Pharmacodynamics Flashcards

1
Q

Effect of the drug on the body

A

Pharmacodynamics

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2
Q

Effect of the body on the drug

A

Pharmacokinetics

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3
Q

What is a Dose-Response Curve?

A

Relationship between a drug and its effects

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4
Q

If the Dose-Response curve is plotted arithmetically, what shape will it be?

A

Hyperbolic

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5
Q

More commonly, if the Dose-Response curve is plotted with the LOG of drug dose, what shape will it be?

A

Sigmoidal

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6
Q

What is Emax and where is it found?

A

Maximal effect produced by a drug

- Top of Y axis (100% response)

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7
Q

What is ED50 and where is it found?

A

Drug dose that produces 50% of maximal effect

- X axis that coordinates to 50% on Y axis

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8
Q

Graded Dose-Response curves represent?

A

MEAN VALUE within a population/person

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9
Q

With Graded Dose-Response curves, the magnitude of response varies ______

A

Continuously

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10
Q

Quantal Dose-Response curves examine?

A

FREQUENCY of a response within a population

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11
Q

What are the 2 types of Quantal Dose-Response curves?

A

Non-cumulative

Cumulative

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12
Q

Non-cumulative Quantal Dose-Response curves measure?

A

% of people responding at a dose and ONLY AT THAT DOSE

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13
Q

Cumulative Quantal Dose-Response curves measure?

A

% of people responding at a dose AND AT ALL DOSES LOWER than that dose

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14
Q

What shape is the Non-cumulative Quantal Dose-response curve?

A

Bell shaped

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15
Q

What shape is the Cumulative Quantal Dose-response curve?

A

Sigmoidal

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16
Q

Median Effective Dose

A

ED50

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17
Q

Median Toxic Dose

A

TD50

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18
Q

Median Lethal Dose

A

LD50

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19
Q

Therapeutic Index (TI) =

A

TD50/ED50

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20
Q

The greater the Therapeutic Index (TI) the?

A

Safer the drug

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21
Q

Drug Potency

A

Amount of a drug required to produce a specific effect

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22
Q

Drug Potency is represented by?

A

ED50

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23
Q

The lower the ED50 on the x axis, the more ___ a drug

A

Potent

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24
Q

Drug Efficacy

A

Maximal effect produced by a drug

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25
Q

Drug Efficacy is represented by?

A

Emax

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26
Q

The higher the Emax on the Y axis, the more ____ a drug

A

Efficacious

27
Q

Drug efficacy is related to the _____ available to bind the drug

A

of receptors available to bind the drug

28
Q

What determines the drug dose used clinically?

A

Drug potency

29
Q

What determines the magnitude of the clinical effect?

A

Drug Efficacy

30
Q

What are 4 parameters to describe the interaction of a drug with its receptor?

A

Binding
Affinity
Selectivity
Intrinsic Activity

31
Q

What type of bonds to most drugs use to bind to their receptors?

A

Reversible Non-covalent bonds

32
Q

How readily and tightly a drug binds to its receptor

A

Affinity

33
Q

A HIGH affinity correlates to _____ drug needed for a response

A

LESS

34
Q

A LOW affinity correlates to ____ drug needed for a response

A

MORE

35
Q

KD

A

Drug concentration at which 50% of binding sites are occupied by the drug

36
Q

KD is on the ___ axis

A

x axis

37
Q

A LOWER KD =

A

HIGHER AFFINITY

38
Q

Property of a drug determined by its affinities at various binding sites

A

Selectivity

39
Q

KD ratio measures?

A

Selectivity

40
Q

KD ratio

A

KD off-target / KD target

41
Q

The HIGHER the KD ratio, the _____ the selectivity

A

HIGHER Selectivity

42
Q

The HIGHER the selectivity, the ____ adverse effects

A

LOWER adverse effects

43
Q

What is Intrinsic Activity?

A

Ability of a drug to change receptor function and produce a physiologic response

44
Q

Ability of a drug to change receptor function and produce a physiologic reponse

A

Intrinsic Activity

45
Q

Bind receptor, stabilizes it, and produces a physiologic reponse

A

Agonists

46
Q

Do Agonists have intrinsic activity?

A

YES

47
Q

Bind receptor, and do NOT change its function

A

Antagonists

48
Q

Do Antagonists have intrinsic activity?

A

NO - do not change receptor function or produce physiologic response

49
Q

3 types of Agonists?

A

Full Agonist
Partial Agonist
Inverse Agonist

50
Q

What type of agonist mimics actions of endogenous chemicals?

A

Full agonists

51
Q

What type of agonist produces opposite effects of the other agonists and decreases receptor signaling/response?

A

Inverse agonist

52
Q

What agonists/antagonists block action of endogenous chemicals?

A

Partial and Inverse agonists

All Antagonists

53
Q

3 broad categories of antagonists?

A

Pharmacologic
Chemical
Physiological

54
Q

2 types of pharmacologic antagonists?

A

Competitive

Non-competitive

55
Q

2 types of Non-competitive pharmacologic antagonists?

A

Irreversible

Allosteric

56
Q

Pharmacologic antagonists act where?

A

Same receptor as agonists/endogenous chemicals

57
Q

Chemical antagonists make drugs?

A

Unavailable

58
Q

Competitive antagonists compete for binding at the receptor. Can they be displaced and overcome?

A

YES

59
Q

With Competitive Antagonists present, describe Emax and EC50 for an Agonist

A
Emax = unchanged
EC50 = increased
60
Q

Can Non-competitive antagonists’ receptor inactivation be overcome?

A

NO

61
Q

How do Irreversible Antagonists work?

A

Occlude Agonist site using covalent bonds (irreversible)

62
Q

How do Allosteric Antagonists work?

A

Bind to site OTHER THAN agonist site

= Decreases agonist binding or receptor activation

63
Q

With Non-competitive Antagonists present, describe Emax and EC50 for an Agonist

A
Emax = decreased
EC50 = unchanged