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Principles Of Pharmacology > Week 5 > Flashcards

Week 5 Flashcards

1
Q

What are the main protein targets for drugs?

A

Enzymes
Receptors
Ion Channels
Carrier proteins

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2
Q

Why do proteins make good target for drugs?

A

Only proteins have the intricate folding which enables a precise receptor site to allow a highly specific response.

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3
Q

What are the 2 possible functions of enzymes in terms of biologically active molecules?

A

Catalyse the breakdown or catalyse the synthesise of biologically active molecules.

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4
Q

What are the benefits of drugs acting on enzymes which catalyse the breakdown of biologically active molecules?

A

A drug may inhibit the breakdown of the biologically active molecules by acting as an inhibitor. This means that less of the biologically active molecule would be broken down and more would be available for therapeutic uses.

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5
Q

What are the negatives of drugs acting on enzymes which catalyse the synthesis of biologically active molecules?

A

A drug may exert therapeutic effects by inhibiting enzymes that aid synthesis of biologically active molecules. Therefore levels of biologically active molecule are reduced.

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6
Q

What type of molecules are monoamines?

A

They are neurotransmitters

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7
Q

Where are monoamines present?

A

In the pre-synaptic neurone

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8
Q

What are the effects of having little monoamines?

A

Depression

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9
Q

What are the effects of having excess monoamines?

A

Mania

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10
Q

What is the purpose of monoamine inhibitors?

A

They reduce Monoamine breakdown therefore making more of he neurotransmitter available in the synaptic cleft.

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11
Q

What are the therapeutic uses of monoamine inhibitors?

A

Antidepressants

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12
Q

What is the effect of Acetylcholinesterase on Acetyl Choline?

A

Breaks down acetyl choline into inactive products of choline and acetate

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13
Q

What happens to the products of acetyl choline being broken down by acetylcholinesterase?

A

Choline products are recycled back into the neurone.

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14
Q

How would you increase the levels of acetyl choline a person has?

A

Use a drug to block acetylcholinesterase. Means less acetyl choline will be broken down.

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15
Q

Name a drug which can block Acetylcholinesterase.

A

Donepezil

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16
Q

What disease is Donepezil often used to treat?

A

Alzheimers

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17
Q

What is Myasthenia Gravis?

A

A disease where the acetyl choline receptors are destroyed in the neuromuscular junctions.

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18
Q

What are ACE inhibitors used to treat?

A

Hypertension and heart failure

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19
Q

How do ACE inhibitors work?

A

They dilate blood vessels to increase blood flow to the heart and lower blood pressure.

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20
Q

How do ACE inhibitors act as catalysts?

A

They aid the conversion of Angiotensin I to Angiotensin II.

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21
Q

What are the effects of Angiotensin II?

A

Increases blood pressure

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22
Q

What are the purpose of ACE inhibitor inhibiting enzymes?

A

They block the conversion of Angiotensin I to angiotensin II so prevent a rise in blood pressure.

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23
Q

What is the purpose of HMG-CoA reductase?

A

Used to convert HMG-CoA to Mevalonic acid

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24
Q

What does Mevalonic acid eventually become after a series of reactions?

A

Cholesterol

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25
Q

What is a beneficial use of Cholesterol?

A

Used to synthesise steroid hormones

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26
Q

What production does aspirin prevent?

A

Prostoglandin production

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27
Q

What are the purpose of prostaglandins?

A

Control inflammation and pain at the sites of tissue damage.

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28
Q

How are Prostoglandins produced when a cell is damaged?

A

Arachidonic acid is produced by the damaged cell and converted to Prostoglandins by Cyclooxygenase enzymes.

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29
Q

What are the purpose of COX enzymes?

A

Convert Archidionic acid to prostoglandins

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30
Q

What are the purpose of NSAIDS?

A

Inhibit Cyclooxygenase (COX) enzymes so inflammation and pain is reduced.

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31
Q

What does NSAIDS stand for?

A

Nonsteroidal anti-inflammatory drugs

32
Q

What is the purpose of transpeptidase?

A

Used to link peptides in bacterial cell walls

33
Q

What effects do penicillin have on bacteria?

A

Bind to transpeptidase enzyme and prevent it linking peptides in bacterial cell walls.
Bacterial cell walls not formed / broken.
Cellular death.

34
Q

What are the properties of receptor agonists?

A

They have affinity and efficacy for the receptor.

35
Q

What are the properties of receptor antagonists?

A

Affinity for the receptor

36
Q

What are the effects of receptor antagonists?

A

Compete with natural substrates by binding to receptors and competing.

37
Q

Give and example of a receptor antagonist.

A

beta blocker

38
Q

What do receptor agnostic do overall?

A

Bind to the receptor and induce a biological response.

39
Q

In a receptor agonists reaction, what is response proportional to?

A

The number of receptors occupied.

40
Q

What is meant by the term ‘efficacy’?

A

A molecule which will activate a key group of the molecule it is targeting.

41
Q

What is meant by a molecule having ‘affinity’ to a receptor?

A

The molecule ‘chemically fits’ the receptor.

42
Q

What values are often used to compare drug potencies?

A

EC50 values

43
Q

How is it clear that one drug is more potent than the other when comparing their curves on a graph of response against log drug concentration?

A

The curve closer to the Y axis is more potent.

44
Q

What is the EC50 of a drug?

A

The concentration of a drug that gives half the maximum response.

45
Q

What are the main drug receptor families?

A

G-protein coupled receptors.
Ion-channel linked receptors.
Enzyme-linked receptors.
Intracellular receptors.

46
Q

What are intracellular receptors used for?

A

They control gene transcription.

47
Q

How do G-protein linked receptors work?

A

An agonist enters the receptor and interacts with a G-protein. This activates the enzyme and causes it to produce a second messenger.
The second messenger causes the cellular response.

48
Q

What type of receptor does Adrenaline use?

A

G-protein linked receptor

49
Q

How does Adrenaline act on receptor to cause a response?

A

In the lungs, adrenaline acts on beta-2 receptors of the bronchial smooth muscle cells and causes cyclic AMP to be produced as a second messenger. This results in bronchodilaton.

50
Q

What are the results of production of the second messenger Cyclic AMP in the body?

A

Bronchodilation

51
Q

What receptors does adrenaline target?

A

Beta-2 receptors in the bronchial smooth muscle cells

52
Q

How do ion-channel linked receptors work?

A

Ligand binds to the receptor and opens the ion channel allowing influx of ions into the cell.

53
Q

What receptors do Acetylcholine act on?

A

Nicotonic

54
Q

What effect does Actylcholine have on Nicotonic receptors and how is this useful?

A

Acetyl choline binds to nicotinic receptors and causes their channels to open. This allows influx of Na+ into the skeletal muscles to allow muscular contraction.

55
Q

What are GABAa receptors used for?

A

GABA binds to GABAa receptors in the CNS and causes the opening of chloride ion channels. Entry of chloride ions reduces neurone excitability.

56
Q

What are GABAa receptor molecules used to treat?

A

Anxiety, insomnia and epilepsy

57
Q

Where are GABAa receptors found?

A

CNS

58
Q

What is the overall effect of chloride ions on neurone excitability?

A

Reduces excitability

59
Q

Outline how tyrosine kinase receptors work.

A

Insulin binds to a receptor and causes Thyrosine Kinase to be activated. This stimulates metabolic changes in cells.

60
Q

What molecule causes activation of Thyrosine Kinase enzymes?

A

Insulin

61
Q

Outline how nuclear receptors work.

A

Lipid soluble hormone or drug penetrates the nuclear membrane and binds to the receptor in the nucleus. This induces gene transcription and therefore protein synthesis.

62
Q

What receptor type do local anaesthetic use?

A

Ion channel

63
Q

What type of receptors do calcium blockers in the smooth muscle use?

A

Ion channel receptors

64
Q

what are mitotic spindle receptor processes often used to treat?

A

Cancer (chemotherapy)

65
Q

What type of receptors are used in chemotherapy?

A

Those in mitotic spindles

66
Q

How do Vinca Alkaloids inhibit cell division?

A

They prevent the formation of mitotic spindles. They bind to tubule molecules to prevent them joining together to form microtubules which make up the spindles.

67
Q

How do taxanes prevent cellular division?

A

Prevent breakdown of mitotic spindles.

68
Q

Other than acting as neurotransmitters, where in the body are Monoamine oxidases present and what do they do?

A

They are present in the Gastrointestinal tract and metabolise tyramine from dietary sources.

69
Q

What does tyramine do to the body?

A

Tyramine is an amino acid that helps regulate blood pressure.

70
Q

What happens if there is too much tyramine in the body?

A

Severe hypertension can occur which can be fatal.

71
Q

What is hypertension?

A

Extremely high blood pressure

72
Q

Name some foods which contain Tyramine

A 
Aged meats
Soy sauce
Tofu
Miso
Broad beans
Snowpeas
Sauerkraut
Pickled herring
Avocados
Bananas
Yeast extracts
Red wine
73
Q

How would you calculate aspirin bioavailability ?

A

The area under a plasma concentration-time curve.

Measure AUC

74
Q

What is AUC in terms of a drug?

A

A measure of the body exposure to a drug after it is administered.

75
Q

What are the units of bioavailability?

A

mg*h/L

76
Q

What is drug AUC directly proportional to?

A

To the total amount of unchanged drug in the systemic circulation.

Principles Of Pharmacology (11 decks)

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