long duration of therapy (up to 48 weeks)

24
Q

Hep C Direct Acting Agents

A

Protease inhibitors

  • Boceprevir
  • Telaprevir
  • Simeprevir

Only used for Genotype 1

25
Q

Protease Inhibitors benefits

A

Increase response rates of Interferon and ribavirin therapy

Decreased length of therapy

26
Q

Harvoni (MOA)

A

Sofosbuvir (Nucleoside analog against HCV NS5B polymerase)

Ledipasvir (NS5A inhibitor)

27
Q

Harvoni (Spectrum)

A

HCV genotypes 1, 4, 5, and 6

28
Q

Zapatier (MOA)

A

Elbasvir (NS5A inhibitor)

Grazoprevir (NS3/NS4A inhibitor)

29
Q

Zapatier (Spectrum)

A

HCV Genotypes 1 and 4

30
Q

Epclusa (MOA)

A

Sofosbuvir (Nucleoside analog against HCV NS5B polymerase)

Velpatsavir (NS5A inhibitor)

31
Q

Epclusa (Spectrum)

A

Pan-Genotypic

HCV Genotypes 1, 2, 3, 4, 5, 6

32
Q

Mayret (MOA)

A

Glecabrevir (NS3/4A protease inhibitor)

Pribrentasvir (NS5A inhibitor)

33
Q

Mayret (Spectrum)

A

Pan-Genotypic

HCV Genotypes 1, 2, 3, 4, 5, 6