Pharmodynamics

Question 1

What is the difference between efficacy and intrinsic efficacy

Answer 1

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

Question 2

What does the Kd show

Answer 2

The 50% occupancy at a certain concentration

Question 3

Why is it good to have a high affinity of a drug

Answer 3

Would mean that a low concentration would be needed

Question 4

What is the potency of the drug

Answer 4

The effective concentration that would produce 50% of the maximal response

Question 5

What is EC50 and Emax

Answer 5

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

Question 6

How can you show the concentration of the drug outside the receptor

Answer 6

Using radioligands
Would release radioactivity
Can show the concentrations when there are 50% or 100% of the drug is bound

Question 7

What is molarity

Answer 7

The concentration

Question 8

How can you calculate the molarity

Answer 8

Molarity = molar weight / g/L

Question 9

What does an agonist do

Answer 9

Attaches to the receptor
The confirmation all change of the receptor
Then the activation

Question 10

What does the antagonists do

Answer 10

How bind to the receptor
Would not activate and would not have the confirmational change

Question 11

What are spare receptors

Answer 11

Receptors that would not be occupied by the Ligands

Question 12

What is good about the spare receptors

Answer 12

They would allow the increased sensitivity
Less ligands would be needed to produce the full response

Question 13

What does changing the receptor number do

Answer 13

Increases the agonist potency so can increase the response

Question 14

What is up-regulation of the receptors

Answer 14

Increasing the number of receptors in the body

Question 15

What is down-regulation

Answer 15

Decreasing the number of receptors

Question 16

What are the characteristics of full agonists

Answer 16

Can produce 100% of the response
Have spare receptors

Question 17

What are the characteristics of partial agonist

Answer 17

Do not have the spare receptors
Do not produce the full response
EC50 = kd50

Question 18

What is intrinsic activity

Answer 18

The ability to produce the maximal response

Question 19

What happens to the intrinsic activity when you move from partial agonist to a full agonist

Answer 19

The intrinsic activity would increase as would produce the max response

Question 20

What is good about partial agonist drugs

Answer 20

Allows easier control
Can be used as antagonists for a drug
Can be used when there is low endogenous or no endogenous ligand

Question 21

What happens when buprenorphine (partial) is used for heroin addiction

Answer 21

Would attach to the heroine ligands would not aLlow heroine to bind
Would 5en reduce the effect of heroine

Question 22

Why does withdrawal occur

Answer 22

Less effective endogenous ligands available
The partial agonist would bind but would have no effect so would lead to withdrawals

Question 23

What is reversible competitive antagonism

Answer 23

Both agonist and antagonists present
Can bind and unbind depending on the concentrations

Question 24

What is the irreversible competitive antagonism

Answer 24

An agonist or antagonists would bind and would not be released

Question 25

What is non-competitive antagonism

Answer 25

Antagonist would bind and would not be released
So would have no response

Question 26

What is the IC50

Answer 26

The concentration of agonist that would inhibit 50% of the maximal response

Question 27

What is special about the partial agonist compared to the drug it’s used against

Answer 27

The partial agonist would have a greater binding affinity to the receptor then the drug its sued against