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BL and DD final > DD Antivirals > Flashcards

DD Antivirals Flashcards

1
Q

List neuramidase inhibitors

which inhibits release of Progeny virus

A
  1. osteltamivir
  2. zanamivir
  3. paramivir
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2
Q

What do neuramidase inhibitors do?

A

inhibit NA → prevent cleavage of SA from host receptors → reduces viral intracellular translocation and budding → prevent release of progeny virus → reduces viral infectivity

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3
Q

Route of administration of:

  1. osteltamivir
  2. zanamivir
  3. paramivir
A
  1. osteltamivir - oral
  2. zanamivir - inhalation (poor oral)
  3. paramivir - IV
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4
Q

Dosing of:

  1. osteltamivir
  2. zanamivir
  3. paramivir
A
  1. osteltamivir - bid for 5 days
  2. zanamivir - bid for 5 days
  3. paramivir - single dose
    ______
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5
Q

half life of:

1. osteltamivir

A
  1. osteltamivir: 6-10 hours
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6
Q

Adverse drug rxn of:

  1. osteltamivir
  2. zanamivir
A
  1. osteltamivir:
    - Nausea and vomiting (better with food)
  2. zanamivir
    - Bronchospasm in patients with asthma or COPD
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7
Q

Which Neuramidase inhibitor is ONLY for the critically ill or immunocompromised?

A

Peramivir

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8
Q

Are NA inhibitors good prophylactics?

Are Uncoating inhibitors good prophylactics??

A

NA inhibitors: yes 80-90% effective prophylactic for both influenza A and B

Uncoating inhibitors: yes good prophylaxis but only for influenza A

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9
Q

Which drug that treats influenza A/B is excreted via hepatic elimination?

A

Rimantadine (flumadine)

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10
Q

How do amantadine and rimantadine inhibit uncoating?

A

Block M2 proteins (virally-encoded H+ ion channel), → prevents intracellular pH changes necessary for uncoating / release of ribonucleoprotein & genome for replication.

  • note: due to resistance, these two drugs are no longer recommended for use
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11
Q

What is special about amantadine and rimantadine’s route of elimination?

A

They can be excreted in breast milk - careful

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12
Q

Adverse drug rxn of oseltamivir

A

nausea, vomiting

better w/ food

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13
Q

Adverse drug rxn of zanamivir

A

bronchospasm in patients with asthma or COPD

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14
Q

Adverse drug rxn of Amantadine (Symmetrel)

A

insomnia,
concentration difficulty,
lighteadedness/dizziness,
headache

  • note rimantadine is better tolerated ;)
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15
Q

Where can amantadine and rimantadine accumulate?

A

in lungs (via oral route)

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16
Q

List the drugs that are Inhibitors of viral genome replication and can be used to treat herpes infxn:

A
  1. Acyclovir (Zovirax)
  2. Valacyclovir (Valtrex)
  3. Penciclovir (Denavir)
  4. Famciclovir (Famvir)
  5. Vidarabine & Trifluridine (Viroptic)
  6. Cidofovir (if acyclovir resistant)
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17
Q

MOA of acyclovir?

A

Acyclovir diffuses into cell → gets triphosphorylated (TP) by viral thymidine kinase → Acyclovir triphosphate inhibits viral DNA polymerase (Selective Toxicity) → Terminates replication and Viral DNA pol inactivation

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18
Q

how do viruses acquire resistance to inhibitors of viral genome replication to treat herpes infxn?

A

Mostly in immunosuppressed patients.

1) loss of viral thymidine kinase
2) ↓kinase specificity for drug as substrate
3) altered affinity of viral DNA polymerase

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19
Q

Which herpes medication is administered topically?

A

Acyclovir (Zovirax)

Penciclovir (Denavir)

Vidarabine & Trifluridine (Viroptic)

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20
Q

Which herpes medication is administered either orally, topically, or via IV?

A

Acyclovir

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21
Q

dosing of:

  1. Acyclovir (Zovirax)
  2. Valacyclovir (Valtrex)
A
  1. Acyclovir (Zovirax) - 5x a day

2. Valacyclovir (Valtrex) - qd

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22
Q

What is the prodrug of acyclovir? Penciclovir?

A

valacyclovir is prodrug of acyclovir

famciclovir is prodrug of penciclovir

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23
Q

Which herpes medication will have renal toxicity with IV use?

A

Acyclovir

Vidarabine & Trifluridine (Viroptic)

24
Q

Minor adverse rxns of herpes medications:

A 
Minor - 
reversible renal dysfunction,   
Pregnancy category B
headache, 
nausea, 
vomiting,
25
Q

Influenza drugs that are teratogenic:

Herpes drugs that are teratogenic:

A

Influenza drugs:

  • amantadine
  • rimantadine

Herpes drugs that are teratogenic:
- Vidarabine & Trifluridine

26
Q

Which herpes drug is more effective than topical acyclovir?

A

penciclovir

27
Q

Which herpes medication is linked to IV encephalopathy?

A

acyclovir

28
Q

Which herpes medication is linked to CNS deficiencies at high doses?

A

valacyclovir

29
Q

Acyclovir comes in 3 routes of admin. Describe their diff clinical use:

A

Oral:

- ↓ symptom duration during primary and recurrent genital herpes (NOT time to healing).   
- at higher doses can treat varicella or shingles,

Topical (less effective)
- Good for 2ndary prevention.

IV:
- best choice for HSV encephalitis, neonatal HSV, and serious HSV of VZV infections.

30
Q

Why is valacyclovir a better option than acyclovir?

A

↑bioavailability, meaning ↑efficacy

Greater compliance than acyclovir (qd)
- qd vs 5x a day

31
Q

Vidarabine & Trifluridine role in treatment

A

Limited to HSV keratoconjunctivitis and
epithelial keratitis.

Useful against acyclovir-resistant strains

32
Q

MOA of docosanol (abreva)? How?

A

Inhibitors of viral penetration

-Inhibits fusion between viral lipid envelope & host membrane

33
Q

What happens if you give docosanol if it is administered too late?

A

fail to elicit therapeutic response (decreasing healing time by 1 day)

34
Q

RSV drugs

A

Ribavirin (Copegus, Rebetol)
Ribavirin (Virazole)
Palivizumab (Synagis)

35
Q

MOA of ribavirin

A

Converted to ribavirin-TP by cellular kinases.

1) Inhibits 5’ capping of viral mRNA, ↓stability and translatability
2) ↑viral suicide

36
Q

MOA of palivizumab

A

Humanized mab to RSV F glycoprotein

- prevents viral attachment/entry

37
Q

Which ribavirin is administered orally? Via inhalation?

A

Oral - Ribavirin (Copegus, Rebetol)

Inhalation - Ribavirin (Virazole)

38
Q

What is the route of elimination for Ribavirin (Copegus, Rebetol)?

A

Hepatic metabolism and Renal excretion

39
Q

adverse drug rxn of:
Ribavirin in general
Ribavirin (Copegus, Rebetol)
Ribavirin (Virazole)

A

Teratogenic (category X)!!!!!!

Ribavirin (Copegus, Rebetol):
- Hemolytic anemia. When given with interferon, causes cough, rash and pruritus.

Ribavirin (Virazole):
- Conjuctival or bronchial irritation; not good for patients with bronchospastic lung disease

40
Q

adverse drug rxn of:

Palivizumab (Synagis)

A

Rare hypersensitivity reactions:

41
Q

Ribavirin (Copegus, Rebetol) -

Role of pharmacotherapy in treatment

A

RSV infxn in bone marrow transplant
RSV infxn in immunocompromised,

Hepatitis C when combined with interferon-α2a

42
Q

Ribavirin (Virazole)

Role of pharmacotherapy in treatment

A

RSV and pneumonia in severe RSV and immunocompromised

43
Q

Palivizumab (Synagis)

Role of pharmacotherapy in treatment

A

RSV Immunoprophylaxis in infants and young children with congenital heart disease.

EXPENSIVE

44
Q

CMV drugs

A

Ganciclovir (Cytovene)

Valganciclovir (Valcyte)

Foscarnet (Foscavir)

Cidofovir (If immunocompromised or resistant to above drugs)

45
Q

MOA of:
Ganciclovir (Cytovene)
Valganciclovir (Valcyte)

A

Phosphorylation of drug to TP by viral protein kinase UL97. →
incorporates into replicating viral DNA→
inhibit viral DNA pol →
slows and ceases chain elongation.

46
Q

Routes of admin. for ganciclovir?

A

IV, Topica, Oral (poor)

47
Q

Which CMV drug also treats HBV?

A

oral ganciclovir

48
Q

Which CMV drug also treats HSV keratitis?

A

topical ganciclovir

49
Q

Adverse drug rxns of CMV drugs

A

Myelosuppression w/ neutropenia and thrombocytopenia(reversible)

Ganciclovir specifically: Rare CNS toxicity, abnormal liver fxn, GI disturbances and nausea

50
Q

What has better bioavailability, ganciclovir or valganciclovir?

A

valganciclovir

51
Q

Most of the CMV drugs are administered via which route?

A

IV

52
Q

MOA of foscarnet?

A

Non-competitively binds RNA and DNA pol to inhibit cleavage of pyrophosphate. Block viral replication

-Does not require cellular activation.

53
Q

adverse drug rxns of foscarnet?

A

Nephrotoxicity and hypocalcemia. Some CNS abnormalities, rash, fever, nausea

54
Q

What special Role of pharmacotherapy in treatment does foscarnet have?

A

Good against:

  • CMV retinitis
  • ganciclovir-resistant CMV
  • acyclovir-resistant HSV and VZV
55
Q

Inhibitors of viral DNA Pol

A
  1. Acyclovir, Valacyclovir, Penciclovir, Famciclovir, Vidarabine & Trifluridine
  2. Ganciclovir, Valganciclovir. Cidofovir
  3. Foscarnet
56
Q

Route of administration of Cidofovir? How often?

A

IV - weekly/biweekly

BL and DD final (15 decks)

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