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Neuro 2-Pharmacology week > Pharmacodynamics-Konorev > Flashcards

Pharmacodynamics-Konorev Flashcards

1
Q

Most drugs bind to receptors via non-covalent bonds and are reversible. List the strongest to weakest types of non-covalent bonds:

A

Ionic –> hydrogen –> hydrophobic interactions –> van der waals

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2
Q

In a dose-response curve, what is on the y-axis and x-axis?

A

Y=response

X=drug dose

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3
Q

What type of curve do you get when you plot drug dose arithmetically on the x-axis vs drug effect on the y-axis?

A

Hyperbolic

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4
Q

In a dose-response curve, it is more common for a concentration-effect curve to be presented by plotting __ on the x-axis and __ on the y-axis

A

X-axis-Log drug dose

Y-axis-% maximum response

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5
Q

When plotting log drug dose (x axis) vs % maximum response (y axis), you get a __ curve

A

Sigmoidal

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6
Q

In the dose-response curve, the maximal effect that can be produced by the drug is called the __

A

Emax

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7
Q

In the dose response curve, the __ is the dose of drug that produces half of its max effect

A

ED50 (Effective Dose 50)

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8
Q

The ___ of a drug for a receptor describes how readily and tightly that drug binds to its receptor

A

Affinity

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9
Q

A drug that has high affinity has good drug-receptor interaction. Do you need more or less drug to produce a response?

A

Less drug needed to produce a response

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10
Q

A drug that has low affinity has poor drug-receptor interaction. Do you need more or less drug to produce a response?

A

More drug needed to produce a response

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11
Q

Describe the affinity of a drug for a receptor with a low Kd

A

The lower the Kd, the HIGHER THE AFFINITY of a drug for a receptor

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12
Q

Describe the affinity of a drug for a receptor with a high Kd

A

The higher the Kd, the lower the affinity of a drug for a receptor

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13
Q

__ is a property of a drug determined by its affinities at various binding sites.

A

Selectivity

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14
Q

Drug selectivity is measured by comparing affinities of a drug to different receptors or by comparing __ for different effects of a drug

A

ED50s

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15
Q

A more selective drug would affect __ targets over a specific concentration range (therapeutic range)

A

Fewer

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16
Q

___ describes the ability of a drug to change a receptor function and produce a physiological response upon binding to a receptor

A

Intrinsic activity

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17
Q

__ bind to the receptor and stabilize it in a particular conformation (usually, the active conformation), producing a physiological response.

A

Agonists

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18
Q

___ bind to the receptor but do not change its function. However, it prevents activation of the receptor in the presence of an agonist.

A

Antagonists

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19
Q

A ___ has intrinsic activity

A ___ does not have intrinsic activity

A

Agonist

Antagonist

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20
Q

___ fully activate receptors, produce a max pharmacological effect when all receptors are occupied, and have maximal intrinsic activity

A

Full agonists

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21
Q

___ do not fully activate the receptor upon binding, produce a sub-maximal pharmacological effect when all receptors are occupied and its intrinsic efficacy varies depending on drug, but is always submaximal

A

Partial agonists

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22
Q

___ decrease receptor signaling, decrease response at receptors with a significant level of constitutive receptor activity. Its intrinsic activity is present and related to the inhibition of receptor function

A

Inverse agonists

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23
Q

__ do not change the function of the receptor upon binding, does not have pharmacological effect in the absence of an agonist, and has no intrinsic efficacy

A

Antagonists

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24
Q

___ produce max pharmacological effects at full receptor occupancy

A

Full agonists

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25
Q

___ produce sub-maximal pharmacological effects at full receptor occupancy

A

Partial agonists

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26
Q

Compare Emax between full agonists and partial agonists

A

Emax is lower in partial agonists than in full agonists

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27
Q

__ produce an effect opposite to a full or partial agonist

A

Inverse agonists

28
Q

___ antagonism-action at the same receptor as endogenous ligands or agonist drugs

A

Pharmacologic (receptor)

29
Q

Chemical antagonism is when a chemical antagonist makes the other drug ___

A

Unavailable

30
Q

__ antagonism occurs between endogenous pathways regulated by different receptors

A

Physiologic

31
Q

Competitive antagonists compete with ___ for binding of the receptor. They can be displaced from the receptor by other drugs (effects are surmountable)

A

Endogenous chemicals or agonist drugs

32
Q

In ___ antagonists, receptor inactivation is not surmountable

A

Non-competitive

33
Q

Irreversible antagonists irreversibly bind to and occlude the agonist site on the receptor by forming ___ bonds

A

Covalent

34
Q

__ bind to a site other than the agonist site to prevent or reduce agonist binding or activation of the receptor

A

Allosteric antagonists

35
Q

Describe EC50 and Emax in competitive antagonism

A

EC50 increases, Emax does not change

36
Q

Describe EC50 and Emax in noncompetitive antagonism

A

Emax decreases, EC50 does not change

37
Q

List the nonreceptor antagonists

A

Chemical and physiologic antagonists

38
Q

Activation of mu opioid receptors by opioid analgesics (pain killers) such as morphine, codeine, and meperidine are examples of ___

A

Full agonists

Beneficial

39
Q

___ block the actions of endogenous ligands at receptors. An example would be the blockade of alpha1 adrenoceptors receptors by the antihypertensive drug Prazosin.

A

Antagonists, partial and inverse agonists

Beneficial

40
Q

___ selective drugs have less side effects

A

Highly

41
Q

__ selectivity leads to the increased incidence of side effects

A

Lower

42
Q

__ describes the amount of drug required to produce a specific pharmacological effect

A

Potency

43
Q

Drugs with __ affinities for a receptor (i.e., drugs with a lower Kd) tend to be more potent

A

Higher

44
Q

__ describes the maximal pharmacological effect that a drug can produce

A

Efficacy

45
Q

Efficacy is related to the total # of receptors available to bind a drug, also known as the ___

A

Bmax

46
Q

Drugs with a ___ Bmax tend to have higher efficacy

A

Higher

47
Q

___ describes the amount of a drug required to produce a specific effect

A

Potency

48
Q

Potency is represented by the ED50. The ___ the ED50, the more potent the drug

A

Lower

49
Q

___ determines the drug dose that will be used clinically

A

Potency

50
Q

___ describes the max effect that a drug can produce

A

Efficacy

51
Q

Efficacy is represented by the ___

A

Emax

52
Q

The __ the Emax, the more efficacious the drug

A

Greater

53
Q

__ determines clinical effectiveness

A

Efficacy

54
Q

___ answers the question of “How much?”, the magnitude of a response varies continuously, and typically represents the mean value within a population or a single subject

A

Graded response

55
Q

___ is all or none; yes-no; “binary” responses. It answers the questions of “does the response occur or not?” Or “how many?”. It requires a pre-defined response (e.g., death, falling asleep, 10% decrease in BP)

A

Quantal response

56
Q

___ is used to determine the frequency of (i.e., the number of individuals showing) a response within a large population

A

Quantal response

57
Q

___ curves relate dose to the magnitude of a drugs effect on a continuous scale (i.e., how much)

A

Graded dose response

58
Q

___ curves relate dose of a drug to the frequncy of a response within a general population (i.e., in how many)

A

Quantal dose-response

59
Q

__ curves represent number or % of individuals responding at a dose of a drug and only at that dose

A

Non-cumulative quantal dose

60
Q

___ is the dose at which 50% of population shows a response to a drug

A

ED50: median effective dose

61
Q

___ curve represents the number or % of individuals responding at a dose of a drug and at all doses lower than that dose

A

Cumulative quantal dose response

62
Q

TD50 represents ___

ED50 represents ___

A

Median toxic dose

Median effective dose

63
Q

Describe the Therapeutic Index (TI)

A

TI: TD50 / ED50

The higher the TI, the safer the drug

64
Q

__ is the range of doses of a drug or of its concentration in a bodily system that provides safe and effective therapy

A

Therapeutic window

65
Q

This type of drug-receptor interaction (bond) is irreversible; drug removal/receptor re-activation requires re-synthesis of the receptor or enzymatic removal of the drug

A

Covalent bond

Neuro 2-Pharmacology week (7 decks)

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