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[MT 6314] - 1st Shifting > [3] NEW Pharmacodynamics > Flashcards

[3] NEW Pharmacodynamics Flashcards

1
Q

Actions/effects of drugs on the body

A

Pharmacodynamics

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2
Q

Specific molecules 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 are selective in _______ characteristics

A

Ligand-binging

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5
Q

Receptors mediate actions of both pharmacologic _____ and ______

A

Agonist and Antagonist

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6
Q

Specific binding region of the macromolecule

A

Receptor Site/ Recognition Site

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7
Q

High and selective affinity to the drug molecule

A

Receptor Site/ Recognition Site

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8
Q

What are the 4 Classification of Receptors

A
  1. Regulatory proteins
  2. Enzymes
  3. Transport proteins
  4. Structural poteins
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9
Q

Classification of Receptors:
Subserve specific physiologic functions

A

Regulatory Proteins

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10
Q

Classification of Receptors:
Catalyzes/facilitates metabolic processes

A

Enzymes

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11
Q

Classification of Receptors:
In cell membrane, the raw material of our metabolism is needed to be transported into the cell because we metabolize inside the cell

A

Transport Proteins

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12
Q

Classification of Receptors:
Cytoskeleton of framework - Cellular Anatomy

A

Structural Proteins

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13
Q

Classification of Receptors:
Best-characterized drug receptors

A

Regulatory Proteins

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14
Q

Classification of Receptors:
Mediates the action of endogenous chemical signals like neurotransmitters, autocoids, and hormones

A

Regulatory Proteins

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15
Q

Classification of Receptors:
Inhibited or activated by binding a drug

A

Enzymes

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16
Q

Classification of Receptors:
Membrane receptors for digitalis

A

Transport Proteins

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17
Q

Classification of Receptors:
Micro and macro anatomic, the receptor for colchicine, an anti-inflammatory drug used for gout

A

Structural Proteins

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18
Q

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

A

Effector

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19
Q

True or False:
A single molecule may incorporate both the drug binding site and the effector mechanism

A

True

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20
Q

What are the 5 Basic Transmembrane Signaling Mechanism

A
  1. Lipid soluble drug
  2. Transmembrane receptor protein
  3. Stimulates Protein tyrosine kinase
  4. Ligand-gated transmembrane ion channel
  5. Transmembrane receptor is coupled with an effector enzyme by G protein
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21
Q

Modulates production of an intracellular second messenger

A

G protein

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22
Q

What is the 1st messenger

A

Drug

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23
Q

Give me the G protein of the ff:
high adenylyl cyclase -> high cAMP

A

GS and Golf (Olfactory epithelium)

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24
Q

Give me the G protein of the ff:
low adenylyl cyclase -> low cAMP

A

Gi1, Gi2, Gi3

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25
Q

Give me the G protein of the ff:
high phospholipase C -> high IP3 diacylglycerol, cytoplasmic Ca2+

A

Gq

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26
Q

Give me the G protein of the ff:
high cGMP phosphodiesterase -> low cGMP (phototransduction)

A

Gt1, Gt2

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27
Q

Give me the G protein of the ff:
Opens cardia K+ channels -> low heart rate

A

Gi1, Gi2, Gi3

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28
Q

What are the 3 Intracellular 2nd messengers

A
  1. cAMP or Cyclic Adenosine Monophosphate
  2. Calcium and phosphoinositides
  3. cGMP or Cyclic Guanosine Monophosphate
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29
Q

2nd messenger that mediates hormonal responses

A

cAMP or Cyclic Adenosine Monophosphate

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30
Q

2nd messenger that mobilizes stored energy of carbohydrates in the liver

A

cAMP or Cyclic Adenosine Monophosphate

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31
Q

2nd messenger that conserves water by kidneys mediated by vasopressin

A

cAMP or Cyclic Adenosine Monophosphate

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32
Q

2nd messenger that bind to receptors linked G proteins while others bind to receptors tyrosine kinases

A

Calcium and phosphoinositides

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33
Q

In calcium and phosphoinositides, _______ produces an activated effect towards the production of the intended response of that receptor system

A

Calmodulin complex

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34
Q

2nd messenger has few signaling roles in a few cell types like intestinal mucosa and vascular smooth muscle cells

A

cGMP or Cyclic Guanosine Monophosphate

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35
Q

2nd messenger that causes relaxation of vascular smooth muscles by a kinase-mediated mechanism that results in dephosphorylation of myosin light chains

A

cGMP or Cyclic Guanosine Monophosphate

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36
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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37
Q

Quantifies the response of the drug to each specific dose

A

Graded Dose-Response Curve

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38
Q

On the Graph of the response versus the drug dose:
x-axis:_______
y-axis:_______

A

x-axis: dose
y-axis: response

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39
Q

True or False:
The smaller the EC50, the greater the potency of the drug

A

True

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40
Q

The maximal response that can be produced by a drug

A

Emax

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41
Q

The presumption is that all receptors are occupied

A

Emax

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42
Q

The basis of the characterization for full and partial agonist

A

Emax

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43
Q

Concentration of drug that produces 50% of the maximal effect

A

EC50

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44
Q

True or False:
EC50 and Potency are inversely proportional

A

True

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45
Q

The total number of receptor sites and all receptors have been occupied

A

Bmax

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46
Q

The total receptor occupancy

A

Bmax

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47
Q

Measure of the affinity of a drug for its binding site on the receptor

A

KD

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48
Q

Concentration drug REQUIRED to bind 50% of the receptors

A

KD

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49
Q

True or False:
Smaller KD = Greater affinity of drug-receptor

A

True

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50
Q

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

A

KD

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51
Q

Curve of Emax

A

Hyperbole

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52
Q

Curve of Bmax

A

Logarithmic Sigmoid Curve

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53
Q

Basis for drug potency

A

EC50

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54
Q

On the Graph of the agonist dose-response curve:
x-axis:_______
y-axis:_______

A

x-axis: agonist dose
y-axis: agonist effect

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55
Q

True or False:
On the agonist dose-response curve, the lower the curve the higher the concentration of the antagonist

A

True

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56
Q

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

A

Coupling

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57
Q

Elicated by a full agonist and spare receptors

A

Coupling

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58
Q

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

A

Coupling

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59
Q

Also known as receptor reserve

A

Spare Receptors

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60
Q

Maximal drug response is obtained at less than the maximal occupation of the receptors

A

Spare Receptors

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61
Q

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

A

Spare Receptors

62
Q

Compare the concentration of 50% maximal EFFECT (EC50) with concentration of 50% maximal BINDING (KD)

A

Spare Receptors

63
Q

Concentration of 50% maximal EFFECT

A

EC50

64
Q

concentration of 50% maximal BINDING

A

KD

65
Q

True or False:
KD > EC50 with spare receptors

A

True

66
Q

True or False:
The actual number of receptors may exceed the number of effectors available

A

True

67
Q

Non-regulatory molecules of the body

A

Inert Binding Sites

68
Q

Binding with these molecules will result in NO DETECTABLE CHANGE in the function of the biological system

A

Inert Binding Sites

69
Q

Also known to buffer the concentration of the drug

A

Inert Binding Sites

70
Q

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

A

Agonist

71
Q

Produces less than the full extent, even when it has SATURATED the receptors

A

Partial Agonist

72
Q

Acts as an inhibitor in the presence of a full agonist

A

Partial Agonist

73
Q

Binds but do not activate the receptors

A

Antagonist

74
Q

Blocks or competes with agonist

A

Antagonist

75
Q

What are the 4 Classification of Antagonists

A
  1. Competitive Antagonist
  2. Irreversible Antagonist
  3. Chemical Antagonist
  4. Physiologic Antagonist
76
Q

Inhibits and competes agonist receptor

A

Competitive Antagonist

77
Q

Bonds to the receptor REVERSIBLY without activating the effector system

A

Competitive Antagonist

78
Q

An antagonist that shifts to the right horizontally on the dose axis

A

Competitive Antagonist

79
Q

True or False:
In Competitive Antagonists, effects are overcome by adding more agonists

A

True

80
Q

True or False:
In Competitive Antagonists, increase the median effective dose (ED50)

A

True

81
Q

Therapeutic Implication of Competitive Antagonist:

The _________ produced by the competitive antagonist depends on the concentration of the ANTAGONIST

A

Degree of inhibition

82
Q

Therapeutic Implication of Competitive Antagonist:

The _________ to a competitive antagonist depends on the concentration of the AGONIST that is competing for binding to the receptor

A

Clinical response

83
Q

Binds with the receptor via Covalent Bonds

A

Irreversible Antagonist

84
Q

An antagonist that makes the receptor unable to bind the agonist

A

Irreversible Antagonist

85
Q

An antagonist dependent on the RATE OF TURNOVER of receptors

A

Irreversible Antagonist

86
Q

An antagonist that moves downward but has no shift of curve in the dose axis

A

Irreversible Antagonist

87
Q

An agonist that binds to a site on the receptor separate or different from the agonist binding site

A

Negative Allosteric Modulators

88
Q

Does not depend on interaction with the agonist’s receptor

A

Chemical Antagonism

89
Q

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

A

Chemical Antagonism

90
Q

Makes use of the regulatory pathway

A

Physiologic Antagonism

91
Q

An antagonist that has less specific effects and is less easy to control

A

Physiologic Antagonism

92
Q

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

A

Physiologic Antagonism

93
Q

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

A

Receptor Desensitization

94
Q

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

A

Structure-Activity Relationship

95
Q

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

A

Quantal Dose Response-Curve

96
Q

It forms sigmoid curve, has minimum dose required to produce a specific response that determines each member of the population

A

Quantal Dose Response-Curve

97
Q

The formula of Quantal Dose Response-Curve

A

TW = MTC -MEC

MEC - Minimum Effective Therapeutic Conc.
MTC - Minimum Toxic Conc.

98
Q

Formula for Estimate Therapeutic Index

A

LD50 / ED50

99
Q

Formula for Estimate Therapeutic Window

A

Minimum Toxic Concentration - Minimum Therapeutic Effective Dose/ Concentration

100
Q

Median effective dose

A

ED50

101
Q

50% manifested desired therapeutic effect

A

ED50

102
Q

Median toxic dose

A

TD50

103
Q

50% manifested toxic effects

A

TD50

104
Q

Median lethal dose

A

LD50

105
Q

Represents an estimate of the safety of the drug

A

Therapeutic Index

106
Q

Dosage ranges between the minimum effective therapeutic concentration or dose (MEC) and the minimum tox concentration or dose (MTC)

A

Therapeutic Window

107
Q

More clinically relevant index of safety

A

Therapeutic Window

108
Q

Maximal Effect, an agonist can produce if the dose is taken to very high levels

A

Maximal Efficacy (Emax)

109
Q

Determined mainly by the nature of receptors and its associated effectors

A

Maximal Efficacy (Emax)

110
Q

Maximal Efficacy (Emax) is measured with [1]________ and not with [2]_________

A

[1] Graded dose-response curve
[2] Quantal dose-response curve

111
Q

Amount of drug needed to produced given effect

A

Potency

112
Q

Potency: Graded dose-response curve, the used dose is ____

A

the dose is EC50 and 50% of the maximal effect

113
Q

Potency: Quantal dose-response curve, the used dose are_____

A

ED50, TD50, and LD50 variables in 50% of the population

114
Q

True or False:
With a graph of concentration and response, the lower the curve is the more potent it is. On the other hand, the higher it is the more greater the maximal efficacy the drug has

A

True

115
Q

Response to the drug is unknown or unusual

A

Idiosyncratic Response

116
Q

Intensity of the drug is decrease, and large dose of the drug is need to have an effect

A

Hyporeactive Response

117
Q

Intensity of the drug is increased or exaggerated

A

Hyperreactive Response

118
Q

Decreased sensitivity acquired as a result of exposure to the drug

A

Tolerance

119
Q

Tolerance develops after a few doses

A

Tachphylaxis

120
Q

Reason for Varied Drug Responses:
- decrease drug absorption
- inhibited drug distribution
- increased elimination of the drug

A

Alteration in conc. of the drug

121
Q

Reason for Varied Drug Responses:
- occurs when foreign or exogenous ligands are introduced

A

Variation in the con. of the endogenous ligands (especially for antagonistic patterns)

122
Q

Reason for Varied Drug Responses:
- down-regulation
- up-regulation

A

Alteration in number or function of receptors

123
Q

Reason for Varied Drug Responses:
- drug taken for a long time then abruptly discontinued

A

Overshoot phenomenon or Rebound hypertension

124
Q

Give the drug that acts on the disease of the patient, no drug causes a single specific effect only, drugs are selective but never specific

A

Clinical Selectivity

125
Q

What to do to avoid toxic effects

A
  • Give low doses
  • Carefully monitor the patient
  • employ ancillary procedures
  • use a safer drug
126
Q

True or False:
high Emax = high efficacy

A

True

127
Q

True or False:
low EC50 = high potency

A

True

128
Q

Mechanism of Pharmacodynamics

A

Additive
Synergism
Potentiation
Antagonism

129
Q

Mechanism of Pharmacokinetics

A

Absorption
Distribution
Metabolism
Excretion

130
Q

What are the 5 Patient Factors

A
  1. Intrinsic drug clearance
  2. Genetics
  3. Gender
  4. Concurrent diseases
  5. Diet
131
Q

What are the 4 Drug Specific Factors

A
  1. Dose
  2. Route of Administration
  3. Drug Formulation
  4. Sequence of Drug Administration
132
Q

What are the two types of drug interaction mechanism

A

Altered Absorption
Altered Metabolism

133
Q

Cholestyramine inhibits the effect of digoxin when combined with it

A

Altered Absorption

134
Q

What are the 6 Pharmacokinetics Mechanism

A
  1. Gastrointestinal Absorption
  2. Altered Drug Distribution
  3. Altered Excretion
  4. Drug Distribution
  5. Metabolism of Drugs
  6. Renal Excretion
135
Q

Pharmacokinetics Mechanism:
It binds or chelates, alters gastric pH, alters gastrointestinal motility, and affects transport proteins

A

Gastrointestinal Absorption

136
Q

Pharmacokinetics Mechanism:
Competition for plasma protein binding, displacement from tissue binding sites, and alterations in local tissue barriers

A

Altered Drug Distribution and Drug Distribution

137
Q

Pharmacokinetics Mechanism:
Probenecid inhibits the secretion of acids

Penicillin inhibits the excretion of probenecid

A

Altered Excretion

138
Q

Pharmacokinetics Mechanism:
Induced or inhibited by concurrent therapy

A

Metabolism of Drugs

139
Q

Pharmacokinetics Mechanism:
Are weak acids or weak bases may be influenced by other drugs that affect urinary pH

A

Penal Excretion

140
Q

What are the Pharmacodynamic Mechanisms

A
  1. Additive
  2. Synergistic
  3. Potentiation
  4. Antagonism
141
Q

The response elicited by combined drugs is equal to the combined response of the individual drugs

[ 1+1=2 ]

A

Additive
[same receptor = additive effects]

142
Q

The response elicited by combined drugs is greater than the combined responses of each individual

[ 1+1=3 ]

A

Synergist

143
Q

In synergist, ____ removes the cell wall

A

Penicillin G

144
Q

In synergist, ____ inhibits the production of protein

A

Gentamicin

145
Q

Drug which has no effect enhances the effect of the second drug

[ 0+1=2 ]

A

Potentation

146
Q

Drug inhibits the effect of another drug

[ 1+1=0 ]

A

Antagonism

147
Q

Pharmacodynamics Mechanism:

Keyword: equal

A

Additive

148
Q

Pharmacodynamics Mechanism:

Keyword: greater >

A

Synergism

149
Q

Pharmacodynamics Mechanism:

Keyword: enhances

A

Potentiation

150
Q

Pharmacodynamics Mechanism:

Keyword: inhibits

A

Antagonism

151
Q

Selectivity can be measured by comparing:

A

Binding affinities and ED50

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

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