Biopharmaceutics/pharmacokinetics: Exam 1

Front 1

Define: absolute bioavailability

Back 1

The extent or fraction of drug absorbed upon extravascular administration in comparison with the dose size administered.

Front 2

Define: absorption

Back 2

The uptake of the compound from the site of administration into the systemic circulation; a prerequisite for absorption is that the drug be in aqueous solution.

Front 3

Define: accumulation

Back 3

The increase of drug concentration in blood and tissue upon multiple dosing until steady state is reached.

Front 4

Define: apparent partition coefficient

Back 4

The ratio of the concentration at equilibrium between a lipid phase and an aqueous phase. The apparent partition coefficient is uncorrected for dissociation or association in either phase.

Front 5

Define: area under the curve

Back 5

The integral of drug blood level over time from zero to infinity and is a measure of quantity of drug absorbed and in the body.

Front 6

Define: area under the first statistical moment curve

Back 6

The area under the curve observed for the product of time and concentration versus time.

Front 7

Define: biliary recycling (enterohepatic recirculatio)

Back 7

The phenomenon that drugs emptied via bile into the small intestine can be reabsorbed from the intestinal lumen into systemic circulation.

Front 8

Define: bioavailability

Back 8

Defined as both the relative amount of drug from an administered dosage form that enters the systemic circulation and the rate at which the drug appears in the bloodstream.

Front 9

Define: bioequivalence

Back 9

A drug product is achieved if its extent and rate of absorption are not statistically significantly different from those of the standard when administered at the same molar dose.

Front 10

Define: bioequivalence requirement

Back 10

Requirement imposed by the Food and Drug Administration for in vitro and/or in vivo testing of specified drug products, which must be satisfied as a condition of marketing.

Front 11

Define: bio-pharmaceutics

Back 11

Deals with the physical and chemical properties of the drug substance, the dosage form, and the body and the biological effectiveness of a drug and/or drug product upon administration, i.e., the drug availability to the human or animal body from a given dosage form, considered as a drug delivery system. The time course of the drug in the body and the quantifying of the drug concentration pattern are explained by pharmacokinetics.

Front 12

Define: biophase

Back 12

The actual site of action of a drug in the body. It is the drug-receptor interaction on the molecular level or the effect of the presence of a drug on biopolymers. The biophase may be the surface of a cell or within the cell.

Front 13

Define: blood flow rate

Back 13

The speed of blood perfusion in an organ, usually expressed in milliliters per 100 grams of organ weight per minute. Blood flow rates may differ several-fold between rest and exercise.

Front 14

Define: blood, plasma, or serum levels

Back 14

Demonstrate the concentration in blood, plasma, or serum upon administration of a dosage form by various routes. Blood, plasma, or serum level curves are plots of drug concentratino versus time on numeric or semilog graph paper. Blood, plasma, or serum levels are obtained from blood samples by venipuncture at certain time intervals after administration of the drug product and chemical or microbiological analysis of the drug in the biological fluid.

Front 15

Define: central compartment

Back 15

The sum of all body regions (organs and tissues) in which the drug concentration is in instantaneous equilibrium with that in blood or plasma. The blood or plasma is always part of the central compartment.

Front 16

Define: chronopharmacokinetics

Back 16

The study of pharmacokinetic drug parameters as affeted by circadian rhythm or diurnal variation

Front 17

Define: circadian rhythm

Back 17

The biological clock controlling rhythms of processes during a 24-hr cycle based on endogenous factors

Front 18

Define: clearance

Back 18

The hypothetical volume of distribution in mL of the unmetabolized drug cleared per unit of time (mL/min or mL/hr) by any pathway of drug removal (renal, hepatic, etc.)

Front 19

Define: clinical pharmacokinetics

Back 19

The application of pharmacokinetics principles in the safe and effective treatment of individual patients and in the optimization of drug therapy

Front 20

Define: compartment

Back 20

An entity that can be described by a definite volume and a concentration of drug contained in that volume. In pharmacokinetics, experimental data are explained by fitting them to compartment models

Front 21

Define: concentration gradient

Back 21

The difference in the concentration in two phases usually separated by a membrane

Front 22

Define: creatine clearance

Back 22

The ratio of creatinine excreted in urine to the concentration of creatinine in plasma. The creatinine clearence decreases with renal impairment and with advancing age.

Front 23

Define: cumulative urinary excretion curves

Back 23

The plots of the acutal cumulative amounts of drug and/or its metabolites excreted into urine versus time after administration of a drug product by various routes.

Front 24

Define: depot phase

Back 24

The portion of a prolonged-release dosage form that liberates the drug from the dosage form at a slower rate than its unrestricted absorption rate.

Front 25

Define: diffusion layer

Back 25

The viscous layer of concentrated drug solution around a dissolving particle

Front 26

Define: disposition

Back 26

The loss of drug from the central compartment through transfer (distribution) into other compartments and/or elimination and metabolism

Front 27

Define: diurnal variation

Back 27

The biological clock controlling rhythms of processes during a 24-hr cycle based on external synchronizers

Front 28

Define: dosage regimen/dose rate

Back 28

The systematized dosage schedule for therapy, i.e. the proper dose sizes and proper dosing intervals required to product clinical effectiveness or to maintain a therapeutic concentration in the body.

Front 29

Define: dose dependency

Back 29

Refers to a change in one or more of the pharmacokinetic processes of absorption, distribution, metabolism, and excretion with increasing dose size.

Front 30

Define: dose dumping

Back 30

A term used to describe the achievement of sustained drug concentration by simply increasing the dose size or by accidental fast release of drug from a sustained-release form.

Front 31

Define: dose-response curve

Back 31

The graphical presentation of pharmacologic or clinical effectiveness or toxicity (response) versus dose. A log dose-response curve is sigmoidal with a straight line middle section; a log dose-probability curve results in an entirely straight line

Front 32

Define: dose size

Back 32

The amount of drug in micrograms, milligrams, units, or other dimension to be administered

Front 33

Define: dosing interval

Back 33

The time period between administration or maintenance doses.

Front 34

Define: drug

Back 34

A chemical compound of synthetic, semisynthetic, natural or biological origin that interacts with human or animal cells. The interactions may be quantified, whereby these resulting actions are intended to prevent, to cure, or to reduce ill effects in the human or animal body or to detect disease-causing manifestations

Front 35

Define: drug delivery system

Back 35

A medical device or a specially prepared drug formulation that is intended to liberate drug(s) at the site(s) of absorption at a specific rate. Drug delivery systems are generally reserved for drug administration via extra-vascular routes

Front 36

Define: drug product/dosage form

Back 36

The gross pharmaceutical form containing the active ingredient(s) and vehicle substances necessary for formulating a medicament of desired dosage, desired volume, and desired application form, ready for administration

Front 37

Define: drug-receptor interaction

Back 37

The combining of a drug molecule with the receptor for which it has affinity and the initiation of a pharmacologic response by its intrinisic activity

Front 38

Define: drug release or liberation

Back 38

The delivery of the active ingredient from a dosage form into solution. The dissolution medium is either a biological fluid or an artificial test fluid (in vitro). Drug release is characterized by the speed and the amount of drug appearing in the solution

Front 39

Define: drug specialty or brand product

Back 39

A drug product, usually of unvarying composition, labeled with a registered trademark of a single company

Front 40

Define: elimination half-life

Back 40

The time in hours necessary to reduce the drug concentration in the blood, plasma, or serum, to one-half after equilibrium is reached.

Front 41

Define: enterohepatic recirculation (biliary recycling)

Back 41

The phenomenon in which drugs emptied via bile into the small intestine can be reabsorbed from the intestinal lumen into systemic circulation

Front 42

Define: enzyme inhibition

Back 42

The decrease in rate of metabolism of a compound, usually by competition for an enzyme system

Front 43

Define: excretion

Back 43

The final elimination from the body's systemic circulation via the kidney into urine, via bile and saliva into intestine and into feces, via sweat, via skin, and via milk

Front 44

Define: extravascular administration

Back 44

Refers to all routes of administration except those in which the drug is directly introduced into the bloodstream

Front 45

Define: feathering

Back 45

A graphical method for the separation of exponents, such as separating the absorption rate constant from the elimination rate constant. The term residual method is synonymous with feathering

Front 46

Define: first-pass effect

Back 46

Describes the phenomenon whereby drugs may be metabolized (not chemically degraded) after absorption but before reaching systemic circulation. Hepatic first-pass effect may occur after PO and deep rectal administration. Pulmonary first-pass effect cannot be avoided by intravenous, buccal, or sublingual routes.

Front 47

Define: flip-flop model

Back 47

The phenomenon observed if the rate of absorption is slower than the rate of elimination, or if one of the distribution rates is slower than the rate of elimination

Front 48

Define: GI tract

Back 48

A part of the alimentary canal comprising stomach, small intestine, and large intestine

Front 49

Define: generic product

Back 49

A drug product marketed under the nonpropreitary or common name of the drug(s)

Front 50

Define: hepatic clearance

Back 50

The hypothetical volume of distribution in mL of the unmetabolized drug that is cleared per unit of time via the liver

Front 51

Define: homeostasis

Back 51

The maintenance of a steady state, which characterizes the internal environment of the healthy organism. An important function of homeostasis is regulation of the fluid medium and volume of the cell.

Front 52

Define: hybrid rate constants

Back 52

Composite rate constants consisting of two or more micro-constants. Alpha and Beta are hybrid rate constants

Front 53

Define: initial phase

Back 53

The portion of a prolonged-release dosage form that is immediately available for absorption

Front 54

Define: intravascular administration

Back 54

Refers to all routes of administration in which the rug is directly introduced into the bloodstream: IV, intra-arterial, and intracardiac; bioavailability = 100%

Front 55

Define: intrinsic clearance

Back 55

The theoretical unrestricted maximum clearance of unbound drug by an eliminating organ

Front 56

Define: IV bolus

Back 56

A physiologic nonsense and misuse of language. A bolus is a bite, something solid that is swallowed and is then absorbed from the intestines. the correct term would be IV push

Front 57

Define: LADMER system

Back 57

Deals with the complex dynamic processes of liberation of an active ingredient from the dosage form, its absorption into systemic circulation, its distribution and metabolism in the body, the excretion of the drug from the body, and the achievement of response

Front 58

Define: lag time

Back 58

The period of time that elapses between the time of administration and the time a measurable drug concentration is found in the blood. Lag times are often found after PO administration, because of slow disintegration and dissolution of tablets or capsules.

Front 59

Define: lean body weight

Back 59

A patient's body weight minus the fat mass. Drugs of low lipid solubility should be dosed in obese patients according to the lean body weight

Front 60

Define: loading dose, priming dose, or initial dose

Back 60

The dose size used in initiating therapy so as to yeild therapeutic concentrations that will result in clinical effectiveness

Front 61

Define: local effect

Back 61

Obtained when the drug product is administered at the site where the pharmacologic response is desired and when the drug released from the product acts by adsorption to the skin or mucosa or penetrates into the skin or mucosa but does not enter the systemic blood circulation or lymphatic stream.

Front 62

Define: maintenance dose

Back 62

The dose size required to maintain the clinical effectiveness or therapeutic concentration according to the dosage regimen

Front 63

Define: mean transit or residence time

Back 63

The time when 63.2% of an intravenous dose has been eliminated from the pharmacokinetic system

Front 64

Define: metabolism

Back 64

The sum of all the chemical reactions for biotransformation of endogenous and exogenous substances that take place in the living cell.

Front 65

Define: metabolomics

Back 65

The study of change in the global pool of intermediary metabolism present in the target tissues or biological fluids following pathophysiologic stimuli

Front 66

Define: Michaelis-Menten kinetics

Back 66

Uses equations to characterize certain phenomena such as protein binding, adsorption, and nonlinear or saturation processes often observed with increasing dose sizes

Front 67

Define: microconstants

Back 67

Those constants that are part of the hybrid constants; examples: K12, K21, and K13

Front 68

Define: monitoring

Back 68

The determination and recording of drug concentrations during the course of therapy in order to adjust, if necessary, the dosage regimen

Front 69

Define: multiple-dose administration

Back 69

When a drug is given repeatedly at intervals shorter than those required to completely eliminate the drug of the previously given dose

Front 70

Define: nonlinear kinetics or saturation kinetics

Back 70

Refers to the change in one or more of the pharmacokinetic parameters during absorption, distribution, metabolism, and excretion by saturation or overloading of processes due to increased dose sizes.

Front 71

Define: oral administration

Back 71

Buccal, sublingual, and perlingual administration routes, in which the drug is absorbed from the mouth cavity (no first-pass effect)

Front 72

Define: peripheral compartment

Back 72

The sum of all body regions to which a drug eventually distributes but is not in instantaneous equilibrium; sometimes further subdivided into a shallow and deep compartment

Front 73

Define: peroral administration

Back 73

Indicates that the dosage form is swallowed and the drug is absorbed from the GI tract (first-pass effect possible)

Front 74

Define: personalized medicine

Back 74

The application of quantitative and qualitative approaches and their integration in a systems biology context to produce individualized approaches to drug therapy. The goal is to select the most appropriate drug and dosing regimen or a given pt by exercising a degree of adaptive control that will account for variability and thereby improve the chances of producing safe and effective treatment

Front 75

Define: pharmaceutical alternatives

Back 75

Drug products that contain the identical therapeutic moeity, or its precursor, but not necessarily in the same amount or dosage form or as the same salt or ester.

Front 76

Define: pharmaceutical equivalents

Back 76

Drug products that contain identical amounts of the identical active drug ingredient, in identical dosage forms, but not necessarily containing the same inactive ingredients

Front 77

Define: pharmacodynamics

Back 77

Both the qualitative and quantitative description of drug effect; this may include physicochemical characterization of drug-receptor or drug-organism interaction and how drug effect changes as a function of exposure (concentration) and time

Front 78

Define: pharmacogenetics

Back 78

Deals with interindividual variation in DNA sequence related to drug absorption and distribution or drug action

Front 79

Define: pharmacogenomics

Back 79

The application of genomic principles and technologies in drug discovery to pharmacologic function, disposition, and therapeutic response

Front 80

Define: pharmacokinetics

Back 80

Deals with the changes of drug concentration in the drug product and changes of concentration of a drug and/or its metabolite(s) in the human or animal body following administration. LADMER

Front 81

Define: polymorphisms

Back 81

Reflect different forms of a gene that control the functional expression of a protein

Front 82

Define: protein binding

Back 82

The phenomenon that occurs when a drug combines with plasma protein or tissue protein to form a reversible complex; usually nonspecific and depends on the drug's affinity for the protein molecule, the number of protein-binding sites, and protein and drug concentrations. Drugs can be displaced from protein-binding sites by other compounds having higher affinity for the binding sites

Front 83

Define: rate-limiting step

Back 83

The process with the slowest rate constant in a system of simultaneous kinetic processes

Front 84

Define: receptor

Back 84

A site in the biophase to which drug moleculescan be bound; a substrate is usually a protein or proteinaceous material

Front 85

Define: relative bioavailability

Back 85

The extent of drug absorbed upon extravascular administration in comparison with the dose size of a standard administered by the same route.

Front 86

Define: renal clearance

Back 86

The hypothetical plasma volume in mL (volume of distribution) of the unmetabolized drug that is cleared per unit of time via the kidney

Front 87

Define: single-dose administration

Back 87

Occurs when the next dose of the same drug is administered only after the drug of the previously given dose is completely eliminated from the body

Front 88

Define: sorption promoters or permeation enhancers

Back 88

Define as substances that have no pharmacologic properties of their own in the amount used, but which can improve the penetration of drugs into the skin or their permeation through skin or mucosa by reducing the barrier resistance

Front 89

Define: steady state

Back 89

A level of drug accumulation in blood and tissue upon multiple dosing when input and output are at equilibrium; drug concentration fluctuate (oscillate) between a max and min. steady-state concentration within each of the dosing intervals

Front 90

Define: structural-nonspecific drugs

Back 90

Those whose pharmacologic action is not directly dependent on chemical structure; they have no functional groups, are highly lipophilic, and do no react easily; they act by physicochemical processes.

Ex: ether, nitrous oxide, halothane, phenol, ethyl alcohol...

Front 91

Define: structural-specific drugs

Back 91

Those whose pharmacologic action results primarily from their chemical structure; they have functional groups and combine to the three-dimensional structure of receptors in the biophase.

Ex: antibodies

Front 92

Define: sustained release

Back 92

The property of prolonged-release dosage forms in which the liberation (drug release) rate constant is smaller than the unrestricted absorption rate constant

Front 93

Define: systemic effect

Back 93

Obtained when the drug released from the drug product enters the bloodstream and/or lymphatic stream and is distributed within the body or at least in several organs, regardless of the site and route of administration

Front 94

Define: total clearance

Back 94

Describes the clearance of the hypothetical plasma volume in mL (volume of distribution) of a drug per unit of time due to excretion and metabolism

Front 95

Define: transporters

Back 95

Consist of transmembrane proteins with specialized functions that enable the translocation of a xenobiotic across a biological membrane and, in most instances, against a concentration gradient; characterized by substrate specificity and can control either drug influx or efflux

Front 96

Define: unit membrane

Back 96

The physical barrier to transport in the body; it is lipoidal in nature and consists of a double row of phospholipids sandwiched between one layer each of protein

Front 97

Define: urinary recycling

Back 97

The phenomenon occurs when drugs filtered through the glomeruli are reabsorbed from the tubuli into systemic circulation

Front 98

Define: vehicle

Back 98

The carrier of the drug in the drug product; it is composed of all necessary vehicle substances

Front 99

Define: vehicle substances

Back 99

Additives that are necessary for formulating a dosage form from the drug; should be chemically inert and should not have any pharmacologic effect on the dose used.

Front 100

Define: volume of distribution

Back 100

Not a "real" volume but an artifact--a hypothetical volume of body fluid that would be required to dissolve the total amount of drug at the same concentration as that found in the blood; it is a proportionality constant relating the amount of drug in the body to the measured concentration in biological fluid (blood, plasma, or serum)

Front 101

4 types of tissue?

Back 101

1. Epithelial

2. Connective

3. Muscular

4. Nervous

Front 102

4 types of epithelial tissue?

Back 102

1. Simple Squamous (single layer of flat cells; alveoli of lungs, GI membrane, glomerular capsule and loop of Henle)

2. Simple Columnar (one row of tall cells; secreting cells of glands, respiratory tract, reproductive organs, GI tract)

3. Stratified Squamous (several layers of cells, top layer flattened; outer layer of skin, mouth, esophagus, pharynx)

4. Stratified Columnar (several layers of cells, top layer columnar; vagina, nose, larynx, trachea, larger bronchi)

Front 103

3 types of muscle tissue?

Back 103

1. Skeletal (voluntary or straited; attached to bones, eyeball muscles, upper 1/3 of esophagus)

2. Visceral (involuntary or smooth; walls of tubular viscera, walls of blood vessels, ducts of glands)

3. Cardiac (branching; wall of heart)

Front 104

6 types of connective tissue?

Back 104

1. Areolar (loose connective tissue; between other tissues)

2. Adipose (fat; padding)

3. Dense fibrous (tendons, ligaments, deep fascia, scars, capsule of kidney)

4. Hematopoietic (myeloid [bone marrow], lymphatic or lymphoid [lymph nodes, spleen, thymus gland, tonsils])

5. Bone (skeleton)

6. Cartilage (hyaline [nasal septum, larynx], fibrocartilage [discs between vertebrae], elastic [external ear]