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PHARM 2-EXAM 1 (kinetics/dynamics/renal) > Kinetics > Flashcards

Kinetics Flashcards

1
Q

This route of drug administration is used to inject drugs directly into the CSF

A

Intrathecal

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2
Q

A parenteral route with a slower onset than IV. Vasoconstrictors may be administered here to reduce the area of action of another drug

A

Subcutaneous

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3
Q

What is the definition of absorption?

A

It is the site of administration to the bloodstream

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4
Q

When dealing with absorption, the rate & efficiency is dependent on

A

The route, which is COMPLETE for IV drugs

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5
Q

When drugs are too big or when they are charged, they often need this in order to move

A

An active transport (carrier protein)

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6
Q

What is ionization?

A

The process of gaining a positive or a negative charge

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7
Q

An Acid tends to _____ a proton

A Base tends to ______a proton

A

Acid- donates/releases

Base- accepts/absorbs

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8
Q

Ionization is dependent on

A

the pH of the solution & the pKa of a drug

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9
Q

What do we know when the pH and the pKa are the same?

A

Half of the drug is ionized

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10
Q

What type of drug CANNOT move freely?

A

Ionized

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11
Q

What type of drug can move through the membranes?

A

Non-ionized

Uncharged

Lipid Soluble

Free

Unbound

Active

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12
Q

What is the ACID equation?

A

HA<–> H+ + A-

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13
Q

Of the ACID equation, which side is NOT charged?

A

HA side

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14
Q

Most drugs are

A

Weak acids/bases, which partially dissociates

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15
Q

What is the BASE equation?

A

B + H+ <–> BH+

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16
Q

What is another name for pKa?

A

Dissociation constant

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17
Q

The pKa measures

A

The strength of interaction of compounds with a proton

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18
Q

The lower the pKa, the

A

Stronger the acid

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19
Q

When computing the acid/base problems, what are you comparing?

A

The pH to the pKa

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20
Q

When the pH is below the pKa,

A

More drug will be in the ionized form

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21
Q

When the pH is above the pKa,

A

There will be less ionization

More NON-ionization

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22
Q

Are Ionized drugs charged or uncharged?

A

Charged

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23
Q

Ionized drugs are (active/inactive)

Ionized drugs are (lipophilic/hydrophilic)

A

INACTIVE

HYDROPHILIC

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24
Q

Ionized drugs are cleared how?

A

They are excreted by the kidneys

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25
Q

Which form is more polar? Unionized or Ionized form?

A

Ionized

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26
Q

The unionized form of a drug is _______ & _______

A

Active & Lipophilic

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27
Q

Unionized drugs go though

A

Hepatic metabolism

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28
Q

What happens when you place an ACID into a BASIC solution?

A

Proton donation

ACIDIC DRUG becomes highly ionized

Cleared & not active

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29
Q

What happens when you place a BASE into an ACIDIC solution?

A

Proton acceptance

BASIC DRUG becomes ionized

Cleared & not active

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30
Q

What happens when you add an acid to an acidic solution?

A

Drug keeps their protons & is unionized

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31
Q

What happens when you add a base to a basic solution?

A

Drug keeps protons & is unionized

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32
Q

What factors affect absorption?

A

Blood Flow

Drug Solubility

Route

Surface Area

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33
Q

Increased resistance means

A

Decreased flow

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34
Q

Which absorption route is the slowest? The fastest?

A

Slow-GUT

Fast-LUNGS

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35
Q

When is bioavailability 1 (100%)?

A

When a drug is given IV

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36
Q

What is bioavailability?

A

A drug fraction that reaches systemic circulation, chemically unchanged

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37
Q

What influences bioavailability?

A

Chemical stability & formulation of the drug

Drug solubility

First pass metabolism

Route

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38
Q

What is distribution?

A

When a drug leaves the site of where it was administered & enters the plasma/cell/tissues

Drug moves from an area of high concentration & disperses throughout the body system in an even more dilute form

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39
Q

What factors influence distribution?

A

Blood flow

Capillary permeability

Chemical structure

Protein binding

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40
Q

What is the most active/common protein for binding?

A

Albumin

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41
Q

What happens once a drug becomes bound?

A

It is now trapped, becoming inactive

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42
Q

What can a drug do when it is not bound and is freely moveable?

A

Can enter tissues (distribute) & is considered pharmacologically active, causing more effect in the body

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43
Q

What has the strongest affinity?

A

Anionic drugs (weak acids) & Hydrophobic

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44
Q

What has the weakest affinity?

A

Basic & neutral drugs (Hydrophilic)

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45
Q

What decreases albumin capacity?

A

Liver damage

Elderly

Kidney damage

Malnourished

Pregnancy

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46
Q

A 70kg person has how much TBW?

A

42L

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47
Q

Of the 42L of total body water, how mush is intracellular & extracellular?

A

Intracellular- 28L

Extracellular- 14 L
10L interstitial; 4L plasma

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48
Q

Central compartments include…

A

Lungs

Endocrine Glands

Brain

Heart

Kidneys

Liver

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49
Q

Peripheral compartments include

A

Skin

Fat

Muscle

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50
Q

What is the equation for Volume of Distribution?

A

Vd=Amount of drug/Desired plasma concentration

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51
Q

Vd tell us…

A

How well/quickly a drug will quickly distribute, free & unbound in the plasma & interstitial fluid

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52
Q

The greater the Vd,

A

The larger the volume

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53
Q

When the Vd is low,

A

It means the drug does not move well

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54
Q

When the Vd exceeds total body water, it means the drug is…

A

Lipophilic

Non-ionized

55
Q

What dose will be required when Vd exceeds total body water/

A

A higher dose will be required to reach Cp (plasma concentration)

56
Q

When the Vd is LESS than total body water, the drug is considered

A

HYDROPHILIC (water loving) and a LOWER dose is required

57
Q

Vd is influenced by

A

Characteristics of the drug & patient

Elimination

Distribution

58
Q

Increasing the Vd will…

A

Reduce the drug in the plasma & increase half-life

59
Q

A larger Vd is harder to get rid of because

A

You need to rid the body of the drug in the plasma

60
Q

When free drug is available & highly protein bound, how does this affect Vd?

A

Vd will be increased

61
Q

Vd can help us determine

A

How much drug we need to reach a specific plasma concentration (Cp)

62
Q

Will your loading dose increase or decrease with a large Vd?

A

Increase

63
Q

What is the equation for loading dose?

A

Loading dose= Vd x Desired Cp/ Bioavailability

64
Q

What is the goal of metabolism?

A

The main goal is to take an active drug and turn it into its inactive form for excretion

65
Q

What happens to a drug after it is metabolized

A

It is no longer in its active, lipid soluble state. It is now inactive & water soluble

66
Q

What are the 2 exceptions for metabolism?

A

An Active metabolite

A prodrug

67
Q

What is a prodrug?

A

It is when a drug is given, but only becomes active once it is metabolized into its active form, meaning the original drug was inactive

68
Q

What is an active metabolite?

A

The original drug and the active metabolite will have similar therapeutic effects

69
Q

What are common sites for metabolism?

A

Liver

Plasma

Kidneys

Lungs

GIT

70
Q

What are the 3 phases of metabolism?

A

Modification

Conjugation

Elimination

71
Q

What happens in the modification stage?

A

The drugs water solubility is increased and may be excreted or prepped for Phase II

72
Q

Conjugation involves…

A

Increasing the drugs water solubility

73
Q

Elimination in the metabolism stage includes

A

Drug transportation across membranes by an ATP-dependent carrier protein

Kidney, Liver, GIT

74
Q

What happens in the Phase I metabolism pathway?

A

Oxidation

Reduction

Hydrolysis

75
Q

Oxidation is ____ of an electron

Reduction is ___ of an electron

A

Oxidation-Removal

Reduction- Add

76
Q

Hydrolysis is…

A

Adding water to split a drug apart, involving plasma or tissue esterases

77
Q

What occurs in the Phase II metabolism pathway?

A

Conjugation, where there is addition of a polar & water soluble substrate (covalent bond)

78
Q

Microsomal enzymes are responsible for

A

Biotransformation in the liver

79
Q

Microsomes are

A

Endoplasmic reticulum fragments from tissue breakdown

80
Q

Cytochrome is an

A

Iron-containing heme bound to a protein

81
Q

What is the primary system for the liver to metabolize sybstances

A

Microsomal enzymes

CYP=450

82
Q

Enzyme Inducers…

A

Increase Clearance

Faster breakdown

Decrease drug plasma level

May need dose increased

83
Q

Enzyme Inhibitors…

A

Decrease Clearance

Slower breakdown

Increase drug plasma levels

May need dose decrease

84
Q

Kinetics of Metabolism is effected by

A

Blood flow

Amount of drug given

Concentration of the drug

Efficiency of metabolizing system

Organ capacity

85
Q

Which kinetic metabolism method involves a constant AMOUNT of drug metabolized per time, has MORE DRUG than enzymes, & is SATURATED?

A

Zero-Order

86
Q

Which kinetic metabolism method involves a constant FRACTION metabolized per time, MORE ENZYME than drug, blood flow dependent, & has NO saturation?

A

First order

87
Q

What are 3 types of plasma metabolism?

A

Hydrolysis (common)

Plasma enzymatic reactions

Hoffman elimination

88
Q

Plasma enzymatic reactions involve…

A

No enzymatic induction, meaning that it will not be influenced by other drugs that will increase enzymes

89
Q

Hoffman elimination is the

A

Spontaneous chemical elimination reaction, which depends on pH & body temperature

It is important to keep the patient away from acidosis & hypothermia

90
Q

Elimination is drug removal from the_____

Excretion is drug removed from the _______

A

Plasma; Body

91
Q

Clearance is

A

The volume of plasma that is completely cleared of a drug per unit of time

92
Q

Clearance is dependent upon

A

Efficiency of the drug being delivered (blood flow) & drug removal (extraction)

93
Q

Clearance is directly related to

A

Organ blood flow

Extraction Ratio

Drug dose

94
Q

Explain extraction ratio

A

Efficiency of an organ removing a drug from the plasma, entering the organ, & it being broken down

95
Q

Clearance is indirectly related to

A

Drug half-life

Drug concentration in the central compartment

96
Q

The greater you clear a drug,

A

The shorter the half-life

97
Q

The greater the clearance, the

A

Lower the concentration

98
Q

What is the extraction ratio equation?

A

Extraction ratio=arterial concentration-venous concentration/arterial concentration

99
Q

When the extraction ratio is >70%, metabolism & clearance are

A

Flow-limited (flow dependent)

100
Q

High extraction ratio is dependent on

A

Free (unbound) drug

101
Q

High extraction ratio is proportional to

A

Change in hepatic blood flow

102
Q

Low extraction ratio <30% is independent of

A

Liver blood flow

103
Q

In low extraction ratio, metabolism & clearance are

A

Capacity limited (capacity dependent)

104
Q

Changes in protein binding affect clearance in

A

Low capacity ratio states

105
Q

Volume of plasma cleared of a drug is determined by…

A

A drugs polarity

pH of glomerular filtrate

Hydrophilic-excreted unchanged (water soluble)

Lipophilic- biotransformed (water soluble)

106
Q

Polar drugs will

A

NOT be reabsorbed

107
Q

When and where will unionized (lipid soluble) drugs (may) be reabsorbed?

A

In the distal tubule depending on urine pH & flow rate

108
Q

When a patient has acidic urine, there is reabsorption of____ & excretion of________

A

Reabsorb acidic drugs

Excrete basic drugs

109
Q

When a patient has alkaline (basic) urine, there is reabsorption of _______ & excretion of _______

A

Reabsorb basic

Excrete acidic

110
Q

When should you adjust your dose of medication?

A

When >50% of the drug is renally cleared

When renal function is decreased 50% of normal

111
Q

Definition of half life

A

It is the time required to remove 50% of a drug from the BODY following a rapid IV injection

112
Q

What is directly related to half life?

Indirectly related?

A

Direct- Vd

Indirectly- Clearance

113
Q

Approximately, how many half lives does it take to eliminate ~97% of a drug?

A

5

114
Q

The more a drug distributed, the longer the

A

Half life

115
Q

Half life equation

A

Half life= Vd/ Rate of Clearance

116
Q

Half life is Increased by…

A

Decreased RBF, extraction ratio & metabolism

Displacement of drug from albumin (free)

117
Q

Cp (plasma concentration) is influenced by…

A

Distribution

Redistribution

Excretion

Metabolism

118
Q

One compartment model is based on

A

Input of drug dosage/interval/rate

Output of constant elimination

119
Q

Multi- compartment model is based on

A

Concentration gradient from central compartment (plasma) to peripheral (tissues)

120
Q

Multi- compartment phases include

A

Rapid

Slow

Terminal

121
Q

Lipophilic drugs will have a larger Vd, causing this on a chart

A

A steeper slope, equalling a rapid reduction in Cp

122
Q

On the graph (slide 65), the flattened slope of B is representing

A

Redistribution & elimination

123
Q

Redistribution involves

A

A drug leaving the tissues & re-entering the plasma

124
Q

In the 3 compartment model, drug movement is dependent on

A

Vd

Plasma & tissue concentrations

Rate constants (k)

Half-lives

Clearance

125
Q

What is the rate constants (k)?

A

The speed at which a drug molecule moves between compartments or is eliminated

126
Q

Define steady state

A

It is measuring how much of a drug coming in equals how much is coming out

127
Q

In steady state, what must equal?

A

Infusion rate/dosing interval must equal clearance

128
Q

How many half lives does it take to reach steady state?

A

4-5

129
Q

What is half time?

A

The time it takes for 50% of a drug to be removed from the plasma during elimination

130
Q

Half time measures a

A

Constant fraction of drug being eliminated & is only applicable in a 1 compartment model

131
Q

What is context sensitive half time?

A

It is the time required for Cp (plasma concentration) to decline by 50%, following a steady state IV infusion

132
Q

What is the “context” in CSHT?

A

The duration

133
Q

What is context-sensitive EFFECT site elimination?

A

Tells us how long it takes to get the drug out of the effect site

PHARM 2-EXAM 1 (kinetics/dynamics/renal) (4 decks)

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