Pharm: Pharmodynamics

Question 1

What activates the receptor to signal as a direct result of binding to it?

Answer 1

Agonists

Question 2

What type of agonist gives a 100% response?

Answer 2

Full agonist

Question 3

What type of agonist produces a lower response at full receptor occupancy than a full agonist?

Answer 3

Partial agonist

Question 4

Do partial agonists or full agonists have higher efficacy?

Answer 4

Full agonists have higher efficacy than partial.

Question 5

Do partial agonists produce a response when alone?

Answer 5

Yes

Question 6

In the presence of a full agonist, how does a partial agonist act?

Answer 6

Like a competitive inhibitor and blocks full agonist - therefore EC50 increases, Emax same (slope moved to the right)

Question 7

Does an allosteric agonist bind at the same site as an endogenous agonist?

Answer 7

No, binds to a different site

Question 8

Does an allosteric agonist produce a signal itself?

Answer 8

No

Question 9

How does an allosteric agonist impact the effect of an endogenous agonist?

Answer 9

Increases the effect of an endogenous agonist allosterically

Question 10

Allosteric modulators _________ effect of endogenous ligands

Answer 10

Potentiate

Question 11

How would an allosteric agonist impact the slope of CRC graph?

Answer 11

Shift slope of the line to the left because it potentiates the effect of the endogenous ligand

Question 12

How do antagonists interact with receptors?

Answer 12

Bind to receptor but do not activate it

Question 13

How do antagonists impact agonists?

Answer 13

Interfere with ability of agonist to activate the receptor

Question 14

What are the two types of Pharmacological Antagonists?

Answer 14

Competitive and non-competitive

Question 15

How do competitive antagonists bind to the receptor?

Answer 15

Bind reversibly to the receptor

Question 16

Can inhibition of a competitive antagonist be overcome? If so, how?

Answer 16

Yes, it can be overcome by increasing the concentration of the agonist

Question 17

How do non-competitive antagonists bind to the receptor?

Answer 17

Bind irreversibly to the receptor

Question 18

Can inhibition of a non-competitive antagonist be overcome? If so, how?

Answer 18

No, it cannot be overcome.

Question 19

E.max is also known as _______________________.

Answer 19

Efficacy or maximal effect produced by drug

Question 20

EC50 is the concentration of drug that gives _______ % of max effect

Answer 20

50%

Question 21

How does receptor binding affinity impact potency?

Answer 21

Increased receptor affinity leads to increased potency

Question 22

Bigger size tablet = ________ potency

Answer 22

Less potency

Question 23

Smaller size tablet = _________ potency

Answer 23

More potency

Question 24

Higher the EC50, ________ the potency

Answer 24

lower

Question 25

What is the Bmax of a drug?

Answer 25

The maximum binding to a receptor. (All receptors are bound)

Question 26

Kd is the conc of the drug at which _______________

Answer 26

Receptor occupancy is 1/2 max

Question 27

The higher the Kd, the ____ the affinity of receptor for its ligand

Answer 27

weaker/lower

Question 28

The lower the Kd, the _____ the affinity of receptor for its ligand

Answer 28

higher

Question 29

How does potency relate to size of pills?

Answer 29

Smaller pill, more potent ## Footnote Larger pill, less potent

Question 30

What is the potency of a drug?

Answer 30

Expression of the concentration required to reach a 50% occupancy (EC50) or dose (ED50)

Question 31

Height reached by a curve in a Concentration response curve graph indicates what?

Answer 31

Emax

Question 32

Partial agonists showed mixed properties. What does this mean?

Answer 32

Has mixed agonist-antagonist properties

Question 33

How does a partial agonist impact the effect of a full agonist when together?

Answer 33

Reduces effect of full agonist

Question 34

If a partial agonist is given in presence of a full agonist, it will __________ effect of the Full agonist

Answer 34

Reduce/block

Question 35

If a partial agonist is given to a patient who has been taking an agonist, pain may be decreased/increased (pick one). And why exactly?

Answer 35

increased! As the partial agonists fight for receptors with the agonists, the effects become less. That mean the pain goes up.

Question 36

How does a competitive antagonist impact Emax and EC50?

Answer 36

Emax will stay the same ## Footnote EC50 will be increased

Question 37

How does a competitive antagonist impact CRC graphs?

Answer 37

Causes line on CRC graph to shift right

Question 38

How do non-competitive antagonists impact Emax and EC50?

Answer 38

Emax is decreased due to receptors being blocked ## Footnote EC50 stays the same

Question 39

What are the 4 groups of antagonistic mechanisms?

Answer 39

PCPP ## Footnote Pharmacological, Chemical, Physiological, Pharmacokinetic

Question 40

Describe why pilocarpine did not help in this patient?

Answer 40

Pilocarpine did not help because while Pilocarpine is a cholinergic agonist, atropine is a cholinergic antagonist. Competitive pharmacological antagonism is taking place which can be overcome with increased concentration

Question 41

What type of antagonism is this an example of? A positive protein binds to and inactivates Heparin which is a (-) charged anticoagulant.

Answer 41

Chemical antagonism

Question 42

What type of antagonism occurs between endogenous regulatory pathways or agonists acting at different receptors?

Answer 42

Physiologic antagonism

Question 43

glucocorticoids vs insulin; PANS vs SANS are examples of what type of antagonism?

Answer 43

Physiologic antagonism

Question 44

When one drug increases metabolism or elimination of another, what type of antagonism is occurring?

Answer 44

Pharmacokinetic antagonism