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DEN 7203 Pharmacological Concepts > Exam 1 Pharmacokinetics > Flashcards

Exam 1 Pharmacokinetics Flashcards

Lecture 3

1
Q

List the steps of the life of a drug in the body

A
  1. Route of administration
  2. Absorption
  3. Distribution
  4. Metabolism (changed so can be extracted)
  5. Excretion
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2
Q

What are the 3 routes of administration?

A
  • Enteral
  • Parenteral
  • Topical (type of parenteral)
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3
Q

____ uses the gastrointestinal tract for ingestion

A

Enteral

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4
Q

What route avoids the GI tract?

A

Parenteral

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5
Q

Topical is also a ____ route

A

Parenteral

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6
Q

Topical drugs can be applied to:

A

Skin or mucous membranes

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7
Q

Once a drug enters the body via enteral route, what happens?

A
  • Absorbed from stomach/intestine
  • Goes to the liver (first pass effect)
  • Distributed to the rest of the body
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8
Q

What is the first pass effect?

A

Most blood supplying the GI tract travels to the liver before going to the rest of the body (portal system), often inactivating drugs

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9
Q

What organ is metabolic (change) machine?

A

Liver

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10
Q

What is the pathway a drug takes in the enteral route?

A
  • Goes to lumen of GI tract
  • Enters hepatic portal system (capillaries –> hepatic portal vein)
  • Liver (metabolizes drugs)
  • General circulation
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11
Q

Special points of the enteral route

A
  • Sublingual
  • Rectal
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12
Q

What point in the enteral route has rapid absorption of certain drugs?

A

Sublingual

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13
Q

True or false: Sublingual route still has first-pass drug metabolism in the liver

A

False - avoids first pass

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14
Q

Is rectal route systemic?

A

Yes

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15
Q

____ is useful for when pt has nausea/vomiting

A

Rectal route

Enteral route special point

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16
Q

True or false: rectal has relatively little first-pass metabolism

A

True

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17
Q

Examples of parenteral routes

A
  • Subcutaneous injection
  • Intramuscular injection
  • Intravenous injection
  • Transdermal
  • Implantation
  • Intrathecal injection (into CSF/spinal cord)
  • Intra-articular injection (arthritis)
  • Inhalation
  • Topical

All forms of injections (IM, SQ, IV)

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18
Q

Topical administration can be given through a ____

A

Transdermal patch (Scopolamine for motion sickness)

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19
Q

In a transdermal patch, dose is ____ to the area of the patch

A

Proportional

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20
Q

Distribution of transdermal patch depends on what?

A

Blood flow

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21
Q

Inhalation involves:

A

Gases or solid/liquid particulate aerosols

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22
Q

What is used for an acute allergic reaction?

A

Epinephrine aerosol

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23
Q

The more layers between the site of administration and the bloodstream, the ___ the rate

A

Slower

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24
Q

Rank order of routes from slowest to fast - IM, SQ, oral

A

Oral < SQ < IM

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25
Q

Rank order of membrane systems from slowest to fast

Muscle, GI, skin

A

GI < skin < muscle

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26
Q

What route will result in the quickest absorption?

A

IV injection

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27
Q

Most oral administered drugs are absorbed in the ____

A

Small intestine

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28
Q

What factors affect speed of absorption in the enteral route?

A
  • Surface area
  • Drug-food interactions
  • Dosage form
  • Drug inactivation
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29
Q

Small intestine has what structures that greatly increase effective surface area?

A

Folds, villi, microvilli

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30
Q

The bigger the surface, the ____ drug gets across

A

More

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31
Q

A glass of water on an empty stomach enters the small intestine ____. Half of water in ____ and all liquid removed from stomach in ____

A

Rapidly; 15 min; 1 hour

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31
Q

A mixed meal of solids and liquids begins to enter the duodenum in about ____ and requires up to ____ to leave stomach completely

A

30 min; 4 hours

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32
Q

How should most drugs be taken?

A

In absence of food but with a full glass of water (exception is drug with high lipid solubility, such as fat soluble vitamins)

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33
Q

Dosage form

Solution vs tablet: concentration of aspirin in plasma after 30 min can be ___ for ____ as for ____

A

2x for solution as for tablet

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34
Q

Other factors affect speed:

What are enteric coated tablets?

A

Film over tablet that is insoluble under acidic conditions of the stomach, but breaks down in alkaline small intestine

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35
Q

Other factors affect speed: Dosage form

What is sustained release?

A

Porous matrix or spheres of drug with different coatings that dissolve at different rates

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36
Q

Other factors affect speed: Drug inactivation

Examples of drug inactivation

A
  • Gastric acid breaks down drugs
  • Enzymatic activity (hydrolysis by pancreatic and intestinal peptidases)
  • Enteric bacterial enzymes
  • Drugs chelate with divalent cations, or form insoluble salts (tetracycline with Ca2+ in dairy products)
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37
Q

What is absorption?

A

Passage of a drug from the site of administration into the bloodstream

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38
Q

All drugs have to:

A

Cross membranes, reach its site of action, and eventually elimination

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39
Q

How do things get across the membrane?

A

Passive transport or active transport

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40
Q

Passive transport is diffusion of ____ soluble substances through:

A

Lipid; Protein channels and facilitated transport

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41
Q

Active transport is transport against ____ through ____

A

Gradients; active, co-transport, counter transport

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42
Q

Absorption is favorable when:

A

A drug is lipid soluble

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43
Q

Oral Ingestion: Influence of pH

The ___ of the surrounding medium affects the degree of ____, and therefore drug absorption

A

pH; Ionization

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44
Q

True or false: H+ concentrations of stomach and small intestine are very similar

A

False - very different, therefore very different patterns of drug absorption

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45
Q

Aspirin is a ____ acid

A

Weak

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46
Q

Codeine is a weak ____

A

Base

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47
Q

Where do acidic drugs favor absorption?

A

Stomach (where pH is low)

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48
Q

Where are basic drugs absorbed?

A

Small intestine (where pH is higher)

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49
Q

The absorption of aspirin is further promoted by:

A

Ion trapping within the plasma

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50
Q

The low pH of the stomach favors ____ of codeine

A

Gastric retention

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51
Q

____ behaves similarly to codeine

A

Local anesthetic

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52
Q

Bioavailability refers to:

A
  • Extent of absorption of intact drug
  • the fraction of an extravascularly administered dose (generally oral) that reaches the systemic circulation in an unchanged form
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53
Q

What do bioavailability studies provide?

A
  • Useful information on the specific dosage and dosage regimen for non-intravenous routes of administration
  • Information regarding the performance of a formulation
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54
Q

If 100 mg of a drug is administered orally and 70 mg of the drug is absorbed unchanged, what is the bioavailability?

A

70% (0.7)

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55
Q

What is the bioavailability for a IV dose administered directly into systemic circulation?

A

100%

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56
Q

____ is when a formulation is interchangeable if it contains the same dose of the same chemical entity, generally int he same dosage form and they exhibit the same rate and extent of absorption

A

Bioequivalence

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57
Q

What is bioequivalence documentation useful for?

A
  • Evaluate different formulations (tablet vs capsule)
  • Compare generic vs branded drug
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58
Q

What is drug distribution?

A

How a drug, once absorbed, gets to tissues and fluids of the body

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59
Q

Total body H2O (42 L) is found where?

A

Inside cells and outside cells

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60
Q

How much water is found inside cells?

A

28 L

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61
Q

How much water is found outside cells?

A

14 L

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62
Q

Where specifically is water found outside cells?

A
  • Between cells and the water in blood (3L of plasma)
  • Interstitial fluid (10L)
  • Transcellular fluid (1L)
63
Q

What is transcellular fluid?

A

Specialized fluids separated from plasma by epithelium (synovial, intraocular, cerebrospinal)

64
Q

____ is the apparent and hypothetical volume in which a drug is dispersed

A

Volume of distribution (equilibrium concept)

65
Q

Volume of distribution formula

A

Dose (mg)/Plasma concentration (mg/mL)

66
Q

Your patient takes 3 tablets of 200 mg ibuprofen. Plasma concentration is measured as 0.043 mg/mL. Calculate Vd and likely location of the ibuprofen?

A

13.9 L; Extracellular fluid

67
Q

True or false: drugs may be hidden from measurement

A

True

68
Q

Drugs can “hide” if they:

A
  • Dissolve well in fat and are stored there
  • Bound to PROTEINS in the blood
69
Q

True or false: Vd is an actual volume

A

False - theoretical volume (used to estimate where a drug is in the body)

70
Q

Vd example: drug that is high molecular weight binds to ____

A

Plasma proteins (heparin –> 3 liters –> plasma)

71
Q

Vd example: drug that is low molecular weight and is hydrophilic

A

Amoxicillin –> 4 to 14 liters –> extracellular fluid

72
Q

Vd example

For a drug that diffuses to intracellular fluid, Vd would equal:

A

Total body water (ethanol is 34 to 41 liters)

73
Q

If a drug binds strongly to tissues, what happens to Vd?

A

Would be higher than total body water (fentanyl is 280 L)

74
Q

Drug distribution depends on?

A

Blood flow

75
Q

To where is blood flow large?

A
  • Heart
  • Liver
  • Kidneys
  • Brain
76
Q

The brain is guarded by tightly bound cells in the ____ (blood brain barrier)

A

Capillary walls

77
Q

What to drugs have to be in order to pass the blood brain barrier?

A
  • Small, lipid soluble or actively pumped in
  • Not bound to protein
78
Q

Why is plasma protein binding important when considering drug absorption?

A
  • If a drug is bound it cannot exert an effect
  • individual variability in protein binding can affect concentration of free drug leading to insufficient therapy or overdose
79
Q

What is alpha1-acid glycoprotein?

A

Plasma protein that binds basic/cationic drugs

80
Q

What is the most predominant protein in plasma?

A

Albumin

81
Q

Albumin has ____ ionized functional groups per molecules, which allows it to ____

A

200; bind many different substances concurrently

82
Q

True or false: drugs differ slightly in affinity for plasma proteins

A

False - drastically

83
Q

Hepatic uptake and glomerular filtration involve only:

A

Free drug

84
Q

During ____, one drug displaces another from plasma proteins

A

Drug interactions

85
Q

The anticoagulant, Coumadin, is highly bound to plasma proteins (only 0.2% is free in the blood). Your classmate administers an analgesic drug that displaces the bound Coumadin from plasma proteins because it too binds there. What happens to the concentration of Coumadin in the plasma?

A

Increases

86
Q

Transfer of drugs into saliva can be thought of as a form of ____ because the drug regains access to the systemic circulation after saliva is swallowed

A

Redistribution

87
Q

Can drugs gaining access to the oral environment from the systemic circulation affect microorganisms or tissue surfaces within the mouth?

A

Yes (antibiotic or antifungal)

88
Q

____ can provide a noninvasive measure of the free plasma concentration of drugs

A

Salivary drug concentrations

89
Q

Drug metabolism is also known as:

A

Biotransformation; change

90
Q

Drug metabolism changes drug from ____ to ____

A

The form in which it was administered to a more water soluble (hydrophilic) form (to pee it out better)

91
Q

The majority of drugs are metabolized by enzymes in the ____
Some drugs are metabolized in what other organs?

A

Liver; kidney, plasma, intestine, lungs

92
Q

Some drugs ____ or ____ enzymes that metabolize drugs
Some drugs inhibit or compete for ____

A

Induce or activate; enzymes

93
Q

80% of all drugs are ____ before metabolism and ____ after metabolism

A

Active; inactive

94
Q

Valacyclovir is ____ before metabolism and ____ after metabolism

A

Inactive (prodrug); Active

95
Q

Tylenol is ____ before metabolism and ____ after metabolism

A

Active; toxic metabolite

96
Q

Aspirin is ____ before metabolism and ____ after metabolism

A

Active; Active

97
Q

How many phases of metabolism are there?

A

2

98
Q

What happens during Phase I metabolism?

A

Converts parent drug to a more polar metabolite by introducing or unmasking a functional group (-OH, -COOH, -NH2, -SH) via oxidation, reduction, or hydrolysis

99
Q

Phase I metabolism usually results in:

A

Loss of pharmacological activity

100
Q

Sometimes, phase I metabolism results in ____ than the parent drug

A

Equally or more active

101
Q

Where does phase I metabolism occur primarily?

A

Liver

102
Q

Where are Cytochrome P450 (CYP) enzymes found?

A

Liver

103
Q

____ is a superfamily of enzymes with very broad substrate activity

A

Cytochrome P450 (CYP) enzymes

104
Q

CYP enzymes are responsible for ____ of drug metabolism

A

75%

105
Q

There are ____ CYP enzymes but only ____ play significant roles in drug metabolism

A

57; a few (mainly CYP3A4)

106
Q

Phase II metabolism involves:

A
  • Conjugation reactions
  • Reaction in which a covalent linkage is formed between the parent drug or Phase I metabolite and an endogenous substrate such as glucuronic acid, sulfate, acetate, or an amino acid
107
Q

After phase II metabolism, the drug becomes ____ so it is rapidly excreted in urine and feces

A

Highly polar

108
Q

Phase II metabolism products are usually ____. What is an exception?

A

Inactive; Morphine 6-glucuronide (still active)

109
Q

Where does Phase II metabolism occur?

A

Liver and kidney (other organs sometimes involved)

110
Q

Major enzymes with phase I metabolism are ____
Major enzymes with phase II metabolism are ____

A

CYP; transferases

111
Q

A useful drug may inhibit the metabolism of many other drugs by:

A
  • Inactivating various CYP 450 enzymes: these drugs or their metabolites bond strongly with specific sites on CYP enzymes
  • The affected CYP enzymes are responsible for inactivation of other therapeutic agents, resulting in drug interactions)

Double negative

112
Q

What can inhibit certain classes of CYP enzymes?

A
  • Macrolide antibiotics
  • Azole antifungals
  • Gingko biloba
  • Grapefruit juice
113
Q

Drugs and environmental toxins can stimulate what?

A

CYP mediated metabolism, including their own biotransformation

114
Q

How do drugs and environmental toxins stimulate CYP mediated metabolism?

A

Usually by activation of receptors/transcription factors that are responsible for the expression of the CYP genes

115
Q

What is pharmacokinetic tolerance?

A

A loss of therapeutic effect due to induction of enzymes

116
Q

Example of pharmacokinetic tolerance

In an epileptic patient taking phenytoin, this induces ____ responsible for ____. Patient will develop ____

A

CYP enzyme; Vitamin D oxidation; rickets (low vitamin D)

117
Q

Where is blood filtered and urine made?

A

Kidney

118
Q

Kidney can only excrete ____

A

Water soluble substances

119
Q

Most drugs excreted have been ____

A

Modified (in the liver)

120
Q

The more ____, the more easily excreted

A

Polar (occurs in the liver)

121
Q

True or false: the kidney is also a site of biotransformation

A

True

122
Q

Some drugs have ____ kidney elimination

A

100%

123
Q

Clearance describes _____

A
  • the efficiency of irreversible elimination of a drug from the body
  • rate/speed at which a drug is eliminated
124
Q

Volume of blood cleared of drug per unit time is referred to as ____

A

Clearance

125
Q

Clearance can be ____ or ____

A

Specific (organ, process) or whole body

126
Q

What is total body clearance?

A

Sum of total of all the different clearances (renal clearance + hepatic clearance + clearance from other organs)

127
Q

What is the formula for elimination rate?

A

Clearance x Plasma drug concentration

128
Q

Elimination rate is equal to?

A

Maintenance dose rate

129
Q

What is maintenance dose formula?

A

Clearance x Css (steady state concentration of drug mg/L)

130
Q

Every drug has a ____ and we want to be in it

A

Therapeutic range (we use maintenance dosing to do this)

131
Q

What is zero order kinetics?

A

A process that occurs at a constant amount per unit time independent of how much is present

132
Q

What is first order kinetics?

A

A process that occurs at a constant fractional rate per unit of time

133
Q

____ generally exhibit first-order kinetics because they generally rely on processes that are first-order in character

A

Absorption, distribution, and elimination of drugs

134
Q

During first order kinetics, as drug load increases:

A

The amount of drug eliminated per unit time increases

135
Q

In first order kinetics, what is half life useful in?

A

Determining the rate of drug disappearance and the concentration of drug remaining after a given period of time

136
Q

____ is the amount of time required to rid the body of half (50%) of the initial concentration of the drug

A

Half life

137
Q

What is the half life formula?

A

(0.693 x Vd)/CL

138
Q

What happens to half life if Vd goes up?

A

Half life increases

139
Q

What happens to half life if CL goes down (liver disease)

A

Half life increases

140
Q

Half life is a combination of:

A

Vd and CL

141
Q

It takes ___ half lives to rid the body of any drug

A

5 (3% at 5th half life)

142
Q

Why do we care about half life?

A
  • Duration of action after a single dose
  • Dosing frequency required to avoid large fluctuations
  • Time required to reach steady state
143
Q

Half life of penicillin (hours)

A

0.5

144
Q

Half life of clindamycin (hours)

A

3

145
Q

Half life of acetaminophen (hours)

A

3

146
Q

Half life of lidocaine (hours)

A

1.8

147
Q

Half life of procaine (hours)

A

0.01

148
Q

Half life of diazepam (hours)

A

45

149
Q

Fluctuations are proportional to:

A

Dosage interval and half life

150
Q

More frequent dosing means:

A

Less fluctuations

151
Q

Longer half life means:

A

Less fluctuations

152
Q

Steady state is generally reached at:

A

4 half lives (independent of dosage and drug)

153
Q

____ is the time from interval administration to therapeutic effect

A

Onset

154
Q

____ is the length of time drug produces therapeutic effect

A

Duration

155
Q

____ is reached when absorption rate = elimination rate

A

Peak

DEN 7203 Pharmacological Concepts (7 decks)

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