Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

drug design > drug design 1 > Flashcards

drug design 1 Flashcards

1
Q

why do we need new drugs

A
  • New ones with less side effects
  • Beuase of drug reisstnce and tolerance
  • To improve treatment of an existing disease
  • To treat new diseases
  • To give specific action on new targets for treating disease
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what needs testing preclinical safety testing

A
  • carcinogenesis
  • not tetragenic
    -non toxic
    -optimal route of administration
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

how is toxicity measured

A

by the LD50 value

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what is the therapuetic index

A

amount causes toxic vs non toxic effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what is pharmacogentic

A

what does the body do to the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what are genotoxic effects tested on

A

yeast

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

what does stage 4 of clinical phases do

A
  • To compare a drug with other driugs already on the market
  • To monitor a drugs long term effects and impact the patients quality of life
  • To determine the cost effectiveness f a drug therpay relative to to other traditional and new therapaies
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

how many drugs tested in clinical trails make it

A

1 in 5

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

reasons for drug failure

A
  • Drug simply doenst work
  • Drugs too toxic
  • Drug comoany issues – loss of interest or finical problems
  • Markert too small for cost of development – rare tumour and orphan indication
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what are analgoues

A

druhgs which share simialr properties can be structural or fucntional

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what is chirality

A

potential of a molecule to occur in two assymteric forms that are non-superimposable mirror images of eachother with out chnaing the atmoic composition, atom-atom connections or binds order

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what types of drug action is tehre

A
  • stimaultion or depressuion of fucntional activity
    -replacement of an essentiasl compound (e.g. under active thyroid)
    -killing forgein organism
    -changinga physiochemical enviroment
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

classification of drugs

A
  • phychopharamaceutical agents acting on CNS
    -pharmacodynamic agents
    -chemotherapuetic agents
    -metabolic agents
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what are primary affects and secondary affects

A

primary - desired therpauetic effects
secondary - side affects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

what is the mechanims of drug action

A

involve interaction between the chemical and parts of the organims

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

what is an agonist

A

a drug that mimics and reproduces a reponse simalr to taht of naturally occuring biological molecule

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

what is an anatagnosist

A

a drug that supresses a naturally occuring event

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

what is a lead structure

A

molecular structure which gives some desired biological activity in an assay

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

what is optimasation

A

modification for example making teh drug more soluble

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what was the first medicinal drug and where was it from

A

asprin from willow leaves

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

how long does it take to initial docovery to a marketable medidicne

A

12-15

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

what is toxoty of drug measured by

A

LD50

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

what saftey is needed with drugs

A
  • not teratogenic
    -carcinogenic
    non toxic
    optimal route of admisitartion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

what is looked for at preclincial level

A

-proof of prinicple
-safe potent and efficacous
-evaluates aspects of PD/PK and toxicology
-ideal preclinical model mimics himan disease
-PD establiushes the therpautoc index of a drug
-PK descibles chnages in plasmsa conc as a consequcen of ADME

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

what is the advanatge of in vitro preclinical studies

A

fast simple and effctive

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

what are genotoxic affectes tested on

A

yeast based systems

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

what are the advnatge of cell lines for invitro preclincial

A

can easily test proliferation against apoptosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

what is main advnatges of invivo precloinical studies

A

ADME suitable can also gentically engeneer mice

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

what are the disadvantge of animal testing

A

doesnt always highlight potentail properties
they have a differnet affect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

what are the disadvatnages of making a too lipidphilic drug

A

would accumalet in liver and kidneys and cause toxic damage

31
Q

what is done at phase 1 clinical trail

A

monitor drug in healthy ppl for about a year

32
Q

what is done at phase 2 clinical trail

A

what does drug do and the dose needed, done in a small amount of patinets (still looking at saftey)

33
Q

what is done at phase 3 clinical trail

A

an increased amount of ppl used

34
Q

what is done at phase 4 clinical trail

A

approval and long term results

35
Q

what are the aims of drug deisgn

A
  • good selectivity
  • good level of activity
  • minimal side affectrs
    -easily synthesised
    -chemically stable
    -acceptible pharmacokinetc properties
    -non toxic
36
Q

what is the funnel affect

A

drug discover
compounds screened
preclincial
clinical
approval

37
Q

what is a new molecular entitiy

A

a drug that has never been approved by FDA or marketed in any form or deriviative

38
Q

what are the advantages of small molecules over macromolecules

A

greater dverity, cheaper, easier to make and manipulate, more scaleable and rapidly diffuse into cells.

39
Q

what are the sources if kead structure

A
  • from obserevd clincial and pharmacological side affect
  • from traditional medecine
  • random screening and high throughpout screening
    -combinational chemistry
40
Q

what is ligand based drug design

A

biologcial affect no idea with mode reaction

41
Q

what is target based drug design

A

serial tetsing of substances with an isolated biological target to indentify an agent that induces a desired biochemical outcoem

42
Q

how are the drugs classified

A
  • molecular target
  • biochemical process
  • pharmacological affect
  • chemical structure
42
Q

how are the drugs classified

A
  • molecular target
  • biochemical process
  • pharmacological affect
  • chemical structure
43
Q

what are the actions of drugs

A

the way the drug excerts teh desired affect

44
Q

what are teh affects of a drug

A

the observed consequences

45
Q

what is mechainims of drug action interactions

A

interaction betwene chemical and parts of organism

46
Q

what are the 9 satges of drug design

A
  • indentify targets
  • extract compound
  • check acticity
  • detrmine molecular structure
    -synthesise analgoges
  • deduce molecular features
  • syntyhesise new compounds with increased acticity
  • test
    -select lead
47
Q

what is a selecetive drug

A

many actions one effect

48
Q

what is a specific drugs

A

1 target many affects

49
Q

what are the aims of preclinical saftey testing

A

to be able to give the patient a dose of the drug that achieves the desired affect with causing harmful side affects

50
Q

in preclincial what does PK describe

A

the changes in the plasma conc as a consequnce of ADME

51
Q

in preclincial what does PD establish

A

the theraputic index

52
Q

what is an example of a ligand based drug

A

penecilin

53
Q

what is an exammpleof a speciific drug

A

atrapine - binds to acetylcholine receptors and affects heart rate and dilution of pupils

54
Q

what is an example of a selective drug

A

heparin, high target numbers but is only an anticoagualnt

55
Q

what type of ddrug do you normal get from targetted drug design

A

specific drugs

56
Q

what type of drug is produced from ligand based drug disovery and give an exmaple

A

selective drugs
asprin (tends to be older drugs)

57
Q

what drug is an example of nieither speicific or selective

A

antihisatmine

58
Q

what is an exmaple of a drug with a very narrow theraputic window

A

warafron - small window between anticogualnt and bleeding out

59
Q

what is an exmaple of antagonoist

A

chemotherpay on cell pathway

60
Q

what types of drugs can be people easily become reistant

A

targetted drugs

61
Q

what is a lead

A

minium structure that is needed to get the desired biological acticity

62
Q

what is a lead

A

minium structure that is needed to get the desired biological acticity

63
Q

what does invivo preclinical trails

A

genticically modified mice
humna tumour xenografts

64
Q

what is invivo

A

in animal studies or people

65
Q

what is in inivtro

A

in petri dish

66
Q

what are advantges if invivo

A

can look at toxicity, PD and pk

67
Q

what is the disadvantage of animals models

A

doesn’t always highlight potentail issues and the main issue is because the drug is too lipophillic and goes to kidneys and livers

68
Q

what is the translational phase

A

bench to bedside

69
Q

what is a new molecular entitiy

A

a whole new drig taht has never been approved by the FDA

70
Q

what are the sources of lead structure and give examples for 3

A
  • side affects of compounds
  • from traditional medicine using natural sources- asprin
  • random and high throughput screening
  • combination chemistry and inital screening
  • me better - captoprill
71
Q

what is an example of a me better drugger

A

captopril

72
Q

how was asprin developed

A

salicin was fouond in willow bark and found to give pain relief, the mechinims was invetsigated, analgoues were found which got rid of mouth irratation and bad taste

73
Q

what is an orphan receptor

A

a nuclear recpetotr taht hasn’t doesnt have a ligand or there is lack of information on it

drug design (12 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions