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Pharmacology 1 > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

Refers to any set of physical properties whose value determine the pharmacokinetic characteristics or behavior of the drug

A

Pharmacokinetic parameters

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2
Q

Absorption (Pharmacokinetic parameter)

A

Bioavailability

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3
Q

Distribution (Pharmacokinetic parameter)

A

Volume of distribution

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4
Q

Metabolism and excretion (2 pharmacokinetic parameters) (HC)

A

Half-life, Clearance

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5
Q

An organelle is that semipermeable; follows the fluid mosaic model

A

Cell membrane

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6
Q

A double layer of amphiphilic phospholipids; found in the cell membrane

A

Lipid bilayer

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7
Q

Proteins that span the cell membrane

A

Integral proteins

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8
Q

Proteins that are attached to the cell membrane; modules function of integral proteins

A

Peripheral proteins

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9
Q

Refers to spontaneous movement of molecules across a concentration gradient; no energy required

A

Diffusion/Passive transport

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10
Q

Refers to transport of molecules against a concentration gradient; requires energy

A

Active transport

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11
Q

Diffusion through the cell membrane or between cells; major process for transport of most drugs (Types of diffusion)

A

Simple diffusion

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12
Q

2 types of simple diffusion (TP)

A

Transcellular, Paracellular

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13
Q

Most drugs that undergo transcellular diffusion through the lipid bilayer are __________, __________, and __________ (HUN)

A

Hydrophobic, Unionized, Nonpolar

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14
Q

Done by carrier proteins; saturation may occur (Types of diffusion)

A

Facilitated diffusion

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15
Q

Glucose, and vitamins B1, B2, and B12 undergo __________ diffusion

A

Facilitated

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16
Q

Transport that is carrier-mediated and is accompanied by an energy-producing process

A

Active transport

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17
Q

Moves substances by using energy produced by ATP hydrolysis; pumps coupled to ATPase (Types of active transport)

A

Primary active transport

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18
Q

Moves substances by using kinetic energy from the concentration gradient established by primary active transport (Types of active transport)

A

Secondary active transport

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19
Q

5-fluorouracil, methyldopa, levodopa, methotrexate, and iron salts undergo __________ transport

A

Active transport

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20
Q

Transport the involves vesicles and requires energy

A

Vesicular transport

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21
Q

Engulfment by the cell membrane of particles larger than 500 nm (Types of endocytosis)

A

Phagocytosis

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22
Q

Polio and other vaccines undergo __________ (Types of endocytosis)

A

Phagocytosis

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23
Q

Engulfment of small droplets of extracellular fluid by membrane vesicles (Types of endocytosis)

A

Pinocytosis

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24
Q

Vitamins A, D, E, K undergo __________ (Types of endocytosis)

A

Phagocytosis

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25
Q

Receptors on cell surfaces bind with ligands to form ligand-receptor complexes on cell surfaces (Types of endocytosis)

A

Receptor-mediated endocytosis

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26
Q

The material internalized by the membrane domain is transported through the cell and secreted on the opposite side (Types of endocytosis)

A

Transcytosis

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27
Q

Refers to the movement of solvent from a less concentrated solution to a more concentrated solution through pores

A

Osmosis

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28
Q

Refers to the movement of small molecules with the solvent during osmosis

A

Solvent drag

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29
Q

Water, sugars, and urea undergo __________ and __________ (SO)

A

Solvent drag, Osmosis

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30
Q

Transport wherein oppositely charged molecules interact and form a neutral complex

A

Ion-pair transport

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31
Q

Quaternary ammonium compounds and sulfonic acids undergo __________ transport

A

Ion-pair transport

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32
Q

Refers to the process of movement of unchanged drug from the site of administration to systemic circulation

A

Absorption

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33
Q

Effects that involves the metabolism of drug before it reaches the circulation

A

First pass effect

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34
Q

Intestinal metabolism is due to __________ enzymes (mainly CYP3A4)

A

CYP450 enzymes

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35
Q

Primary site of drug metabolism

A

Liver

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36
Q

A measure of the extent to which the drug reaches the systemic circulation following administration by any route

A

Bioavailability (F)

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37
Q

Compares the amount of the active drug reaching the systemic circulation following extravascular administration with the amount of the same drug following intravenous administration (Types of bioavailability)

A

Absolute bioavailability

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38
Q

Compares the amount of the active drug reaching the systemic circulation following administration of a test formulation with the amount of the same drug following administration from a reference formulation (Types of bioavailability)

A

Relative bioavailability

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39
Q

A measure that compares the bioavailability of multisource drug products with the innovator drug product

A

Bioequivalence

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40
Q

Drug products that contain the same active drug substance; marketed by more than one pharmaceutical manufacturer; examples include generic drug products

A

Multisource drug products

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41
Q

Drug products that are marketed as new chemical entities

A

Innovator drug products

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42
Q

Means that there is no clinically significant difference in bioavailability

A

Bioequivalent

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43
Q

Bioavailability and bioequivalence testing may be __________ or __________

A

In vivo, In vitro

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44
Q

Refers to the maximum concentration of drug in the plasma

A

Peak plasma concentration (Cmax)

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45
Q

Unit of peak plasma concentration (Cmax)

A

mcg/mL

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46
Q

Refers to the time for a drug to reach peak plasma concentration after administration

A

Time of peak concentration (Tmax)

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47
Q

Unit of time of peak concentration (Tmax)

A

Hours

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48
Q

Refers to the total integrated area under the plasma drug concentration-time profile

A

Area under the curve (AUC)

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49
Q

Unit of area under the curve (AUC)

A

mcg-h/mL

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50
Q

Refers to the minimum concentration of drug in the plasma required to produce the therapeutic effect

A

Minimum effective concentration (MEC)

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51
Q

The level of plasma drug concentration below MEC

A

Subtherapeutic level

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52
Q

Refers to the minimum concentration of drug in the plasma that produces adverse or unwanted effects

A

Minimum toxic concentration (MTC) or Maximum safe concentration (MSC)

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53
Q

The time required for the drug to start producing pharmacologic response

A

Onset of action

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54
Q

F=1 by definition (Route of administration)

A

Intravenous

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55
Q

0.75 < F < 1 (2 routes of administration) (SI)

A

Subcutaneous, Intramuscular

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56
Q

0.05 < F < 1 (Route of administration)

A

Oral ingestion

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57
Q

Bioavailability is complete (F=1); distribution is rapid (Route of administration)

A

Intravenous (IV)

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58
Q

The rate of absorption via simple diffusion is constant and slow to provide a sustained effect (Route of administration)

A

Subcutaneous (SC)

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59
Q

Drugs can be in aqueous solutions (absorbed rapidly) or in specialized depot preparations (absorbed slowly) (Route of administration)

A

Intramuscular (IM)

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60
Q

A drug is injected directly into an artery to localize its effect in a particular tissue or organ (Route of administration)

A

Intra-arterial (IA)

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61
Q

Produces local and rapid effects of drugs on the meninges or cerebrospinal axis (Route of administration)

A

Intrathecal

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62
Q

Access to the circulation is rapid by this route because the lung’s surface area is large (Route of administration)

A

Inhalational

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63
Q

It achieves a local and direct effect (Route of administration)

A

Topical

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64
Q

This route is most often used for the sustained delivery of drugs (Route of administration)

A

Transdermal

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65
Q

It is the safest and most common, convenient, and economical method of drug administration (Route of administration)

A

Oral (PO)

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66
Q

Venous drainage from the mouth is to the superior vena cava, bypassing the portal circulation (Route of administration)

A

Sublingual (SL)

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67
Q

Approximately 50% of the drug that is absorbed from the rectum will bypass the liver (Route of administration)

A

Rectal

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68
Q

pH range of the stomach

A

pH 1-3.5

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69
Q

pH range of the small intestine

A

pH 6-7.5

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70
Q

According to this theory, the unionized form of an acidic or basic drug, if sufficiently lipid soluble, is absorbed but the ionized form is not

A

pH partition theory

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71
Q

The higher the surface area, the __________ the extent and rate of absorption

A

Greater

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72
Q

Most drugs are absorbed in the __________ because of its large surface area and gradually changing pH

A

Small intestine

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73
Q

Refers to the distribution of the drug into interstitial and intracellular fluids

A

Distribution

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74
Q

A __________ is not a real physiologic or anatomic region but is considered a tissue or group of tissues that have similar blood flow and drug affinity

A

Compartment

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75
Q

The body is a single homogenous compartment; most drugs follow this model (Types of compartment models)

A

One-compartment model

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76
Q

Its subtypes include central compartment and tissue compartment (Types of compartment models)

A

Two-compartment model

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77
Q

Includes the blood and highly perfused lean organs such as the heart, brain, liver, lung, and kidneys (Types of two-compartment models)

A

Central compartment

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78
Q

Includes the slowly perfused tissues such as muscle, skin, fat, and bone (Types of two-compartment model)

A

Tissue compartment

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79
Q

Refers to the measure of the apparent space in the body available to contain the drug

A

Volume of distribution (Vd)

80
Q

Humans are ___________% water

A

60%

81
Q

The Vd of the plasma compartment for a 70 kg man or 6% of body weight is __________ L

A

4

82
Q

Drugs with ___________ are too large to move out through the endothelial slit junctions and are effectively trapped within the plasma compartment

A

Very large molecular weight

83
Q

The Vd of the extracellular fluid for a 70 kg man or 20% of body weight is __________ L

A

14

84
Q

In extracellular fluid, drugs with low molecular weight and are __________ can move through the endothelial slit junctions of the capillaries into the interstitial fluid

A

Hydrophilic

85
Q

The Vd of the total body water for a 70 kg man or 60% body weight is __________ L

A

42 L

86
Q

In total body water, drugs with low molecular weight and are __________ can move into the interstitium through the slit junctions

A

Hydrophobic

87
Q

Small water-soluble molecules: eg, ethanol (Fluid compartment in the body)

A

Total body water

88
Q

Larger water-soluble molecules: eg, gentamicin (Fluid compartment in the body)

A

Extracellular fluid/water

89
Q

Larger protein molecules: eg, antibodies (Fluid compartment in the body)

A

Plasma compartment

90
Q

Highly lipid-soluble molecules: eg, diazepam (Fluid compartment in the body)

A

Fat

91
Q

Certain ions: eg, lead, fluoride (Fluid compartment in the body)

A

Bone

92
Q

Refers to the volume of blood that circulates in the cardiovascular system and reaches different organs and tissues in the body per unit of time

A

Blood flow

93
Q

Unit of blood flow

A

mL/min

94
Q

Refers to the amount of xenobiotic that can be stored or distributed in a tissue that depends on the mass of tissue or size of organ

A

Tissue size

95
Q

Refers to the distribution of a compound in a region of the body that depends on the blood flow to that region

A

Tissue perfusion

96
Q

Refers to the diffusion of drug into extravascular tissues

A

Tissue diffusion

97
Q

Are proteins that are neutral molecules and are highly lipophilic

A

Lipoproteins

98
Q

Are proteins that are acidic/weakly acidic compounds in ionized form with moderate or marked lipophilicity

A

Albumin

99
Q

Are proteins that are ionized, basic compounds with moderate lipophilicity

A

α-1-acid glycolprotein

100
Q

Phenytoin, salicylates, phenylbutazone, disopyramide, and penicillins bind to ___________

A

Albumin

101
Q

Propanolol, saquinavir, imipramine, quinidine, and lidocaine bind to ____________

A

α-1-acid glycoprotein

102
Q

Chlorpromazine binds to ___________

A

Lipoproteins

103
Q

Happens when drugs with the same binding site compete for interaction

A

Drug displacement

104
Q

Refers to a barrier composed of tight junctions of endothelial cells of cerebral capillaries; drug distribution is highly regulated and limited here

A

Blood-brain barrier (BBB)

105
Q

Cells that forma solid envelope around the brain capillaries

A

Astrocytes

106
Q

Most antibiotics like __________ cannot penetrate the blood-brain barrier (BBB)

A

Penicillins

107
Q

One must use ___________ for parkinsonism instead of dopamine

A

Levodopa

108
Q

A barrier that is not effective as the blood-brain barrier (BBBB)

A

Placental barrier

109
Q

Many drugs such as ethanol, sulfonamides, barbiturates, gaseous anesthetics, and some antibiotics cross the placental barrier by __________

A

Simple diffusion

110
Q

Nutrients for fetal growth such as glucose, amino acids, minerals, some vitamins, purines, and pyrimidines cross the placental barrier by __________

A

Carrier-mediated/Energy requiring process

111
Q

Drugs such as thalidomide, phenytoin, isotretinoin, testosterone, and methotrexate show teratogenic effects during the __________, which is the stage where fetal organs develop

A

1st trimester

112
Q

Refers to the conversion of drugs into more hydrophilic metabolites for elimination and termination of biological and pharmacological activity

A

Metabolism/Biotransformation

113
Q

Primary organ for drug metabolism

A

Liver

114
Q

Lungs, kidneys, intestine, placenta, adrenals, and skin are organs that perform __________ metabolism

A

Extrahepatic

115
Q

Are enzymes that are different from the enzymes that metabolize food

A

Drug metabolizing enzymes

116
Q

Enzymes that metabolize the majority of drugs; catalyze oxidation, reduction, hydrolysis, and glucuronidation reactions (Types of drug metabolizing enzymes)

A

Microsomal enzymes

117
Q

Microsomes (fragments that contain microsomal enzymes) are derived from __________

A

Rough endoplasmic reticulum

118
Q

Enzymes that include those that are present in the cytoplasm and those attached to the mitochondria but not to the RER (Types of drug metabolizing enzymes)

A

Non-microsomal enzymes

119
Q

2 phases of metabolism

A

Phase I, Phase II

120
Q

A polar functional group is introduced/unmasked on the otherwise lipid-soluble substrate; include oxidation, reduction, and hydrolysis (Phases of metabolism)

A

Phase I

121
Q

Products of Phase I metabolism

A

Primary metabolites

122
Q

A flavoprotein; contains FMN and FAD; a monooxygenase in Phase I metabolism

A

NADPH cytochrome P450 oxidoreductase

123
Q

A hemeprotein; a monooxygenase in Phase I metabolism

A

Cytochrome P450

124
Q

Represents a superfamily of heme containing enzymes; involved in Phase I metabolism

A

Cytochrome P450

125
Q

A member of the oxidoreductase family; present in high concentrations in the liver and kidney; involved in metabolism of alcohols (Other Phase I enzymes)

A

Alcohol dehydrogenase

126
Q

Metabolize aldehydes to less reactive forms (Other Phase I enzymes)

A

Aldehyde dehydrogenase

127
Q

Deamination of diamines not monoamines (Other Phase I enzymes)

A

Diamine oxidase (Histaminase)

128
Q

Metabolism of purine bases and hypoxanthine to xanthine and finally to uric acid (Other Phase I enzymes)

A

Xanthine oxidase (XOD)

129
Q

Catalyze the hydrolysis of a large number of structurally diverse esters, aides, thioesters, and carbamates in humans (Other Phase I enzymes)

A

Carboxylesterases (CES)

130
Q

Hydrolyze the peptide bonds of proteins and peptides (Other Phase I enzymes)

A

Peptidase (Protease/Proteinase)

131
Q

Small polar endogenous compounds are covalently attached to the unchanged drug or products of Phase I metabolism; involves conjugation or synthetic reactions (Phases of metabolism)

A

Phase II

132
Q

Enzymes involved in Phase II metabolism

A

Transferases

133
Q

Refers to the increased drug metabolizing ability of the enzymes by drugs and other substances

A

Enzyme induction

134
Q

The agent that brings about enzyme induction

A

Inducers

135
Q

Most inducers are __________ lipophilic with long elimination half lives

A

Lipophilic

136
Q

Includes several drugs and pesticides (Types of inducers)

A

Phenobarbital type inducers

137
Q

Includes 3-methyl cholanthrene and cigarette smoke (Types of inducers)

A

Polycyclic hydrocarbon type inducers

138
Q

Carbamazepine, meprobamate, cyclophosphamide, and rifampicin are capable of __________ or __________

A

Auto-induction/Self-induction

139
Q

Result from interaction at the enzymatic site, the net outcome being a change in enzyme activity (Type of enzyme inhibition)

A

Direct inhibition

140
Q

Structurally similar competes compete for the same site (Type of direct inhibition)

A

Competitive inhibition

141
Q

A structurally unrelated compound interacts with the enzyme at a different site from the drug being metabolized (Type of direct inhibition)

A

Noncompetitive inhibition

142
Q

Metabolic products compete with the substrate for the same enzyme (Type of direct inhibition)

A

Product inhibition

143
Q

Involves decrease in enzyme content (Type of indirect inhibition)

A

Repression

144
Q

Ethionine, puromycin, and actinomycin D results in __________

A

Decreased synthesis

145
Q

CCl4, CS2, and disulfiram results in __________

A

Increased degradation

146
Q

Involves nutritional deficiency or hormonal balance (Type of indirect inhibition)

A

Altered physiology

147
Q

Metabolism is __________ related to volume of distribution (Vd)

A

Inversely

148
Q

The microsomal enzyme system is not fully developed up to __________ months

A

2

149
Q

__________ is well developed in newborns (e.g. sulfate conjugation of paracetamol)

A

Sulfation

150
Q

__________ is not developed in newborns (e.g. chloramphenicol in newborns lead to kernicterus and gray baby syndrome)

A

Glucuronidation

151
Q

Infants _________ months to __________ year old have similar profile as neonates in metabolizing drugs with improvement as age advances and as enzyme activity increases

A

2 months - 1 year old

152
Q

Children that are __________ to __________ years old metabolize several drugs faster than adults

A

1-12

153
Q

In the __________, liver size is reduced, microsomal enzyme activity is decreased, and hepatic blood flow declines; overall metabolism is slow

A

Elderly

154
Q

A __________ protein diet decreases metabolizing activity

A

Low

155
Q

A __________ protein diet increases metabolizing activity

A

High

156
Q

__________ alcoholism decreases enzyme activity

A

Acute

157
Q

__________ alcoholism increases enzyme activity

A

Chronic

158
Q

____________ disease leads to increased half life of drugs

A

Liver

159
Q

__________ disease leads to decrease of glycine conjugation of salicylates, oxidation of vitamin D, and hydrolysis of procaine

A

Kidney

160
Q

__________ and __________ leads to decreased blood flow to the liver and decreased metabolism

A

Congestive heart failure (CHF), Myocardial infarction (MI)

161
Q

__________ leads to decreased UDPGA and glucuronidation

A

Diabetes

162
Q

Refers to the removal of the drug from the body either as the unchanged drug or as a metabolite

A

Excretion

163
Q

Principal organ of excretion

A

Kidneys

164
Q

Basic unit of the kidneys

A

Nephron

165
Q

3 steps in renal excretion (GTT)

A

Glomerular filtration, Tubular reabsorption, Tubular secretion

166
Q

A nonselective, unidirectional process whereby most compounds, ionized or unionized, are filtered

A

Glomerular filtration

167
Q

Refers to the volume of blood that is filtered per unit time

A

Glomerular filtration rate (GFR)

168
Q

Glomerular filtration rate (GFR) is around __________% of renal blood flow

A

20%

169
Q

Normal glomerular filtration rate

A

125 mL/min

170
Q

A carrier mediated process which requires energy for transport of substances against a concentration gradient

A

Tubular secretion

171
Q

Tubular secretion occurs primarily in the __________

A

Proximal tubule

172
Q

Happens with endogenous substances that are needed by the body such as electrolytes, glucose, vitamins, amino acids, and uric acid (Types of tubular reabsorption)

A

Active tubular reabsorption

173
Q

Happens with exogenous substances; driven by the concentration gradient established by back diffusion of water, sodium, and inorganic ions (Types of tubular reabsorption)

A

Passive tubular reabsorption

174
Q

Clearance is __________ proportional to plasma drug concentration

A

Directly

175
Q

Clearance is __________ related to volume of distribution

A

Inversely

176
Q

Example of acidic drug

A

Penicillin

177
Q

Example of basic drug

A

Gentamicin

178
Q

Example of very weakly acidic, nonpolar drug (pKa >8)

A

Phenytoin

179
Q

Example of very weakly basic, nonpolar drug (pKa <6)

A

Propoxyphene

180
Q

Example of a strongly acidic drug (pKa≤2)

A

Cromoglycic acid

181
Q

Example of a strongly basic drug (pKa≥12)

A

Guanethidine

182
Q

Example of acidic drugs with pKa 3-8

A

NSAIDs

183
Q

2 examples of basic drugs with pKa 6-12 (MT)

A

Morphine analogs, Tricyclic antidepressants

184
Q

__________ causes hypertension, DM, hypovolemia, pyelonephritis, and buildup of nephrotoxic agents

A

Renal impairment

185
Q

Function that can be determined by measuring the GFR

A

Renal function (RF)

186
Q

Is exogenous and tedious; used to determine renal function (RF)

A

Inulin

187
Q

Is endogenous and is the most widely used to determine renal function (RF)

A

Creatinine

188
Q

Involves the measurement of serum creatinine

A

Creatinine clearance

189
Q

Bile is synthesized in the __________

A

Liver

190
Q

Bile is stored in the __________

A

Gallbladder

191
Q

Bile is secreted in the __________

A

Duodenum

192
Q

Rate of elimination is convenient because it is constant (Types of elimination)

A

Zero-order elimination

193
Q

Rate of elimination changes with respect to drug plasma concentration (Types of elimination)

A

First order elimination

194
Q

Refers to the factor that predicts the rate of elimination in relation to the drug concentration

A

Clearance (CL)

195
Q

Unit of clearance

A

Volume/time

196
Q

Clearance of drug by several organs is __________

A

Additive

197
Q

Refers to the time required to change the amount of drug in the body by one-half during elimination

A

Half-life (t1/2)

Pharmacology 1 (5 decks)

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