Pharmodynamics Flashcards
What is the difference between efficacy and intrinsic efficacy
Efficacy would be the defined response
Intrinsic efficacy would be the activation of the receptor that would lead to a full or partial responses
Both would change the confirmation all shape of the receptor
What does the Kd show
The 50% occupancy at a certain concentration
Why is it good to have a high affinity of a drug
Would mean that a low concentration would be needed
What is the potency of the drug
The effective concentration that would produce 50% of the maximal response
What is EC50 and Emax
EC50 would be the concentration that would have the 50% of the maximal response
Emax would be the concentration that would give 100% of the response
How can you show the concentration of the drug outside the receptor
Using radioligands
Would release radioactivity
Can show the concentrations when there are 50% or 100% of the drug is bound
What is molarity
The concentration
How can you calculate the molarity
Molarity = molar weight / g/L
What does an agonist do
Attaches to the receptor
The confirmation all change of the receptor
Then the activation
What does the antagonists do
How bind to the receptor
Would not activate and would not have the confirmational change
What are spare receptors
Receptors that would not be occupied by the Ligands
What is good about the spare receptors
They would allow the increased sensitivity
Less ligands would be needed to produce the full response
What does changing the receptor number do
Increases the agonist potency so can increase the response
What is up-regulation of the receptors
Increasing the number of receptors in the body
What is down-regulation
Decreasing the number of receptors
What are the characteristics of full agonists
Can produce 100% of the response
Have spare receptors
What are the characteristics of partial agonist
Do not have the spare receptors
Do not produce the full response
EC50 = kd50
What is intrinsic activity
The ability to produce the maximal response
What happens to the intrinsic activity when you move from partial agonist to a full agonist
The intrinsic activity would increase as would produce the max response
What is good about partial agonist drugs
Allows easier control
Can be used as antagonists for a drug
Can be used when there is low endogenous or no endogenous ligand
What happens when buprenorphine (partial) is used for heroin addiction
Would attach to the heroine ligands would not aLlow heroine to bind
Would 5en reduce the effect of heroine
Why does withdrawal occur
Less effective endogenous ligands available
The partial agonist would bind but would have no effect so would lead to withdrawals
What is reversible competitive antagonism
Both agonist and antagonists present
Can bind and unbind depending on the concentrations
What is the irreversible competitive antagonism
An agonist or antagonists would bind and would not be released
What is non-competitive antagonism
Antagonist would bind and would not be released
So would have no response
What is the IC50
The concentration of agonist that would inhibit 50% of the maximal response
What is special about the partial agonist compared to the drug it’s used against
The partial agonist would have a greater binding affinity to the receptor then the drug its sued against
