[3] OLD Chapter 2 Pharmacodynamics Flashcards
(132 cards)
1
Q
Actions/ effects of the drug on the body
A
Pharmacodynamics
2
Q
Specific molecules in a biologic system with which drugs interact to produce changes in the function of the system
A
Receptors
3
Q
Determine the quantitative relations between dose or concentration of drug and pharmacologic effects
A
Receptors
4
Q
Receptors: _______ in choosing a drug molecule to bind to avoid constant activation by promiscuous binding of many different molecules
A
Selective
5
Q
Receptors: Selective in _______ characteristics (respond to proper chemical signals and not to meaningless ones)
A
ligand-binding
6
Q
Receptors mediate the actions of both pharmacologic _____ and ________
A
agonist and antagonist
7
Q
Specific binding region of the macromolecule
A
Receptor Site
8
Q
High and selective affinity to the drug molecule
A
Receptor Site
9
Q
Interaction between the drug and the receptor is the fundamental event that initiates the action of the drug
A
Receptor Site
10
Q
What are the 4 Classification of Receptors
A
- Regulatory proteins
- Enzymes
- Transport proteins
- Structural protein
11
Q
Classification of receptors:
Subserve specific physiologic functions
A
Regulatory proteins
12
Q
Classification of receptors:
Catalyzes/facilitates metabolic processes
A
Enzymes
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
14
Q
Classification of receptors:
Cytoskeleton of framework, cellular anatomy
A
Structural proteins
15
Q
What is the best characterized drug receptor
A
Regulatory proteins
[they produce overt observable effects]
16
Q
Inhibited (or less commonly, activates) by binding a drug
A
Enzymes
17
Q
The membrane receptor for digitalis
A
Transport proteins
18
Q
This is the receptor for colchine, an anti-inflammatory drug used for gout
A
Structural proteins
19
Q
Molecules that translate the drug-receptor interaction into a change in cellular activity
A
Effector
20
Q
A single molecule may incorporate both the drug binding site and the effector mechanism
A
Effector
21
Q
Crossing the plasma membrane and acts on intracellular receptors
A
Lipid soluble drug
22
Q
Intracellular enzymatic activity is regulated by a ligand that binds to the proteins extracellular domain
A
Transmembrane receptor protein
23
Q
______ binds and stimulates a protein tyrosine kinase
A
Transmembrane receptor
24
Q
Regulates the opening of the ion channel
A
Ligand-gated transmembrane ion channel
25
Transmembrane receptor is coupled with an effector enzyme by _____ which modulates production of an intracellular second messenger
G protein
26
What is the first messenger
Drug
27
G proteins and their receptors and effects:
Gs: ____ Adenylyl cyclase -> _____ cAMP
increase , increase
28
G proteins and their receptors and effects:
Gi1, Gi2, Gi3: ____ Adenylyl cyclase -> _____ cAMP
decrease, decrease
29
G proteins and their receptors and effects:
Golf: ____ Adenylyl cyclase -> _____ cAMP
increase , increase
30
G proteins and their receptors and effects:
Go: ____ Adenylyl cyclase -> _____ cAMP
Not clear
31
G proteins and their receptors and effects:
Gq: ____ Phospholipase C -> _____ IP3 diacylglycerol cytoplasmic CA2+
increase , increase
32
G proteins and their receptors and effects:
Gt1, Gt2: ____ cGMP phosphodiesterase -> _____ cGMP phototransduction
Increase, decrease
33
What is the secondary messenger producing phototransduction
cGMP
34
What G protein is inversely proportional
Gt1 and Gt2
35
Acting as an intracellular second messenger that mediates hormonal responses
cAMP
[Cyclic adenosine monophosphate]
36
In cAMP, conservation of water by the kidneys mediated by ______
vasopressin
37
When substrate is added to metabolic processes, the reaction is pushed _____ to create products
forward
38
What is the crucial step in calcium and phosphoinositide
Stimulation of membrane enzyme phospholipase C
39
Few signaling roles in a few cell types like the intestinal mucosa and vascular smooth muscle cells
cGMP
[Cyclic guanosine monophosphate]
40
Response of a particular receptor-effector system is measured against increasing concentration of a drug
Graded - dose response curve
41
Quantifies the response of the drug to each specific dose
Graded - dose response curve
42
On the x-axis, we have the [1]_____
On the y-axis, we have the [2]______
[1] Dose
[2] Response
43
In a linear scale, double double are usually seen in pharmacology experiments because of
Sigmoidal curve
44
Based on the Sigmoidal curve, as you increase the dose, the response will ______ up to a certain level, known as the Emax
increase
45
The _____ the EC50, the greater the potency of the drug
smaller
46
True or False:
Low EC50 = More potency of the drug
True
47
Maximal response that can be produced by a drug
Emax
48
The basis for characterization for full and partial agonists
Emax
49
Concentration of drug that produces 50% of maximal effect
EC50
50
The basis for drug potency
EC50
51
True or False:
EC50 is inversely proportional
True
52
Total number of receptor sites
Bmax
53
All receptors have been occupied
Bmax
54
The presumption is that all receptors are occupied
Emax
55
The total receptor
occupancy
Bmax
56
True or False:
KD = equilibrium dissociation constant
True
57
It is a measure of drug affinity
KD
58
True or False:
Higher affinity = High KD
False
Low KD [correct answer]
59
True or False
Smaller KD = greater affinity of drug to receptor
True
60
True or False:
KD is inversely proportional or reciprocal fashion
True
61
Represents the concentration of free drug at which half-maximal binding is observed
KD
62
Transduction process between the occupancy of receptors and production of specific effect
Coupling
63
Highly efficient _______ can be elicited by a full
agonist and spare receptors.
Coupling
64
“downstream” biochemical events that transduce receptor occupancy into cellular response
Coupling
65
True or False
In Coupling, Full agonist tend to shift the conformational equilibrium of receptors more strongly than partial agonist
True
66
Also known as receptor reserve
Spare receptors
67
Drugs with low binding affinity for receptors will be able to produce full response even at low
concentration
Spare receptors
68
Concentration of 50% EC50 and Concentration of 50% KD
KD____ EC50
>
[less than]
69
May be demonstrated by using irreversible antagonists to prevent binding of agonist to a proportion of available receptors
Spare Receptors
70
Non regulatory, binding with these molecules will result to no detectable change in the function of the biologic system
Inert binding sites
71
Buffers the concentration of the drug
Inert binding sites
72
Binds to the receptor and directly or indirectly bring about an effect
Agonist
73
Full activation of the effector system
Agonist
74
Produces less than the full effect, even when
it has saturated the receptors
Partial Agonist
75
Acts as an inhibitor in the presence of a full agonist
Partial Agonist
76
Binds but do not activate the receptors and blocks or competes with agonist
Antagonist
77
What are the 4 Classification of Antagonist
1. Competitive Antagonist
2. Irreversible Antagonist
3. Chemical Antagonist
4. Physiologic Antagonist
78
Some antagonists exhibit inverse agonist activity
because they also reduce receptor activity below
basal levels observed in the absence of any
agonist at all
Irreversible Antagonist
79
High antagonist concentrations prevent the response almost completely
Competitive Antagonist
80
Irreversible antagonist bind with the receptor via _____
Covalent bonds
81
Antagonist that are more dependent on the rate of turnover of receptors
Irreversible Antagonist
82
Antagonist that does not depend on interaction with the agonist’s receptor
Chemical Antagonist
83
Drug that interacts directly with the drug being antagonized to remove it or to prevent it from reaching its target
Chemical Antagonist
84
Antagonist that makes use of the regulatory pathway
Physiologic Antagonist
85
Binds to a different receptor producing an effect opposite to that produced by the drug it is antagonizing
Physiologic Antagonist
86
_______ catabolic effects of increase in sugar is physiologically
opposed by insulin
Glucocorticoids
87
Response gradually diminishes even if the drug is still there (after reaching an initial high level of
response)
Receptor Desensitization
88
Cells use more than one signaling mechanism to
respond to the drug
Structure Activity Relationship
89
Graph of the fraction of a population that shows a
specified response to increasing doses of a drug
Quantal dose response curve
90
Median effective dose, 50% of the individuals
manifested the desired
therapeutic effect
ED50
91
Median toxic dose, 50% of the individuals
manifested the toxic effects
TD50
92
Median lethal dose
LD50
93
>, <, =
TD50 _____ LD50
<
[LD50 is lethal while TD50 is toxic]
94
Ratio of the TD50 (or LD50 ) to the ED50 determined
from the quantal dose-response curves
Therapeutic Index
95
Represents an estimate of the safety of the drug
Therapeutic Index
96
Dosage range between the minimum effective
therapeutic concentration or dose (MEC) and the minimum toxic concentration or dose (MTC)
Therapeutic window
97
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
Maximal Efficacy
98
Concentration of drug that produces 50% of maximal
effect
EC50
99
Is the amount of drug needed to produce a given effect
POTENCY
100
Total number of receptor sites
Bmax
101
Equilibrium dissociation constant
KD
102
Transduction process between the occupancy of receptors
and production of specific effect
COUPLING
103
Receptor Reserve
SPARE RECEPTORS
104
Drugs with low binding affinity for receptors will be able to produce full response event at low concentration
SPARE RECEPTORS
105
Non-regulatory molecules of the body to which drugs can attach to
INERT BINDING SITES
106
Binds to the receptor and directly or indirectly bring about an effect
AGONIST
107
Produces less than the full effect, even when it has saturated the receptors
PARTIAL AGONIST
108
Binds but do not activate the receptors
ANTAGONIST
109
Competes with agonist receptor - same binding site
COMPETITIVE ANTAGONISM
110
Binds to the receptor reversibly without activating the effector system
COMPETITIVE ANTAGONISM
111
produced by the competitive
antagonist depends on the concentration of antagonist
Degree of inhibition
112
to a competitive antagonist depends on
the concentration of agonist that is competing for binding to the receptor.
Clinical response
113
Binds with the receptor via covalent bonds
IRREVERSIBLE ANTAGONISM
114
Does not depend on interaction with the agonist's receptor
CHEMICAL ANTAGONISM
115
Makes use of the regulatory pathway (separate regulatory pathway)
PHYSIOLOGIC ANTAGONISM
116
Response gradually, have a diminishing response to a certain drug after an initial high level of response so usually this would be idiopathic
RECEPTOR DESENSITIZATION
117
Cells use more than one signaling mechanism to respond to the drug
STRUCTURE ACTIVITY RELATIONSHIP
118
those wherein 50% of the test population would already manifest with the therapeutic effect
ED50 or the median effective
119
so wherein this is the dose at which 50% or majority of the test population would already manifest the toxic effect
TD50 or the Median toxic dose
120
is done in test animals
LD50 or the lethal dose
121
Relates the dose of a drug required to produce a desired effect to that which produces an undesired effect
THERAPEUTIC INDEX
122
Dosage range between the minimum effective therapeutic concentration or dose (MEC) and the minimum toxic concentration or dose (MTC)
THERAPEUTIC WINDOW
123
Not commonly observed among patients
Idiosyncratic Response
124
Intensity of the drug is decreased compared with the effect seen in normal reactions
Hyporeactive Response
125
Intensity of the drug is increased or exaggerated compared with the effect seen in normal reactions
Hyperreactive Response
126
Decreased sensitivity acquired as a result of frequent exposure (several doses) to the drug
Tolerance
127
Tolerance develops after a few doses
Tachyphylaxis
128
Give the drug that really acts on the disease of the patient
CLINICAL SELECTIVITY
129
correct receptor on the
intended tissue
Beneficial
130
same receptor on the wrong
tissue
Toxic
131
Low doses for prevention of blood clots
Heparin
132
