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ADT Module 1-4 > Principles of Pharmacokinetics/Pharmacodynamics Review > Flashcards

Principles of Pharmacokinetics/Pharmacodynamics Review Flashcards

1
Q

What is the term for first hand reports including research, clinical cases and case series?

A

Primary Medical Literature

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2
Q

What is the term for second-hand reviews of primary literature sources which include meta-analyses and systematic reviews?

A

Secondary Medical Literature

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3
Q

What is the term for publications that utilize both primary and secondary sources and includes textbooks, and online sources such as Epocrates?

A

Tertiary Medical Literature

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4
Q

What is the preferred literature source?

A

An original study (primary)

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5
Q

What is the term for a rigorous review process by experts in the field or specialty prior to publication?

A

Peer Review

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6
Q

What is the term for any literature source that is not peer reviewed prior to publication and may include professional publications and patient education?

A

Non-peer Reviewed

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7
Q

Which database contains the largest and most diverse list of references?

A

PubMed

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8
Q

Which database is more focused on literature relevant to health professions such as nursing?

A

CINAHL

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9
Q

Which database is focused on drug therapy?

A

International Pharmacy Abstracts (IPA)

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10
Q

Which database is the European equivalent to PubMed?

A

Embase

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11
Q

What is the term for the study of the action of drugs in the body?

A

Pharmacology

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12
Q

What is the term for the science that studies and describes how drugs are absorbed, distributed, transported, and eliminated form the body?

A

Pharmacokinetics

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13
Q

What is the term for the study of the relationship between drug concentrations at the site of action and the pharmacologic activity of the drug?

A

Pharmacodynamics

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14
Q

What are the five steps in the pharmacokinetic process?

A

1) Liberation
2) Absorption
3) Distribution
4) Metabolism
5) Elimination

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15
Q

What term defines the breakdown of the dosage form?

A

Liberation

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16
Q

How can liberation be enhanced?

A

By giving a drug already in solution

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17
Q

What can be controlled by regulating the process of liberation?

A

The rate of absorption

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18
Q

What term defines the process of getting the drug into systemic circulation?

A

Absorption

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19
Q

In what two ways can absorption be bypassed?

A

Giving a drug by IV or direct local administration

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20
Q

What term defines the transport and transfer of drug to the various parts of the body?

A

Distribution

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21
Q

The distribution process is influenced by what three factors?

A

1) Protein binding capacity
2) Water and lipid solubility
3) Size of the drug molecule

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22
Q

What term defines the process by which the body breaks down the the chemical compound that is administered?

A

Metabolism

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23
Q

What is the goal of metabolism?

A

To alter the drug chemically, so that it can be easily eliminated from the body

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24
Q

What term defines the process by which active drug or drug metabolites are excreted from the body?

A

Elimination

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25
Q

What organs are involved in elimination?

A

1) Kidney
2) Liver
3) Intestine
4) Lungs
5) Skin

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26
Q

What are the protein sites called where drugs bind to produce their action in the body?

A

Receptors

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27
Q

On what two sites are receptors are usually located?

A

1) Cell

2) Enzyme

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28
Q

What is the term for the relative amount of drug needed to elicit a response as compared to another drug?

A

Potency

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29
Q

What is the term for the amount of drug in a dosage form?

A

Strength

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30
Q

What term describes the relationship between the dose or concentration needed to produce a pharmacologic effect and the dose or concentration that produces toxic effects?

A

Therapeutic index

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31
Q

What term describes the time it takes for a drug to produce its pharmacological action?

A

Onset of action

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32
Q

What is the term for a drug that binds to a receptor and produces stimulation or increased activity of the receptor (mimics or enhances activity)?

A

Agonist

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33
Q

What is the term for a drug that binds to a receptor and blocks or inhibits the activity of the receptor?

A

Antagonist

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34
Q

What is the term for a drug that has both agonist and antagonist properties?

A

A mixed agonist-antagonist or a mixed-effects drug

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35
Q

On what parts of a cell can a receptor be present?

A

1) Membrane
2) Ion channel
3) Nucleus
4) Ribosome

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36
Q

What are some factors that influence drug binding to receptors?

A

1) Drug concentration at site
2) pH
3) # of receptors
4) Affinity for the receptor
5) Selectivity of the drug for that receptor
6) Change in shape of the receptor (caused by diseases or drugs)

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37
Q

What is the term for a reduction in the number of receptors or the reduced affinity of a drug for a receptor?

A

Down-regulation (compensation for overstimulation)

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38
Q

What is the term for an increased need of a higher dose of a drug to obtain the pharmacologic effects of the drug?

A

Tolerance

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39
Q

Down-regulation occurs in response to what type of drug?

A

Agonist

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40
Q

What is the term for an increased number of receptors or the increased affinity of a receptor?

A

Up-regulation (compensation for blockade)

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41
Q

Up-regulation often occurs in response to what kind of drug?

A

Antagonist

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42
Q

What are the two types of binding typically used to describe drug interaction with enzymes instead of cells?

A

1) Competitive binding

2) Non-competitive binding

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43
Q

What is the term used to describe the process of a drug binding to the actual site on an enzyme that breaks down an endogenous substance?

A

Competitive

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44
Q

What is the term used to describe the process of a drug binding to an alternate site on an enzyme resulting in a conformational change that blocks the binding of an endogenous substance?

A

Non-competitive

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45
Q

Which type of binding can be overcome by the production of more endogenous substance?

A

Competitive

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46
Q

What is the term for tight capillary walls that prevent the passage of certain substances into the brain?

A

Blood Brain Barrier

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47
Q

What are some processes that can alter this barrier?

A

1) Infection
2) Inflammation
3) Trauma
4) Tumor growth
5) Mechanical manipulation

48
Q

What type of drugs differ because of their ability to bind with cells or enzymes on infectious organisms versus those in the body?

A

Antibiotics

49
Q

Concerning antibiotics, what is the term for the lowest concentration where the drug has any activity against bacteria growth?

A

Minimum Inhibitory Concentration (MIC)

50
Q

Concerning antibiotics, what is the term for the lowest concentration of the drug where bacteria are killed?

A

Minimum Bactericidal Concentration (MBC)

51
Q

If MIC values are low, the bacteria are considered _____ to the antibiotic

A

Sensitive

52
Q

If MIC values are high, the bacteria are considered ____ to the antibiotic

A

Resistant

53
Q

If MICs are increasing for a specific antibiotic against a particular bacteria, there is concern about __________

A

Increased resistance of the bacteria to the antibiotic

54
Q

What is the form in which MIC data are typically reported?

A

An antibiogram

55
Q

What are the four steps that occur for a drug to move to a receptor? (the first three are steps in the absorption process)

A

1) Disintegration
2) Dissolution
3) Transfer to blood
4) Distribution

56
Q

What is the term for the breakdown of the dosage form to release or liberate the drug?

A

Disintegration

57
Q

Disintegration control is altered for what three reasons?

A

1) Minimize adverse effects
2) Shorten time of absorption
3) Improve absorption

58
Q

What is the term that means the drug has been taken up in a solution?

A

Dissolution

59
Q

What are the four most commonly used oral dosage forms?

A

1) Oral disintegrating (burst release)
2) Immediate release (regular release)
3) Delayed release (pulsatile release)
4) Sustained or extended release (controlled release)

60
Q

What oral dosage form mimics an IV infusion and provides a constant blood level?

A

Sustained or continuous release

61
Q

What oral dosage form may result in a “ghost” tablet?

A

Sustained or continuous release

62
Q

What is the term that describes movement of a drug from a higher concentration to a lower concentration?

A

Passive diffusion

63
Q

What is the term that refers to movement across a membrane which requires help in the form of a carrier?

A

Active transport

64
Q

What are three barriers to absorption?

A

1) Solubility (pH, particle size, water solubility)
2) Enzymes (P450)
3) Hepatic portal circulation

65
Q

What are some other factors that influence ORAL absorption?

A

1) Food
2) Age
3) GI blood flow
4) Liver blood flow
5) Protein binding

66
Q

Absorption is affected by the route of administration. List the fastest to the slowest using the four most common routes of administration:

A

IV
IM
Oral
Topical

67
Q

What is the term for the rate and extent to which the active ingredient of active moiety is absorbed from a drug product and becomes available at the site of action?

A

Bioavailability

68
Q

What is the term that describes expected in vivo biological equivalence of two proprietary preparations of a drug that are for all intents and purposes, the same

A

Bioequivalence

69
Q

What is the value that correlates to the total amount of drug absorbed and is defined by time and concentration?

A

The Area Under the Curve (AUC)

70
Q

For a drug to be bioequivalent, the AUC must fall within what range of the brand product?

A

80% - 125%

71
Q

How do you calculate a loading dose of a drug?

A

Desired peak concentration x volume of distribution of drug in the body and divide by the bioavailability

72
Q

What is the term that describes when a drug rapidly distributes to all the places it will go in the body immediately following the administration?

A

One compartment distribution

73
Q

What is the term that describes when a drug rapidly distributes to a small part of the body (usually total body water) followed by deeper parts?

A

Two compartment distribution

74
Q

What kind of drug can leave the bloodstream to bind to receptors, other peripheral sites and to sites of metabolism such as the liver?

A

Unbound drug

75
Q

What do drugs typically bind to in the blood or cells?

A

Protein, namely albumin

76
Q

What is the term for the amount of time it takes for 50% of the amount of a drug in the body to be eliminated?

A

Half-life

77
Q

What are two important uses for half-life?

A

1) Determining dosing frequency

2) Determining steady-state

78
Q

What is the type of elimination followed by most drugs where the rate of metabolism or elimination is directly proportional to the concentration of the drug?

A

First order elimination

79
Q

What is the type of elimination where the rate of elimination does not change in relationship to the concentration to the drug?

A

Zero elimination

80
Q

What are the common drugs that have zero elimination?

A

1) Phenytoin
2) Ethanol
3) High dose aspirin

81
Q

What are the two stages of metabolism called?

A

1) Phase I

2) Phase II

82
Q

In which phase of metabolism is the primary enzyme Cytochrome P450 (CYP)?

A

Phase I

83
Q

In which phase of metabolism is the primary enzyme UDP/UGT?

A

Phase II

84
Q

In which phase are active metabolites a concern for toxicity?

A

Phase I

85
Q

Cytochrome P450 is broken down into what five common isoenzymes involved in drug metabolism?

A

1) CYP 1A2
2) CYP 2C9
3) CYP 2C19
4) CYP 2D6
5) CYP 3A4

86
Q

What is the term for the drugs that are metabolized through specific isoenzymes?

A

Substrates

87
Q

What is the term for drugs that increase CYP450 isoenzymes?

A

Inducers

88
Q

If an inducer (drug) is added to a drug regimen in which a substrate (drug) is altered by an isoenzyme, the dose of the substrate would need to be _______

A

Increased

89
Q

What is the term for drugs that reduce the activity of CYP450 isoenzymes?

A

Inhibitors

90
Q

If an inhibitor (drug) is added to a drug regimen in which a substrate (drug) is altered by an isoenzyme, the dose of the substrate would need to be _______

A

Reduced

91
Q

Warfarin is given as a mixture of what two types of enantiomers?

A

1) R-warfarin (less anticoagulation activity)

2) S-warfarin (most anticoagulation activity)

92
Q

R-warfarin is metabolized by what isoenzyme?

A

CYP 1A2

93
Q

S-warfarin is metabolized by what isoenzymes?

A

CYP 2C9 and CYP 3A4

94
Q

Name the primary organ of elimination

A

The kidney

95
Q

Normal kidney function is considered to be equal to or greater than _____

A

100 ml/min

96
Q

What are some ways in which age affects the principles of pharmacokinetics?

A

1) Altered metabolism (children often require larger doses on a mg/kg basis)
2) Altered protein binding (neonates and elderly have low albumin)
3) Altered receptor sensitivity (elderly more sensitive)
4) Declining organ function (renal function decreases with age)

97
Q

What are some ways in which physiology affects the principles of pharmacokinetics?

A

1) Pregnancy (altered protein binding, renal function, hepatic function and body composition)
2) Acute illness (trauma, MI, burns)

98
Q

What are some ways in which organ function affects the principles of pharmacokinetics?

A

1) Liver function (metabolism, production of proteins)

2) Renal function (body composition, protein binding)

99
Q

Name three types of drug interactions?

A

1) Duplication
2) Opposition
3) Alteration

100
Q

What is the term for administering two drug products that contain the same drug or similarly acting drugs?

A

Duplication

101
Q

What are common drugs for duplication?

A

Acetaminophen and anticholinergics

102
Q

What are the acetaminophen parameters for adults?

A

Over 1000 mg per dose or 4000 mg per day

103
Q

What are the acetaminophen parameters for children?

A

Over 10-15 mg/kg/dose or 2600 mg per day

104
Q

What complication does an acetaminophen overdose cause?

A

Hepatotoxicity

105
Q

What are the effects of anticholinergic duplication?

A

Dry mouth, blurred vision, urine retention, constipation, decreased memory, delusions and hallucinations

106
Q

What is the term for giving two drugs with opposite reactions?

A

Opposition

107
Q

What is the term for drug interactions which alter the effect of the drug itself?

A

Alteration

108
Q

What types of drug alterations can take place?

A

1) Altered absorption
2) Altered metabolism or elimination
3) Altered protein binding

109
Q

What is the term for the study of differences in drug response or metabolism as it relates to a specific genetic change?

A

Pharmacogenetics

110
Q

What is the term for the study of difference in drug response or metabolism as it relates to large populations?

A

Pharmacogenomics

111
Q

What are different genetic forms of an isoenzyme called?

A

Polymorphisms

for example CYP 2C9 has 6 different alleles

112
Q

What is the main site of action for warfarin?

A

The enzyme vitamin K epoxide reductase

113
Q

What is the gene that codes for the vitamin K enzyme where warfarin works?

A

VKORC1

114
Q

Name the three VKORC1 polymorphisms:

A

1) 1639 GG
2) 1639 AA
3) 1639 GA

115
Q

Warfarin pharmacogenetic dosing is based on what two factors?

A

1) VKORC1 polymorphism

2) CYP 2C9 alleles

116
Q

What polymorphism is associated with increased risk factors for serious dermatological reactions when taking carbamazepine?

A

HLA-B*1502 allele

117
Q

What ethnicities does the HLA-B affect?

A

1) Chinese, Thai, Malaysian, Indonesian, Filipino 10-15% of population
2) Japanese and Korean

ADT Module 1-4 (21 decks)

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