Antiviral Drugs Flashcards

1
Q

What’s the degree of variation of viral infections

A

Self resolving to acute fatal disease

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2
Q

Which disease causing organism is an obligate intracellular parasite that uses the host cell to replicate?

A

Virus

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3
Q

How does virus infect a cell?

A

They hijack the infected cell, making it difficult for drugs to combat viral disease effectively.

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4
Q

Why are drugs targeted against virus selective toxic?

A

This is because they may also destroy cell, hence they are designed to inhibit the virus particles without adversely affecting the host.

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5
Q

What are the viral combating approach of antiviral drugs?

A

By targeting the virus themselves or

Host cell factors.

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6
Q

List the direct virus targets of viral agent?

A

Inhibition of virus attachment or entry.
Uncoating inhibitors.
Inhibition of viral replication.
Inhibition of viral protein synthesis.
Inhibition of viral assembly.
Inhibition of viral release.

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7
Q

What do inhibitors of viral attachment and entry target??

A

Host receptors
Co receptors
Viral spike proteins

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8
Q

Drugs that inhibit attachment and entry prevent all subsequent steps of viral replication cycle and virus replication

True /false

A

True

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9
Q

What inhibitor class permits the clearing of viron by host immune system at the beginning??

A

Inhibitors of viral attachment and entry

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10
Q

Another name for maraviroc is??

A

Selz entry

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11
Q

Mode of action of maraviroc

A

It selectively binds to CCR5 of a host cell receptor.

Hence preventing the interaction of hiv-1 gp120 with CCR5.

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12
Q

Name two drug inhibitors of viral attachment and entry??

A
  • Maraviroc
  • Enfuvritide
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13
Q

Mechanisms of action of Enfuvritide?

A
  • Binds glycoprotein 41 of viral envelope
  • Thereby inhibiting viral fusion with the host cell memberane
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14
Q

What type of virus does membrane fusion inhibitors target?

A

Enveloped virus

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15
Q

Example of a viral Uncoating inhibitors

A

Amantadine

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16
Q

Mechanism of action of amantadine

A
  • Blocks M2 ion channel function
  • Hence prevents acidification, dissociation and Uncoating.
  • This prevents release of nucleic acid from the endosome to host cell cytosome.
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17
Q

Name two viral disease condition that require use of amantadine?

A

Influenza A and parkinsonism

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18
Q

Name two types of inhibitor analog used in inhibiting viral replication??

A

Nucleoside (nrti) analog and non nucleoside analog reverse transcriptase INHIBITOR (NNRTI)

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19
Q

Name three NRTI?

A

-Zidovudine
-Acyclovir triphosphate
-Lamivudine

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20
Q

Mechanism of action of NRTI?

A
  • Resembles a normal nucleoside
  • Chemically resembles normal nucleotide on addition of a phosphate group by host cell/viral cell
  • Binds to active site of RT and gets inserted into a growing DNA strand in place of a normal nucleotide
    -Once inserted, synthesis is stopped bcus of inability of attachment of new DNA strands
  • An incomplete provirus is formed
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21
Q

What nucleic base is seen in Zidovudine?

A

Thymine

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22
Q

What feature helps acyclovir terminate the synthesis of dna chain?

A

Absence of 3-OH which prevents attachment of additional nucleoside

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23
Q

Does NNRTI resemble regular DNA building block??

A

No

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24
Q

Mechanism of action of NNRTI

A

-Binds to allosteric site that regulates RT inhibitors
-Impairs function of RT

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25
Q

Examples of NNRTI

A

-Nivirapine
-Efavirens
-Rilpilvirine
-Etravirine
-Delaviridine

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26
Q

Another name for Nivirapine?

A

Viramune

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27
Q

Another name for delaviridine?

A

Rescriptor

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28
Q

Another name for Efavirenz?

A

Sustiva

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29
Q

Another name for Rilpilvirine?

A

Edurant

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30
Q

Another name for Etravirine?

A

TMC 125, intellence

31
Q

Which mechanism does viral protein synthesis inhibitors use?

A

Antisense mechanism

32
Q

How does antisense inhibitor mechanism work??

A

-Antisense antiviral drug is a short synthetic nucleic acid that complements a specific part of mRNA.
-It Binds to mRNA and prevent protein from being translated.

33
Q

Example of viral protein synthesis inhibitor

A

Formivirsen

34
Q

Examples of integrase inhibitors?

A

Raltegrvir
Elvitegravir
Dolutegravir

35
Q

Another name for raltegrvir

A

Isentress

36
Q

Mechanism of action of integrase inhibitors

A

They disable hiv integrase enzyme that inserts the hiv dsDNA intermediate into the host cell DNA.

Hence, preventing production of a provirus.

37
Q

Which class of antiviral drugs inhibit viral maturation and produces non infectious viral particles??

A

Inhibitors of viral assembly

38
Q

Fxn of protease

A

Cleaves precursor viral protein into a functional component of viral assembly

39
Q

Which class of viral inhibitors inhibits the last step?

A

Inhibitors of viral release

40
Q

Fxn of neuramidase

A

It is required to release a new virus

41
Q

Examples of viral inhibitors that inhibits viral release?

A

Oseltamivir

42
Q

Mechanism of action of oseltamivir

A

It Binds to neuramidase

43
Q

The drugs that target direct host cells are called?

A

Immunomodulators

44
Q

Mechanism of axn of immunomodulators

A

Modify or modulate immune response to help the body respond to a disease

They either stimulate or suppress the immune system.

When it stimulates, it gives the immune system the boost it needs to respond to an illness.

45
Q

What treatment condition requires immunomodulators to stimulate immune system

A

Cancer treatment

46
Q

Why are immunosuppressants used and in which condition?

A

Used to suppress immune system. Example autoimmune disorder

47
Q

What are interferons?

A

LMW proteins produced by virus infected cells.

Induce protein formations inhibiting transcription of mRNA

48
Q

Uses of artificial interferons

A

Used as antiviral drug

49
Q

Benefits of artificial interferons

A

They increase cell’s resistance to virus.

Suppress viral adsorption in a cell.

Also essential in deproteinization process.

Has antimetabolites that inhibit nucleic acid synthesis.

50
Q

Mechanism of action of nitazoxanide?

A

It interferes with host regulated pathways of virus replication,

amplifies both type 1 interferon pathway.

cytoplasmic RNA sensing

51
Q

Antiretroviral hiv drugs are divided into classes based on??

A

How each drug interferes with the hiv life cycle.

52
Q

How is drug class grouped

A

Based on:

Common properties-

Similar mechanisms of axn
Chemical structure
Approved use

53
Q

What are the drug classes of hiv:

A

Entry inhibitors
NRTI
NNRTI
Integrase inhibitors
Protease inhibitors

54
Q

What are the sub classes of entry inhibitors

A

Attachment inhibitors
Post attachment inhibitors
Fusion inhibitors
CCR5 antagonist

55
Q

Why are drugs from two or more classes combined

A

To ensure efficacy

56
Q

Explain triple therapy in hiv treatment

A

Combination of:
2 NRTI + integrase inhibitor.
2NRTI + 1 NNRTI.
2NRTI + protease inhibitor.

57
Q

Which drug class inhibitor prevents hiv from entering healthy cd4 cells

A

Entry inhibitors

58
Q

Which viral spike proteins does entry inhibitors target?

A

Gp120 and gp41 surface protein

59
Q

List the host cell receptor/Co receptor proteins targeted by entry inhibitors

A

Cd4 protein, CCR5, CxCR4

60
Q

Mechanism of axn of gp120 inhibitors

A

Bind to gp120 portion of the hiv envelop protein.

Prevents virus from attaching to cd4 receptors which it uses to gain entrance to the cell.

61
Q

Example of attachment inhibitors

A

Fostemsavir

62
Q

Another name for fostemsavir is??

A

Rukobia

63
Q

Another name for post attachment inhibitors is?

A

Monoclonal antibodies

64
Q

Mechanism of axn of post attachment inhibitors

A

They attach to cd4 cells and prevent the hiv gp120 from changing its shape and attaching to a co receptor

Block infected cell from spreading to uninfected

65
Q

Example of post attachment inhibitors

A

Ibalizumabuiyk aka trogerzo

66
Q

Mechanism of fusion inhibitors

A

Block hiv from entering healthy cells by binding to gp41

67
Q

List the NRTI for hiv

A

Cabacavir
Emtricitabin
Lamivudine
Zidovudine aka retrovir
Tenofovir disoprosil fumarate (tdf)

68
Q

Examples of NNRTI for hiv

A

Doravirin
Efavirens
Etravirine
Rilpilvirine

69
Q

Mechanism of axn of protease inhibitors in hiv

A

They block the activities of protease enzymes and prevent it from cleaving the long gag polyprotein and gag polyprotein into essential proteins of hiv required for assembly of new viral particles.

70
Q

Example of protease inhibitors :

Tip: all the “Navir”

A

Saquinavir.
ritonavir
Idinavir

71
Q

What are booster drugs

A

Drugs used to boost the effect of protease inhibitors

72
Q

Mechanism of action of booster drugs

A

Makes the liver break down antiretroviral drugs more slowly making it stay in the body for longer time at higher levels

73
Q

What is essentially added to a prescribed dose of a primary drug to make it effective?

A

Booster drugs

74
Q

List the possible side effects of antiretroviral treatment

A

Nausea
Vomiting
Headache
Dizziness
Rash
Pain
Diarrhea
Fatigue
Difficulty sleeping
Dry mouth