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APEX Pharmacology > PHARMACOLOGY-pharmacokinetics > Flashcards

PHARMACOLOGY-pharmacokinetics Flashcards

1
Q

Define loading dose

Loading dose equation

A

The amount of drug required to achieve a therapeutic plasma concentration quickly

Loading dose = (Vd x desired Cp)/bioavailability

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2
Q

Describe volume of distribution

A

The relationship between the administered drug dose and the resulting plasma concentration

Theoretical measure of how drugs are distributed in the body

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3
Q

Define concentration as it pertains to pharmacokinetics

A

The measure of the amount of drug in a given volume

A drug is most concentrated before it is given

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4
Q

At what Vd is a drug considered lipophilic

A

When Vd exceeds total body water

>0.6 L/kg or >42 L

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5
Q

How does a loading dose correlate with Vd

A

The higher the Vd, the higher the loading dose that must be given to achieve effect

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6
Q

Describe the breakdown of body water distribution in a 70-kg patient

Total body water =

  • ECF =
  • -Plasma volume =
    • Interstitial fluid =
  • ICF = 28 L
A

Total body water = 42 L

  • ECF = 14 L (33%)
  • -Plasma volume = 4 L (10% TBW/29% of ECF)
    • Interstitial fluid = 10 L (24% TBW/71% ECF)
  • ICF = 28 L (67%)
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7
Q

Define clearance in relation to pharmacokinetics

A

The volume of plasma cleared of a drug per unit time

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8
Q

What 3 variables is clearance directly proportional to

A

Drug dose
Extraction ratio
Blood flow to target organ

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9
Q

What 2 variables is clearance inversely proportional to

A

Half-life

Drug concentration in central compartment

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10
Q

How can a stead-state concentration of a drug in plasma be achieved

A

The infusion rate or dose interval (time) must equal the rate of drug clearance

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11
Q

How many half-times before stead-state is achieved

A

5

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12
Q

How can steady-state be achieved fast in drugs that have long half-lifes

A

Administer loading dose

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13
Q

What are 3 major routes drugs are eliminated

A

Liver
Kidney
Organ independent (Hoffman elimination or ester hydrolysis in plasma)

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14
Q

Describe the plasma concentration curve as it relates to the multi-compartment model
i.e. alpha and beta phase of curve

A

Alpha phase represent distribution of drug from central compartment (plasma) to the peripheral compartment (tissues)

  • This represents Vd
  • steeper slope = more lipophilic drug

Beta phase represents elimination from the central compartment (plasma)

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15
Q

What does the beta portion of the plasma concentration curve represent

A

Elimination

As plasma concentration declines due to elimination, drug is redistributed from tissues following the concentration gradient

flatter slope represents elimination from the central compartment

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16
Q

Define rate constant pertaining to pharmacokinetics

A

Describes the speed at which a reaction occurs, how fast a molecule moves between compartments

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17
Q

Define elimination half-life

A

The time it takes for 50% of the drug to be eliminated from the body after IV injection

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18
Q

When is a drug considered fully cleared from the plasma

A

When 96.9% has been cleared or 5 half-times

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19
Q

What is the difference between elimination half-life and context-sensitive half-time.

A

Context-sensitive half-time takes the duration of drug administration into account

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20
Q

Define context-sensitive half-time

A

The time required for the plasma concentration to decline by 50% after an infusion is stopped

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21
Q

What is elimination half-TIME

A

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

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22
Q

How does ionization affect medications in the body

A

It’s when a molecule gains a positive or negative charge affecting the ability to diffuse through lipid membranes

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23
Q

How do drugs that are weak acids or bases react in plasma/water

A

Weak acids will donate a proton to water

weak bases will accept a proton from water

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24
Q

Definition of a drug’s pKa

A

When the pKa equals the pH where 50% of the drug is ionized and the other 50% is non-ionized

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25
Q

Describe the difference between acids and bases

A

acids DONATE a proton
HA+ H+ + A

Bases ACCEPT a proton
B- + H+ BH

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26
Q

What does pH measure

A

the concentration of hydrogen ions in an aqueous solution determining the acidity or alkalinity of a solution

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27
Q

What is the difference between strong acids and bases

A

when strong acids or bases in water, they will completely dissociate

When a weak acid or base is in water, they will partially dissociation leaving a fraction of ionized and non-ionized acid/base

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28
Q

What 2 factors is ionization dependent on

A

pH of a solution

pKa of a drug

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29
Q

What does the level of pKa indicate

A

How much a molecule wants to behave like an acid
low pKa = amazing acid
high pKa = terrible acid

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30
Q

What is the Henderson-Hasselbach equation

A

pH = pKa + log([base]/[conjugate acid])

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31
Q

According to the henderson-hasselbach equation, how does a basic drug act in an acidic environment

A

It predicts that ionized fraction (conjugate acid) will dominate the base

More ionized than non-ionized

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32
Q

How does a drug that is a weak base act in a weak base solution
Is it lipid-soluble or not?

A

more NON-IONIZED than ionized

Lipid-soluble

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33
Q

How does a drug that is a weak base act in an acidic solution
Is it lipid-soluble or not?

A

More IONIZED than non-ionized

Water-soluble NOT lipid-soluble

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34
Q

How does a drug that is a weak acid act in an acidic solution
Is it lipid-soluble or not?

A

More NON-IONIZED than ionized

YES lipid-soluble

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35
Q

How does a drug that is a weak acid act in a basic solution

Is it lipid-soluble or not?

A

More IONIZED than non-ionized

NOT lipid-soluble – water soluble

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36
Q

How does ionization affect a drugs activity

A

It determines if a drug can pass through cell membranes (lipophilic)

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37
Q

How are drugs compounded to become weak acids or bases

A

ACIDS:
combined with Na+, Ca++, Mg++

BASES:
combined with Cl- or SO4(2-)

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38
Q

How does ionization affect solubility.

A

ionization affects ability to be lipophilic vs hydrophilic

Ionized in water

  • hydrophilic
  • lipophobic

Non-ionized lipid

  • lipophilic
  • hydrophobic
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39
Q

How does ionization alter the pharmacologic effect

A 
Ionized = not active
Non-ionized = active
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40
Q

How does ionization affect hepatic biotransformation

A

Ionized = less likely to transform

Non-ionized = more likely to transform

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41
Q

How does ionization affect renal elimination

A

Ionized = More likely to eliminate

Non-ionized = less likely to be eliminated

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42
Q

How does ionization affect diffusion across the following barriers?
BBB
GI tract
Placenta

A

Ionized

  • No
  • No
  • No

Non-ionized

  • Yes
  • Yes
  • Yes
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43
Q

In what situations dose the ionized fraction predominate

A

-Molecule is a weak base and the solution pH < pKa of drug
(base added to an acid)

-Molecule is a weak acid and the solution pH > pKa of drug
(acid added to a base)

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44
Q

In what situations does the non-ionized fraction predominate

A

-Molecule is a weak base and solution pH > pKa of drug
(base added to basic soln)

-Molecule is weak acid and solution pH < pKa of drug
(acid added to acidic soln)

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45
Q

How does being pregnant affect ion trapping

A

Fetal pH < maternal pH
A basic drug in a basic solution has more non-ionized molecules and can pass through the placenta

Once the basic drug is in the acidic fetus it becomes more ionized and cannot pass back through the placenta

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46
Q

Which local anesthetic is most likely to cross the placenta and undergo fetal ion trapping

A

Lidocaine

Chloroprocaine is least likely to be ion-trapped

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47
Q

What plasma proteins can drugs bind to?

A

albumin
alpha 1-acid glycoprotein
beta-globulin

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48
Q

Which plasma protein primarily binds with acidic drugs

A

Albumin

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49
Q

Which plasma protein primarily binds with basic drugs

A

Alpha 1-acid glycoprotein

Beta-globulin

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50
Q

What do drugs bound to plasma proteins do?

A

nothing

They are not available to bind to any receptors or to be eliminated

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51
Q

What are 5 conditions that can decrease protein concentration

A 
Liver disease
Renal disease
Old age
Malnutrition
Pregnancy
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52
Q

When plasma protein levels are decreased, what is the effect on the drug

A

The unbound drug fraction is increased

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53
Q

What is the liver’s role in plasma proteins. How is this affected with liver disease

A

The liver synthesizes plasma proteins

Liver disease will decrease plasma protein production

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54
Q

Which plasma protein is most plentiful

A

Albumin

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55
Q

What charge does albumin carry

A

negative

which is why it primarily binds to acidic drugs

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56
Q

What is the half-life of albumin

A

3 weeks

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57
Q

What 5 factors increase alpha 1-acid glycoprotein concentration

A 
Surgical stress
Myocardial infarction
Chronic pain
Rheumatoid arthritis
Advanced age
58
Q

If a drug is 98% protein bound then becomes 96% protein bound, what percent increase has become unbound
What is the formula

A

100%

Percent change = ([NEW % - OLD%]/old%) x 100%

([4-2]/2) x 100% = 100%

59
Q

If a drug is 50% protein bound then becomes 48% protein bound, what percent increase has become unbound?

What is the formula?

A

4% increase unbound

Percent change = ([NEW % - OLD%]/old%) x 100%

([52-50]/50) x 100 = 4%

60
Q

What 3 physiologic factors decrease plasma protein

A
  1. Reduced synthetic function (liver dz, malnutrition)
  2. Increased protein excretion (renal dz)
  3. Altered distribution (3rd trimester)
61
Q

How is volume of distribution related to the degree of plasma protein binding

A

INVERSELY related

higher Vd = decreased degree of protein binding

Lower Vd = increased degree of protein binding

62
Q

What does an increased unbound fraction of drug clinically look like

A

increased potency

63
Q

How is metabolism and elimination affected by highly protein-bound drugs

A

Both are slower

64
Q

What drug characteristic increases the risk for adverse effects with increased unbound fraction

A

When the drug has a narrow therapeutic index

65
Q

Define zero order kinetics

A

Constant amount of drug is metabolized per unit time

66
Q

Define first order kinetics

A

constant FRACTION of drug is metabolized per unit time

67
Q

What 2 factors does the rate of metabolism for most drugs depend on

A
  1. The concentration of a drug at the site of metabolism

2. The intrinsic rate of the metabolic process

68
Q

What influences the concentration of a drug at the site of metabolism

A

Blood flow to the site of metabolism

69
Q

What influences the intrinsic rate of the metabolic process

A

Genetic and enzyme activity

70
Q

What does Zero order kinetics describe

A

Situations where there is more drug than enzyme
So the drug metabolizes at a constant AMOUNT per unit time
drug > enzyme (saturation)

71
Q

What are examples of drugs following zero order kinetics

A

aspirin, phenytoin, alcohol, warfarin, heparin, theophylline

72
Q

What does first order kinetics describe

A

Situations where there is less drug than enzyme
The enzyme will metabolize a constant FRACTION per unit time

drug < enzyme (non-saturation)

73
Q

What are the 3 phases of drug metabolism

A

Phase 1 = modification (oxidation, reduction, hydrolysis)
Phase 2 = conjugation
Phase 3 = excretion

74
Q

Define metabolism and what is the primary metabolic organ

A

Biotransformation via an enzymatic process that alters the drugs chemical structure allowing it to be eliminated or active

Primary organ = liver

75
Q

What hepatic system metabolizes molecules

A

Hepatic microsomal enzymes of the P450 system

76
Q

What are 4 lesser sites of metabolism

A

Kidneys, plasma, lung, intestines

77
Q

What is the purpose of drug metabolism

A

To change a lipid-soluble, pharmacologically active compound into a water-soluble, pharmacologically inactive byproduct for elimination

78
Q

Define the 3 examples of phase 1 reactions.

A
  1. Oxidation = removal of electron from compound
  2. Reduction = addition of electron to compound
  3. Hydrolysis = adds H2O to a compound to split it apart (usually an ester)
79
Q

What is the purpose of phase 1 reaction

A

modification of a compound (via oxidation, reduction, or hydrolysis) preparing it for phase 2 reaction

80
Q

What occurs during a phase 2 reaction and how

A

Conjugation of a highly polar, water-soluble substrate to the molecule
This makes the drug inactive and ready for elimination

81
Q

What occurs during a phase 3 reaction

A

Involvement of ATP dependent carrier proteins that transport a drug across a cell membrane
These proteins are present in the kidney, liver, and GI tract

82
Q

Where are microsomal enzymes of the P450 system located

A

In smooth endoplasmic reticulum of the liver. Some are present in the kidney and GI tract

83
Q

What metabolic reactions occur in the plasma

A 
Hofmann elimination (pH & temperature dependent)
Hydrolysis via non-specific plasma esterases and pseudocholinesterase
84
Q

Describe how water solubility affects a molecules ability to be eliminated

A
  • Molecules that are more water soluble increases ionization
  • Ionization decreases the Vd
  • This increases delivery to kidneys for elimination.
  • Since the molecule is ionized, it will be eliminated in the urine instead of being reabsorbed from the renal tubule.
85
Q

What happens to lipid-soluble drugs in the renal tubules

A

They are reabsorbed and continually circulated until metabolized into water-soluble compounds

86
Q

How are prodrugs treated by metabolism

A

Prodrugs are inactive molecules that are converted into pharmacologically active molecules via metabolism

87
Q

Where do most phase 1 biotransformation’s occur

A

By hepatic microsomal enzymes of the P450 system

88
Q

What are 5 common substrates for phase 2 conjugation

A 
Glucuronic acid
Glycine
Acetic acid
Sulfuric acid
Methyl group
89
Q

What is significance of enterohepatic circulation.

Name 2 drugs that can undergo enterohepatic circulation.

A

Some conjugated compounds are excreted in the bile and become REACTIVATED in the intestines. They are then reabsorbed into the systemic circulation
i.e. diazepam and warfarin

90
Q

Define perfusion-dependent hepatic eliminiation

A

Drugs with high extraction ratios are dependent on liver blood flow for extraction

Hepatic BF&raquo_space; enzymatic activity
therefore, increased BF = increased clearance
decreased BF = decreased clearance

91
Q

Define capacity-dependent hepatic elimination

A

Drugs with low extraction ratios (< 0.3) clearance is dependent on the liver’s ability to extract the drug from the blood
Blood flow minimally affects clearance

Amount of enzyme influences the liver’s ability to remove drug. Enzyme dependent

92
Q

What is an extraction ratio

A

The measure of how much drug is delivered to the clearing organ vs how much drug is removed by that organ

93
Q

What is an extraction ratio

A

The measure of how much drug is delivered to the clearing organ vs how much drug is removed by that organ

94
Q

What does an extraction ratio (ER) of 1.0 vs 0.5 mean

A

ER 1.0 = 100% of the drug delivered to the clearing organ is removed
ER 0.5 = 50% of the drug delivered to the clearing organ is removed

95
Q

For drugs with a high hepatic extraction ratio (>0.7), what is clearance dependent on?
Examples of drugs with high ER?

A

Liver blood flow (PERFUSION dependent)

Fentanyl, sufentanil, morphine, ketamine, propofol

96
Q

For drugs with a low hepatic extraction ratio (<0.3), what is clearance dependent on?
Examples of drugs with low ER?

A

The ability of the liver to extract the drug from the blood (CAPACITY dependent)

Rocuronium, diazepam, methadone

97
Q

What are orally administered drugs with a high extraction ratio subjected to?

A

First-pass metabolism

98
Q

How is capacity-dependent hepatic clearance altered

A

Enzyme induction = increased clearance

Enzyme inhibition = decreased clearance

99
Q

Examples of drugs that have low hepatic ER

A 
ENZYME DEPENDENT
Rocuronium
Diazepam
Lorazepam
Methadone
Thiopental
Theophylline
Phenytoin
100
Q

Examples of drugs that have intermediate hepatic ER

A

Midazolam
Vecuronium
Alfentanil
Methohexital

101
Q

Examples of drugs with high hepatic ER

A 
FLOW DEPENDENT
Fentanyl
Sufentanil
Morphine
Meperidine
Naloxone
Ketamine
Propofol
Lidocaine
Bupivacaine
Metoprolol
Propranolol
Nifedipine
Diltiazem
Verapamil
102
Q

Describe the effect of drugs that undergo enterohepatic circulation

A

Prolong duration of effect

103
Q

What is the most important cytochrome P450 enzyme. Why?

A

CYP 3A4

It metabolized 50% of drugs we administer

104
Q

What is an enzyme inducer? Why is it significant?

A

Exogenous chemical that can stimulate the synthesis of additional enzymes

This increases drug clearance reducing t1/2. Less circulating drug available and increased dose may be required

105
Q

Examples of enzyme inducers

A 
Ethanol
Tobacco 
Phenytoin
Barbiturates
Rifampin
Carbamazepine
106
Q

What is an enzyme inhibitor?

Why is it significant?

A

Exogenous chemicals that compete for binding sites on the enzyme

This reduces drug clearance, increasing drug plasma levels. Decreased doses may be required

107
Q

Examples of common enzyme inhibitors

A 
SSRIs
Omeprazole
Grapefruit
Cimetidine
Erythromycin
Ketoconazole
108
Q

List 6 inducers of CYP 3A4

A 
(increase clearance)
Ethanol
Rifampin
Barbiturates
Tamoxifen
Carbamazepine
St. John's Wort
109
Q

List 6 inhibitors of CYP 3A4

A 
(decrease clearance)
Grapefruit juice
Cimetidine
Erythromycin
Erythromycin
Azole antifungals
SSRIs
110
Q

Which opioid substrates are cleared by CYP3A4

A

Fentanyl
Alfentanil
Sufentanil
Methadone

111
Q

Which benzodiazepine substrates are cleared by CYP 3A4

A

Midazolam

Diazepam

112
Q

Which local anesthetics are cleared by CYP 3A4

A

Lidocaine
Bupivacaine
Ropivacaine

113
Q

Which drug is an important CYP 2D6 inducer

A

(increased clearance)

Disulfiram

114
Q

Which drugs are CRP 2D6 inhibitor

A

(decreased clearance)
Isoniazid
SSRIs
Quinidine

115
Q

What are examples of drugs utilizing CYP 2D6 clearance

A

Codeine = morphine
Oxycodone
Hydrocodone

116
Q

Which compounds are CYP 1A2 inducers

A

(increased clearance)
Tobacco
Cannabis
Ethanol

117
Q

Which drugs are CYP 1A2 inhibitors

A

(decrease clearance)
Erythromycin
Ciprofloxacin

118
Q

What 2 factors determine the renal clearance of a drug

A

Drug polarity

pH of the ultrafiltrate

119
Q

How is glomerular filtration affected by highly protein-bound drugs

A

It isn’t
These protein-bound drugs are resistant to glomerular filtration
Only free fraction is filtered

120
Q

What 2 processes deliver a drug to the renal tubule

A
  1. Glomerular filtration

2. Organ ion transporters

121
Q

What type of drugs in the ultrafiltrate tend to be eliminated in urine

A

Hydrophilic drugs

122
Q

What type of drugs in the ultrafiltrate tend to be reabsorbed

A

Lipophilic drugs

123
Q

3 examples of drugs that rely on organic ion transporters for renal clearance.
Where are these located?

A

Drugs = furosemide, morphine, dopamine

location = proximal renal tubules

124
Q

Describe how urine pH influences whether drugs are excreted in urine or reabsorbed into peritubular capillaries

A

Acidity vs alkalinity
like dissolves like

Acidic urine favors REABSORPTION of acidic drugs and EXCRETION of basic drugs

Basic urine favors REABSORPTION of basic drugs and EXCRETION of acidic drugs

125
Q

What happens to hydrophilic drugs excreted in urine

A

Unchanged

126
Q

How are lipophilic drugs excreted in urine

A

by undergoing biotransformation reaction to increase their water solubility

127
Q

What happens to lipophilic drugs in the kidneys

A

It is reabsorbed into the peritubular fluid by diffusion

128
Q

How does organic ion transporter elimination work in the kidneys

A

Active secretion or organic acids and bases at the proximal renal tubules

129
Q

Where are organic ion transporters in the kidneys and what is excreted

A

proximal renal tubules

secretes organic acids and bases

130
Q

Describe the 2 types of organic ion transporters and what they eliminate

A

Organic ANION transporters (OAT) = furosemide, thiazide diuretics, PCN

Organic cation transporters (OCT) = morphine, meperidine, dopamine

131
Q

Describe the types of drugs reabsorbed and excreted when acidic urine is present

A

Reabsorb acidic drugs
Excrete basic drugs
AAA = ACIDIC drugs are better ABSORBED in ACIDIC urine

132
Q

Describe the types of drugs reabsorbed and excreted when basic urine is present

A

Reabsorb basic drugs
Excrete acidic drugs
BBB = BASIC drugs are BETTER absorbed in BASIC urine

133
Q

How can urine pH be altered to become more acidic?

What will be eliminated?

A

Altered with ammonium chloride or cranberry juice

Eliminates BASIC drugs

134
Q

how can urine pH be altered to become more basic?

What will be eliminiated?

A

Altered with sodium bicarbonate or acetazolamide

Eliminates ACIDIC drugs

135
Q

What drugs are metabolized by pseudocholinesterases

A 
Succinylcholine
Cocaine (+liver)
Tetracaine
Procaine
Chloroprocaine
Mivacurium
136
Q

What drugs are metabolized by nonspecific plasma esterases

A 
Esmolol
Remifentanil
Atracurium (+hofmann)
Etomidate (+hepatic)
Clevidpine
137
Q

What are 4 metabolic pathways in plasma

A

Pseudocholinesterase
Nonspecific esterases
Alkaline phosphatase
Hofmann elimination

138
Q

How does enzymatic metabolism occur in the plasma

A

Hydrolysis via water to cleave an ester linkage

139
Q

What drugs are metabolized via Hofmann elimination

A

Cisatracurium

Atracurium (+nonspecific esterases)

140
Q

What drug is metabolized via alkaline phosphatase

A

Fospropofol

141
Q

How does pseudocholinesterase deficiency affect metabolism? Which drugs are impacted?

A

Extends the duration of action of succinylcholine, mivacurium, cocaine, and ester LA

APEX Pharmacology (8 decks)

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