Basic concepts Flashcards

1
Q

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

A

Absolute bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

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.

A

Absorption

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

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

A

Absorption rate constant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

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

A

Accumulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

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.

A

Apparent partition coefficient

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

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

A

Area under the curve

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

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

A

Biliary recycling/

Enterohepatic recirculation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

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

A

Bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

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

A

Bioequivalence

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

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

A

Bioequivalence requirement

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

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

A

Biopharmaceutics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

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

A

Biophase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

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

A

Blood flow rate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

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

A

Blood, plasma, serum level

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

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

A

Central compartment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

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

A

Clearance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

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

A

Compartment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

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

A

Concentration gradient

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

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.

A

Cumulative urinary excretion curve

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

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

A

Depot phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

the viscous layer of concentrated drug solution around a dissolving particle

A

Diffusion layer

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

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

A

Disposition

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

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.

A

Dosage regimen/

Dose rate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

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

A

Dose dependency

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

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

A

Dose dumping

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

amount of drug in µg, mg, units

A

Dose size

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

time period between administration of maintenance doses

A

Dosing interval

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

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

A

Drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

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

A

Drug candidates

30
Q

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

A

Drug product/

Dosage form

31
Q

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.

A

Drug release/

Liberation

32
Q

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

A

Drug specialty/

Brand product

33
Q

active ingredients within a dosage form

A

Drug substances

34
Q

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

A

Elimination half-life

35
Q

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

A

Enzyme induction

36
Q

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

A

Enzyme inhibition

37
Q

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

A

Excretion

38
Q

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.

A

Extravascular administration

39
Q

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.

A

Feathering

40
Q

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.

A

First pass effect

41
Q

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

A

Generic product

42
Q

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

A

Hepatic clearance

43
Q

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

A

Initial phase

44
Q

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

A

Intravascular administration

45
Q

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

A

IV Bolus

46
Q

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

A

LADMER system

47
Q

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.

A

Lag time

48
Q

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

A

Leads

49
Q

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

A

Loading / Primary / Initial dose

50
Q

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

A

Local effect

51
Q

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

A

Maintenance dose

52
Q

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

A

Metabolism

53
Q

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

A

Peripheral compartment

54
Q

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

A

Pharmaceutical alternatives

55
Q

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

A

Pharmaceutical equivalence

56
Q

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

A

Pharmacokinetics

57
Q

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

A

Protein binding

58
Q

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

A

Rate-limiting step

59
Q

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

A

Receptor

60
Q

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

A

Relative bioavailability

61
Q

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

A

Semi-logarithmic plot

62
Q

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

A

Sorption promoters / permeation enhancers

63
Q

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

A

Steady state

64
Q

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

A

Structural nonspecific drugs

65
Q

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.

A

Structural specific drugs

66
Q

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

A

Sustained release

67
Q

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

A

Systemic effect

68
Q

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.

A

Unit membrane

69
Q

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

A

Urinary cycling

70
Q

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.

A

Vehicle substances

71
Q

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

A

Volume of distribution