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Pharm Exam 4 > Antiviral drugs > Flashcards

Antiviral drugs Flashcards

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1
Q

Drug for:

HSV1/HSV2/VZV/CMV?

A
  • acyclovir
  • valacyclovir
  • ganciclovir
  • valganciclovir
  • foscarnet
  • trifluridine
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2
Q

Drugs for influenze viruses?

A
  • osteltamivir
  • zanamivir
  • amantadine
  • rimantadine
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3
Q

Drugs for Respiratory syncytial virus?

A

-aerosolized ribavarin

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4
Q

Drugs for Chronic HCV

A
  • ribavarin
  • pegylated interferon
  • sofosbuvir
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5
Q

Which viral enzyme does oseltamivir inh

A

(-activated by liver esterases)
-binds to active site of neuraminidase = inh function
==> stops spread of progeny virons through respiratory tract

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6
Q

Which viral enzyme does zanamivir inh?

A

-(-activated by liver esterases)
-binds to active site of neuraminidase = inh function
==> stops spready of progeny virons through respiratory tract

SAME AS OSELTAMIVIR JUST INHALATION ROUTE NOT ORAL

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7
Q

Which viral enzyme does amantadine inh?

A

1) symmetric tricyclic amine
2) MOA
- inh activity of **INFLUENZA A M2 PROTEIN*
- its an ion channel forming protein needed for nucleocapsid release

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8
Q

Which viral enzyme does rimantadine inh?

A

1) symmetric tricyclic amine
2) MOA
- inh activity of **INFLUENZA A M2 PROTEIN*
- its an ion channel forming protein needed for nucleocapsid release

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9
Q

Virus life cycle

A
  • Attachment
  • Entry
  • mRNA production
  • Protein and genome synthesis
  • viron assembly
  • Egress
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10
Q

Herpes virus - genome type?

A

DNA viruses that encode own polymerase

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11
Q

Therapeutic target for Herpes virus drugs?

A

Herpes own encoded DNA polymerase

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12
Q

Which herpes stage is suppresed by antivirals?

A

lytic (productive/contagious) stage

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13
Q

Herpes tx goals?

A
  • speed healing

- inc time bw outbreaks

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14
Q

Which herpes virus diseases almost exclusively occur in immunocompromised patients?

A

1) HSV1&2
- Disseminated herpes infections
2) cytomegalovirus (only immnocomp individuals)
- pneumonia
- gastroenteritis
- retinitis

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15
Q

Acyclovir

  • *-MOA?
  • Resistance development?
A
  • -MOA:
    1) phosphorylated by viral thymidine kinase**
    2) competitive inh of viral DNA polymerase**
    3) chain termination upon incorporation into viral DNA
  • Resistance:
    1) mutation in thymidine kinase gene
    2) cross-resistance with other antivirals with similar mech
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16
Q

Acyclovir

*-therapeutic indications?

A

1) oral
- genital herpes
- varicella zoster
2) IV
- severe disesminated mucocutaneous disease
- neonate infections
- HSV encephalitis
- VZV in immunocomp

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17
Q

Acyclovir

*-special adverse effects?

A

-reversible crystalline nephrotox and neurological effects ESPECIALLY WHEN PATIENT IS DEHYDRATED

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18
Q

Cautious use of this drug in dehydrated or pt already on nephrotoxic drug?

A

acyclovir

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19
Q

Valacyclovir

  • MOA?
  • Why use this drug?
A
  • Same as acyclovir - Vala is a PRODRUG of acyclovir activated in the liver and intestines
  • MOA:
    1) phosphorylated by viral thymidine kinase**
    2) competitive inh of viral DNA polymerase**
    3) chain termination upon incorporation into viral DNA*
  • BETTER BIOAVAILABILTY
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20
Q

Valacyclovir

-Therapeutic indications:

A

GREAT ORAL ROUTE

  • primary and recurrent genital herpes
  • varicella in older children and adults
  • zoster
  • orolabial herpes
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21
Q

**-What is the difference bw foscarnet and acyclovir/valacyclovir?

A
  • ***-Foscarnet does NOT need to be phosphorylated by thymidine kinase for activity
  • How would resistance be developed to fosc—> in DNA Poly (Rare)
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22
Q

**Foscarnet route of administration?

A

ONLY IV!**

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23
Q

Foscarnet MOA?

A
  • No activation required by thymidine kinase

- acts directly on DNA POL - binds where pyrophosphate binds so no adding new nucleotides

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24
Q

-When to use foscarnet?

A
  • If patient infection shows resistance to acyclovir or valacyclovir
  • good for all CMV infections
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25
Patient has CMV retinitis, CMV colitis or CMV esophagitis - give which antiviral drug?
- foscarnet | - ganciclovir
26
Foscarnet - adverse:
-DO NOT USE foscarnet when patient is on othe rnephrotoxic drugs (acyclovir/valacyclvir only need to use caution with nephrotox drugs)
27
Ganciclovir - Similar to what drug? - MOA? - why better?
- nucleoside analog like acyclovir - initial phosphorylating by viral kinase CMV UL97 --> much more efficient than acyclovir ===> 100x more active than acyclovir - competitive inh of viral **DNA POL** = chain termination
28
Direct Inh of viral DNA POL via binding to pyrophosphate binding area so virus cant add new nucleotides??
-foscarnet
29
Competitive inh of DNA poly by acting as nucleotide analogs that terminate the chain when added?
- acyclovire - valacyclovir - ganciclovir
30
Ganciclovir - Bioavailability? - Route of administration?
- Poor oral | - given IV, oral, or intraoccular
31
Ganciclovir | -Therapeutic indication:
1) IV= - CMV retinitis (AIDS) - CMV colitis, pneumonitis, esophagitis 2) IV then ORAL= - reduce risk of CMV disease in transplant patients 3) Intraoccular= - CMV reitinitis
32
Ganciclovir | -Adverse:
- myelosuppression - CNS tox many IV adverse rxns
33
Valganciclovir - MOA? - why use this drug over ganciclovir?
1) PRODRUG OF GANCICLOVIR 2) MOA - nucleoside analog like acyclovir - initial phosphorylating by viral kinase CMV UL97 --> much more efficient than acyclovir ===> 100x more active than acyclovir - competitive inh of viral **DNA POL** = chain termination Better oral bioavailabilty than ganciclovir
34
Valganciclovir | -Therapeutic indications:
- CMV retinitis (AIDS) | - prevent CMV in transplant patients (prophylactic)
35
Trifluridine - type of drug? - MOA?
1) fluorinated nucleoside (nucleotide mimic) 2) MOA - phosphorylated by cellular enzymes - competitive inh of thymidine for incorporation into newly synthesized genomes
36
Trifluridine | -Therapeutic indications:
- low selectivity = not for systematic administration (can insert into HOST DNA=not good) - OCCULAR addministration for keratoconjunctivtis and recrrent epithelial ketatitis due HSV1&2
37
Different bw Trifluridine and the other -vir antivirals?
- trifluridine is activated by HUMAN CELLULAR ENZYMES | - other -vir antivirals are activated by viral enzymes
38
INfluenza virus - genome type - which serotypes and which we worry about? - protection/prophyaxis?
- segmented RNA virus - orthomyxovirus family - A B and C serotypes - A and B are serious ones -We have vaccines - injectable inactivated & attenuated
39
How to tx influenza?
antivirals must be given within first 48 hours or no effect on disease progression
40
Oseltamivir - type - MOA?
1) sialic acid analogue -administered as prodrug - activated by HUMAN liver esterases 2) binds to active site of neuraminidase - cleaves sialic moities = inh function ==> stops spready of progeny virons through respiratory tract
41
Oseltamivir - Therapeutic indications - adverse effects?
- ok for children 1+ yo and up - effective against A and B serotypes - must be given within first 48 hours for effect in uncomplicated -usual - headahce, nausea, faituge.... RARELY =rash and neuropsychiatric events
42
Zanamivir - type - MOA?
-just like oseltamivir 1) sialic acid analogue -administered as prodrug - activated by HUMAN liver esterases 2) binds to active site of neuraminidase - cleaves sialic moities = inh function ==> stops spready of progeny virons through respiratory tract
43
Zanmivir | -administration
INHALATION (POWER)
44
oseltamivir vs zanamivir - use in children
- oseltamivir good for children 1+ | - zanamivir good for children 7+
45
Zanamivir | -adverse effects:
- cough - bronhcospasm - temp decrease in pulmonary function - irritation nose and throat - DO NOT GIVE TO PATIENTS WITH PULMONARY DISEASE
46
Amantadine & Rimantadine - type drug? - MOA?
1) symmetric tricyclic amine 2) MOA - inh activity of **INFLUENZA A M2 PROTEIN** - its an ion channel forming protein needed for nucleocapsid release
47
Amantadine & Rimantadine | -therapeutic indications?
- must be given within 48 for INFLUENZA A VIRUS INF to decrease illness by ~1 day... awesome - not really used = HIGH LEVELS OF RESISTANCE
48
Respiratory syncytial virus (RSV) - type of virus/family? - Who gets this/what happens?
- enveloped - RNA - paramyxovirus family - children under 1 year = bronchilitis and pneumonia - immunosuppressed get - common cold in everyone else
49
RSV - | Tx? When treat?
Ribavirin - only in infants and immunocomp infection
50
Ribavirin - type of drug? - MOA?
1) guanosine analogue 2) phosphorylated by HUMAN adenoside kinase --> interferes with synthesis of guanosine triphos ==> inh viral mRNA capping
51
Which drug INH RNA depependent RNA pol for RSV and HCV
Ribavirin
52
Ribavirin | -route of administration:
- AEROSOL ROUTE FOR RSV | - ORAL for HCV (with pegylated interferon for chronic)
53
Which drugs can be administered by inhalation?
- Ribavirin (aerosol for RSV) | - zanamivir (fine power)
54
Ribavirin | -Adverse:
-hemolytic anemia -depression fatigue rash cough insomnia ...
55
Ribavirin | -contraindication:
- pregnancy - anemia - ischemic vascular disease - severe renal disease
56
HCV - type virus/family? - genotypes and significance? - transmission?
- ssRNA / flavivirus - 6 genotypes where #1 is the least responsive to antiviral tx - parenteral - close contact
57
Acute & Chronic HCV?
- acute is mild | - 70% progress to chronic = cirrhosis and HCC
58
*Treatment for CHRONIC HCV genotypes 1, 4, 5, and 6?
COMBO THERAPY - Ribavirin - pegylated interferon - sofosbuvir
59
*Treatment for CHRONIC HCV genotypes 2 and 3?
COMBO THERAPY - sofosbuvir - ribavirin
60
Ribavirin administration for chronic HCV?
oral
61
Interferon - MOA? - administration?
- binds interferon receptors on immune cells and Jak/Stat paths ==> invoked antiviral state is cells - IV
62
Sofosbuvir - type of drug? - MOA? - administration?
1) nucleic acid prodrug 2) MOA - incorporated into synthesized RNA via RNA dependent RNA poly = premature chain termination - ORAL
63
Do not give sofosbuvir with what stuff?
-do not with inducers of p-glycoproteins - St johns wort, rifampin (TB drug)
64
Sofosbuvir | -therapeutic indications?
- HCV 1,4,5,6 give triple therapy (sofos, ribavirin, peg-interferon) - HCV 2,3 give dual or triple therapy (sofos, ribavirin +/-peg-interferon)' NEVER MONOTHERAPY

Pharm Exam 4 (10 decks)

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