Drug-receptor Interactions

Question 1

Drug or ligand which binds to the same site as the endogenous ligand and produces the same signal

Answer 1

Agonist

Question 2

Drug or ligand whihc binds to a different site than the endogenous agonist without producing a signal itself; this type of agonist enhances the response of endogenous agonists allosterically

Answer 2

Allosteric agonist

Question 3

Drug which produces a lower response when at full receptor occupancy than do full agonists. By themselves, they evoke a response, but in the presence of an agonist, they act to competitively inhibit full agonist binding to the receptor

Answer 3

Partial agonist

Question 4

Drug that binds to the receptor or components of the effector system used by the endogenous ligand and inhibits the action of the agonist; they initiate no effect on themselves

Answer 4

Antagonists

Question 5

Typical of drugs that bind reversibly to the receptor, inhibition can be overcome by increasing the concentration of the agonist, ultimately achieving the same maximal effect

Answer 5

Competitive antagonist

Question 6

Typical of drugs that bind irreversibly or allosterically to the receptor; this is a drug that prevents the agonist at any concentration from producing a maximum effect on a give recepto

Answer 6

Non-competitive antagonist

Question 7

Agonist receptor

Answer 7

Same

Question 8

Allosteric agonist receptor

Answer 8

Different site on the same receptor

Question 9

Partial agonist receptor

Answer 9

Same

Question 10

Antagonist receptor

Answer 10

Same

Question 11

Agonist signal

Answer 11

Same

Question 12

Allosteric agonist siglan

Answer 12

None by itself

Question 13

Partial agonist signal

Answer 13

Same

Question 14

Antagonists signal

Answer 14

None, just block

Question 15

Agonist response

Answer 15

Same

Question 16

Response of allosteric agonist

Answer 16

Greater than ag

Question 17

Partial agonist response

Answer 17

Less than ag

Question 18

Antagonists response

Answer 18

Less than Ag

Question 19

Which drug-receptor interaction binds to a different spot than the agonist

Answer 19

Allosteric agonist. Binds to a different spot on the same receptor

Question 20

Which two drug-receptor interactions have the same signal by themselves as the agonist

Answer 20

Agonist

Partial agonist

Question 21

Which drug-receptor interactions have no signal by themselves

Answer 21

Allosteric a agonist

Antagonist

Question 22

Which two drug-receptor interactions have a lesser response than the agonist

Answer 22

Partial agonist

Antagonist

Question 23

Which drug-receptor interaction has a greater affect than agonist alone

Answer 23

Allosteric agonist

Question 24

Which drug-receptor interaction has the same response when in the presence of an agonist

Answer 24

Agonist

Question 25

When looking at a graph plotting % max effect against log [agonsit], which type of drug-receptor interaction will not reach 100% max effect?

Answer 25

Partial agonist

Question 26

What can a partial agonist sometimes look like

Answer 26

An antagonist

Question 27

What does a %max effect vs log[A] curve look like when a competitive antagonist is added

Answer 27

It does not reduce the max effect, can give more agonists to overcome. Each curve should look the same on the graph

Question 28

What does a non competitive antagonist look like on the % max effect vs log [A] graph

Answer 28

The more antagonists that are added, the less steep the curve will get. The most common type is irreversible. No binding sites for agonists to bind to and make up for.

Question 29

Enahances activity of agonists

Answer 29

Allosteric agonist

Question 30

Potentiates the agonist

Answer 30

Allosteric agonist

Question 31

What does it mean when there is a left shift on the % max effect vs log [A] curve

Answer 31

Potentiation by an allosteric agonist Shifts curve in opposite direction as competitive antagonists

Question 32

Which direction will the curve shift in competitive antagonism

Answer 32

Right

Question 33

Which direction will the curve shift in noncompettive antagonism?

Answer 33

Down

Question 34

What happens to drug response when the dose increases

Answer 34

Generally as the dose increases, the response increases proportionally, however, as the dose increase the response increment diminishes until a dose is reached where no further increase in response can be achieved

Question 35

Example of dose-response relationships

Answer 35

Beta blocker to slow the heart down - 10mg, decrease HR by 10BPM - 20mg, decrease HR by 20 bpm - 40mg decrease HR by 30 - 80mg decrease HR by 30 The most you want to give of this drug is 40mg

Question 36

What is the equation for looking at dose-response relationships and the max effect (efficacy)

Answer 36

E= (Emax x C)/(C+EC50) Emax is the max response EC50 is the cxn that produces 50% of the max effect

Question 37

What is the equation for looking at dose-response relationships in terms of receptor binding

Answer 37

B=Bmax x C/(C+Kd) Bmax=total number of receptor sites Kd=cxn of free drug at which 1/2 max binding is observed

Question 38

When the graph reads "drug effect" on the y axis, what value are we looking at half way up the curve?

Answer 38

EC50

Question 39

When we are looking at a graph with the y axis reads as "receptor bound drug", what value are we getting half way up the curve

Answer 39

Kd

Question 40

When reading EC50, do you take the number off the Y axis or the X axis?

Answer 40

X

Question 41

When reading the Emax, do you read from the Y or the X axis

Answer 41

Y

Question 42

When reading Bmax, do you read from the Y or the X axis

Answer 42

Y

Question 43

When reading Kd, do you read from the Y or the X axis

Answer 43

X

Question 44

When can EC50 and Kd be identical

Answer 44

When bind half the receptors, you get half max response

Question 45

Refers to the concentration required to produce 50% of that drugs maximal response, refers to EC50

Answer 45

Potency

Question 46

Reflects the upper limit of the dose response relation on the response axis (max effect), associated with Emax

Answer 46

Efficacy

Question 47

Which is more important when choosing a drug, potency or efficacy

Answer 47

Efficacy. Care more about fixing the headache than how much drug you have to take.

Question 48

Between Emax and Kd, which is proabaky more important

Answer 48

Emax, efficacy is more important

Question 49

When looking at a response curve, how do you know the efficacy of a drug

Answer 49

By reading the Emax. If there is a partial agonist, the Emax will be lower

Question 50

What axis is associated with efficacy on the response curve

Answer 50

Y

Question 51

What axis is associated with potency on the response curve

Answer 51

X

Question 52

The curve that is the furthest _______ will be the most potent drug (on response graph)

Answer 52

Left

Question 53

The clinical effectiveness of a drug depends not on its __________ but on its ________ and its ability to reach relevant receptors

Answer 53

Potency (EC50) | Maximal efficacy

Question 54

When talking about therapeutic index on a graph, is a safer drug closer together or are the curves farther apart?

Answer 54

Father apart

Question 55

2 drugs, 1 receptors

Answer 55

Pharmacological antagonism

Question 56

Drugs may bind to and antagonize action of drug. 2 drugs, 0 receptors

Answer 56

Chemical antagonism

Question 57

Antagonist produces a physiological action that is opposite of agonsit and by a separate mechanism. 2 receptors, 2 drugs, the two receptors oppose each other

Answer 57

Physilogic antagonism

Question 58

Movement of a drug from the site of administration into the blood

Answer 58

Absoprtion

Question 59

Once in the blood, the drug moves to various parts of the body

Answer 59

Distribution