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
Examples of NNRTI
-Nivirapine -Efavirens -Rilpilvirine -Etravirine -Delaviridine
26
Another name for Nivirapine?
Viramune
27
Another name for delaviridine?
Rescriptor
28
Another name for Efavirenz?
Sustiva
29
Another name for Rilpilvirine?
Edurant
30
Another name for Etravirine?
TMC 125, intellence
31
Which mechanism does viral protein synthesis inhibitors use?
Antisense mechanism
32
How does antisense inhibitor mechanism work??
-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
Example of viral protein synthesis inhibitor
Formivirsen
34
Examples of integrase inhibitors?
Raltegrvir Elvitegravir Dolutegravir
35
Another name for raltegrvir
Isentress
36
Mechanism of action of integrase inhibitors
They disable hiv integrase enzyme that inserts the hiv dsDNA intermediate into the host cell DNA. Hence, preventing production of a provirus.
37
Which class of antiviral drugs inhibit viral maturation and produces non infectious viral particles??
Inhibitors of viral assembly
38
Fxn of protease
Cleaves precursor viral protein into a functional component of viral assembly
39
Which class of viral inhibitors inhibits the last step?
Inhibitors of viral release
40
Fxn of neuramidase
It is required to release a new virus
41
Examples of viral inhibitors that inhibits viral release?
Oseltamivir
42
Mechanism of action of oseltamivir
It Binds to neuramidase
43
The drugs that target direct host cells are called?
Immunomodulators
44
Mechanism of axn of immunomodulators
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
What treatment condition requires immunomodulators to stimulate immune system
Cancer treatment
46
Why are immunosuppressants used and in which condition?
Used to suppress immune system. Example autoimmune disorder
47
What are interferons?
LMW proteins produced by virus infected cells. Induce protein formations inhibiting transcription of mRNA
48
Uses of artificial interferons
Used as antiviral drug
49
Benefits of artificial interferons
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
Mechanism of action of nitazoxanide?
It interferes with host regulated pathways of virus replication, amplifies both type 1 interferon pathway. cytoplasmic RNA sensing
51
Antiretroviral hiv drugs are divided into classes based on??
How each drug interferes with the hiv life cycle.
52
How is drug class grouped
Based on: Common properties- Similar mechanisms of axn Chemical structure Approved use
53
What are the drug classes of hiv:
Entry inhibitors NRTI NNRTI Integrase inhibitors Protease inhibitors
54
What are the sub classes of entry inhibitors
Attachment inhibitors Post attachment inhibitors Fusion inhibitors CCR5 antagonist
55
Why are drugs from two or more classes combined
To ensure efficacy
56
Explain triple therapy in hiv treatment
Combination of: 2 NRTI + integrase inhibitor. 2NRTI + 1 NNRTI. 2NRTI + protease inhibitor.
57
Which drug class inhibitor prevents hiv from entering healthy cd4 cells
Entry inhibitors
58
Which viral spike proteins does entry inhibitors target?
Gp120 and gp41 surface protein
59
List the host cell receptor/Co receptor proteins targeted by entry inhibitors
Cd4 protein, CCR5, CxCR4
60
Mechanism of axn of gp120 inhibitors
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
Example of attachment inhibitors
Fostemsavir
62
Another name for fostemsavir is??
Rukobia
63
Another name for post attachment inhibitors is?
Monoclonal antibodies
64
Mechanism of axn of post attachment inhibitors
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
Example of post attachment inhibitors
Ibalizumabuiyk aka trogerzo
66
Mechanism of fusion inhibitors
Block hiv from entering healthy cells by binding to gp41
67
List the NRTI for hiv
Cabacavir Emtricitabin Lamivudine Zidovudine aka retrovir Tenofovir disoprosil fumarate (tdf)
68
Examples of NNRTI for hiv
Doravirin Efavirens Etravirine Rilpilvirine
69
Mechanism of axn of protease inhibitors in hiv
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
Example of protease inhibitors : Tip: all the "Navir"
Saquinavir. ritonavir Idinavir
71
What are booster drugs
Drugs used to boost the effect of protease inhibitors
72
Mechanism of action of booster drugs
Makes the liver break down antiretroviral drugs more slowly making it stay in the body for longer time at higher levels
73
What is essentially added to a prescribed dose of a primary drug to make it effective?
Booster drugs
74
List the possible side effects of antiretroviral treatment
Nausea Vomiting Headache Dizziness Rash Pain Diarrhea Fatigue Difficulty sleeping Dry mouth