Antiviral Agents Flashcards

1
Q

What is acyclovir effective against?

A

herpes simplex 1,2 and herpes zoster virus

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2
Q

What does acyclovir convert?

A

To monophosphate acyclo-GMP by viral thymidine kinase, then to triphosphate by a cellular enzyme

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3
Q

How does acyclovir work?

A

The triphosphate formed inhibits DNA polymerase through chain terminations

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4
Q

How is acyclovir administered?

A

Topically
Orally
IV

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5
Q

How are some adverse effects of acyclovir?

A

psychiatric = Cotards

Toxicity if overdose = lethargy, confusion, myoclonus

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6
Q

What is the difference between valacyclovir and acyclovir?

A

Vala is acyclovir esterified to valine

greater oral bioavilability

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7
Q

How does resistance to acyclovir and valaciclovir occur?

A

Mutation of viral thymidine kinase and/or DNA polymerase

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8
Q

What is idoxuridine used for?

A

Topically only = herpes keratitis

- too toxic for systemic use

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9
Q

What are ganciclovir and valganciclovir against?

A

Active CMV

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10
Q

What is acyclovir an analogue of?

A

Guanosine

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11
Q

What is ganciclovir an analogue of?

A

Deoxyguanosine

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12
Q

What does ganciclovir do?

A

Phosphorylated to monophosphate by CMB thymidine kinase then to triphosphate by cellular kinases

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13
Q

How does ganciclovir work?

A

Inhibits viral DNA polymerase by acting as a chain terminator

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14
Q

What is the difference between valganciclovir and ganciclovir?

A

Valine ester of it

Greater oral bioavailability

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15
Q

What are the adverse effects of valganciclovir and ganciclovir?

A

Adverse effects such as bone marrow suppression

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16
Q

Which drugs are effective against herpes?

A
foscarnet
acyclovir
valacyclovir
ganciclovir
valgancyclovir
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17
Q

Which drugs are reverse transcriptase inhibitors?

A

Nuceloside and nucleotide analgoues (NRTIs)

  • nuceloside analogues = zidovudine, lamivudine
  • nucleotide analogues = tenofovir
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18
Q

What do NRTIs do?

A

inhibit reverse transcriptase by incorporating into growing DNA chain and not linking subsequent base

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19
Q

Adverse effects of zidovudine?

A

GI, haem, headache, hepatotoxic, cardiomyopathy

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20
Q

Adverse effects of lamivudine?

A

nausea, fatigue, headache, diarrhoeaa, cough, pro-inflamm response, autoimmunity

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21
Q

Adverse effects of tenofovir?

A

renal insufficiency

Fanconi syndrome

22
Q

What do NNRTIs do?

A

Non-nucleoside/tide reverse transcriptase inhib

- bind to reverse transcriptase enzyme not at active site and distort it

23
Q

Examples of NNRTIs?

A
  • nevirapine
24
Q

What are some adverse effects of nevirapine?

A

hepatitis

Stevens-Johnson

25
Q

What do protease inhibitors do?

A

Bind to viral protease which cuts viral precursor proteins into virion structure parts

26
Q

Examples of protease inhibitors?

A

Saquinavir
Indinavir
Ritonavir

27
Q

What are some adverse effects of Saquinavir?

A

GI, rash, neuro, metabolic, QT prolonged

28
Q

What do integrase inhibitors do?

A

Inhibit integrase which is a viral enzyme for HIV DNA integration into host genome

29
Q

What do fusion inhibitors do?

A

Block gp41 on surface of HIV virion which mediates fusion between HIV envelope and cell membrane

30
Q

What do entry inhibitors do?

A

Block CCR5 (chemokine) receptor on cell surface which with CD4 enables gp120 on HIV surface to bind and enter

31
Q

What is ribvarin an analogue of?

A

Guanosine

Ribo-nucleoside

32
Q

How does ribvarin work?

A

Inhibits viral RNA dependent RNA polymerase so terminates chain

33
Q

What does ribvarin do?

A

Against hep C, viral haemorrhagic fevers, resp syncytial virus
Influenza

34
Q

What are adverse effects of ribvarin?

A

Haemolytic anaemia
Bone Marrow suppression
Depression
Cough

35
Q

Which drugs are effective against retroviruses?

A
NRTIs
NNRTIs
Protease inhibitors
Integrase inhibitors
fusion inhibitors
entry inhibitors
ribvarin
36
Q

How does neurominidase inhibitors work?

A

viral neurominidase cleaves siliac acid release virion from host cell,

  • aggregation of virions,
  • viral inactivation by host mucus
37
Q

Examples of neurominidase inhibitors?

A

Oseltamivir

Zanamivir

38
Q

How do M2 inhibitors work?

A

Inhibit M2 protein of virus to decrease hydrogen ion influx

Inhibits upcoating and recoating

39
Q

Examples of M2 inhibitors?

A

Amantidine

Rimantadine

40
Q

Which drugs are used in influenza treatment

A

Ribvarin
Neurominidase inhibtiors
M2 inhibtiors

41
Q

Which drugs treat Hep C?

A
Protease Inhibitors (DAA)
NSSA Inhib
NSSB Inhib
Ribvarin
Pegylated interferon
42
Q

What do DAA do?

A

Direct acting agents

Inhibit viral NS3/4A serine protease

43
Q

Examples of DAAs?

A

Telaprevir

44
Q

What is NSSA?

A

Viral protein enabling assembly

45
Q

Example of NSSA inhib?

A

Ledipasvir

46
Q

What does NSSB inhib do?

A

Inhibits Viral RNA polymerase

47
Q

Examples of NSSB inhib?

A

Sofosbuvir

Dasabuvir

48
Q

What does PEGylated interferon do?

A

Interferon alpha or beta

Human cytokines enhancing immune response

49
Q

What does PEGylated mean?

A

Linked to poly-ethylene glycol to prolong half life

50
Q

Which drugs are used in hep B treatment?

A

Reverse transcriptase inhibitors
Iamivudine
Tenfovir
Interferon pegylated

51
Q

What drugs are used for resp syncytial virus?

A

Monoclonal antibody against RSV fusion glycoprotein (palvizumab)
Ribvirine (inhaled)

52
Q

What are the stages of the viral replication cycle from entry to release?

A
  • docking on
  • escape from the vacuole
  • replication of DNA/RNA
  • integration of DNA into genome
  • assembly of virions
  • escape from host cell