INTRODUCTION TO PHARMACOLOGY - Warner …classpages.warnerpacific.edu/BDupriest/BIO 420/Intro...
Transcript of INTRODUCTION TO PHARMACOLOGY - Warner …classpages.warnerpacific.edu/BDupriest/BIO 420/Intro...
INTRODUCTION TO PHARMACOLOGY
Pharmacology is the study of how chemicals
interact with the body
Endogenous ndash hormones growth factors etc
Exogenous ndash drugs
Two areas of study
Pharmacodynamics
Interaction of chemicals with receptors or enzymes
Pharmacokinetics
Absorption distribution metabolism excretion
1
Pharmacokinetics
ldquoWhat the body does to a drugrdquo
LADME
Liberation
Absorption
Distribution
Metabolism
Excretion
2
Pharmacokinetics
Routes of drug administration
Oral
Sublingual
Intravenous (IV)
Intraperitoneal (IP)
Intramuscular (IM)
Subcutaneous (SC)
Rectal
Epidural
Intracerebroventricular
3
Pharmacokinetics
Liberation
How is a drug released from its delivery vehicle
Pills must dissolve or be broken down
Forms of oral medications
Tablet
Caplet
Liquid
Liqui-Gel
4
Pharmacokinetics
Absorption
How is a drug absorbed into the tissue or
bloodstream
Depends on route of administration
Oral ndash absorbed via gastrointestinal tract goes to liver
Sublingual ndash absorbed via blood vessels under the
tongue bypasses the liver
IV ndash na
IP ndash absorbed via peritoneal mucosae
IM ndash absorbed via muscle lymphatics amp capillaries
Bioavailability how much ingested drug is
actually absorbed
5
For an orally-administered medication
absorption can only occur once which of these
other processes has occurred
A) Distribution
B) Metabolism
C) Liberation
D) Excretion
6
Why does the previous question include the
qualifer ldquoFor an orally-administered
medicationrdquo
7
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
ldquoWhat the body does to a drugrdquo
LADME
Liberation
Absorption
Distribution
Metabolism
Excretion
2
Pharmacokinetics
Routes of drug administration
Oral
Sublingual
Intravenous (IV)
Intraperitoneal (IP)
Intramuscular (IM)
Subcutaneous (SC)
Rectal
Epidural
Intracerebroventricular
3
Pharmacokinetics
Liberation
How is a drug released from its delivery vehicle
Pills must dissolve or be broken down
Forms of oral medications
Tablet
Caplet
Liquid
Liqui-Gel
4
Pharmacokinetics
Absorption
How is a drug absorbed into the tissue or
bloodstream
Depends on route of administration
Oral ndash absorbed via gastrointestinal tract goes to liver
Sublingual ndash absorbed via blood vessels under the
tongue bypasses the liver
IV ndash na
IP ndash absorbed via peritoneal mucosae
IM ndash absorbed via muscle lymphatics amp capillaries
Bioavailability how much ingested drug is
actually absorbed
5
For an orally-administered medication
absorption can only occur once which of these
other processes has occurred
A) Distribution
B) Metabolism
C) Liberation
D) Excretion
6
Why does the previous question include the
qualifer ldquoFor an orally-administered
medicationrdquo
7
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Routes of drug administration
Oral
Sublingual
Intravenous (IV)
Intraperitoneal (IP)
Intramuscular (IM)
Subcutaneous (SC)
Rectal
Epidural
Intracerebroventricular
3
Pharmacokinetics
Liberation
How is a drug released from its delivery vehicle
Pills must dissolve or be broken down
Forms of oral medications
Tablet
Caplet
Liquid
Liqui-Gel
4
Pharmacokinetics
Absorption
How is a drug absorbed into the tissue or
bloodstream
Depends on route of administration
Oral ndash absorbed via gastrointestinal tract goes to liver
Sublingual ndash absorbed via blood vessels under the
tongue bypasses the liver
IV ndash na
IP ndash absorbed via peritoneal mucosae
IM ndash absorbed via muscle lymphatics amp capillaries
Bioavailability how much ingested drug is
actually absorbed
5
For an orally-administered medication
absorption can only occur once which of these
other processes has occurred
A) Distribution
B) Metabolism
C) Liberation
D) Excretion
6
Why does the previous question include the
qualifer ldquoFor an orally-administered
medicationrdquo
7
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Liberation
How is a drug released from its delivery vehicle
Pills must dissolve or be broken down
Forms of oral medications
Tablet
Caplet
Liquid
Liqui-Gel
4
Pharmacokinetics
Absorption
How is a drug absorbed into the tissue or
bloodstream
Depends on route of administration
Oral ndash absorbed via gastrointestinal tract goes to liver
Sublingual ndash absorbed via blood vessels under the
tongue bypasses the liver
IV ndash na
IP ndash absorbed via peritoneal mucosae
IM ndash absorbed via muscle lymphatics amp capillaries
Bioavailability how much ingested drug is
actually absorbed
5
For an orally-administered medication
absorption can only occur once which of these
other processes has occurred
A) Distribution
B) Metabolism
C) Liberation
D) Excretion
6
Why does the previous question include the
qualifer ldquoFor an orally-administered
medicationrdquo
7
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Absorption
How is a drug absorbed into the tissue or
bloodstream
Depends on route of administration
Oral ndash absorbed via gastrointestinal tract goes to liver
Sublingual ndash absorbed via blood vessels under the
tongue bypasses the liver
IV ndash na
IP ndash absorbed via peritoneal mucosae
IM ndash absorbed via muscle lymphatics amp capillaries
Bioavailability how much ingested drug is
actually absorbed
5
For an orally-administered medication
absorption can only occur once which of these
other processes has occurred
A) Distribution
B) Metabolism
C) Liberation
D) Excretion
6
Why does the previous question include the
qualifer ldquoFor an orally-administered
medicationrdquo
7
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
For an orally-administered medication
absorption can only occur once which of these
other processes has occurred
A) Distribution
B) Metabolism
C) Liberation
D) Excretion
6
Why does the previous question include the
qualifer ldquoFor an orally-administered
medicationrdquo
7
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Why does the previous question include the
qualifer ldquoFor an orally-administered
medicationrdquo
7
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Distribution
How is a drug distributed to the various fluid
compartments or tissues of the body
Plasma vs interstitial vs intracellular fluid
Adipose tissue vs lean tissues
Distribution is unequal amp distinct for each drug
ldquoVolume of distributionrdquo ndash theoretical volume a drug
would occupy if it were present in all compartments at
the same concentration as in the plasma
8
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
ldquoVolume of distributionrdquo is based MOSTLY onhellip
A) how much blood a patient has
B) how much drug was in a particular pill
C) how soluble a particular drug is in lipids
vs water
9
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
True or false The volume of distribution of a
drug may be larger than the total volume of the
patient
A) True
B) False
10
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Metabolism
Is a drug chemically modified by the body If sohellip
Are the metabolites more or less active
Are the metabolites safer or more toxic
Can the metabolites be more easily excreted
Which tissues metabolize the drug
What enzyme systems or other reactions are used to
metabolize the drug
11
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Metabolism
Phase I reactions
Liver
Cytochrome P450 (cyp450) enzymes
Eg Oxidation reduction hydrolysis (de)cyclization
Often produce active metabolites
First-pass effect
Phase II reactions
Liver and kidney
Addition of polar functional groups
Usually produce non-functional metabolites for excretion
Eg Glucuronidation glutathione conjugation
12
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Metabolic clearance of drugs hormones
Metabolized into non-active form
Bound to cells amp degraded recycled
Excreted
These processes are not mutually exclusive
Drugs can be metabolized to inactive metabolites then
excreted
13
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Metabolic clearance of drugs hormones
Rate of removal depends on solubility
Peptide hormones
Degraded in blood or tissues
Cleared rapidly (seconds to minutes)
Steroid hormones
Bounds to plasma proteins
Cleared slowly (minutes to days)
14
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Drug Hormone Clearance
Metabolic clearance rate (MCR)
Rate of disappearance from plasma
Infuse at increasing rate until plasma concentration
reaches steady-state
Infusion rate = rate of disappearance
Concentration of hormone in plasma
15
MCR (mLmin) = rate of hormone disappearance (ngmin)
Concentration of hormone (ngmL)
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacokinetics
Excretion Elimination
Urine
Feces
Breath
Skin
16
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Metabolic clearance rate refers tohellip
A) How fast kidneys produce urine
B) How much drug is filtered by the kidneys
C) A theoretical volume of plasma that can be
100 cleared of drug in a particular amount of
time
17
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacodynamics
ldquoWhat a drug does to the bodyrdquo
Drug (ligand)-receptor interactions
Receptor types ndash membrane vs intracellular
Enzymes amp structural proteins can act as drug ldquoreceptorsrdquo
Signal transduction pathways
Enzyme-based biochemical pathways
18
L + R L R
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacodynamics
Potential actionsroles of drugs
Agonist
Stimulating action vs depressing action
Full or partial agonist
Antagonist
Direct beneficial chemical reaction
Direct harmful chemical reaction
19
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacodynamics
Dose-response curves
Increased [drug] increased effect
EC50 (effective dose yielding 50 max effect)
Curve shifts
Upward ndash higher efficacy
Leftward ndash higher potency (sensitivity)
20
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacodynamics
21
0 50 100 1500
25
50
75
100
125
LPO AdLib (n=15)
NPO AdLib (n=11)
NPO FR (n=5)
LPO FR (n=8)
KCl (mM)
Ten
sio
n (
mN
mm
)
01 1 10 10
010
00
1000
0
1000
00
0
20
40
60
80
100
120
140
160
NorEpi (nM)
Ten
sio
n (
mN
mm
)
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
A leftward shift of a dose-response curve
indicates that a systemhellip
A) is more senstive to a particular ligand
B) is less sensitive to a particular ligand
C) has a higher concentration of ligand
C) has a lower concentration of ligand
22
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Pharmacodynamics
Beneficial actions of drugs must be
weighed against unintended harmful
effects
Side effects
Therapeutic window
The range of doses which provide benefits
without producing toxicity
Varies for each drug and may vary between
individuals
23
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
True or false Medications with side effects are
not approved by the FDA
A) True
B) False
24
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Measurement of Hormone Concentration
Radioimmunoassay
Use specific antibody to detect hormone
Mix radioactive ldquotracerrdquo hormone antibody and
sample together
Competitive assay [Ab] is lower than combined
tracer and endogenous [hormone]
Remove all unbound mixture leaving Ab bound
to either tracer or endogenous hormone
High [endogenous hormone] low tracer
Low [endogenous hormone] high tracer
25
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Measurement of Hormone Concentration
Radioimmunoassay
Measure radioactivity of remaining sample
compare to standard curve
Fig 74-9 26
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Measurement of Hormone Concentration
ELISA (enzyme-linked immunosorbent
assay)
Coat sample wells with antibody
Add test sample
Add antibody conjugated to enzyme
Add enzyme substrate
Color development
indicates presence of
test substance
concentration
determined by dilution
factor amp comparison to
standard curve 27
Fig 74-10
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
Mouse ICAM-1 ELISA Standard Curve
httpswwwthermofishercomordercatalogproductEMICAM1
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
What kind of molecule is used as a ldquomolecular
toolrdquo to measure how much of a particular
substance a sample has
A) Protein
B) Receptor
C) DNA
D) Antibody
29
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30
RIA standard curves have a negative slope
ELISA standard curves are positive Why are
they different
30