Introduction to Pharmacology - Lecture 1 Flashcards

1
Q

What does a Endogenous substance mean?

A

Refers to a substance from within the body

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2
Q

What does a Exogenous Substance mean?

A

Refers to a substance from outside the body

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3
Q

What does Pharmacology comprise of?

A

Pharmacodynamics

Phamcokinetics

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4
Q

What is Pharmacodynamics?

A

This is what a drug does to the body (Biological effects and mechanism of action)

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5
Q

What is Pharmacokinetics?

A

This is what the body does to a drug (Absorption, distribution, Metabolism, Elimination)

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6
Q

What is a drug?

A

Any synthetic or natural substance that is used in the treatment or prevent of disease

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7
Q

What must a drug have to be effective as a therapeutic agent?

A

A degree of selectivity

  • Targets a particular biological process
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8
Q

How do drugs act?

A

Act by binding to target molecules

  • Lock and Key Hypothesis
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9
Q

How is selectivity achieved for drugs?

A

The Chemical structure of the drug is only recognised by the target receptors

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10
Q

What do drugs general bind to, to cause an effect?

A
Enzymes 
Carrier Molecules 
Ion Channels 
Receptors 
RNA 
DNA
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11
Q

What is a receptor?

A

Receptors are macromolecules that mediate the biological actions of hormones and neurotransmitters

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12
Q

Drugs acting on receptors can act in two ways - what are these ways?

A

As an Agonist

As an Antagonists

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13
Q

What is a ligand?

A

A molecules that binds to another l(usually larger) molecule

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14
Q

What is an agonist?

A

A substance that binds to a receptor to produce a cellular response

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15
Q

What is an antagonist?

A

A substance that blocks the actions of an agonist. `

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16
Q

What does an agonist do to the receptor?

A

Agonist binding causes a conformation change in a receptor

17
Q

What is the equation to define an agonist’s reaction with a receptor?

A

A + R AR AR* (activated)

18
Q

What is the efficacy of a reaction?

A

Efficacy is the ability of an agonist to evoke a cellular response

19
Q

What is the affinity of a reaction?

A

Affinity is the strength of association between a ligand and a receptor
(The longer the agonist stays on the receptor the higher the affinity)

20
Q

What is the term used when the receptors are 100% occupied?

A

Saturation point

21
Q

What is the relationship between receptor occupancy and agonist concentration?

A

Hyperbolic

22
Q

What is the Effective Concentration 50?

A

EC50 is the concentration of agonist that elicits a half maximal response (At which 50% of the receptors are occupied)

23
Q

What is the symbol given for Effective Concentration 50?

24
Q

What type of graph is often used instead of a hyperbola?

A

Semi-logarithmic plot (Response % vs Agonist concentration)

EC50 can still be calculated

25
What defines potency?
The EC50 value
26
What will a highly potent drug have in terms of EC50?
It will have a lower EC50 As less of the drug is required to elicit a response
27
What will weak (no potent drug have) for an EC50 value?
It will have a high EC50 value
28
How is Efficacy determined?
The Maximum response
29
Do Antagonists have "affinity"?
Yes - as they elicit a response by binding to them and blocking them, but not activating them
30
Do Antagonists have "Efficacy"?
No
31
What are the two types of antagonism?
Competitive antagonism | Non-competitive antagonism
32
What is competitive antagonism?
COMPETITIVE ANTAGONISM is where binding of agonist and antagonist occur at the same (orthosteric) site and is thus competitive and mutually exclusive. [Orthosteric Site is the site where endogenous substance binds]
33
What is non-competitive antagonism?
Where the agonist binds at the orthosteric site and the antagonist binds at the allosteric site. Both may occupy simultaneously. Activation cannot occur when the antagonist is bound
34
What happens to the Semi-logarithmic plot (Response % vs Agonist concentration) in the presence of a competitive antagonist?
Curve is shifted parallel to the right Slope remains the same shape Maximum remains the same EC50 is increased - The drug becomes less potent
35
What happens to the Semi-logarithmic plot (Response % vs Agonist concentration) in the presence of a Non-competitive antagonist?
Position of the agonist response curve stays the same Slope is decreased Maximum response is deceased EC50 is unchanged (Potency is unchanged) Efficacy is reduced