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DEN 7203 Pharmacological Concepts > Exam 1 Intro to Pharmacology and Pharmacodynamics > Flashcards

Exam 1 Intro to Pharmacology and Pharmacodynamics Flashcards

9/4 Lecture 1 and 2

1
Q

What is pharmacology?

A

The science of drugs and how they affect living systems

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2
Q

Why is pharmacology important to dentists?

A

If a patient is taking more than one drug, there is potential for drug interactions and adverse consequences

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3
Q

True or false: every drug can affect the entire body

A

True

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4
Q

A ____ is a substance used in the diagnosis, treatment, or prevention of a disease

A

Drug

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5
Q

Drugs are usually what type of structure?

A

Small molecules (smaller than proteins, smaller than polypeptides)

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6
Q

Why is it advantageous for drugs to be small?

A
  • Quicker access into the body
  • Reach target (chemically sensitive site) sooner
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7
Q

Most drugs are smaller than proteins and polypeptides. What is the exception?

A
  • Small active peptides
  • Monoclonal antibodies
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8
Q

What is the non-proprietary name of a drug?

A

Official name, such as ibuprofen

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9
Q

What is the proprietary name of a drug?

A

Brand or trade name (such as Advil)

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10
Q

____ is what a drug does to the body

A

Pharmacodynamics

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11
Q

____ is what the body does to a drug

A

Pharmacokinetics

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12
Q

____ is involved with the drug/receptor interaction/study of the biochemical and physiologic effects of drugs and their mechanisms of action

A

Pharmacodynamics

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13
Q

What are the 4 principles of drug action?

4 ways in which drugs act on the body

A
  • Stimulation
  • Depression
  • Replacement
  • Cytotoxic action
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14
Q

What is stimulation?

A
  • Enhancement of the level of a specific biological activity, usually already an ongoing physiological process
  • Ex: Adrenaline/epinephrine stimulates heart rate
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15
Q

What is depression?

A
  • Decrease in the level of a specific biological activity, usually already ongoing physiological process
  • Ex: Opioids depress the CNS

Principles of Drug Action

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16
Q

What is replacement?

A
  • Replacement of the natural hormones or enzymes (any substance) which are deficient in our body
  • Ex: Insulin for treating diabetes
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17
Q

What is cytotoxic action?

A

Toxic effects on invading microorganisms or cancer cells (ex: antibiotics)

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18
Q

In what ways do drugs produce their effects?

A
  • Physical action
  • Chemical action
  • Counterfeit biochemical constituents
  • Through stimulating/inhibiting enzymes
  • Through receptors
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19
Q

During ____, the physical property is responsible for drug action

A

Physical action

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20
Q

During ____, the drug reacts extracellularly according to simple chemical equations (not entering a cell or system)

A

Chemical action (Ex: tums to neutralize gastric acid)

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21
Q

____ is the most common way of producing action

A

Receptor action

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22
Q

What are the major classifications of receptors?

A
  • GPCR
  • Ion channels
  • Enzymatic receptors
  • Intracellular receptors (regulates gene expression)
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23
Q

Where are steroid receptors located?

A

Intracellular

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24
Q

What is affinity?

A

The ability of a drug to bind to the receptor (just bind)

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25
Q

What is intrinsic activity?

A

It is the ability of a drug to activate a receptor following receptor occupation

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26
Q

What is a receptor agonist?

A

Any drug that binds to a receptor and activates it to produce an effect

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27
Q

Morphine has both ____ and ____

A

Affinity and maximal intrinsic activity

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28
Q

What is a receptor antagonist?

A

A drug that binds to the receptor and prevents the action of an agonist, but does not have an action on its own

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29
Q

Example of a receptor antagonist

A

Naloxone (antagonist of opioids at mu-opioid receptors)

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30
Q

Receptor antagonists have ____ but no ____

A

Affinity but no intrinsic activity

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31
Q

____ rapidly reverses opioid overdose

A

Naloxone

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32
Q

What is a partial agonist?

A

A drug that binds to the receptor and activates it, but produces a submaximal effect (less than a full agonist)

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33
Q

____ blocks the full agonist action

A

Partial agonist

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34
Q

A partial agonist has ____ but ____

A

Affinity; Submaximal intrinsic activity

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35
Q

What is an inverse agonist?

A

Any drug that activates a receptor to produce an effect in the opposite direction to that of the agonist

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36
Q

____ inhibits endogenous (constitutive) activity of a receptor

A

Inverse agonist

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37
Q

____ reduces background activity of a receptor

A

Inverse agonist

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38
Q

An inverse agonist has ____ and _____

A

Affinity and negative intrinsic activity

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39
Q

Describe the activity level comparing agonist and inverse agonist

A
  • Agonist has increasing activity level with increasing drug concentration, above the baseline level
  • Inverse agonist has the opposite effect (decreased activity of the receptor) with increasing drug concentration, below the baseline level
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40
Q

Are receptors specific?

A

Usually, but not always

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41
Q

Are there receptor subtypes?

A

Sometimes - for instance, there are several types of epinephrine receptors

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42
Q

True or false: there can be several types of receptors

A

True

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43
Q

Beta1 epinephrine receptors are located in the ____
Beta2 receptors found in ____

A

Heart; Bronchioles

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44
Q

True or false: receptor diversity may differ due to genetic differences among individuals

A

True

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45
Q

Epinephrine is a non-specific drug: it is an agonist for both ____ and ____. Why might this be a problem for someone with asthma and hypertension? What is a solution?

A

B1 and B2 receptors; Epinephrine will treat the asthma but also raise BP even higher; Terbutaline (more specific agonist of B2) used to treat people with asthma

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46
Q

In most cases of a drug-receptor interaction, drug (D) binds to a receptor (R) in a ______

A

Reversible bimolecular reaction

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47
Q

Drug-receptor interaction equation

A

D+R <-> DR <-> DR* —-> Response

48
Q

In a drug-receptor interaction, agonists that have the appropriate structural features force the bound receptor into what?

A

Active conformation (DR*)

49
Q

Conformational change of DR* leads to:

A

Series of events causing a cellular response

50
Q

Antagonists participate in which part of the drug-receptor interaction equation?

A

First equilibrium (D+R <-> DR)
No conformational change of the receptor

51
Q

____ is used as a measure of affinity of a drug for its receptor

A

Kd

52
Q

A lower value of Kd means:

A

Higher affinity/receptor occupation

53
Q

Generally, the intensity of a response ____ with dose

A

Increases

54
Q

The drug receptor interaction obeys what?

A

Law of mass action

55
Q

____ is usually equal to EC50

A

Kd

56
Q

The dose-response curve increases in response until it reaches a ____. Later it remains ____ despite increase in dose which is called the ____

A

Maximum; constant; Plateau effect

57
Q

What is threshold concentration?

A

Lowest concentration to elicit a measurable response

58
Q

At EMax, increasing doses have what effect?

A

Progressively smaller incremental effect

59
Q

____ refers to the maximal response produced by a drug

A

Efficacy

60
Q

What does efficacy depend on?

A

The number of drug-receptor complexes formed

61
Q

____ is a measure of how much drug is required to elicit a given response

A

Potency

62
Q

The ____ the dose required to elicit the response, the more potent the drug is

A

Lower

63
Q

Which scale is used to graph dose-response curves to be able to compare two drugs?

A

Log scale (difficult to compare with arithmetic scale)

64
Q

What is EC50?

A

The dose of the drug at which it gives 50% of the maximal response

65
Q

A drug with a low EC50 is more ____ than a drug with larger EC50

A

Potent

66
Q

The further ____ a DRC is, the more potent it is

A

Left (relative position on x-axis)

67
Q

The height of the DRC indicates:

A

Efficacy of the drug

68
Q

The taller the DRC, the ____ efficacious the drug

A

More

69
Q

____ relates only to binding of drug to receptor

A

Affinity

70
Q

____ and ____ both encompass binding and subsequent signal transduction events leading to a response

A

Intrinsic activity and potency

71
Q

Full agonists are those that have what?

A

Emax that is the highest for any agonist at that receptor

72
Q

Partial agonists have ____ and therefore have lower intrinsic activity

A

Lower Emax values

73
Q

A steep slope in a DRC indicates what?

A

A small increase in dose produces a large change in response

74
Q

True or false: the slope of the mid-portion of the DRC varies from drug to drug

A

True

75
Q

Is a steep DRC desired?

A

No

76
Q

In a steep DRC, moderate increase in dose leads to what?

A

More increase in response

77
Q

In a flat DRC, moderate increase in dose leads to what?

A

Little increase in response

78
Q

True or false: If a drug has a steep DRC, dose needs no individualization for different patients

A

False - does need individualization

79
Q

If a drug has a flat DRC, does the dose need individualization for different patients?

A

No

80
Q

What DRC is desired and common?

A

Flat DRC (drug is administered more safely)

81
Q

What is ED50?

A

Looks like EC50 but indicates the dose for a therapeutic effect in 50% of the population

82
Q

Therapeutic index is a measurement of:

A

Drug safety

83
Q

What is TD50?

A

Median toxic dose

84
Q

Formula to calculate Therapeutic Index

A

TD50/ED50

85
Q

Safer drugs have ____ TI values

A

Higher

86
Q

Toxic dose (TD50) and Lethal dose (LD50) is estimated in what kind of studies?

A

Preclinical animal studies

NOT HUMAN STUDIES

87
Q

Is LD50 calculated in humans?

A

NO

88
Q

What is therapeutic window?

A
  • Clinically relevant index of safety
  • Describes the dosage range between the minimum effective therapeutic concentration or dose, and the minimum toxic concentration or dose
89
Q

Drugs with a ____ should be used with caution and needs periodic monitoring, such as warfarin and theophylline

A

Narrow therapeutic window

90
Q

Drugs with a ____ can be used relatively safely and does not need close monitoring

A

Large therapeutic window

91
Q

When 2 drugs are given together or in quick succession, what 3 things can happen?

A
  • Nothing (indifferent to each other)
  • Synergism (action of one drug is facilitated by the other)
  • Antagonism (action of one drug may decrease or inhibit the action of the other drug)
92
Q

What are the two types of synergism?

A
  • Additive effect
  • Supra-additive effect
93
Q

____ is when the effect of two drugs are in the same direction and simply add up

A

Additive effect

Synergism

94
Q

____ is when the effect of combination is greater than the individual effect of the components

A

Supra-additive effect

Synergism

95
Q

What are the different types of antagonism?

A
  • Physical
  • Chemical
  • Physiological antagonism
  • Receptor antagonism
96
Q

Physical antagonism is based on:

A

Physical property of a drug

97
Q

Chemical antagonism is based on:

A

Chemical properties resulting in an inactive product

Ex. chelating agent like EDTA

98
Q

What happens in physiological antagonism?

A

Two drugs act on different receptors or by different mechanisms, but have opposite effects

99
Q

What happens in receptor antagonism?

A

Antagonist interferes with the binding of the agonist with its receptor and inhibits the generation of a response

100
Q

Is receptor antagonism specific?

A

Yes

101
Q

Receptor antagonism can be ____ and ____

A

Competitive and noncompetitive

102
Q

____ antagonism is surmountable

A

Competitive

103
Q

In ____, antagonist competes with agonist in reversible fashion for the same receptor site

A

Competitive antagonism

104
Q

If competitive antagonism occurs, it is necessary to have:

A

Higher concentration of agonist to achieve same response

105
Q

____ antagonism is insurmountable

A

Noncompetitive

106
Q

What happens during noncompetitive antagonism?

A

Antagonist binds to a different site to that of an agonist

107
Q

True or false: in noncompetitive antagonism, no matter how much agonist, antagonism cannot be overcome

A

True

108
Q

How does the DRC change in competitive antagonism?

A

Parallel rightward shift

109
Q

How does the DRC change in noncompetitive antagonism?

A

Flattens

110
Q

True or false: Number and affinity of receptors do not change

A

False, may change

Upregulation or downregulation of receptors

111
Q

Upregulation

A

Increase in receptor number

112
Q

Downregulation

A

Decrease in receptor number

113
Q

What is the clinical relevance of downregulation?

A

Patient’s response to drug therapy may change over time

Prolonged/frequent use of a drug may decrease number of receptors

114
Q

What is tolerance?

A

Gradual reduction in response to drugs that occurs over a period of time

115
Q

What are 2 reasons for tolerance?

A
  • Receptor downregulation (pharmacodynamic reasons)
  • Chronic use leads to enhanced clearance (pharmacokinetics), leading to a less effective concentration

DEN 7203 Pharmacological Concepts (7 decks)

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