Antiviral Agents Flashcards

(43 cards)

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
Ganciclovir (Valganciclovir) Adr?
Bone marrow depression | CNS: HA, behavioral changes
26
Cidofovir MoA?
Nucleotide analog --> inhibit 2nd phosphorylation steps by host kinase--> inhibits viral DNA pol
27
Cidofovir Pharmacokinetics?
Long intracellular 1/2 life --> 17-35 hrs
28
How often giving cidofovir?
IV weekly/bi-weekly
29
Cidofovir Spectrum?
Against DNA virus | CMV infection
30
When to give Cidofovir for CMV infection?
If resistant to ganciclovir or foscarnet
31
Cidofovir Adr?
Nephrotoxicity = kidney toxic | Rash HIV patient
32
How to decrease nephortoxicity of cidofovir?
using concurrent with Probenecid
33
Foscarnet MoA?
1. pyrophosphate analog --> NO activation step | 2. inhibits "all" DNA/RNA pol and RT
34
Foscarnet Pharmacokinetics?
Poor oral | Continuous infusion!!
35
Foscarnet Spectrum?
CMV infection: if Ganciclovir resistant Herpes infection: if acyclovir resistant HIV: 2nd line
36
Foscarnet Adr?
Renal impairment | Severe n/v electrolyte imbalance (hypocalcemia)
37
Ribavirin MoA?
1. triphosphorylated to active form 2. inhibits IMP dehydrogenase 3. inhibits viral RNA-dependent RNA pol
38
Ribavirin Pharmacokinetics
aerosol administration Good Oral Long intracellular 1/2 life
39
Ribavirin Spectrum
Respiratory syncital virus (RSV): inhalation | Hepatitis : oral (with interferon)
40
Ribavirin Adr?
Low aerosol toxicity | Systemic toxicity: anemia, bone marrow depression
41
Which Herpes drugs are eliminated by kidney? (3)
1. Acyclovir 2. Peniclovir 3. Ganciclovir
42
Which type of analog is Ribavirin?
purine nucleoSIDE analog
43
1. Whose kinase is responsible for phosphorylating ribavirin? 2. What is the product?
1. By cellular (host) kinasese | 2. ribavirin-TP