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Veterinary Pharmacology > Drug Discovery And Development > Flashcards

Drug Discovery And Development Flashcards

1
Q

What occured in the rinderpest cattle 1709

A

Major outbreak in Western Europe
Wiped out most of the cows at that time

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2
Q

What is rinderpest

A

Major viral disease
Causes fever, anorexia and eye discharge

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3
Q

What happened in the anthrax outbreak 1712

A

Killed cattle quickly
Fatal bacterial disease
Humans can et the disease

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4
Q

Is anthrax used as a biological warfare agent

A

Yes

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5
Q

What happpend in the 1715 foot and mouth disease outbreak

A

Contagious viral disease
Blisters, fever in cloven hoofed animals

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6
Q

What is the one health initiative

A

Recognises the inter-relationship between animal health, human heath and environment health

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7
Q

Wh was the one health initiative made

A

This because they all link together. If environment is affected it effects humans animals as we eat animals

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8
Q

Where did drugs originally come from

A

Herbs and potions

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9
Q

What did scientists do in the 19th century

A

Isolate and identify the biological activity components from herbs and plants

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10
Q

What is the 1st step to drug discovery

A

Identification of a disease where there is a need for a new drug

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11
Q

What are economical factors pharcuetical companies face when making a new drug

A

Developing a drug is complex - takes 10 to 15 years
Costs over 100 million pounds
Make sure there is good financial return for their investment

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12
Q

What is the problem in the western world when it comes to making new drugs

A

They aren’t as rich therefore drugs for new diseases do not get created unless the rich areas take notice and create the drug

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13
Q

What is the issue with drug making and the veterinary world

A

Not a lot of money in veterinary mediciene compared to human mediciene

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14
Q

What are the approaches o drug discovery

A

Bo-assay based
Target based

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15
Q

What is bio-assay based drug discovery?

A

Develop compounds to use against the disease to see if they’re active at killing the biological compound.

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16
Q

What is target based drug discovery

A

Identify the disease and then the target - receptor, enzyme etc
It synthesized agonists, antagonist or inhibitors against the except or/enzyme of the disease

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17
Q

What is the bioassay-based drug discovery method

A

Raw material - crude extract
Extract compounds using solvents
Test crude extract on bioassay to see if the crude extract shows potency and biological activity
Biologically evaluate the compounds showing biological activity using mass spectrometry
Medicinal chemiss then modify the compounds to make a more potent and selective drug
Clinical trials - if new drug gets through clinical trials it can then be licensed and marketed

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18
Q

What is the right bioassay for bioassay drug discovery?

A

Need to choose right bioassay - important to success to drug research programme
Needs to be quick and simple cant test compounds
Tests should be done on enzymes, tissues and isolated cells
Suitable biological assay - antimicrobial assay

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19
Q

What is artemisinin

A

Traditional Chinese medicene
Herbal plant

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20
Q

What is artemisinin effective against?

A

It was active against the strain of malaria that north Vietnam where facing in 1972

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21
Q

What is cephalosporins

A

Derived from a fungus found in sees in Sardinia
Looked at water and noticed that there was a clearing of turbid water
This then created the antibiotic cephalosporin

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22
Q

What created the drug hypertension

A

Venom from jaraca

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23
Q

What drug comes from teprotide venom

A

Captopril

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24
Q

What are chemical extractions

A

Extract compounds from material

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25
Q

What do you do in chemical extractions

A

Take plant and grind it in the solvent and look at the components in the solution you can use more than one solved to measure polarities in the plant

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26
Q

What is semi-purification

A

Removal of sugars and amino acids

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27
Q

Why do you remove sugars and amino acids from plants

A

We need to know if something is working due to the components of the plant and not the sugars in the plant

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28
Q

What happens during screening for biological activity

A

Once biological activation occurs you purify that compound more and separate into fractions and look at each fraction to see which one shows biological actity

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29
Q

What is purification

A

Separation and purification of individual compounds from the extract, screening for biological activity and purify using chromatography

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30
Q

What chromatography do you use if compounds are non polar

A

Normal phase chromatography

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31
Q

What chromatography do you use if compounds are polar

A

C18 reverse phase chromatography

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32
Q

What is preclinical testing

A

Biological evaluation in vitro and in vivo - identification of mode of action
Individual purified compounds can be tested in vitro assay and in vivo assays to identify the active components

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33
Q

What is high performance liquid chromatography

A

Giveees molecular weight and forums
Compound can be broken into fragments that can build up to make the molecule
Sensitive method - you can use nano-grams of the particle
Doesn’t tell you the carbon/hydrogen frame work

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34
Q

What is nuclear magnetic resonance spectroscopy

A

Gives the carbon framework of molecular and environment of the hydrogens
Gives information on the shape of the molecule
Information on how the compound binds to its target
Need 1 milligram for it to work

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35
Q

What is proto NMR

A

Tells us the environments of the hydrogens in the molecule
Usually locate double bonded hydrogens

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36
Q

What is cosy NMR

A

Find out which hydrogens are held by 3 bonds

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37
Q

What is NOESY nmr

A

Look up at hydrogens close up in space to other hydrogens - gives shape of molecule

38
Q

What is HSQC NMR -

A

tells us which hydrogen is bonded to which carbon

39
Q

What is HMBC NMR

A

Tells u what hydrogen is connected to carbon through 2-3 bonds

40
Q

What is SARS

A

Structure acitvity relationships

41
Q

What does SARS do

A

Identify which parts of the molecule are important for activity

42
Q

How do you identify which parts of the molecule are important for activity in SARS

A

Changing each functional group of the molecule and investigate how it affects the way the molecule acts.

43
Q

What drug do we aim for

A

A drug with god selectivity and no side effects
Or little to no side effects

44
Q

What do they look at in clinical trials

A

Drug absorption
Distribution
Metabolism
Excretion
Efficacy
Dosage
Toxicity

45
Q

What are the process of drugs in the body

A

Drug is administered
Drug is absorbed
Drug is now in systemic circulation
Drug gets distributed to tissues or he site of action
Drug is metabolised or excreted
Drug site of action creates a pharmological effect which creates a clinical response which can be efficacy

46
Q

What is pharmokinetics

A

Where drugs go and what happens to it

47
Q

What are pharmacodynamics

A

What does the drug do we it reaches the site of action

48
Q

What is an effective dose

A

Dose or amount of drug that produces a therapeutic response

49
Q

What is efficacy

A

Ability of the drug to elicit a response when it binds to the receptor

50
Q

What does veterinary medicenes need

A

A marketing authorisation

51
Q

What animal medicines not need a MA

A

Medicenes for small animals used as pets
Aquarium animals

52
Q

What drugs need a MA

A

Antibiotics
Psychotics

53
Q

What medicines with a MA need

A

A MA number
Should carry the symbol vm on packaging and printed material

54
Q

What are the advantages of natural products

A

Novel structures - novel molecules

55
Q

Disadvantages of using natural products

A

Impossible to synthesize certain materials
Some atrial moprducts are available in small amounts
Takes years to synthesize drugs

56
Q

Example of drug that takes years to synthesize

A

Palitaxal - taken from bark of taxis brevoila - non renewable as tree got chopped down
They now use needles of the tree but takes 10 years to synthesize

57
Q

What is the top down method

A

Candidate drugs screened for effect on phenotype

58
Q

What does the top down method screen

A

Whole animals, organs or cells

59
Q

What are the advantages of top down

A

Directly reliant to the disease if we have a good animal/experiemntal model of the disease

60
Q

What is top down screening based on?

A

Screening for phenotypic changes relevant to treatment of disease

61
Q

Why is top down method called top down?

A

Your testing at the most complex level and dining out what the biochemical target is

62
Q

Disadvantages of top down methods

A

Very low throughout and cant test many compounds

63
Q

What is the bottom up method

A

Candidate drugs tested for effect on biomechanical target molecule

64
Q

What targets do bottom up test on

A

Receptors, enzymes dna

65
Q

What is bottom up based on

A

Screeening of libraries or structure based design

66
Q

What is the early essential step of bottom up procedures

A

Identification and validation of biomechanical target - protein dna -

67
Q

What are the advantages of bottom up

A

Know the target
Get the structure of target
If you have structure - structure based design can be done

68
Q

Disadvantages of bottom up

A

Although you find a target you dont know if it is valid or not

69
Q

What is target identification and validation - bottom -up

A

Coming up with a good target to identify
Validation - making sure it is the right target

70
Q

What is hit generation - bottom - up

A

When you evaluate hit compounds more and test various parameters

71
Q

Bottom up process or target based drug discovery

A

Target identification and validation
Hit generation
Lead discovery and de novo synthesis
Lead optimisation
Preclinical tests
Clinical trials
Licensing and marketing

72
Q

What is lead optimisation - bottom uo

A

Look at strucutre acitvity relationships and improve reactivity of the drug to make it more potent and selective

73
Q

What does validation of target ensure

A

That if the drug binds to the target, the desired phenotypic change is achieved

74
Q

What is the first step in drig discovery

A

Identify the target and validate it as its essential for target based bottom up drig discovery

75
Q

What is a target in drug doscbery

A

A molecule in the body which is usually a protein which is associated to a particular disease pathway, or modified and could be addressed if we get the drug bound to the target to treat the disease

76
Q

What happens if you try to inhibit an enzyme

A

If you inhibit a whole enzyme there are chances you can inhibit every pathway the enzyme is associated too which leads to on target toxicity

77
Q

What is the method used before we test the design of a new drug

A

Identification
Assessment
Validation

78
Q

What is identification

A

Understanding where the drug comes from and how it works
Biochemical pathways
Signalling pathways

79
Q

What is assessment

A

Assess the target
Need to assess certain things before making the drug
Drug ability - success rate? Can we get a drg to bind to the target selectivity

80
Q

What is validation

A

Making sure if we binge a drug to the target we actually get the outcome we want
Proving that all the steps done before this process will give us the outcome needed

81
Q

What is knock-down.knock-out/Sirna

A

Ways to validate drugs - reduce amount of target proteins in the cells

82
Q

What is knock-in/over expression

A

Add more copies of the gene for the protien target, does the disease get worse

83
Q

What is drugabilit

A

Will it be possible to design a drug to bind to a target
Is structure available
Is it crystal or NMR
Where is the binding site

84
Q

Why are broad fat eaturls - hydrophobic - sites not good

A

Drug cant bind to the compound

85
Q

What do you have to think about when it comes to selectivity

A

Is binding site exclusive to this enzyme
That al the kinases bind atp
These two issues cause selectivity to be really hard

86
Q

What is on-target selectivity

A

Toxicity resulting from the drug binding to the intended protein target
Unintended consequence - down regulation of the target n the cell

87
Q

What is off target toxicity

A

Toxicity resulting from the drug binding to other protein targets in the cell
Can be addressed by design of drugs which are more selective for the target protein

88
Q

Why do we need to sign dual set inhibitors and extend outside the active site

A

Use strucutre of biochemical to build inhibitor molecule to recognise the features of inside and outside section of the active site to create more potency and selectivity

89
Q

What are the drug targets of bacterial cells

A

Enzymes
DNA/rna
Ribosomes
Cell walls
Polymyxins

90
Q

Once we have a validated target what’s next

A

Identify hit compounds which bind to the target as inhibitors, agonists, or antagonist through target screening

91
Q

Why do you need to design compounds using the strucutre of the target

A

Drug needs to fill up the space of the active site otherwise it will be ineffective
You can do this with computer models and make 3D strucutres of the target protein and the drug

Veterinary Pharmacology (12 decks)

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