Brainscape's Knowledge GenomeTM

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


See full index

Pharmacology > Pharmacodynamics 2 > Flashcards

Pharmacodynamics 2 Flashcards

1
Q

DR complex causes ..

A

biological effect

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

drug binding to the receptor is governed by

A

affinity for the receptor

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

how does the drug create the biological effect

A

by causing a conformational change - efficacy or intrinsic activity

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

partial agonist

A

– no matter how much drug – cannot achieve full response in tissue

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

what can a log conc. curve tell you

A

what drug is more potent

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

what would you use to compare potencies from a conc response curve?

A

EC50 values

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

Antagonists have

A

affinity for a receptor - but they have zero efficacy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Antagonists - zero efficacy

A

do not activate a receptor they just block

- con observe an effect but there is no response

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

beta blocker

A

antagonist which stops the endogenous ligands binding - lowers HR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

agonist potency only involves

A

affinity

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

antagonists

A

block the action of agonists

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

agonist and increasing agonist cone-response curve

A

shifts the curve rights
drug - receptor interaction is reduced
alters the effective association - changing the apparent affinity of the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

concentration ratio (r)

A

EC50 Antagonist /EC50 agonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

r - 1

A

[B] /Kb

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

what should the axis for the Schild plot be?

A

X - Log [B] M

Y - Log (r-1)

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

what is the X intercept on the Schild plot

A

Kb

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

Log (r-1) =

A

Log [B] - LogKb

Think that B is the conc of the antagonist

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

what is the gradient of the schild plot slope for a competitive antagonist?

A

gradient 1

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

pA2 =

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

what measures of affinity do we use for agonist or antagonist

A

agonist - Kd

antagonist - pA2

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

what would the child plot slope being less than 1 suggest?

A

negative cooperativity - something happening to deplete it - overestimated the affinity of the agonist to start
- agonist acting on a second receptor type

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

what would schild slope being greater than 1 suggest?

A

cooperativity between the agonist and the antagonist - r the antagonist is being inhibited by being bound to somewhere else
- non specific binding, depletion of agonist

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

what must hold true for the child plot to work?

A

one molecule binding to one receptor (agonist or antagonist)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

what wold you see in a IRREVERSIBLE competitive antagonist graph?

A

the graphs shift down - get less response with higher conc of antagonist

(could also see some parallel shift but draw above in exam)

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

what happened to Kd with a irreversible competitive antagonist?

A

KD stays the same as the amount required to occupy receptors stays same – reducing amount of receptors
(not changing the affinity)

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

what allows irreversible antagonism?

A

a covalent bond being formed

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

what is non-competitive antagonism?

A

Preventing receptor activation or significantly reducing the receptor activation – reduced

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

what is chemical antagonism?

A

Two substances combine in solution

Result effect of active drug is lost

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

what are 2 examples of chemical antagonists?

A
  • Dimercaprol -

- infliximab

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

what do collating agents do?

A

mop up the excess - for excretion

31
Q

what does Dimercaprol do?

A

use to to treat heavy metal poisoning – lead – makes lead excretal by the body

32
Q

what does Infliximab do?

A

– anitinflamatory drug that targets tumor nercrosis factor – mops up TNF – less inflamation – antibody concept

33
Q

what receptors in the heart does noradrenaline act on? Effect?

A

B2 receptors

increase HR

34
Q

what receptors in the heart does Acetylcholine act on? Effect?

A

mAchR

decrease HR

35
Q

explain biased agonism

A

1 receptor type - 2 different agonists - would produce both responses equally or favour making more of one response than the other - but creates more of one response than the other

  • select which pathway becomes activated on binding
36
Q

what is pharmacokinetic antagonism?

A

injected somethnig – another drug affects something making the first drug less effective
(one drug affecting another metabolism - dangerous)

37
Q

what is allosteric modulation?

A

a substance which indirectly influences (modulates) the effects of a receptor agonist or inverse agonist at its receptor protein target.

38
Q

how would a positive modulator affect the conc. response curve?

A

curve would shift left – positive effect on affinity

39
Q

what would happen to the conc response curve if there was an allosteric modulator which has a negative affect on efficacy?

A

would become more squished down

40
Q

what is efficacy? (Emax)

A

maximum response achievable from an applied or dosed agent, for instance, a small molecule drug. Intrinsic activity is a relative term that describes a drug’s efficacy relative to a drug with the highest observed efficacy.

41
Q

what is the therapeutic index equation?

A

TD50 / ED50

TD - toxic dose
ED - effective dose

42
Q

what is the therapeutic window between?

A

MED and MTD

minimum effective dose and maximum tolerated dose

43
Q

what would a therapeutic index of 2 or less be

A

very risky

44
Q

what do the allosteric modulators valium/diazapan do?

A

positively modulate and calm down inhibitory neurones GABA receptor

45
Q

Ion-Channel Linked Receptors: Location/effector

A

membrane channel

46
Q

Ion-Channel Linked Receptors: coupling

A

direct

47
Q

Ion-Channel Linked Receptors: time

A

milliseconds

48
Q

Ion-Channel Linked Receptors: Structure

A

Many different sub-units, generally 4-5 f

49
Q

Ion-Channel Linked Receptors: Examples

A

Nicotinic ACh

GABAA

50
Q

G-protein Coupled Receptor: location and effector

A

membrane, enzyme or channel

51
Q

G-protein Coupled Receptor: coupling

A

G - protein

52
Q

G-protein Coupled Receptor: time

A

seconds

53
Q

G-protein Coupled Receptor: structure

A

A single protein with no subunit. Has 7 transmembrane α-helices as the binding domain with an intra-cellular G-protein coupling domain

54
Q

G-protein Coupled Receptor: examples

A

Muscaranic Ach

adrenorerceptors

55
Q

Tyrosine-Kinase Linked Receptors: location and effector

A

membrane, enzyme

56
Q

Tyrosine-Kinase Linked Receptors: coupling

A

direct or indirect

57
Q

Tyrosine-Kinase Linked Receptors: time

A

mins - hours

58
Q

Tyrosine-Kinase Linked Receptors: structure

A

A single α-helix which passes through the membrane. The catalytic domain contains the tyrosine kinase which phosphorylates tyrosine

59
Q

Tyrosine-Kinase Linked Receptors: examples

A

insulin and cytokine receptors

60
Q

Receptors Linked to Gene Transcription (nuclear receptors : locations and effector

A

intracellular and geen transcription

61
Q

Receptors Linked to Gene Transcription (nuclear receptors: coupling

A

via the DNA

62
Q

Receptors Linked to Gene Transcription (nuclear receptors time

A

hours

63
Q

Receptors Linked to Gene Transcription (nuclear receptors - structure

A

Close to nucleus and causes changes in DNA transcription. Has a binding domain and a DNA-binding domain (“zinc fingers”)

64
Q

RTK examples

A

Steroid receptors

Thyroid Hormone receptors

65
Q

ligand gated ion channels - where does the drug bind

A

N terminus tail outside the cell

C terminus is also outside the cell

66
Q

where is the N terminus on the RTK

A

on the top - where the drug binds - C terminus inside the cell

67
Q

Gas

A

coupled to adenylate cyclase which converts ATP –> cAMP

cAMP acts as a second messenger to phosphate kinase

68
Q

Gai

A

inhibitory

inhibits cAMP formation - less PK action

69
Q

Gaq

A

coupled to phospholipase C (membrane bound)

PLC activates and cleaves PIP2 to form DAG and IP3

DAG activates PKC and IP3 regulates [Ca} intracellularly

70
Q

which G protein dos the cholera toxin activate?

A

Gas - which blocks GTPase activity preventing inactivation

71
Q

GPCRs how much genome

A

1% of the human genome

huge diversity

72
Q

in GPRCs which ion channels activated how

A

Betagamma subunit principly activates K channels and inactivate voltage-gated calcium channels

73
Q

what is pharmacogenomics?

A

Genetic variability in the way drugs behave in the body

74
Q

Pharmacodynamic:

A

receptor variants

Pharmacology (18 decks)

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