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intro to clinical sciences phase 2 > drug & receptors > Flashcards

drug & receptors Flashcards

1
Q

give 4 targets of drugs

A

receptors
enzymes
transporters
ion channels

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2
Q

define drug

A

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

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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 receptor

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 the 2 categories of ligand

A

exogenous - drugs

endogenous - hormones, neurotransmitters etc

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6
Q

how do chemicals communicate

A

via receptors

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7
Q

give examples of chemicals

A

neurotransmitters - acetylcholine, serotonin

autacoids (local) - cytokines, histamine

hormones - testosterone, hydrocortisone

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8
Q

give 4 types of receptors

A
  1. ligand gated ion channels
  2. g protein coupled receptors
  3. kinase-linked receptors
  4. cytosolic/nuclear receptor
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9
Q

example of ligand gated ion channel

A

nictonic ACh receptor

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10
Q

describe g protein coupled receptors

A

they are the largest and most diverse group of membrane receptors in eukaryotes
G proteins act as molecular switches (GDO = on. GTP= off)
Targeted by >30% of drugs
Ligands include light energy, peptides, lipids, sugars and proteins

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11
Q

what are ion channels

A

pore forming membrane proteins that allow ions to pass through the channel pore so that the cell undergoes a shift in electric charge distribution

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12
Q

what can mediate a change in charge

A

an influx of any kind of cation (+ve) or an influx of any kind of anion (-ve)

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13
Q

what are g proteins also known as

A

guanine nucleotide binding proteins

a family of proteins (35) involved in transmitting signals from GPCRs

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14
Q

what regulates activity of g proteins

A

factors that control their ability to bind and hydrolyse gunaosine triphosphate to guanisine diphosphate

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15
Q

what chemical causes allergies

A

increased histamine

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16
Q

what chemical causes parkinsons

A

reduced dopamine

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17
Q

what are kinases

A

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

the substrate gains a phosphate group donated by ‘ATP’

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18
Q

how do kinase linked receptors work

A

transmembrane receptors become activated when the binding of an extra cellular ligand causes enzymatic activity on the intracellular side

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19
Q

what uses kinase linked receptors

A

growth factors

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20
Q

which receptors cause myasthenia gravies

A

loss of Ach receptors

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21
Q

which receptors cause mastocytosis

A

increased c-kit receptor

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22
Q

how do nuclear receptors work

A

they are steroid receptors

work by modifying gene transcription

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23
Q

define ligand

A

a molecule that binds to another (usually larger) molecule

24
Q

define agonist

A

a compound that binds to a receptor and activates it

25
Q

define antagonist

A

a compound that reduces the effect of an agonist

26
Q

how does tamoxifen work

A

Breast Cancer) acts as a selective estrogen receptor modulator (SERM), or as a partial agonist of the estrogen receptors - Used in ER+ cancers.

27
Q

how to make a therapeutic strategy

A
  1. Identify the receptor involved in a pathophysiological response
  2. Develop drugs that act at that receptor

3,. uantify drug action at that receptor

28
Q

what is the 2 state model of receptor activation

A

describes how drugs activate receptors by inducing or supporting a conformational change in the receptor from ‘off’ to ‘on’

29
Q

what is intrinsic activity

A

also referred to as efffiacy

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

30
Q

what is competitive antagonist

A

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

31
Q

what is a non competitive antagonism

A

antagonist reverses the effect of the agonist

the anatagonist binds to an allostric site on the receptor -different to the agonist

32
Q

what is selective agonist

A

potency of a range of agonist

33
Q

what is selective antagonist

A

competitive antagonists

34
Q

what are the 2 categories of choliogernic receptors

A

nicotinic and muscarinic

35
Q

what is the antagonist and receptor for muscadine

A

agonist - muscarine

antagonist - atropine

receptor - mAChR

36
Q

what is the antagonist and receptor for nicotine

A

agonist - nicotine

antagonist - curare

receptor - nAChR

37
Q

what are the factors governing drug action

A

tissue related
- receptor number
- signal amplification

receptor related
- affinity
- efficacy

38
Q

define affinity

A

describes how well a ligand binds to the receptor

39
Q

define efficacy

A

describes how well a ligand activates the receptor

40
Q

what do agonists have

A

efficacy and affinity

41
Q

what do antagonists have

A

have affinity and ZERO efficacy

42
Q

what happens if b2 adrenoreceptors are inactivated

A

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

relaxation of pre-contracted human bronchial rings

43
Q

what are irreversible antagonists

A

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

44
Q

why are receptor reserves important

A

Some agonists needs to activate only a small fraction of the existing receptors to produce the maximal system response.
• This holds for a full agonist in a given tissue – reserve can be large or small; depends on tissue
• No receptor reserve for a partial agonist
– even with 100% occupancy, maximal response not seen

45
Q

define signal transduction

A

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

46
Q

define signal amplification

A

to increase the strength of a signal

47
Q

what is allosteric modulation

A

a type of receptor ligand interaction

When an allosteric ligand binds to a different site on the molecule and prevents the signal from being transmitted.

48
Q

what is tolerance

A

slow
Reduction in drug effect (agonist) over time
Continuously, repeatedly, high concentrations
occurs in asthma

49
Q

describe desensitisation

A

fast
whole system becomes Uncoupled - fail to get a response
could be due to:
- Internalized
- Degradation

50
Q

what is inverse agonism

A

when a drug that binds to the same receptor as a agonist but induces a pharmacological response opposite to that of the agonist

51
Q

is any compound specific

A

no - no compound is ever truly specific

better to use selective to describe

52
Q

what is isoprenaline

A

a non selective B adrenoreveptor agonist

53
Q

what is isoprenaline used for

A

bradycardia
heart block
rarely for asthma

54
Q

what is salbutamol

A

a selective b2 adrenoreceptor agonist

55
Q

what does salbutamol do

A

up the medium and large airways in the lungs, used for COPD/asthma

intro to clinical sciences phase 2 (48 decks)

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