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Principles of Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

what are the protein targets for drugs?

A

enzymes, receptors, ion channels and carrier channels

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2
Q

why are proteins good targets for drugs?

A

due to having a narrow specificity as they are very intricately folded

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3
Q

how can an inhibitor cause an increase of biological availability of a drug?

A

if the inhibitor binds to an enzyme that catalyses the breakdown of the drug then less of the drug will be broken down so more present in the body

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4
Q

what are examples of monamine oxidase transmitters?

A

dopamine, noradrenaline and serotonin

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5
Q

what is MAO designed to do?

A

prevent constant release of neurotransmitter

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6
Q

how is MAO able to reduce the level of neurotransmitter in the synaptic cleft?

A

a transport protein will pump the neurotransmitter back into the pre-synaptic cleft and MAO will then convert this to inactive products

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7
Q

what can MAO inhibitors be used to treat?

A

depression as if MAO is inhibited then it will not be able to breakdown the neurotransmitter so more will be present in order to bind to receptors and cause effect

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8
Q

what does Ach do?

A

it is a neurotransmitter that binds to nicotinic receptors

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9
Q

what is the effect of inhibiting AchE?

A

this prevents as much Ach from being broken down so that more is able to bind to nicotonic receptors

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10
Q

what can AchE inhibitors be used to treat?

A

donepezil is used to treat Alzheimers as preventing the breakdown of acetylcholine results in better communication between nerve cells

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11
Q

how does AchE inhibitors help myasthenia gravis?

A

drugs such as neostigmine prevents breakdown of Ach so greater stimulation of nicotinic receptors

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12
Q

what does ACE do? what effect does this have?

A

converts angiotensin I to angiotensin II which then leads to an increased blood pressure

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13
Q

what can ACE inhibitors be used to treat?

A

hypertension and heart failure due to blocking the production of angiotensin II so blood pressure levels do not increase

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14
Q

what is HMG CoAR?

A

HMG-CoA reductase, which converts HMG-CoA to mevalonic acid which is then converted to cholestrol

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15
Q

what kind of drugs inhibit HMG-CoAR and why?

A

statins as they inhibit the enzyme and therefore result in reduced cholesterol production for diseases such as atherosclerosis

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16
Q

what are COX inhibitors?

A

cyclooxyrgenase inhibitors

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17
Q

how is COX produced and what does this cause?

A

cell membrane damage liberates arachidonic acid to be converted to prostaglandins via COX

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18
Q

why might the production of prostaglandins want to be reduced?

A

because they are associated with inflammation and pain

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19
Q

what kind of drugs inhibit COX?

A

NSAIDS (non-steroidal anti-inflammatory drugs) such as aspirin

20
Q

how might enzyme inhibition lead to bacterial cell death?

A

transpeptidase inhibitors prevent the formation of transpeptidase that holds the peptides in the cell wall together, so when inhibited, this causes inability to synthesise a cell wall so leads to cell death

21
Q

what is an example of a drug that is a transpeptidase inhibitor?

A

penicillin

22
Q

what is a receptor agonist?

A

binds to a receptor due to affinity and also has high efficacy so has the ability to activate the key group and therefore generate a cellular response

23
Q

what is a receptor antagonist?

A

binds to the receptor due to affinity yet does not have efficacy so only able to block the receptor rather then cause a response

24
Q

what is an example of a receptor antagonist?

A

beta blockers

25
Q

what is the dose-response relationship?

A

the response to an agonist is proportional to the number of receptors used

26
Q

what is the shape of the curve for a dose-response relationship?

A

hyperbolic curve

27
Q

what is the EC50 of a drug?

A

the concentration that produces 50% of the maximum response

28
Q

how can the EC50 be calculated?

A

the log of the concentration of the drug is plotted against the response from which the EC50 can be determined

29
Q

why is an EC50 graph useful?

A

allows comparison of drug potencies

30
Q

what are the receptor families?

A

G-protein receptors, ion-channel linked receptors, enzyme linked receptors, intracellular receptors, voltage ion channels and carrier proteins

31
Q

why is a G-protein coupled receptor metabotrobic?

A

because it works through a second messenger model

32
Q

how does a G-protein coupled receptor work?

A

an agonist occupies the receptor which allows it to interact with a G-protein, which then activates an enzyme which produces a 2nd messenger chemical

33
Q

what receptors work via G-protein coupling?

A

Ach receptor and beta 2 adrenoreceptor

34
Q

what is an example of a second messenger?

A

cyclic AMP

35
Q

what are examples of drugs that work via G-proteins?

A

adrenaline or salbutamol

36
Q

how does an ion channel-linked receptor work?

A

the receptor is directly linked to an ion channel so when an ion binds, this causes the opening of the channel, allowing the ion to enter

37
Q

what is an example of an ion channel-linked receptor?

A

ligand binding to its receptor or Act binding to a nicotinic receptor and causing the opening of sodium ion channels

38
Q

how does a GABA receptor work?

A

in the CNS, GABA binds to the GABA receptor which causes the opening of chloride ion channels which reduces neurone excitability

39
Q

what are enzyme linked receptors?

A

mainly peptides or protein receptors that are usually linked to kinases

40
Q

how does the insulin enzyme linked receptor work?

A

when insulin binds, the tyrosine kinases becomes activated which then causes a change to metabolic activity

41
Q

what are intracellular receptors?

A

receptors that control gene expression, a lipid soluble drug enters the nucleus and binds to a receptor that controls gene expression

42
Q

how does the binding to an intracellular receptor cause a change in cellular effects?

A

stimulation of protein synthesis which causes a production of a protein that causes the cellular effects

43
Q

what is an example of a drug that binds to intracellular receptor?

A

anti-inflammatory steroids such as hydrocortisone which causes the production of a protein that inhibits synthesis of prostaglandins

44
Q

what kind of drugs use voltage operated ion channels?

A

local anaesthetics

45
Q

what do vinca alkaloids do?

A

inhibit cell division by preventing formation of the mitotic spindle by binding to tubules molecules and preventing them from forming the spindle

46
Q

what do taxanes do?

A

bind to tubules molecules and prevent disassembly

Principles of Pharmacology (12 decks)

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