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MUSC Pharmacology > Exam 1 Pharmacokinetics > Flashcards

Exam 1 Pharmacokinetics Flashcards

1
Q

Who writes drug prescribing information

A

drug companies

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2
Q

who approves drug prescribing information?

A

FDA

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3
Q

What is pharmacokinetics?

A

the way the drug moves in and through the body

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4
Q

What is LADME?

A 
Liberation
Absorption 
Distribution
Metabolism
Elimination
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5
Q

You can’t get absorption until you have ____.

A

Liberation

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6
Q

drug movement through compartments

A

distribution

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7
Q

drug removal from body

A

elimination

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8
Q

transformation of parent compound

A

metabolism

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9
Q

drug enters circulation

A

absorption

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10
Q

drug release- from whatever dosage form it is

A

liberation

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11
Q

Tpk

A

time to peak concentration

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12
Q

F means

A

fraction of drug that is bioavailable

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13
Q

PPB means

A

protein binding

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14
Q

Vd means

A

volume of distribution

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15
Q

T1/2

A

Half life

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16
Q

How can liberation be modified?

A

by making drug buffered,
enteric coated, delayed/controlled/extended,
sustained release,
and abuse resistant

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17
Q

what is the purpose of enteric coated medicine?

A

it won’t dissolve until it gets into intestine

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18
Q

traditional liberation

A

a tablet dissolving/breaking apart in liquid

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19
Q

buffered medicine changes liberation how?

A

medicine needs to be in basic environment to disassociate.

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20
Q

example of buffered medicine

A

aspirin

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21
Q

4 different types of movement across membranes that is involved in absorption

A

Passive diffusion
Active transport
Facilitated diffusion
Endocytosis

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22
Q

most common absorption movement

A

passive diffusion

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23
Q

movement of molecules is gradient driven (concentration dependent.

A

passive diffusion

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24
Q

in passive transport, Rate of transport is dependent on ____.

A

concentration gradient

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25
Q

diffusion through pumps, it uses energy and can go against concentration gradient

A

Active transport

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26
Q

type of diffusion through channels, it requires energy. it is the same as active transport

A

Facilitated diffusion

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27
Q

fastest absorption route

A

IV

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28
Q

slow absorption routes

A

otic and ocular

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29
Q

fast absorption routes

A

Sublingual/Buccal
Inhalation
IV

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30
Q

Variable absorption routes

A

IM
SubQ
Topical
Rectal

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31
Q

example of slow IM absorption

A

DEPO shot for contraception

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32
Q

Absorption Factors (8)

A
  1. Physical state
  2. Area of absorbing surface
  3. concentration
  4. solubility and binding
  5. membrane permeability
  6. vascularity and blood flow
  7. GI motility and emptying
  8. Vehicle
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33
Q

Absorption Factors

For physical state, what effects rate for absorption drug when it is a liquid versus a solid

A

liquid is absorbed faster

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34
Q

Absorption Factors

Why are liquids absorbed faster than solids?

A

it doesn’t have to go through liberation phase like solid does. It is closer to particle size that it needs to be to get absorbed.

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35
Q

Absorption Factors

how does the area of absorbing surface effect absorption?

A

larger surface = more absorbed

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36
Q

Absorption Factors

how does concentration affect absorption?

A

higher concentration of drug gets absorbed more rapidly

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37
Q

Absorption Factors

membrane permeability can be affected by ____.

A

disease

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38
Q

example of disease that affects BBB

A

meningitis

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39
Q

Absorption Factors

What is the vehicle of the drug?

A

how drug is carried- example is cream vs ointment

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40
Q

What is absorption?

A

when drug moves from site of administration to site of “measurement” in body

movement of one area to area of “measurement”

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41
Q

in absorption, what is the step slowing things down?

A

rate limiting step: crossing membranes

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42
Q

drug must be in a dissolved state in order to _______-.

A

penetrate membranes

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43
Q

Oral dosage form issues for absorption

A
  1. Emesis
  2. pH
  3. Food
  4. Other drugs
  5. GI motility
  6. Surface area
  7. dosage form
  8. H20 Solubility
  9. drug at absorption site
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44
Q

Example of other drugs affecting absorption

A

taking antacids with Iron, Iron needs acidic environment to dissolve and get into system

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45
Q

What is delayed release?

A

when you take drug in a solid form, wait a period of time, and then the drug gets released

46
Q

IR release is ________.

A

immediate release

47
Q

SR release is_______.

A

sustained release

48
Q

XR release is_______.

A

extended release

49
Q

SR,CR, and XR release drugs cause what to happen to absorption time?

A

absorption time gets stretched out instead of all of it being absorbed at once

50
Q

CR release is_______.

A

controlled release

51
Q

what is immediate release?

A

taking a standard tablet, as soon as you take it it gets into your system

52
Q

Drug formulation, ionization, size, and solubility affect ____.

A

absorption

53
Q

how can a patient affect absorption?

A 
pH
food,liquid
other meds
gi motility
surgery
54
Q

do intravenous medication skip the absorption phase?

A

yes

55
Q

how does IV drug administration skip absorption phase?

A

it gets automatically inserted into central compartment (blood), it does not need to cross membranes

56
Q

reversible transfer of drug to and from a body compartment/ tissue space

A

distribution

57
Q

is a bound drug considered a free or active drug?

A

no

58
Q

cardiac output, regional blood flow to tissue, tissue volume, and tissue selective binding are things that can affect _____.

A

distribution

59
Q

what is function of efflux pumps?

A

to get something out/ get rid of it

60
Q

p-glycoprotein is an example of an _____.

A

efflux pump

61
Q

function of p-glycoprotein

A

to pump drugs out of cells that aren’t supposed to be there

62
Q

tumor cells produce a lot of this

A

p-glycoprotein

63
Q

problem with p-glycoprotein concerning drugs

A

can be difficult to get drug to pass these to get into cells, a reason why cancer cells are so hard to treat.

64
Q

this allows tissue penetration without crossing the lipid bilayer

A

paracellular transport via capillary membrane

65
Q

what is paracellular transport dependent on?

A

blood flow

66
Q

this is key to protecting and maintaining homeostasis environment in brain

A

blood brain barrier (BBB)

67
Q

a drug leaving brain capillaries has to traverse through _____ and ______.

A

the capillary wall
and
astrocyte membrane

68
Q

these are tightly joined and covered by fatty barrier called the glial sheath (astrocytes)

A

brain capillaries

69
Q

what type of drugs penetrate the BBB poorly?

A

highly ionized

70
Q

what type of drugs penetrate the BBB more rapidly?

A

fat-soluble drugs

71
Q

drugs that penetrate the central nervous system need to be ________ to penetrate the brain and reach their target site

A

lipid soluble

72
Q

What is metabolism?

A

Changing one chemical to another chemical

73
Q

Why does metabolism occur?

A

Trying to metabolize thing so we can get them out of the body

74
Q

are all drugs metabolized?

A

no, Not all drugs are metabolized, some drugs are eliminated unchanged

75
Q

Where does metabolism occur?

A

Most occurs in liver

76
Q

Phase I metabolism phase

A

function to convert lipophilic molecules into more polar molecules

77
Q

Introduces or unmasks a polar functional group in which metabolism phase?

A

Phase I

78
Q

Phase II metabolism phase

A

conjugation reaction to increase polarity

79
Q

__________ is most common of Phase II reactions – adds a glucose-like molecule

A

Glucuronidation

80
Q

Cytochrome P450 enzymes are mostly located in the _____.

A

liver

81
Q

six Cytochrome P450 enzymes that metabolize over 90% of drugs

A 
CYP3A4 – 60%
CYP2C9 – 15%
CYP2C19 – 15%
CYP2E1 – 2%
CYP1A2 – 2%
82
Q

60% drugs metabolized through this pathway

A

CYP3A4

83
Q

A drug may be a ______ for more than one isozyme

A

substrate

84
Q

the drug/molecule that gets metabolized

A

substrate

85
Q

drug/molecule that increases synthesis of one or more CYP isozymes

A

Inducer

86
Q

reduces activity of or competes for isozyme

A

inhibitor

87
Q

drug increases synthesis of isozyme for which it is a substrate

A

Autoinducer

88
Q

metabolism is what kind of rxn?

A

chemical

89
Q

this facilitates the chemical conversion of a substrate (drug) to a metabolite product

A

enzyme

90
Q

this results in increased serum metabolite concentration (or decreased drug concentration)

A

CYP 450 Enzyme Induction

91
Q

When an enzyme ______ is present, the activity of the enzyme is increased which pushes the reaction to the right

A

inducer

92
Q

This results in increased serum drug concentration

A

CYP 450 Enzyme Inhibition

93
Q

When an enzyme _______ is present, the activity of the enzyme is decreased which pushes the reaction to the left

A

inhibitor

94
Q

Drug “A” is substrate of CYP3A4
Drug “B” is an inducer of 3A4
If drug “B” is added to the drug regimen, what would happen to the serum concentration of drug “A”?

A

there would be more metabolite of A

95
Q

Routes of removal of drug from the body:

A

KIDNEY, liver, bile, intestine, lung, milk, dialysis,

96
Q

“artificial kidney” where we remove toxic things synthetically from body

A

Dialysis

97
Q

renal elimination type where there is passive diffusion of free drug, drug can’t be bound to protein. move from capillary to glomerular space

A

Glomerular filtration

98
Q

renal elimination type where there is Active transport, from capillary to PCT, drugs can compete for active transport (e.g. probenecid)

A

Proximal tubular secretion

99
Q

renal elimination type where drug concentration increases as filtrate moves distally, drug may diffuse back into systemic circulation

A

Distal tubular reabsorption

100
Q

What lab tests might help determine renal function?

A

Creatinine, BUN

101
Q

Usually drug interaction are ______ issues

A

metabolism

102
Q

in pediatrics, why should IM be given in lateral thigh vs. buttocks or arm

A

↓ muscle mass in those areas

103
Q

In neonates, why is IV preferable to IM?

A

erratic absorption

104
Q

pediatric metabolism depends on what variables?

A

Drugs mother was on during pregnancy

Age of patient

105
Q

During first few weeks/months why would baby need lower doses

A

metabolic rate is lower

106
Q

During toddler and early childhood, metabolic rate is higher than even at adult so dose would have to be ______.

A

higher

107
Q

A full term newborn has what percent of glomerular filtration rate (GFR) and tubular excretion capacity of an adult

A

33%

108
Q

when does GFR reach adult values

A

6-12 months

109
Q

what is steady state?

A

Concentration when the amount in = the amount out.

110
Q

can you get steady state concentration with just one dose?

A

no

111
Q

What determines how long to steady state?

A

half life

112
Q

what is half life

A

time required to change the amount of drug in the body by one-half during elimination (or during a constant infusion)

MUSC Pharmacology (10 decks)

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