Pharmacodynamics

Question 1

Effect of the drug on the body

Answer 1

Pharmacodynamics

Question 2

Effect of the body on the drug

Answer 2

Pharmacokinetics

Question 3

What is a Dose-Response Curve?

Answer 3

Relationship between a drug and its effects

Question 4

If the Dose-Response curve is plotted arithmetically, what shape will it be?

Answer 4

Hyperbolic

Question 5

More commonly, if the Dose-Response curve is plotted with the LOG of drug dose, what shape will it be?

Answer 5

Sigmoidal

Question 6

What is Emax and where is it found?

Answer 6

Maximal effect produced by a drug

- Top of Y axis (100% response)

Question 7

What is ED50 and where is it found?

Answer 7

Drug dose that produces 50% of maximal effect

- X axis that coordinates to 50% on Y axis

Question 8

Graded Dose-Response curves represent?

Answer 8

MEAN VALUE within a population/person

Question 9

With Graded Dose-Response curves, the magnitude of response varies ______

Answer 9

Continuously

Question 10

Quantal Dose-Response curves examine?

Answer 10

FREQUENCY of a response within a population

Question 11

What are the 2 types of Quantal Dose-Response curves?

Answer 11

Non-cumulative

Cumulative

Question 12

Non-cumulative Quantal Dose-Response curves measure?

Answer 12

% of people responding at a dose and ONLY AT THAT DOSE

Question 13

Cumulative Quantal Dose-Response curves measure?

Answer 13

% of people responding at a dose AND AT ALL DOSES LOWER than that dose

Question 14

What shape is the Non-cumulative Quantal Dose-response curve?

Answer 14

Bell shaped

Question 15

What shape is the Cumulative Quantal Dose-response curve?

Answer 15

Sigmoidal

Question 16

Median Effective Dose

Answer 16

ED50

Question 17

Median Toxic Dose

Answer 17

TD50

Question 18

Median Lethal Dose

Answer 18

LD50

Question 19

Therapeutic Index (TI) =

Answer 19

TD50/ED50

Question 20

The greater the Therapeutic Index (TI) the?

Answer 20

Safer the drug

Question 21

Drug Potency

Answer 21

Amount of a drug required to produce a specific effect

Question 22

Drug Potency is represented by?

Answer 22

ED50

Question 23

The lower the ED50 on the x axis, the more ___ a drug

Answer 23

Potent

Question 24

Drug Efficacy

Answer 24

Maximal effect produced by a drug

Question 25

Drug Efficacy is represented by?

Answer 25

Emax

Question 26

The higher the Emax on the Y axis, the more ____ a drug

Answer 26

Efficacious

Question 27

Drug efficacy is related to the _____ available to bind the drug

Answer 27

of receptors available to bind the drug

Question 28

What determines the drug dose used clinically?

Answer 28

Drug potency

Question 29

What determines the magnitude of the clinical effect?

Answer 29

Drug Efficacy

Question 30

What are 4 parameters to describe the interaction of a drug with its receptor?

Answer 30

Binding Affinity Selectivity Intrinsic Activity

Question 31

What type of bonds to most drugs use to bind to their receptors?

Answer 31

Reversible Non-covalent bonds

Question 32

How readily and tightly a drug binds to its receptor

Answer 32

Affinity

Question 33

A HIGH affinity correlates to _____ drug needed for a response

Answer 33

LESS

Question 34

A LOW affinity correlates to ____ drug needed for a response

Answer 34

MORE

Question 35

KD

Answer 35

Drug concentration at which 50% of binding sites are occupied by the drug

Question 36

KD is on the ___ axis

Answer 36

x axis

Question 37

A LOWER KD =

Answer 37

HIGHER AFFINITY

Question 38

Property of a drug determined by its affinities at various binding sites

Answer 38

Selectivity

Question 39

KD ratio measures?

Answer 39

Selectivity

Question 40

KD ratio

Answer 40

KD off-target / KD target

Question 41

The HIGHER the KD ratio, the _____ the selectivity

Answer 41

HIGHER Selectivity

Question 42

The HIGHER the selectivity, the ____ adverse effects

Answer 42

LOWER adverse effects

Question 43

What is Intrinsic Activity?

Answer 43

Ability of a drug to change receptor function and produce a physiologic response

Question 44

Ability of a drug to change receptor function and produce a physiologic reponse

Answer 44

Intrinsic Activity

Question 45

Bind receptor, stabilizes it, and produces a physiologic reponse

Answer 45

Agonists

Question 46

Do Agonists have intrinsic activity?

Answer 46

YES

Question 47

Bind receptor, and do NOT change its function

Answer 47

Antagonists

Question 48

Do Antagonists have intrinsic activity?

Answer 48

NO - do not change receptor function or produce physiologic response

Question 49

3 types of Agonists?

Answer 49

Full Agonist Partial Agonist Inverse Agonist

Question 50

What type of agonist mimics actions of endogenous chemicals?

Answer 50

Full agonists

Question 51

What type of agonist produces opposite effects of the other agonists and decreases receptor signaling/response?

Answer 51

Inverse agonist

Question 52

What agonists/antagonists block action of endogenous chemicals?

Answer 52

Partial and Inverse agonists | All Antagonists

Question 53

3 broad categories of antagonists?

Answer 53

Pharmacologic Chemical Physiological

Question 54

2 types of pharmacologic antagonists?

Answer 54

Competitive | Non-competitive

Question 55

2 types of Non-competitive pharmacologic antagonists?

Answer 55

Irreversible | Allosteric

Question 56

Pharmacologic antagonists act where?

Answer 56

Same receptor as agonists/endogenous chemicals

Question 57

Chemical antagonists make drugs?

Answer 57

Unavailable

Question 58

Competitive antagonists compete for binding at the receptor. Can they be displaced and overcome?

Answer 58

YES

Question 59

With Competitive Antagonists present, describe Emax and EC50 for an Agonist

Answer 59

``` Emax = unchanged EC50 = increased ```

Question 60

Can Non-competitive antagonists' receptor inactivation be overcome?

Answer 60

NO

Question 61

How do Irreversible Antagonists work?

Answer 61

Occlude Agonist site using covalent bonds (irreversible)

Question 62

How do Allosteric Antagonists work?

Answer 62

Bind to site OTHER THAN agonist site | = Decreases agonist binding or receptor activation

Question 63

With Non-competitive Antagonists present, describe Emax and EC50 for an Agonist

Answer 63

``` Emax = decreased EC50 = unchanged ```