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phase 2a > drugs and receptors > Flashcards

drugs and receptors Flashcards

1
Q

define the term drug

A

a medicine or other substance which has a physiological effect when ingested or otherwise introduced into the body

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2
Q

what are the 4 drug targets?

A

Receptors
Enzymes
Transporters
Ion channels

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3
Q

define pharmacology

A

the branch of medicine concerned with the uses, effects and modes of action of drugs

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4
Q

define receptors

A

a component of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to the ligands observed effects.

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5
Q

what are exogenous receptors?

A

drugs ( extrinsic)

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6
Q

what are endogenous receptors?

A

hormones, neurotransmitters (intrinsic)

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7
Q

what chemicals communicate via receptors?

A

neurotransmitters -(acetylcholine, serotonin), autacoids -(cytokines, histamine) and hormones-(testosterone, hydrocortisone).

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8
Q

what are the type of receptors?

A

ligand gated ion channeles
G protein coupled receptors
kinase linked receptors
cytosolic/ nuclear receptors

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9
Q

name an example of a ligand gated ion Channel?

A

nicotinic ACh receptor

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10
Q

what are ion channels?

A

are pore-formingmembrane proteinsthat allowionsto pass through the channel pore so that the cell undergoes a shift inelectric chargedistribution

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11
Q

describe G protein coupled receptors

A
  • have 7 membrane spanning region ( largest/most diverse group of membrane receptors)
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12
Q

give examples of ligands

A

light energy, peptides, lipids, sugar and proteins

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13
Q

what are G proteins?

A

also known asguanine nucleotide-binding proteins, are a family of proteins (35 in humans) involved in transmitting signals from GPCRs

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14
Q

what is the activity of G proteins regulated by?

A

by factors that control their ability to bind to and hydrolyzeguanosine triphosphate(GTP) toguanosine diphosphate(GDP

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15
Q

what are kinases?

A

enzymes that catalyse the transfer of phosphate groups between proteins- phosphorylation

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16
Q

what are kinase linked receptors?

A

receptors for growth factors

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17
Q

how do kinase linked receptors work?

A

activated when binding of an extracellular ligand causes enzymatic activity on the intracellular side

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18
Q

how do nuclear receptors work?

A

work by modifying gene transcription in. aligns or oestrogen dependant manner

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19
Q

what are nuclear receptors?

A

steroid receptors

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20
Q

how does tamoxifen work?

A
  • acts as aselective estrogen receptor modulator(SERM), or as apartial agonistof theestrogen receptors
  • Used in Oestrogen positive cancers.
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21
Q

what happens if you have increased histamine?

A

allergy

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22
Q

what happens if you have reduced dopamine?

A

parkinsons

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23
Q

what happens if you loose acetylcholine receptors?

A

myasthenia gravis

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24
Q

what happens if you have increased c kit receptor?

A

mastocytosis

25
Q

features needed to develop a therapeutic strategy?

A

Identify the receptor involved in a pathophysiological response

Develop drugs that act at that receptor

Quantify drug action at that receptor

26
Q

describe agonist

A

a compound that binds to a receptor and activates it

27
Q

describe antagonists

A

a compound that reduces the effect of an agonist

28
Q

describe ligands

A

a molecule that binds to another (usually larger) molecule

29
Q

what are the two categories of cholinergic receptors?

A

nicotinic
muscarinic

30
Q

antagonist of muscarine

A

atropine

31
Q

receptor of muscarine

A

mAChR

32
Q

antagonist of nicotine

A

curare

33
Q

receptor of nicotine

A

nAChR

34
Q

define affinity

A

describes how well a ligand binds to the receptor

35
Q

describe efficacy?

A

describes how well a ligand activates the receptor

36
Q

describe agonists in terms of affinity and efficacy

A

have both

37
Q

what is intrinsic activity?

A

refers to the ability of a drug-receptor complex to produce a maximum functional response

38
Q

what is competitive antagonism

A

when the antagonist and agonist bind to the same site and compete

39
Q

what is non competitive antagonism?

A

antagonist reverses the effect of the agonist
the antagonist bins to an allosteric site on the receptor- different to the agonist

40
Q

what is selective agonism?

A

potency of a range of agonists

41
Q

what is selective antagonist

A

competitive antagonist

42
Q

what are the two categories receptors are classified in?

A

Selective agonism
Selective antagonist

43
Q

what are the factors governing drug action?

A

receptor related
tissue related

44
Q

what does receptor related include?

A

affinity
efficacy

45
Q

what does tissue related include?

A

receptor number
signal amplification

46
Q

what happens if b2-adrenoceptors are inactivated?

A

Isoprenaline is a non-selective β adrenoreceptor agonist an analog of adrenaline).

relaxation of pre-contracted human bronchial rings

47
Q

what are irreversible antagonists

A

the receptor itself will never become available for signalling again
will be stuck to it

48
Q

what is the importance of reserve receptors?

A

Some agonists needs to activate only a small fraction of the existingreceptors to produce the maximal system response.

-reserve can be large or small; depends on tissue

49
Q

do partial agonists have reserves

A

No receptor reserve for a partial agonist
even with 100% occupancy, maximal response not seen

50
Q

what is sign transduction?

A

a basic process involving the conversion of a signal from outside the cell to a functional change within the cell.

51
Q

what does signal amplification do?

A

increase the strength of a signal
( Can be a large response or a short response)

52
Q

what is allosteric modulation?

A

When an allosteric ligand binds to a different site on the molecule and prevents the signal from being transmitted.
- ultimately effecting the same pathway

53
Q

what is inverse agonism?

A

When a drug that binds to the same receptor as anagonistbut induces a pharmacological response opposite to that of theagonist.

54
Q

describe tolerance

A
  • the reduction in drug effect over time
  • Used continuously, repeatedly in high concentrations
    -slow
55
Q

describe desenstitization

A

-suddenly whole system becomes uncoupled
-failed to get any sort of response
-could be due to degradation
-internalised
-rapid

56
Q

how to describe activity of compounds?

A

better to say selective when describing activity than specific as no compounds is every truly specific

57
Q

what is salbutamol an agonist for?

A

a b2-adrenoceptor agonist

58
Q

What is salbutamol selective for?

A

is selective for b2-adrenoceptors

59
Q
A

phase 2a (67 decks)

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