Relationship btw amount of drug and effect

Question 0

what relationships are linear?

Answer 0

dose of drug and [drug] at target site

[drug-receptor complex] and response

Question 1

Dose response causal chain

Answer 1

dose of drug -> drug at target site -> drug-receptor complex -> response

Question 2

what relationships are non linear?

Answer 2

[drug] at target site -> [drug receptor complex]

Question 3

what is the dominant non linear relationship in the causal chain?

Answer 3

formation of the drug-receptor complex

Question 4

what does the drug-receptor complex determine?

Answer 4

the shape of the dose-effect and the concentration-effect relationships

Question 5

A plot of [D]free versus [R-D] is

Answer 5

hyperbolic

Question 6

A plot of log [D]free versus [R-D] is

Answer 6

sigmodial

Question 7

A plot of [D]free versus response is

Answer 7

hyperbolic

Question 8

A plot of log [D]free versus response is

Answer 8

sigmoidal

Question 9

The [drug] which causes 1/2 maximal response is called

Answer 9

EC50 and corresponds to the Kd if there is a linear relationship between [D-R] and response

Question 10

Potency refers to

Answer 10

EC50 of a drug

Question 11

when the assumption of linearity does not hold, the EC50

Answer 11

no longer approximates the Kd

Question 12

Spare receptors

Answer 12

when present, the EC50 will be much smaller than the Kd

Question 13

Tissue express “spare receptors” when

Answer 13

only a small fraction of the receptor population must be occupied by drug to give a maximal response

Question 14

The lower the Ec50, the

Answer 14

greater the potency

Question 15

A low Kd and high number of spare receptors increases

Answer 15

the potency of the drug

Question 16

Efficacy

Answer 16

refers to the maximal response of a drug

Question 17

the greater the maximal response,

Answer 17

the greater the efficacy

Question 18

The more effectively a drug engages signal-transduction systems in a cell per unit receptor occupied, the

Answer 18

greater is the efficacy of that drug

Question 19

best in class

Answer 19

Full agonist and any drug that generates a maximal response equal to the “best in class” is also referred to as “full agonist”

Question 20

Partial agonist

Answer 20

any drug that generates a maximal response less than that elicited by the “best in class”

Question 21

Even if Drug A is a full agonist and Drug B is a partial agonist, they can still the same what?

Answer 21

Potency

Question 22

Shape of dose versus Response

Answer 22

Hyperbolic

Question 23

shape of Log dose vs. Response

Answer 23

sigmoidal

Question 24

ED50

Answer 24

dose which causes 1/2 maximal response | affected by Kd and EC50 it is greatly influenced by apparent volume in which drug is distributed

Question 25

ED50 is never equal to

Answer 25

EC50 or Kd

Question 26

characteristics of surmountable antagonist

Answer 26

produces parallel shift in concentration-response curve of agonist Full effect of agonist can be restored by increasing concentration of agonist

Question 27

Common mechanism of surmountable antagonism

Answer 27

competitive interaction between agonist (potency and efficacy) and antagonist (potent but no or little efficacy) at binding site on receptor

Question 28

The net effect of a competitive antagonist is to increase the apparent

Answer 28

Kd, or said differently to decrease the apparent potency of the agonist

Question 29

Addition of competitive antagonist causes

Answer 29

apparent shift in EC50 for the agonist | because takes higher concentration for a response

Question 30

Characteristics of insurmountable antagonist

Answer 30

produce non-parallel shift in concentration-response curve of agonist full effect of agonist cannot be restored by increasing concentration of agonist

Question 31

Common mechanism of insurmountable antagonism

Answer 31

competitive but irreversible binding of antagonist to binding site on receptor allosteric modulation of receptor by antagonist so as to attenuate coupling of receptor to signal transduction blockade of signal transduction "downstream" of receptor

Question 32

Quantal effect

Answer 32

is an effect that is either present or absent

Question 33

Quantal concentration

Answer 33

or dose response curve is a plot of concentration or dose versus % patients in the population who exhibit the quantal response at the given concentration or dose

Question 34

we represent the effect of a drug in an Individual as a concentration or

Answer 34

dose response curve in which the graded effects of the drug are related to concentrations or doses of the drug

Question 35

we represent the effect of a drug in a Population as a concentration or

Answer 35

dose response curve in which the Quantal effect of the drug is related to concentrations or doses of the drug

Question 36

If quantal response happens to be death then ED50 is called

Answer 36

LD50

Question 37

Although both graded and quantal relationships have ED50s and EC50s, the parameter are

Answer 37

NOT the same for graded and Quantal relationships

Question 38

Graded relationships

Answer 38

Ed50s and EC50s indicate doses and concentrations that cause 1/2 maximal response in a given individual

Question 39

Quantal relationships

Answer 39

ED50s and Ec50s indicate doses and concentrations that cause 1/2 of the population to respond

Question 40

Since the log dose-response curve is sigmoidal, increasing

Answer 40

the dose of a drug when the response is submaximal will enhance the therapeutic effect

Question 41

Since the log dose-response curve is sigmoidal, increasing

Answer 41

the dose of a drug when the response is maximal will not improve the therapeutic effect but may subject the patient to toxicity

Question 42

The log dose-response curve is sigmoidal, regardless of whether the

Answer 42

"response" is therapeutic or toxic

Question 43

The safety of a drug can be assessed by examining the log dose-response curves for

Answer 43

therapeutic versus toxic effects

Question 44

The more separation between the therapeutic log dose-response curves and the toxic log dose-response curves, the

Answer 44

safer the drug

Question 45

A drug with low potency and high efficacy may be better than a drug with

Answer 45

low efficacy and high potency

Question 46

Potency is a determinant of

Answer 46

how much of the drug must be given to obtain a "ceiling" effect

Question 47

Efficacy refers to the magnitude of

Answer 47

the "ceiling" effect

Question 48

In an antagonist is being employed to block the effect of an agnoist, it is important to know whether the antagonist is of

Answer 48

surmountable or insurmountable type

Question 49

Dose of insurmountable antagonist usually does not need upward adjustment as amount of

Answer 49

agonist in body increases

Question 50

Dose of surmountable antagonist must be increased if amount of agonist (endogenous or exogenous) in the patient

Answer 50

increases

Question 51

Graded dose/concentration relationships help to understand

Answer 51

how changing dose of drug will effect the degree of response of an individual patient

Question 52

Quantal dose/concentration relationships help to understand

Answer 52

how changing dose of drug will effect the % of your patients who will experience a defined response