Basic concepts

Question 1

is the extent or fraction of drug absorbed upon extravascular administration in comparison to the dose size administered

Answer 1

Absolute bioavailability

Question 2

the process of 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. The only rare exception is absorption by pinocytosis.

Answer 2

Absorption

Question 3

rate constant of the entire process of drug transfer into the body, through all biological membranes.

Answer 3

Absorption rate constant

Question 4

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

Answer 4

Accumulation

Question 5

the ratio of the concentrations at equilibrium between a lipid phase (usually n-octanol) and an aqueous phase (usually buffer pH 7.4). The apparent partition coefficient is uncorrected for dissociation or association in either phase.

Answer 5

Apparent partition coefficient

Question 6

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

Answer 6

Area under the curve

Question 7

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

Answer 7

Biliary recycling/

Enterohepatic recirculation

Question 8

rate and extent to which an active drug substance or moiety is absorbed from the pharmaceutical dosage form and becomes available at its site of action

Answer 8

Bioavailability

Question 9

achieved if its extent and rate of absorption are not statistically different from those of the standard when administered at the same molar dose

Answer 9

Bioequivalence

Question 10

requirement imposed by the FDA for in vitro and/or in vivo testing of specified drug products which must be satisfied as a condition of marketing

Answer 10

Bioequivalence requirement

Question 11

deals with the physical & chemical properties of the drug substance, the dosage form, and the body and the biological effectiveness of a drug and/or drug products 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

Answer 11

Biopharmaceutics

Question 12

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, i.e. one of the organelles

Answer 12

Biophase

Question 13

speed of blood perfusion in an organ, usually expressed in mL/100 g organ weight/min. Blood flow rates may differ several-fold between rest and exercise

Answer 13

Blood flow rate

Question 14

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

Answer 14

Blood, plasma, serum level

Question 15

sum of all body regions (organs and tissue) 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

Answer 15

Central compartment

Question 16

is the hypothetical volume of distribution in mL of the unmetabolized drug which is cleared per unit of time (mL/min or mL/h) by any pathway of drug removal

Answer 16

Clearance

Question 17

an entity which can be described by a definite volume and a concentration of drug contained in that volume.

Answer 17

Compartment

Question 18

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

Answer 18

Concentration gradient

Question 19

are plots of the actual cumulative amounts of drug and/or its metabolites excreted into urine versus time upon administration of a drug product by various routes of administration.

Answer 19

Cumulative urinary excretion curve

Question 20

portion of a prolonged release dosage form which liberates the drug from the dosage form at a slower rate than its unrestricted absorption rate

Answer 20

Depot phase

Question 21

the viscous layer of concentrated drug solution around a dissolving particle

Answer 21

Diffusion layer

Question 22

the loss of drug from the central compartment due to distribution into other compartments and/or elimination.

Answer 22

Disposition

Question 23

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

Answer 23

Dosage regimen/

Dose rate

Question 24

change of one or more of the pharmacokinetic processes of absorption, distribution, metabolism, & excretion with increasing dose size

Answer 24

Dose dependency

Question 25

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 dosage form

Answer 25

Dose dumping

Question 26

amount of drug in µg, mg, units

Answer 26

Dose size

Question 27

time period between administration of maintenance doses

Answer 27

Dosing interval

Question 28

chemical compound of synthetic, semisynthetic, natural, or biological origin which interacts with human or animal cells

Answer 28

Drug

Question 29

pharmacologically active compounds undergoing evaluation of their potential as future drug substances

Answer 29

Drug candidates

Question 30

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

Answer 30

Drug product/ | Dosage form

Question 31

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 (liberation rate constant) and the amount of drug appearing in solution.

Answer 31

Drug release/ | Liberation

Question 32

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

Answer 32

Drug specialty/ | Brand product

Question 33

active ingredients within a dosage form

Answer 33

Drug substances

Question 34

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

Answer 34

Elimination half-life

Question 35

the increase in enzyme content or rate of enzymatic processes resulting in faster metabolism of a compound.

Answer 35

Enzyme induction

Question 36

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

Answer 36

Enzyme inhibition

Question 37

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

Answer 37

Excretion

Question 38

refers to all routes of administration except those where the drug is directly introduced into the blood stream. Examples are IM, SC, PO, Oral, Rectal, IP, Topical.

Answer 38

Extravascular administration

Question 39

graphical method for the separation of exponents such as separating the absorption rate constant from the elimination rate constant. It is synonymous with Residual method.

Answer 39

Feathering

Question 40

the phenomenon whereby drugs may be metabolized (not chemically degraded) following absorption but before reaching systemic circulation. Hepatic first pass effect may occur following PO and deep rectal administration. It may be avoided by using sublingual and buccal routes of administration.

Answer 40

First pass effect

Question 41

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

Answer 41

Generic product

Question 42

hypothetical volume of distribution in mL of the unmetabolized drug which is cleared in one minute via the liver.

Answer 42

Hepatic clearance

Question 43

portion of a prolonged release dosage form which is immediately available for absorption

Answer 43

Initial phase

Question 44

all routes of administration where the drug is directly introduced in the blood stream such as IV, IA, IC. Its BA is 100 percent

Answer 44

Intravascular administration

Question 45

physiologic nonsense and poor use of language. The correct term is IV Push

Answer 45

IV Bolus

Question 46

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

Answer 46

LADMER system

Question 47

period of time which elapses between the time of administration and the time a measurable drug concentration is found in blood. Lag times are often found upon PO administration due to slow disintegration and dissolution of tablets or capsules.

Answer 47

Lag time

Question 48

series of structurally related chemical compounds that have shown interesting pharmacological activity and from which drug candidates may be selected

Answer 48

Leads

Question 49

the dose size used in initiating therapy so as to yield therapeutic concentration which will result in clinical effectiveness.

Answer 49

Loading / Primary / Initial dose

Question 50

obtained when the drug product is administered at the site where the pharmacological 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

Answer 50

Local effect

Question 51

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

Answer 51

Maintenance dose

Question 52

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

Answer 52

Metabolism

Question 53

sum of all body regions to which a drug eventually distributes, but is not in instantaneous equilibrium.

Answer 53

Peripheral compartment

Question 54

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

Answer 54

Pharmaceutical alternatives

Question 55

drug products that contain identical amounts of the active pharmaceutical ingredient, i.e. the same salt or ester of the same therapeutic moiety, in identical dosage forms, but not necessarily containing the same inactive ingredients

Answer 55

Pharmaceutical equivalence

Question 56

deals with the changes of drug concentration in the drug product and changes of concentration of a drug and/or its metabolites in the human or animal body following administration

Answer 56

Pharmacokinetics

Question 57

occurs when the drug combines with plasma protein to form a reversible complex

Answer 57

Protein binding

Question 58

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

Answer 58

Rate-limiting step

Question 59

site in the biophase to which drug molecules can be bound. A receptor (substrate) is usually a protein or proteinaceous material

Answer 59

Receptor

Question 60

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

Answer 60

Relative bioavailability

Question 61

method of representing experimental data describing exponential processes that allow them to be presented in linear form

Answer 61

Semi-logarithmic plot

Question 62

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

Answer 62

Sorption promoters / permeation enhancers

Question 63

level of drug accumulation in blood and tissue upon multiple dosing when input and output are at equilibrium.

Answer 63

Steady state

Question 64

those whose pharmacological action is not directly dependent on chemical structure. They have no functional group, are highly lipophilic, and do not react easily. They act by physicochemical processes. Examples include ether, nitrous oxide, halothane, phenol, ethyl alcohol, octyl alcohol, and acetone

Answer 64

Structural nonspecific drugs

Question 65

those whose pharmacological action results primarily from their chemical structure. They have functional groups and combine to the three dimensional structure of receptors in the biophase. Examples include antibiotics, sulfonamides, glycosides, alkaloids, etc.

Answer 65

Structural specific drugs

Question 66

property of prolonged release dosage forms where the liberation (drug release) rate constant is smaller than the unrestricted absorption rate constant

Answer 66

Sustained release

Question 67

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

Answer 67

Systemic effect

Question 68

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.

Answer 68

Unit membrane

Question 69

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

Answer 69

Urinary cycling

Question 70

additives which are necessary in formulating a dosage form from the drug. The vehicle substances should be chemically inert and should not have any pharmacological effect in the dose used.

Answer 70

Vehicle substances

Question 71

hypothetical volume of body fluid that would be required to dissolve amount of drug at the same concentration as that found in the blood.

Answer 71

Volume of distribution