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There is no response that can be achieved with drug A that cannot be achieved with Drug B – you just need
to take a larger dose of drug B
Potency by itself does not infer superiority
Partial agonist: drug which binds to a receptor (has affinity) but even a full receipt occupancy it has left efficacy or
intrinsic activity than a full agonist
Competitive antagonists: drug which can combine with a receptor (has affinity) but does not activate the receptor
(no efficacy or intrinsic activity)
Competes with agonist to combine with a receptor and inhibits (blocks) the action of the agonist
Lock and key analogy
The effect is of a competitive agonist can be overcome by increasing the concentration of the agonist
The inhibitory effect of the competitive antagonist is surmountable because the binds between the
competitive antagonist and the receptor, are relatively weak and easily broken
A competitive antagonist shifts the agonist dose response curve to the right
Examples
o Narcotic antagonists such as naloxone which inhibit opioid mu receptors
o Antihistamines such as loratadine which inhibit histamine H1 receptors – inverses agonists?