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[MT 6314] - 1st Shifting > [3] OLD Chapter 2 Pharmacodynamics > Flashcards

[3] OLD Chapter 2 Pharmacodynamics Flashcards

1
Q

Actions/ effects of the drug on the body

A

Pharmacodynamics

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2
Q

Specific molecules in a biologic system with which drugs interact to produce changes in the function of the system

A

Receptors

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3
Q

Determine the quantitative relations between dose or concentration of drug and pharmacologic effects

A

Receptors

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4
Q

Receptors: _______ in choosing a drug molecule to bind to avoid constant activation by promiscuous binding of many different molecules

A

Selective

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5
Q

Receptors: Selective in _______ characteristics (respond to proper chemical signals and not to meaningless ones)

A

ligand-binding

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6
Q

Receptors mediate the actions of both pharmacologic _____ and ________

A

agonist and antagonist

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7
Q

Specific binding region of the macromolecule

A

Receptor Site

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8
Q

High and selective affinity to the drug molecule

A

Receptor Site

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9
Q

Interaction between the drug and the receptor is the fundamental event that initiates the action of the drug

A

Receptor Site

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10
Q

What are the 4 Classification of Receptors

A
  1. Regulatory proteins
  2. Enzymes
  3. Transport proteins
  4. Structural protein
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11
Q

Classification of receptors:
Subserve specific physiologic functions

A

Regulatory proteins

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12
Q

Classification of receptors:
Catalyzes/facilitates metabolic processes

A

Enzymes

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13
Q

Classification of receptors:
Usually in the cell membrane, the raw materials of our metabolism is needed to be transported into the cell because we metabolize inside the cell

A

Transport protein

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14
Q

Classification of receptors:
Cytoskeleton of framework, cellular anatomy

A

Structural proteins

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15
Q

What is the best characterized drug receptor

A

Regulatory proteins

[they produce overt observable effects]

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16
Q

Inhibited (or less commonly, activates) by binding a drug

A

Enzymes

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17
Q

The membrane receptor for digitalis

A

Transport proteins

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18
Q

This is the receptor for colchine, an anti-inflammatory drug used for gout

A

Structural proteins

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19
Q

Molecules that translate the drug-receptor interaction into a change in cellular activity

A

Effector

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20
Q

A single molecule may incorporate both the drug binding site and the effector mechanism

A

Effector

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21
Q

Crossing the plasma membrane and acts on intracellular receptors

A

Lipid soluble drug

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22
Q

Intracellular enzymatic activity is regulated by a ligand that binds to the proteins extracellular domain

A

Transmembrane receptor protein

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23
Q

______ binds and stimulates a protein tyrosine kinase

A

Transmembrane receptor

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24
Q

Regulates the opening of the ion channel

A

Ligand-gated transmembrane ion channel

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25
Q

Transmembrane receptor is coupled with an effector enzyme by _____ which modulates production of an intracellular second messenger

A

G protein

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26
Q

What is the first messenger

A

Drug

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27
Q

G proteins and their receptors and effects:

Gs: ____ Adenylyl cyclase -> _____ cAMP

A

increase , increase

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28
Q

G proteins and their receptors and effects:

Gi1, Gi2, Gi3: ____ Adenylyl cyclase -> _____ cAMP

A

decrease, decrease

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29
Q

G proteins and their receptors and effects:

Golf: ____ Adenylyl cyclase -> _____ cAMP

A

increase , increase

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30
Q

G proteins and their receptors and effects:

Go: ____ Adenylyl cyclase -> _____ cAMP

A

Not clear

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31
Q

G proteins and their receptors and effects:

Gq: ____ Phospholipase C -> _____ IP3 diacylglycerol cytoplasmic CA2+

A

increase , increase

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32
Q

G proteins and their receptors and effects:

Gt1, Gt2: ____ cGMP phosphodiesterase -> _____ cGMP phototransduction

A

Increase, decrease

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33
Q

What is the secondary messenger producing phototransduction

A

cGMP

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34
Q

What G protein is inversely proportional

A

Gt1 and Gt2

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35
Q

Acting as an intracellular second messenger that mediates hormonal responses

A

cAMP
[Cyclic adenosine monophosphate]

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36
Q

In cAMP, conservation of water by the kidneys mediated by ______

A

vasopressin

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37
Q

When substrate is added to metabolic processes, the reaction is pushed _____ to create products

A

forward

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38
Q

What is the crucial step in calcium and phosphoinositide

A

Stimulation of membrane enzyme phospholipase C

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39
Q

Few signaling roles in a few cell types like the intestinal mucosa and vascular smooth muscle cells

A

cGMP
[Cyclic guanosine monophosphate]

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40
Q

Response of a particular receptor-effector system is measured against increasing concentration of a drug

A

Graded - dose response curve

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41
Q

Quantifies the response of the drug to each specific dose

A

Graded - dose response curve

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42
Q

On the x-axis, we have the [1]_____

On the y-axis, we have the [2]______

A

[1] Dose
[2] Response

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43
Q

In a linear scale, double double are usually seen in pharmacology experiments because of

A

Sigmoidal curve

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44
Q

Based on the Sigmoidal curve, as you increase the dose, the response will ______ up to a certain level, known as the Emax

A

increase

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45
Q

The _____ the EC50, the greater the potency of the drug

A

smaller

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46
Q

True or False:
Low EC50 = More potency of the drug

A

True

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47
Q

Maximal response that can be produced by a drug

A

Emax

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48
Q

The basis for characterization for full and partial agonists

A

Emax

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49
Q

Concentration of drug that produces 50% of maximal effect

A

EC50

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50
Q

The basis for drug potency

A

EC50

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51
Q

True or False:

EC50 is inversely proportional

A

True

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52
Q

Total number of receptor sites

A

Bmax

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53
Q

All receptors have been occupied

54
Q

The presumption is that all receptors are occupied

55
Q

The total receptor
occupancy

56
Q

True or False:

KD = equilibrium dissociation constant

57
Q

It is a measure of drug affinity

58
Q

True or False:
Higher affinity = High KD

A

False

Low KD [correct answer]

59
Q

True or False

Smaller KD = greater affinity of drug to receptor

60
Q

True or False:

KD is inversely proportional or reciprocal fashion

61
Q

Represents the concentration of free drug at which half-maximal binding is observed

62
Q

Transduction process between the occupancy of receptors and production of specific effect

63
Q

Highly efficient _______ can be elicited by a full
agonist and spare receptors.

64
Q

“downstream” biochemical events that transduce receptor occupancy into cellular response

65
Q

True or False

In Coupling, Full agonist tend to shift the conformational equilibrium of receptors more strongly than partial agonist

66
Q

Also known as receptor reserve

A

Spare receptors

67
Q

Drugs with low binding affinity for receptors will be able to produce full response even at low
concentration

A

Spare receptors

68
Q

Concentration of 50% EC50 and Concentration of 50% KD

KD____ EC50

A

> [less than]

69
Q

May be demonstrated by using irreversible antagonists to prevent binding of agonist to a proportion of available receptors

A

Spare Receptors

70
Q

Non regulatory, binding with these molecules will result to no detectable change in the function of the biologic system

A

Inert binding sites

71
Q

Buffers the concentration of the drug

A

Inert binding sites

72
Q

Binds to the receptor and directly or indirectly bring about an effect

73
Q

Full activation of the effector system

74
Q

Produces less than the full effect, even when
it has saturated the receptors

A

Partial Agonist

75
Q

Acts as an inhibitor in the presence of a full agonist

A

Partial Agonist

76
Q

Binds but do not activate the receptors and blocks or competes with agonist

A

Antagonist

77
Q

What are the 4 Classification of Antagonist

A
  1. Competitive Antagonist
  2. Irreversible Antagonist
  3. Chemical Antagonist
  4. Physiologic Antagonist
78
Q

Some antagonists exhibit inverse agonist activity
because they also reduce receptor activity below
basal levels observed in the absence of any
agonist at all

A

Irreversible Antagonist

79
Q

High antagonist concentrations prevent the response almost completely

A

Competitive Antagonist

80
Q

Irreversible antagonist bind with the receptor via _____

A

Covalent bonds

81
Q

Antagonist that are more dependent on the rate of turnover of receptors

A

Irreversible Antagonist

82
Q

Antagonist that does not depend on interaction with the agonist’s receptor

A

Chemical Antagonist

83
Q

Drug that interacts directly with the drug being antagonized to remove it or to prevent it from reaching its target

A

Chemical Antagonist

84
Q

Antagonist that makes use of the regulatory pathway

A

Physiologic Antagonist

85
Q

Binds to a different receptor producing an effect opposite to that produced by the drug it is antagonizing

A

Physiologic Antagonist

86
Q

_______ catabolic effects of increase in sugar is physiologically
opposed by insulin

A

Glucocorticoids

87
Q

Response gradually diminishes even if the drug is still there (after reaching an initial high level of
response)

A

Receptor Desensitization

88
Q

Cells use more than one signaling mechanism to
respond to the drug

A

Structure Activity Relationship

89
Q

Graph of the fraction of a population that shows a
specified response to increasing doses of a drug

A

Quantal dose response curve

90
Q

Median effective dose, 50% of the individuals
manifested the desired
therapeutic effect

91
Q

Median toxic dose, 50% of the individuals
manifested the toxic effects

92
Q

Median lethal dose

93
Q

> , <, =

TD50 _____ LD50

A

<
[LD50 is lethal while TD50 is toxic]

94
Q

Ratio of the TD50 (or LD50 ) to the ED50 determined
from the quantal dose-response curves

A

Therapeutic Index

95
Q

Represents an estimate of the safety of the drug

A

Therapeutic Index

96
Q

Dosage range between the minimum effective
therapeutic concentration or dose (MEC) and the minimum toxic concentration or dose (MTC)

A

Therapeutic window

97
Q

Maximal effect (Emax) an agonist can produce if the dose is taken to very high levels, measured with a graded dose-response curve but
not with quantal dose-response curve

A

Maximal Efficacy

98
Q

Concentration of drug that produces 50% of maximal
effect

99
Q

Is the amount of drug needed to produce a given effect

100
Q

Total number of receptor sites

101
Q

Equilibrium dissociation constant

102
Q

Transduction process between the occupancy of receptors
and production of specific effect

103
Q

Receptor Reserve

A

SPARE RECEPTORS

104
Q

Drugs with low binding affinity for receptors will be able to produce full response event at low concentration

A

SPARE RECEPTORS

105
Q

Non-regulatory molecules of the body to which drugs can attach to

A

INERT BINDING SITES

106
Q

Binds to the receptor and directly or indirectly bring about an effect

107
Q

Produces less than the full effect, even when it has saturated the receptors

A

PARTIAL AGONIST

108
Q

Binds but do not activate the receptors

A

ANTAGONIST

109
Q

Competes with agonist receptor - same binding site

A

COMPETITIVE ANTAGONISM

110
Q

Binds to the receptor reversibly without activating the effector system

A

COMPETITIVE ANTAGONISM

111
Q

produced by the competitive
antagonist depends on the concentration of antagonist

A

Degree of inhibition

112
Q

to a competitive antagonist depends on
the concentration of agonist that is competing for binding to the receptor.

A

Clinical response

113
Q

Binds with the receptor via covalent bonds

A

IRREVERSIBLE ANTAGONISM

114
Q

Does not depend on interaction with the agonist’s receptor

A

CHEMICAL ANTAGONISM

115
Q

Makes use of the regulatory pathway (separate regulatory pathway)

A

PHYSIOLOGIC ANTAGONISM

116
Q

Response gradually, have a diminishing response to a certain drug after an initial high level of response so usually this would be idiopathic

A

RECEPTOR DESENSITIZATION

117
Q

Cells use more than one signaling mechanism to respond to the drug

A

STRUCTURE ACTIVITY RELATIONSHIP

118
Q

those wherein 50% of the test population would already manifest with the therapeutic effect

A

ED50 or the median effective

119
Q

so wherein this is the dose at which 50% or majority of the test population would already manifest the toxic effect

A

TD50 or the Median toxic dose

120
Q

is done in test animals

A

LD50 or the lethal dose

121
Q

Relates the dose of a drug required to produce a desired effect to that which produces an undesired effect

A

THERAPEUTIC INDEX

122
Q

Dosage range between the minimum effective therapeutic concentration or dose (MEC) and the minimum toxic concentration or dose (MTC)

A

THERAPEUTIC WINDOW

123
Q

Not commonly observed among patients

A

Idiosyncratic Response

124
Q

Intensity of the drug is decreased compared with the effect seen in normal reactions

A

Hyporeactive Response

125
Q

Intensity of the drug is increased or exaggerated compared with the effect seen in normal reactions

A

Hyperreactive Response

126
Q

Decreased sensitivity acquired as a result of frequent exposure (several doses) to the drug

127
Q

Tolerance develops after a few doses

A

Tachyphylaxis

128
Q

Give the drug that really acts on the disease of the patient

A

CLINICAL SELECTIVITY

129
Q

correct receptor on the
intended tissue

A

Beneficial

130
Q

same receptor on the wrong
tissue

131
Q

Low doses for prevention of blood clots

[MT 6314] - 1st Shifting (23 decks)

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