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Biopharmaceutics and Pharmacokinetics > Unit 2: Pharmacokinetic Modelling > Flashcards

Unit 2: Pharmacokinetic Modelling Flashcards

1
Q

reduces complexity of pharmacokinetics

A

pharmacokinetic modelling

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2
Q

simplification of reality

A

model

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3
Q

are models qualitative or quantitative

A

can be qualitative or quantitative

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4
Q

general template; something you want to replicate

A

model

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5
Q

more variables make a template more ______

A

specific

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6
Q

hypothesis using mathematical terms to concisely describe quantitative relationships

A

model

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7
Q

wants to predict plasma drug conc

A

pharmacokinetic modelling

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8
Q

is pharmacokinetic modelling quantitative or qualitative

A

mathematical/quantitative

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9
Q

mathematical description of a biologic system

A

pharmacokinetic model

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10
Q

can be used to simulate rate processes describing the movement of drug in the body

A

pharmacokinetic model

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11
Q

mathematical tool that allow simulating drug concentration levels in the blood prior to real administration

A

pharmacokinetic model

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12
Q

allow more accurate interpretation of the relationship between plasma drug levels and pharmacologic response

A

pharmacokinetic model

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13
Q

pharmacokinetic models uses:
predict _______, _______, and ______ drug levels with any dosage regimen

A

plasma, tissue and urine

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14
Q

pharmacokinetic models uses:
calculate the optimum dosage regimen for each patient ________

A

individually

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15
Q

pharmacokinetic models uses:
estimate the possible _______ of drugs and/or metabolites

A

accumulation

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16
Q

pharmacokinetic models uses:
correlate drug concentrations with ________ or _______ activity

A

pharmacologic or toxicologic

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17
Q

pharmacokinetic models uses:
evaluate differences in the rate or extent of availability between formulations (________)

A

bioequivalence

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18
Q

pharmacokinetic models uses:
describe how changes in _______ or _______ affect the absorption, distribution, or elimination of the drug

A

physiology or disease

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19
Q

pharmacokinetic models uses:
explain ______ interactions

A

drug

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20
Q

when 2 drugs are able to deliver the same or equivalent bioavailability

A

bioequivalence

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21
Q

the # of parameters needed depends on: (2 answers)

A
  1. complexity of the process (ADME)
  2. route of drug administration
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22
Q

more # of parameters make it (easier/more difficult) to accurately estimate

A

more difficult

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23
Q

3 classification of pharmacokinetic models

A

1) empirical
2) compartmental
3) physiological

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24
Q

pharmacokinetic models aim to (reduce/increase) complexity

A

reduce

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25
Q

simply interpolates the data and allows an empirical formula to estimate drug level over time

A

empirical models

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26
Q

justified when limited information is available

A

empirical models

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27
Q

practical but not very useful in explaining the mechanism of the actual processes

A

empirical models

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28
Q

aka statistical

A

empirical models

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29
Q

main specimen of pharmacokinetic model

A

plasma/blood

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30
Q

model is not factual and does not following the theory at all

A

empirical models

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31
Q

instead of understanding whole ADME, model focuses on experiences of pharmacokineticist and observation on the drug product

A

empirical models

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32
Q

treatment which give drugs without knowing causative agent

A

empirical treatment

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33
Q

does not know the functional group present

A

empirical formula

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34
Q

simple and useful tool

A

compartmental model

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35
Q

simplistic view of drug disposition in the human body

A

compartmental model

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36
Q

provides a simple way of grouping all the tissues into one or more compartments where drugs move to and from the central or plasma compartment

A

compartmental model

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37
Q

most popular model used

A

compartmental model

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38
Q

an assigned place/group of tissues

A

compartment

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39
Q

is not a real physiologic or anatomic region

A

compartment

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40
Q

is considered a tissue or group of tissues that have a similar blood flow and drug affinity

A

central compartment

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41
Q

in a compartment, mixing of drug is _____ and ______

A

rapid and homogenous

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42
Q

considered to be connected to each other by pathways (reversible or irreversible)

A

compartment

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43
Q

two conditions for a central compartment

A

should have similar hyperfusion (blood flow) and drug affinity

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44
Q

administered drug dose is removed from the body by an excretory mechanism as the unchanged drug or as metabolite (kidneys and other excretory organs)

A

open model

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45
Q

all pharmacokinetic models are _________

A

open model

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46
Q

model with a process of elimination and point of exit

A

open model

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47
Q

compartmental model can be divided into 2

A

open and closed

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48
Q

administered drug dose is not removed from the body by an excretory mechanism

A

closed model

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49
Q

drug will persist in the body forever

A

closed model

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50
Q

most common model used in pharmacokinetics

A

mamillary model

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51
Q

useful when little information is known about the tissues

A

mamillary model

52
Q

one or more compartments around a central compartment – “satellites”

A

mamillary model

53
Q

drug is both added to and eliminated from a central compartment

A

open one-compartment model (mamillary model)

54
Q

plasma and highly perfused tissues that rapidly equilibrate with drug

A

central compartment

55
Q

drug can move between the central or plasma compartment to and from the tissue compartment

A

open two-compartment model (mamillary model)

56
Q

tissue compartment

A

peripheral compartment

57
Q

plasma compartment

A

central compartment

58
Q

total amount of drug in the body = drug in central compartment + drug in tissue compartment

A

open two-compartment model (mamillary model)

59
Q

rate of elimination/elimination constant

A

k or k10

60
Q

first order absorption; often from oral route; point of entry

A

ka

61
Q

apparent first-order rate constant of transfer of drug from the central compartment into the tissue compartment

A

k12

62
Q

apparent first-order rate constant of transfer of drug from the tissue compartment into the central compartment

A

k21

63
Q

is the open two-compartment model reversible or irreversible

A

reversible

64
Q

apparent first-order rate constant of absorption

A

ka

65
Q

apparent first-order rate constant of drug elimination from central compartment

A

k or k10

66
Q

significance: enables writing different eq to describe drug conc changes in each compartment

A

mamillary model

67
Q

compartment 1 has more than 2 satelites

A

open multi-compartment

68
Q

for multi-compartment model, identify the subscript representation of:
a) central compartment
b) deep tissue compartment
c) shallow tissue compartment

A

a) 1
b) 3
c) 2

69
Q

apparent first-order rate constant of transfer of drug from the central compartment into compartment 3

A

k13

70
Q

apparent first-order rate constant of transfer of drug from compartment 3 into the central compartment

A

k31

71
Q

not all compartments are connected to the central compartment

A

catenary model

72
Q

significance: visual representation of rate processes (first order and zero order)

A

mamillary model

73
Q

significance: estimate the number of pharmacokinetic constants are necessary to describe the process adequately

A

mamillary model

74
Q

everything is connected to central compartment

A

mamillary model

75
Q

connection of compartments is like a chain/train

A

catenary model

76
Q

does not apply to the way most functional organs in the body are directly connected to the plasma

A

catenary model

77
Q

are assigned and are not constant in a model

A

compartments

78
Q

aka blood flow or perfusion model

A

physiologic pharmacokinetic model

79
Q

based on known anatomic and physiologic data

A

physiologic pharmacokinetic model

80
Q

realistic means of modeling tissue drug levels

A

physiologic pharmacokinetic model

81
Q

disadvantage: it is difficult to acquire tissue samples to measure drug concs

A

physiologic pharmacokinetic model

82
Q

advantage: modelling tissue drug levels are accurate as it is close to realistic

A

physiologic pharmacokinetic model

83
Q

each tissue volume must be obtained and its drug concentration described

A

physiologic pharmacokinetic model

84
Q

on physiologic pharmacokinetic model –> if there’s no perfusion, ______ is excluded

A

organ (e.g. brain, bones, others parts of CNS are often excluded)

85
Q

the # of tissue compartments varies with drug

A

physiologic pharmacokinetic model

86
Q

tissue drug conc of which drugs (4) has been described by the perfusion model

A

digoxin, lidocaine, methotrexate, thiopenthal

87
Q
  1. The size of the organ tissue
  2. Blood flow to the organ tissue
  3. The experimentally determined ratios of drug concentration between the tissue and the blood
A

factors that predict conc of drug in tissues in physiologic pharmacokinetic model

88
Q

physiologic pharmacokinetic model:
relationship of organ to drug concentration

A

directly proportional

89
Q

physiologic pharmacokinetic model:
relationship of blood flow to drug concentration

A

directly proportional

89
Q

physiologic pharmacokinetic model:
relationship of blood flow to absorption

A

directly proportional

90
Q

organs are represented instead of compartments

A

physiologic pharmacokinetic model

91
Q

physiologic pharmacokinetic model:
represents the rate of blood perfusion to the tissue

A

Q

92
Q

liver and kidney are (highly/lowly) perfused organs

A

highly

92
Q

liver and kidney are (highly/lowly) perfused organs

A

highly

93
Q

physiologic pharmacokinetic model:
represent kinetic constants

A

ks

94
Q

physiologic pharmacokinetic model:
is the first-order rate constant for urinary drug excretion

A

ke

95
Q

physiologic pharmacokinetic model:
is the rate constant for hepatic elimination

A

km

96
Q

physiologic pharmacokinetic model:
RET means

A

rapidly equilibrating tissue

97
Q

physiologic pharmacokinetic model:
SET means

A

slowly equilibrating tissue

98
Q

liver and kidneys belong under (RET or SET)

A

RET

99
Q

advantage: information derived from these models can be applied to several species (humans, experimental animals)

A

physiologic pharmacokinetic model

100
Q

disadvantage: fewer data points than parameters that one tries to fit and therefore projected data are not well constrained

A

physiologic pharmacokinetic model

101
Q

disadvantage: data can be experimentally difficult to obtain

A

physiologic pharmacokinetic model

102
Q

disadvantage: data can be affected by pathophysiologic conditions which can cause variation to blood flow, tissue size, drug tissue-blood ratios

A

physiologic pharmacokinetic model

103
Q

actual tissue volume is used

A

physiologic pharmacokinetic model

104
Q

estimated tissue Vd (volume of distribution) is used

A

compartmental model

105
Q

experimentally determined in ANIMALS –> extrapolated to humans

A

physiologic pharmacokinetic model

106
Q

no data fitting required

A

physiologic pharmacokinetic model

107
Q

in physiologic pharmacokinetic model:
drug concentrations in various tissues are predicted by (3)

A

organ tissue size, blood flow, experimentally determined drug tissue- blood ratios

108
Q

2 ways to measure drug concentration

A

HPLC, Mass spectrometry

109
Q

HPLC meaning

A

high performance/high precision liquid chromatography

110
Q

ways to retrieve biologic specimen (2)

A

invasive and noninvasive methods

111
Q

retrieval of biologic specimen:
requires parenteral or surgical intervention in the patient

A

invasive

112
Q

retrieval of biologic specimen:
needs insertion or cutting open a patient

A

invasive

113
Q

retrieval of biologic specimen:
operation, anaesthetics

A

invasive

114
Q

retrieval of biologic specimen:
blood, spinal fluid, synovial fluid, tissue biopsy

A

invasive

115
Q

retrieval of biologic specimen:
urine, saliva, feces, breastmilk

A

noninvasive

116
Q

retrieval of biologic specimen:
can be obtained without parenteral or surgical intervention

A

noninvasive

117
Q

biologic specimen:
most direct approach, most used to measure drug conc in body, most accessible invasive part

A

plasma

118
Q

biologic specimen:
total plasma drug concentration

A

unfiltered plasma

119
Q

biologic specimen:
unbound drug concentration

A

filtered plasma

120
Q

biologic specimen:
indirect method to ascertain bioavailability

A

urine

121
Q

biologic specimen:
drug that has not been absorbed after an oral dose

A

feces

122
Q

biologic specimen:
has been biliary secreted after systemic absorption

A

feces

123
Q

biologic specimen:
unbound drug, noninvasive

A

saliva

124
Q

biologic specimen:
determination if drug reached the tissues at right concentration

A

tissue

Biopharmaceutics and Pharmacokinetics (5 decks)

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