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2S PC & TC > U2.2 DRG CONCENTRATION & RESPONSE : GDRC > Flashcards

U2.2 DRG CONCENTRATION & RESPONSE : GDRC Flashcards

1
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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2
Q

Graph of the response versus the drug dose

A

Graded-Dose Response Curve

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3
Q

derived from Graded Dose-Response Curve

A

Efficacy (Emax) and potency (EC50)

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4
Q

↓ EC50, ___ potency

A

↑ potency

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5
Q

Maximal response that can be produced by a drug

A

MAXIMAL EFFICACY (Emax)

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6
Q

T/F In Emax all receptors are occupied

A

T

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7
Q

Measured with a graded dose-response curve but not with quantal dose-response curve

A

Emax

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8
Q

Concentration of drug that produces 50% of maximal effect

A

EC50

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9
Q

drug dose will be half saturate the receptors and achieve for half the efficacy (at equilibrium)

A

EC50

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10
Q

amount of drug needed to produce a given effect

A

Potency

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11
Q

Total number of receptor sites

A

Bmax

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12
Q

All receptors have been occupied

A

Bmax

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13
Q

Equilibrium dissociation constant

A

KD

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14
Q

Concentration of the drug required to bind 50% of the
receptors

A

KD

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15
Q

Difference of EC50 and KD

A

EC50 - response
KD - receptors

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16
Q

___ KD, ↑ drug affinity to receptor / binding affinity

A

↓ KD

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17
Q

___ affinity drugs = ↓ binding affinity

A

↓ affinity drugs

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18
Q

Paramters:

Emax
EC50
KD

A

Emax - efficacy
EC50 - potency
KD - affinity

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19
Q

Agonist response in the absence of antagonist = ____ potency

A

↑ drug potency

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20
Q

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

A

COUPLING

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21
Q

Highly effective coupling can be elicited by a full agonist and spare receptors


A

COUPLING

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22
Q

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


A

Spare Receptors

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23
Q

T/F Spare receptors are qualitatively different from non-spare receptors, not hidden or unavailable


A

False, not qualitatively different (same receptor pool)

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24
Q

T/F Spare Receptrs are temporal in character, when occupied, they can be
coupled to respond, there is still effect


A

True

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25
T/F Drugs with low binding affinity for receptors will be able to produce full response event at low concentration

True
26
KD drug amount () EC50 with spare receptors
KD drug amount > EC50 with spare receptors
27
T/F Drugs with low binding affinity for receptors will be able to produce full response event at low concentration

True
28
T/F Spare receptors cant compare concentration for 50% of maximal effect (EC50 with concentration for 50% maximal binding (Kd)
False, it can compare
29
T/F Actual number of receptors may exceed the number of effectors available

True
30
Binding with these molecules will result to no detectable change/response in the function of the biologic system
Inert Binding Sites
31
Non-regulatory molecules of the body to which drugs can attach to

Inert Binding Sites
32
Binds to the receptor and directly or indirectly bring about an effect

Agonist
33
bind to receptor and bring full activation

Full agonist
34
Produces less than the full effect, even when it has saturated the receptors

Partial Agonist
35
Acts as an inhibitor in the presence of a full agonist

Partial Agonist
36
Binds but do not activate the receptors
Antagonist
37
Blocks or competes with agonist
- whether full or partial agonist
Antagonist
38
Type of Agonist Competes with agonist receptor - same binding site
Competitive Antagonist
39
Type of Antagonist Binds to the receptor reversibly without activating the effector system

Competitive Antagonist
40
T/F In competitive antagonist, antagonist increases the agonist concentration needed for a given degree of response

True
41
Effects of competitive antagonist can be overcomed by (increasing/decreasing) agonist
increasing
42
Type of antagonist Same maximal effect is reached

Competitive Antagonist
43
T/F Degree of inhibition produced by the competitive antagonist depends on the concentration of antagonist
True
44
T/F Clinical response to a competitive antagonist does not depend on the concentration of agonist that is competing for binding to the receptor.
False, it depends on the concerntration of the agonist
45
Type of Antagonist Binds with the receptor via covalent bonds

Irreversible Antagonist
46
Type of Antagonist Receptor is not available to bind the agonist

Irreversible Antagonist
47
Type of Antagonist Duration of action is relatively independent 

Irreversible Antagonist
48
Type of Antagonist phenoxybenzamine binding with alpha receptors
Irreversible Antagonist
49
T/F With an irreversible antagonist, Emax will not be reached, no increase in median effective dose unless there are special receptors
True
50
T/F With an irreversible antagonist, there is an increase in median dose (ED50) when there are spare receptors
True
51
Type of Antagonist Does not depend on interaction with the agonist's receptor
Chemical Antagonist
52
Type of antagonism that do not involve a receptor at all
Chemical Antagonist
53
Type of antagonist Protamine counteracts the effect of heparin
Chemical Antagonist
54
Type of antagonist Drug that interacts directly with the drug being antagonized to remove it or to prevent it from reaching its target
Chemical Antagonist
55
Type of antagonist Makes use of the regulatory pathway (separate regulatory pathway)
Physiologic Antagonist
56
Type of Antagonist Effects that are less specific and less easy to control
Physiologic Antagonist
57
Type of Antagonist Glucocorticoids and Histamine
Physiologic Antagonist
58
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
59
T/F During receptor desensitization the reason for its effect is still unknown.
True
60
Cells use more than one signaling mechanism to respond to the drug
Structure Activity Relationship
61
↑ competitive antagonist, _____ agonist concentration
↑ agonist concentration
62
↑ EC50 =_____ drug concentration
↑ drug concentration
63
↑ EC50, ↑ drug concentration = ___ potency, ____ affinity
↓ potency, ↓ affinity
64
↑ noncompetitive antagonist = ___ Emax (efficacy)
↓ Emax
65
T/F With spare receptors, Emax (maximal effect) is already achieved even without reaching the Bmax (all receptors).
True

2S PC & TC (17 decks)

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