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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
Q

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


A

True

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26
Q

KD drug amount (</>) EC50 with spare receptors

A

KD drug amount > EC50 with spare receptors

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27
Q

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


A

True

28
Q

T/F Spare receptors cant compare concentration for 50% of maximal effect (EC50
with concentration for 50% maximal binding (Kd)

A

False, it can compare

29
Q

T/F Actual number of receptors may exceed the number of
effectors available


A

True

30
Q

Binding with these molecules will result to no detectable change/response in the function of the biologic system

A

Inert Binding Sites

31
Q

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


A

Inert Binding Sites

32
Q

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


A

Agonist

33
Q

bind to receptor and bring full activation


A

Full agonist

34
Q

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


A

Partial Agonist

35
Q

Acts as an inhibitor in the presence of a full agonist


A

Partial Agonist

36
Q

Binds but do not activate the receptors

A

Antagonist

37
Q

Blocks or competes with agonist
- whether full or partial agonist

A

Antagonist

38
Q

Type of Agonist

Competes with agonist receptor - same binding site

A

Competitive Antagonist

39
Q

Type of Antagonist

Binds to the receptor reversibly without activating the effector system


A

Competitive Antagonist

40
Q

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


A

True

41
Q

Effects of competitive antagonist can be overcomed by (increasing/decreasing) agonist

A

increasing

42
Q

Type of antagonist

Same maximal effect is reached


A

Competitive Antagonist

43
Q

T/F Degree of inhibition produced by the competitive
antagonist depends on the concentration of antagonist

A

True

44
Q

T/F Clinical response to a competitive antagonist does not depend on
the concentration of agonist that is competing for binding
to the receptor.

A

False, it depends on the concerntration of the agonist

45
Q

Type of Antagonist

Binds with the receptor via covalent bonds


A

Irreversible Antagonist

46
Q

Type of Antagonist

Receptor is not available to bind the agonist


A

Irreversible Antagonist

47
Q

Type of Antagonist

Duration of action is relatively independent 


A

Irreversible Antagonist

48
Q

Type of Antagonist

phenoxybenzamine binding with alpha receptors

A

Irreversible Antagonist

49
Q

T/F With an irreversible antagonist, Emax will not be reached, no increase in median effective dose unless there are special receptors

A

True

50
Q

T/F With an irreversible antagonist, there is an increase in median dose (ED50) when there are spare receptors

A

True

51
Q

Type of Antagonist

Does not depend on interaction with the agonist’s receptor

A

Chemical Antagonist

52
Q

Type of antagonism that do not involve a receptor at all

A

Chemical Antagonist

53
Q

Type of antagonist

Protamine counteracts the effect of heparin

A

Chemical Antagonist

54
Q

Type of antagonist

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

A

Chemical Antagonist

55
Q

Type of antagonist

Makes use of the regulatory pathway (separate regulatory pathway)

A

Physiologic Antagonist

56
Q

Type of Antagonist

Effects that are less specific and less easy to control

A

Physiologic Antagonist

57
Q

Type of Antagonist

Glucocorticoids and Histamine

A

Physiologic Antagonist

58
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

59
Q

T/F During receptor desensitization the reason for its effect is still unknown.

A

True

60
Q

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

A

Structure Activity Relationship

61
Q

↑ competitive antagonist, _____ agonist concentration

A

↑ agonist concentration

62
Q

↑ EC50 =_____
drug concentration

A

↑ drug concentration

63
Q

↑ EC50, ↑
drug concentration = ___ potency, ____ affinity

A

↓ potency, ↓ affinity

64
Q

↑ noncompetitive antagonist = ___ Emax (efficacy)

A

↓ Emax

65
Q

T/F With spare receptors, Emax (maximal effect) is already achieved even without reaching the Bmax (all receptors).

A

True

2S PC & TC (17 decks)

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