Week 1 - Pharmacodynamics and Cell Signalling Flashcards Preview

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Flashcards in Week 1 - Pharmacodynamics and Cell Signalling Deck (28)
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1
Q

Details a Full Agonist

A
  • Produces maximum response

- High Efficacy

2
Q

Details of Partial Agonist

A
  • Cannot achieve maximal response.

- Low Efficacy

3
Q

Action of a Inverse Agonist

A
  • Decreases receptor activity (uncommon)
4
Q

Action of an Agonist

A
  • Binds to a receptor and activates it.

Eg: noradrenaline

5
Q

Action of an Antagonist

A
  • Binds to a receptor and produces no response

Eg: Atenolol (B-blocker)

6
Q

Actions of a Reversible Antagonist

A
  • Binds then quickly dissociates
  • may compete with agonist for binding site
  • surmountable
7
Q

Actions of an Irreversible Antagonist

A
  • binds then dissociates very slowly
  • inactivates a proportion of receptor
  • not surmountable (not affected by agonist concentration) population
8
Q

Action of a Competetive Antagonist

A
  • bind to same site an agonist uses

- can alter shape of receptor to make it inaccessible to agonist.

9
Q

Action of a Non-competetive Antagonist

A
  • binds only when agonist is not bound
10
Q

Action of an Uncompetitive Antagonist

A
  • binds even when agonist is bound
11
Q

What is Affinity?

A

the tendency to bind to a receptor

12
Q

What is Efficacy?

A

the ability to initiate a response once bound

13
Q

What is Intrinsic Activity?

A

the capacity of a single drug-receptor to evoke a response

14
Q

What is Pharmacokinetics?

A

Mechanisms of a drugs:
absorption, distribution and elimination
(i.e. the action of the body on the drug)

15
Q

What is Pharmacodynamics?

A

The mechanism of action of drugs on life processes

i.e. the actions of the drug on the body

16
Q

What is a Concentration-effect curve?

A

the relationship between

drug concentration and its pharmacological response

17
Q

What is Potency?

A
  • the concentration that produces a certain
    pharmacological response
  • Determined by affinity and efficacy
18
Q

What is EC50?

A

The concentration of a drug to produce 50% of a maximum response.
(measures potency)

19
Q

Example of Full Agonists and their receptor

A

morphine, heroine, codeine

at the mu opioid receptor

20
Q

Example of Antagonist and their receptor

A

naloxone and naltrexate

at the opioid receptors

21
Q

Example of Partial Agonist and their receptor

A

methadone

at opioid receptors

22
Q

Types of True Receptors

A
  • Ligand-gated ion channels
  • G-protein coupled
  • Kinase-linked
  • nuclear
23
Q

Examples of Ligand-gated Ion Channels receptors

A
  • GABA A and C
  • Glycine
  • 5-HT3
  • Purine P2x
24
Q

What is the location and coupling of a Ligand-gated Ion channel, giving an example?

A
  • membrane bound
  • direct coupling
    Eg. nicotinic ACh receptor; GABA
25
Q

What is the location and coupling of a G-protein-coupled receptors, giving an example?

A
  • membrane bound
  • channel or enzyme
  • G-protein
    Eg. muscurinic ACh receptor; all adrenoceptors
26
Q

What is the location and coupling of a Kinase-linked receptors giving an example?

A
  • membrane bound
  • direct coupling
    Eg. insulin; growth factors; cytokines
27
Q

What is the location and coupling of a Nuclear receptor giving an example?

A
  • Itracellular
  • gene transcription
  • via DNA
    Eg. steroid; thyroid receptors
28
Q

What are the 3 stages of Cell signalling?

A

Reception
Transduction
Response