mechanism of drug action Flashcards

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1
Q

What is an agonist?

A

chemical that binds to and activates a receptor to produce a biological response

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2
Q

What is an antagonist?

A

blocks the actions of an agonist

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3
Q

What is a quantal response?

A

An all or nothing response

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4
Q

What are constitutively active receptors?

A

receptors that have a background activity even when an agonist is not present

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5
Q

What is the Two-State Model of Receptors?

A
  • receptors can be active or resting
  • under baseline circumstances, most receptors remain in the resting state
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6
Q

What are some targets for drug action?

A
  • ion channels
  • enzymes
  • carrier molecules
  • receptors
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7
Q

What are some type of receptors that are targets for drug action?

A
  • type 1: ligand gated ion channels
  • type 2: G-protein coupled receptors
  • type 3: enzyme-linked and related (kinase-linked)
  • type 4: nuclear ‘intracellular’ receptors
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8
Q

Give an example of a drug that directly interacts with ion channels?

A
  • lidocaine can block them in nerves
  • local anaesthetic
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9
Q

How does aspirin work on enzymes to treat pain?

A
  1. enzyme cyclo-oxygenase (COX) converts arachidonic acid into prostaglandins (PGs) which mediate pain and inflammation
  2. aspirin (acetyl-salicylic acid) targets COX and inhibits its activity
  3. reduce generation of inflammatory prostaglandins
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10
Q

Give an example of a ‘loop-diuretic’ drug and how does it work

A
  • furosemide used to increase urine production by blocking Na+K+2Cl- transporter
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11
Q

What is GABA?

A
  • gamma-aminobutyric acid
  • predominant inhibitory neurotransmitter in the brain
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12
Q

How does GABA inhibit things?

A
  1. interacts with GABAa receptor on Cl- channel
  2. allows Cl- to enter cell
  3. makes depolarisation difficult
  4. stabilises tissue
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13
Q

Describe the cAMP pathway in G-protein coupled receptors?

A
  1. Gs activated (Gi does opposite)
  2. adenylate cyclase (AC) activated, converts ATP to cAMP
  3. cAMP is second messenger, causes physiological response
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14
Q

Describe the calcium pathway in G-protein coupled receptors?

A
  1. Gq activated
  2. activated phospholipase C (PLC)
  3. activates IP3 and DAG
  4. they increase Ca2+ levels
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15
Q

What are some examples of physiological beta 2 receptor antagonists?

A
  • noradrenaline
  • adrenaline
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16
Q

What is cAMP broken down by?

A

phosphodiesterase

17
Q

Give an example of a synthetic beta 2 receptor agonist and what its for

A
  • salbutamol
  • leads to bronchodilation, good for asthma
18
Q

Describe type 4 receptors (nuclear receptors)

A
  • also called steroid hormone receptor
  • normally at rest in cytosol
  • move to nucleus when they bind to their ligand
  • control gene expression and lead to protein synthesis
19
Q

How do type 3 receptors work?

A
  • enzyme linked receptors
  • usually lead to protein phosphorylation cascade
20
Q

Rank the time each type of receptor takes

A
  1. type 1 (millisceonds)
  2. type 2 (seconds)
  3. type 3 (minutes)
  4. type 4 (hours)
21
Q

What drug helps with high blood pressure and how?

A

atenolol blocks beta 1 receptors to reduce blood pressure

22
Q

What are the difference types of beta receptors?

A
  • beta 1 (heart rate)
  • beta 2 (bronchodilation)
  • beta 3
23
Q

What is receptor desensitisation?

A
  • short term effect
  • happens very quickly (days)
  • involves loss of intrinsic activity of receptor complexes
24
Q

What is receptor down-regulation?

A
  • longer term effect (weeks)
  • involves a loss of number of receptors from cell surface
  • takes longer to recover
25
Q

What are some other mechanisms for a loss of effect of a drug?

A
  • exhaustion of mediators
  • increased metabolic degradation
  • physiological adaptation
26
Q

What are the possible effects of drug action?

A
  • therapeutic effects
  • side effects
  • adverse effects
  • toxic effects
27
Q

What are therapeutic effects of drug action?

A

drug produces the intended biological effect

28
Q

What is a side effect of drug action?

A
  • nuisance (e.g dry mouth)
  • can become harmful (e.g sedation)
29
Q

What is an adverse effect of drug action?

A

undesired effects that can be harmful (e.g allergies, anaphylactic shock)

30
Q

What is a toxic effect of drug action?

A
  • drug poisoning
  • harmful, may be life threatening (e.g liver damage associated with paracetamol overdose)
31
Q

Are agonists or antagonists more likely to produce unwanted effects and why?

A
  • antagonists
  • they are more likely to interact with multiple receptor types bc there are fewer constraints for molecular structure