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Pharm Exam 2 > Antiviral Drugs > Flashcards

Antiviral Drugs Flashcards

1
Q

Antivirals are generally

A

virostatic

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2
Q

Cross resistance example given with TK mutation

A

Idoxuridine and acyclovir

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3
Q

Three categories of agents that prevent entry

A

Attachment inhibitors

Coreceptor antagonists

Fusion inhibitors

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4
Q

Maraviroc MOA

A

CCR5 coreceptor antagonist

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5
Q

HIV1 can resist maraviroc by

A

using drug-bound form of CCR5

This is called nonompetitive resistance

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6
Q

Cenicriviroc MOA

A

dual CCR5 and CCR2 antagonist

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7
Q

Enfuvirtide MOA

A

inhibits gp41

(derived from natural gp41 HR2 sequence)

**does NOT have good oral BA

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8
Q

Inhibition of uncoating at the level of the endosomme/lysosome may be a good target because it…

A

takes place at a specific pH (low)

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9
Q

Arildone MOA

A

inhibits picornavirus uncoating

*inserts into a canyon in the VP1 viral protein and blocks ion transport

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10
Q

Plecoranil MOA

A

stops shedding of nucleocapsid proteins from RNA

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11
Q

First integrase inhibitor

A

Raltegravir

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12
Q

Second generation integrase strand transfer inhibitor (INSTI)

A

Dolutegravir

has a limited cross-resistance profile

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13
Q

Best class of AV drugs

A

Ones that act on replication of the genome

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14
Q

Because thymidine kinase is _____, nucleoside analogs can be administered in _______ form.

This provides what sort of advantage?

A

Viral TK is less specific

administered in unphosphorylated form

*Un-P drug enters cells more easily than phosphorylated ones

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15
Q

Nucleoside analog drugs generally cause ____

A

chain termination

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16
Q

Examples of nucleoside analogs

A

Idoxuridine

Ribavirin

Acyclovir/Gancyclovir

Azidothimidine

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17
Q

Two drugs that can interfere with mRNA transcription processing

A

Ribavirin

Interferon

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18
Q

Drugs that target proein translation

A

no specific inhibitors!

Interferon is non-specific for this

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19
Q

Post-trans modifications that can be targetss

A

glycosylation

phosphorylation

myristoylation

sialidation

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20
Q

Neuraminidase inhibitor drugs

A

Zanamavir

Oseltamavir

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21
Q

Neuraminidase function

A

“sialidase” = removes sialic acid from surface at level of glyccoproteins and glycolipids

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22
Q

Zanamavir MOA

A

inhibits NA of influenza A + B

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23
Q

Zanamavir requires

A

aersosol delivery

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24
Q

Oseltamavir is an analog of

A

carbocyclic sialic acid

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25
Q

Other drug related to NA inhibitors

A

laninamivir

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26
Q

What is nirazoxamide?

A

a thiazolide

it might block glycosylation of viral hemagglutinin in the Golgi

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27
Q

Nitazoxanide is effective against

A

Yes

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28
Q

Protease inhibitors are all ____

Examples?

A

substrate analogs

Aquinavir, ritonavir, indinavir, lopinavir, tipranavir, darunavir

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29
Q

Protease inhibitors for HCV

A

Boceprevir and Telprevir

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30
Q

Amantadine is ___

A

lysosomotropic

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31
Q

Amantadine MOA

A

Inhibits viral RNA uncoating (A only)

also acts on maturation of influenza hemagglutinin glycoprotein = reduce infective potential

32
Q

Rimantadine vs amantadine

A

3-4x greater activity

less toxic

33
Q

Idoxuridine MOA

Uses?

Alternative drug?

A

Pyrimidine analog that inhibits viral DNA synthesis after activation by phosphorylation by TK

mainly for Herpes and Poxviruses, but has HIGH TOXICITY so isnt really used

Trifluridine = used topically for herpes keratitis + primary keratoconjunctivitis

34
Q

Nuceoside analogs of cytosine and adenine

They require…

A

Cytarabine + Vidarabine

both have to be phosphorylated to be active

35
Q

Ribivirin is a ___.

Inhibits ________

A

triazole

inhibits 5’ cap formation on mRNA

36
Q

Ribavirin toxicity

A

dose-dependent HA

mutagen and teratogen

37
Q

Acyclovir MOA

A

Purine analog that competes with dGTP

Two pronged effect:

  1. Binds to and inhibits Viral Polymerase
  2. Terminates the chain (doesn’t have a 3’ OH)
38
Q

Acyclovir causes tissue irritation if _____

A

extravasation occurs when given IV

39
Q

Acyclovir uses

A

Herpesviruses

(HSV, VZV, EBV, CMV)

40
Q

What is valacyclovir?

Other related drugs?

A

Prodrug to acyclovir

(3-5x higher levels)

Famciclovir >> penciclovir

41
Q

Gancyclovir MOA

A

Similar to acyclovir, but initial phosphorylation can be carried out by cellular enzymes

**selectivity is due to the fact that it is 30x higher affinity for viral enzymes

42
Q

Gancyclovir major toxicity (tissue) and use?

A

Toxicity = rapidly dividing tissues

Use for AIDS-related CMV infections

43
Q

AZT MOA

A

Chain terminator that is phosphorylated by cellular enzymes

( = can be used against viruses that dont bring own kinase)

Reverse transcriptase is more sensitive to AZT than host DNA pol, therefore it is targeted to infected cells

44
Q

Mutants against AZT tend to have…

A

changes in RT

45
Q

AZT AE’s are mainly _____

A

hematologic

(granulocytopenia and anemia)

46
Q

AZT commonly used with ____ for _____

A

Lamivudine (cytosine analog)

HIV

47
Q

In addition to AZT, HIV treatment may involve _______ and ______

A

Dolutegravir (INSTI)

NRTI’s Abacavir and Lamivudine

48
Q

Lamivudine is very efficient againt

A

HBV

49
Q

Adefovir MOA and use

Toxicity?

A

Analog of adenosine monophosphate… competitively inhibits HBV DNA polymerase

Dose dependent nephrotoxicity

50
Q

NNRTI MOA and recommended use

A

noncompetitive inhibitors that physically prevent RT from working

should NOT be used as monotherapy (d/t resistance)

51
Q

5 NNRTIs

A

N/D/E

Etravirine, Rilpivirine

52
Q

Drug that prevents HIV transmission to neonate

A

Neviripine

53
Q

Drug used in HIV patients in combo with at least two active drugs

A

Etravirine

54
Q

Competitive inhibitor of DNA polymerase that binds to pyrophosphate site

A

Foscarnet

also an inhibitor of RNA pol and HIV RT

Particularly potent to inhibit herpes DNApol

55
Q

Foscarnet effective for ____

A

CMV retinitis

56
Q

Protease inhibitors generally prevent ____

A

the maturation of viral particles

57
Q

Protease inhibitors have been developed against…

A

the active site of aspartyl protease of HIV

This protein is NOT similar to any known host proteolytic enzyme

58
Q

Saquinavir is the ____

A

least effective PI

59
Q

PI that has ben shown to reduce death by 58%

A

Ritonavir

Used in combo therapy with other PI’s

60
Q

Amprenavir or fosamprenavir are generally used as ____

A

combo therapy

61
Q

PI that has lower level of resistace

A

Darunavir

Approved for treatment-naive patients

62
Q

Given with ritonavir for salvage option

A

Tipranavir

63
Q

Benefit of Indinavir

A

Reduces HIV load (PCR can’t even detect in 85% of patients)

64
Q

Protease inhibitors for HCV

What do they target?

A

Telaprevir and boceprevir

target NS3.4A HCV serine protease

65
Q

Target of Asunaprevir

A

NS5A inhibitor

66
Q

Drug that targets the viral terminase complex

A

Letermovir

67
Q

alpha and beta interferon mechanisms

A
  1. bind to specific receptors on adjacent cells and protect from viral infection
  2. enhance MHCI and MHCII on infected cells = enhance viral antigen presentation
68
Q

What is truvada

A

emtricitabine/tenofovir disoproxil fumurate

Used fo preexposure prophylaxis

69
Q

Adamantanes mechanism

A

M2 ion channel inhibitors

70
Q

Gamma interferon secreted by ___

Function?

A

T cells

Enhances specific Tcell mediated immune response

71
Q

general interferon functions (2)

A

Enhance specific immune response

Have direct antiviral effects (penetration, uncoating, degradation, inhibition of mRNA synthesis or methylation)

72
Q

How do interferons interfere with protein synthesis?

A

Phosphorylating EIF-2

73
Q

Single point mutation at different positions of M2 is sufficient to…

A

induce cross-resistance to amantadine and rimantadine

74
Q

Oseltamavir vs Zanamavir - ages

A

Oselt = 1 yr.

Zan = 7 for treatment, 5 for chemoprophylaxis

75
Q

Sensitivity for RIDT’s (rapid influenza diagnostic tests)

A

10-70%

76
Q

Treatment vs lab confirmation of influenza

A

Treatment should NOT wait for lab confirmation of influenza

Pharm Exam 2 (12 decks)

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