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PJ1310 Science Of Medicines Yr1 > Principles Of Pharmacology 1 > Flashcards

Principles Of Pharmacology 1 Flashcards

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1
Q

What is the need for receptors?

A

Signalling molecules or hormones in the blood reaching a large no. Of cells

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2
Q

Do all cells respond to receptors?

A

Specificity is applicable where only specific cells have receptors for that chemical.

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3
Q

What is the receptor concept?

A

Chemicals produce and effect by combining to specific receptor - lock and key model.

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4
Q

What is affinity?

A

The strength of a drug receptor interaction

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5
Q

What are receptors?

A

Proteins with specific binding site that has both affinity and receptive to ligand

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6
Q

Receptor locations

A

Name different receptor locations

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7
Q

What are the four types of receptors?

A

Ion gated channels, g protein couples receptors, kinase linked receptors, nuclear receptors

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8
Q

How to ion gated channels work?

A

Hyperpolarisation/ depolarisation affects ion gates whether they open or close

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9
Q

How do G PC receptors work?

A

Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein and promotes exchange of GTP for GDP

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10
Q

How do kinase linked receptors work?

A

play an important role in protein phosphorylation, gene transcription, protein synthesis and cellular effect

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11
Q

How do nuclear receptors work?

A

Change what type of gene is expressed or depressed

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12
Q

List transmitters?

A

Hormones, neurotransmitters, autocoids, neuropeptides, neuromodulators

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13
Q

What are hormones?

A

Released from one cell to an extracellular cell to travel to new site if action

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14
Q

How are neurotransmitters released?

A

By exocytosis

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15
Q

Name types of neurotransmitter degradation and recovery

A

Diffusion- away from synapse /reuptake- nt reenter presynaptic axon terminal/ enzymatic degradation - in cytosol or synaptic cleft

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16
Q

Give types of neurotransmitters:

A

Acetylcholine, monomanies such as noradrenaline and dopamine/ amino acids such as GABA and GLUTAMATE/ neuropeptides such as endorphins/ purines such as ATP / soluble gases such as nitric acid

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17
Q

Give amino acid types of neurotransmitters and their functions?

A

GABA- 40% inhibit
GLUTAMATE- 50% excite

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18
Q

Whats the difference between a hormone and neurotransmitter?

A

N- diffused from presynaptic cleft into extracellular space to act in adjacent neurones
H- chemical released by an organ to be transportd in blood to reach targetted organ/tissue

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19
Q

Difference between adrenaline and noradrenaline

A

Adrenaline is a hormone released in blood for fight or flight and noradrenaline is a neurotransmitter

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20
Q

Recall types of receptors based on ligand

A

Cholinoreceptors- muscarinic and nicotinic
Histamine- h1/h2h3
Adrenoreceptors- alpha and beta

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21
Q

What are the different acetylcholine receptors

A

Muscarinic and nicotinc

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22
Q

Tell me more about nicotinc receptors

A

Ligand gated ion channels permeable to na+ ions and are excitatory
They are pentaremic and have 5 sub units alpha beta etc.

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23
Q

Tell me more about muscarinic recrptors

A

G protein coupled receptors, with 5 subtypes, M1/3/5 excite and M2/4 inhibit

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24
Q

What are gluttamate receptors

A

Theyre both ionotropic and metabotropic

25
Q

What are ionotropic receptors?

A

Receptors that open cation channels

26
Q

Talk about Gaba receptors

A

Gaba a- ionotropic- chloride channel
Gaba b - metabotropic - stop voltage gated ca channels and open k channels

27
Q

What are G coupled protein receptors

A

Muscarinic alpha beta receptors work by turning on transducer proteins specifically guanine

28
Q

Structural motifs

A

7 hydrophobic channels, single polypeptide chain with extracellular n terminus and intracellular c terminus

29
Q

What does an active g protein interact with

A

Ion channel to allow influx of ion or enzyme to produce a substance that helps to make another thing known as second messenger

30
Q

Whats the role of an agonist

A

Cellular response

31
Q

Whats the role of an antagonist

A

No response

32
Q

Explain the role of a pharmacological agonist

A

Combines with receptor and produces a response so has efficacy and affinity

33
Q

Explain the role of an antogonist

A

Combines with receptor does not cause a response but prevents agonist binding
Has affinity but no efficacy

34
Q

Whats the difference between blocker and modulator?

A

Blocker permeation is blocked whereas modulator increased/ decreased probability of opening

35
Q

What effect does a substrate have on enzyme?

A

Normal reaction =normal metabolite produced

36
Q

What effect does inhibitor have on enzyme?

A

Normal reaction inhubitted

37
Q

What effect does false substrate have on enzyme

A

Abnormal metabolite produced

38
Q

What does effect does prodrug have on enzyme

A

Active drug produced

39
Q

How do you study the effects of a drug on a receptor?

A

Use an isolated tissue preparation within an organ bath and investigatethe effects of the addition of the drug
OR
Use an animal/human and give them an increasing dose of the drug and monitor particular effect

40
Q

What information does the EC50 provide to us?

A

If drug had low EC50, drug has high affinity
If drug has high EC50, drug has low affinity

41
Q

How should a drug with different affinity be used in terms of dosage

A

If a drug has high affinity it should only be used in low concs and if a drug has low affinity it should be used in high concs

42
Q

How do you determine EC50?

A

By looking at the drug response at 50 and noting down the antilog

43
Q

Define EC50

A

The affinity of an agonist for its receptor

44
Q

In humans do we use affinity or potency

A

Potency

45
Q

Define potency

A

The required amount of drug to gain particular effect in an intact animal

46
Q

What is the amount of drug in relation to effect?

A

Some drugs have different potency but will have same efficacy

47
Q

On a graph, how do you know that all receptors have bound?

A

Maximum response of curve has levelled off

48
Q

What are the different types of agonist

A

Partial
Full

49
Q

What does 100% occupancy mean

A

100% effect

50
Q

What is drug efficacy

A

The ability of drug to produce a therapeutic effect

51
Q

What is the intrinsic activity equation

A

Maximum response to TESTagonist/maximal response to FULL agonist

52
Q

How do you calculate intrinsic activity

A

Small h/H

53
Q

What are the theee types on antagonist

A

Chemical, physiological, pharmacological

54
Q

What is a chemical antagonist?

A

A drug that counters the effects of another by binding the agonist drug (not the receptor)

55
Q

What is a physiological antagonist

A

Where the effect of the drug starts a reaction opposite to what is currently happening
Does not act at same receptor site
Usually pharmacological agonist

56
Q

What is a pharmacological antagonist?

A

Agonist meets receptor to stop action of agonist DOES NOT CAUSE A RESPONSE

57
Q

What is a irreversible antagonist

A

Binds in irreversible manner by covalent bond modification, causing irreversible effects= agonist cannot bind
Adding more agonist WILL NOT FIX THIS
WILL HAVE TO MAKE NEW RECEPTORS VIA PROTEIN SYNTHESIS

58
Q

What are non comp antagonists?

A

Binds to allosteric site, CANNOT BE OVERCOME BY ADDING MORE AGONIST
May not impair binding of ligand to make complex but will cause a conformational change= response

PJ1310 Science Of Medicines Yr1 (15 decks)

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