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Agonist
Drug which interacts with its receptors
Drug receptor complex generates a response
Size of response varies with
Proportion of receptors occupied
Proportion of receptors occupied varies with
Conc of agonist
Occupancy varies with
Agonist conc
What is measured instead of occupancy
Biological response
Dose response curve shows
Response against log10 agonist
Full agonist
Which elicit max response
Partial agonist
Which cannot produce maximal response
Why is not every agonist a full agonist
Characteristics of the tissue involved
Agonist receptor complex
Characteristics of the tissue involved
The total no of receptors present
Nature of receptor and response coupling
Agonist receptor complex
Intrinsic efficacy and is a property of the drug receptor complex
Affinity decreases
Dose response curve shifts further to the right
Efficacy increases
Max response that the agonist can produce also increases
Spare receptor hypothesis
To get a full response it is not always necessary for all receptors to be occupied, only a fraction of the total no. of the receptors
Spare receptors
More receptors present than are needed to generate the full response
Antagonist
Drug which reduces the response to another drug
Competitive antagonist
Interacts with same receptor as agonist
Types of competitive antagonists
Reversible competitive antagonists
Irreversible competitive antagonist
Reversible competitive antagonists
Effects can thus be reduced by adding more agonists
Antagonist dissociates from the receptor
Adding a reversible competitive antagonists
dose response curve shifts to the right along x-axis
Max response does not change
Irreversible competitive antagonist
Increasing conc has no effect
Antagonist does not dissociate from receptor
Adding an irreversible competitive antagonists
The curve does not shift
Max response decreases
Non-competitive Antagonism
Does not compete for the agonist receptors
Note 
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