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DD/BL Final > Antiviral Agents > Flashcards

Antiviral Agents Flashcards

1
Q

Drugs against influenza?

A
  1. Amantadine
  2. Rimantadine
  3. Oseltamivir
  4. Zanamivir
  5. Peramivir
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2
Q

Amantadine & Rimantadine Mechanism of action?

A

inhibit viral uncoating by block of viral M2 proton chanel

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3
Q

Amantadine & Rimantadine Pharcokinetics?

A

Oral
accumulate in lung
Amantadine: Renal elimination
Rimantadin: Hepatic elimination

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4
Q

Amantadine & Rimantadine Spectrum/Use?

A

Treatment influenza A

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5
Q

Amantadine & Rimantadine Adverse Reactions?

A
  1. Amantadine:
    * GI upset
    * Insomnia
    * Confusion headache
  2. Rimantadine:
    * better tolerated
    * Poor CNS penetration
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6
Q

Oseltamivir, Zanamivir, Peramivir Mechanism of action?

A

inhibit viral neuraminidase to decrease viral budding (decrease infectivity)

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7
Q

Oseltamivir, Zanamivir, Peramivir Pharmacokinetics

A

All Renal excretion
Oseltamivir: oral as prodrug
Zanamivir: inhalation
Peramivir: IV

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8
Q

Oseltamivir, Zanamivir, Peramivir Spectrum

A

Treatment influenza A, B, C

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9
Q

Oseltamivir, Zanamivir, Peramivir Adverse reaction

A

oseltamivir: Nausea/ vomitting
Zanamivir: bronchospasm

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10
Q

Drugs against Herpes (HSV-VZV)/Cytomegalovirus (CMV)/ Respiratory Syncitial Virus (RSV)?

A
  1. Acyclovir (Valacyclovir)
  2. Penciclovir ( Famciclovir)
  3. Docosanol
  4. Ganciclovir
  5. Cidofovir
  6. Foscarnet
  7. Ribavirin
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11
Q

Acyclovir & Penciclovir Mechanism of Action (MoA)?

A

phosphorylated by viral thymidine kinase –> inhibits viral DNA polymerase & chain termination

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12
Q

Acyclovir Pharmacokinetics?

A

Topical, oral, IV
Acyclovir: 15-30% prodrugs
Valacyclovir: 80% prodrugs
Renal excretion

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13
Q

Penciclovir Pharmacokinetics?

A

Topical
Renal excretion
Famciclovir: 80% prodrugs

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14
Q

Acyclovir & Penciclovir spectrum?

A

HSV-1/HSV-2 : mucosal, genital, encehalitis

Varicella-zoster: higher dose

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15
Q

Acyclovir & Valacyclovir Adverse reaction (Adr)?

A
  1. Minor toxicity: headache, n/v
  2. Renal toxicity in IV route
  3. Valacyclovir: higher IV route –> CNS effect
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16
Q

Problem with higher levels valacyclovir?

A

increase risk CNS & renal side effects

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17
Q

Docosanol MoA?

A

inhibit fusion between plasma membrane and Herpes viral envelope

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18
Q

Docosanol Pharmacokinetic?

A

Topical (5x daily)

19
Q

Docosanol Spectrum

A

HSV-1 labialis

20
Q

Docosanol Adr?

A

well tolerated

21
Q

Ganciclovir (Valganciclovir) MoA?

A

phosphorylated by viral thymidine kinase to active form that inhibits viral DNA polymerase

22
Q

Ganciclovir (Valganciclovir) Pharmacokinetics?

A

Ganciclovir: Poor Oral
Valganciclovir: Good Oral
Distribute to CNS
Renal excretion

23
Q

Ganciclovir (Valganciclovir) Spectrum?

A

Herpes (HSV-VZV)

Cytomegalovirus (CMV)

24
Q

Ganciclovir comparing with Acyclovir?

A

More active, more toxic

Slight threatening CMV retinitis

25
Q

Ganciclovir (Valganciclovir) Adr?

A

Bone marrow depression

CNS: HA, behavioral changes

26
Q

Cidofovir MoA?

A

Nucleotide analog –> inhibit 2nd phosphorylation steps by host kinase–> inhibits viral DNA pol

27
Q

Cidofovir Pharmacokinetics?

A

Long intracellular 1/2 life –> 17-35 hrs

28
Q

How often giving cidofovir?

A

IV weekly/bi-weekly

29
Q

Cidofovir Spectrum?

A

Against DNA virus

CMV infection

30
Q

When to give Cidofovir for CMV infection?

A

If resistant to ganciclovir or foscarnet

31
Q

Cidofovir Adr?

A

Nephrotoxicity = kidney toxic

Rash HIV patient

32
Q

How to decrease nephortoxicity of cidofovir?

A

using concurrent with Probenecid

33
Q

Foscarnet MoA?

A
  1. pyrophosphate analog –> NO activation step

2. inhibits “all” DNA/RNA pol and RT

34
Q

Foscarnet Pharmacokinetics?

A

Poor oral

Continuous infusion!!

35
Q

Foscarnet Spectrum?

A

CMV infection: if Ganciclovir resistant
Herpes infection: if acyclovir resistant
HIV: 2nd line

36
Q

Foscarnet Adr?

A

Renal impairment

Severe n/v electrolyte imbalance (hypocalcemia)

37
Q

Ribavirin MoA?

A
  1. triphosphorylated to active form
  2. inhibits IMP dehydrogenase
  3. inhibits viral RNA-dependent RNA pol
38
Q

Ribavirin Pharmacokinetics

A

aerosol administration
Good Oral
Long intracellular 1/2 life

39
Q

Ribavirin Spectrum

A

Respiratory syncital virus (RSV): inhalation

Hepatitis : oral (with interferon)

40
Q

Ribavirin Adr?

A

Low aerosol toxicity

Systemic toxicity: anemia, bone marrow depression

41
Q

Which Herpes drugs are eliminated by kidney? (3)

A
  1. Acyclovir
  2. Peniclovir
  3. Ganciclovir
42
Q

Which type of analog is Ribavirin?

A

purine nucleoSIDE analog

43
Q
  1. Whose kinase is responsible for phosphorylating ribavirin?
  2. What is the product?
A
  1. By cellular (host) kinasese

2. ribavirin-TP

DD/BL Final (11 decks)

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