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kinetics > EXAM 1 > Flashcards

EXAM 1 Flashcards

1
Q

kinetic homogeneity

A

The predictable relationship between plasma drug concentration and the concentration at the site of action
–>we assume that the plasma drug conc. directly relate to concentrations in the tissues

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2
Q

biopharmaceutics

A

the interrelationship of the physicochemical properties of a drug, the dosage form in which the drug is given, and the route of administration on the rate and extent of systemic absorption

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3
Q

pharmacokinetics

A

study of the time course of the drug process that determines the concentration of drugs in body fluid and tissues over time

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4
Q

clinical pharmacokinetics

A

The application of PK principles to the safe and effective therapeutic management of drugs in an individual patient

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5
Q

pharmacodynamics

A

the study of the detailed mechanism of action by which drugs produce their pharmacological effect. Refers to the relationship between the drug conc. at the site of action and the resulting effect

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6
Q

therapeutic drug monitoring

A

measurement of drug concentrations and assessment and application of the resulting concentrations to design safe and effective drug regimens

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7
Q

population-based mathematical model

A

determination of parameters based on population PK/PD information, clinical trial data, and patient clinical and/or demographic data

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8
Q

patient-specific mathematical model

A

the utilization of patient-specific drug concentration data to determine PK/PD parameters and individualize the drug regimen

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9
Q

one compartment model

A

all uniform distribution
drug dose–> compartment–> elimination
-Absorption is instantaneous and complete

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10
Q

zero order elimination

A

the amount of drug eliminated does not change with the amount of drug/concentration in the body
-the amount removed remains constant
-the FRACTION of drug eliminated
VARIES

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11
Q

first-order elimination

A

the amount of drug eliminated in a certain period is directly proportional to the amount of drug in the body
-the FRACTION of a drug eliminated remains CONSTANT

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12
Q

Elimination rate constant

A

-Ke
-always a negative number

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13
Q

what does the elimination rate constant tell you

A

the fraction or percentage of the drug dose administered that is removed per unit of time

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14
Q

half-life equation

A

=0.693/Ke

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15
Q

cmax equation

A

dose/Vd

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16
Q

elimination rate constant equation

A

(Ln Cp1/Cp2)/t

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17
Q

Factors affecting drug movement

A

molecular size and structure
degree of ionization
lipid solubility
binding affinity to serum and tissue proteins
drugs affinity for a tissue component

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18
Q

passive diffusion

A

rate is proportional to drug concentration gradient, partition coefficient, and SA for absorption

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19
Q

Active transport

A

carrier mediated
requires a form of energy

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20
Q

facilitated diffusion

A

carrier mediated
does not require energy
Movement occurs down a concentration gradient

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21
Q

surface area effect on absorption

A

small surface area=decreased absorption
duodenum and jejunum are optimal for absorption

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22
Q

GI factors that affect drug absorption

A

surface area
pH
motility
gastric emptying
perfusion
food
disease

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23
Q

bioavailability

A

fraction of the unchanged drug dose that is absorbed from the drug product and reaches the systemic circulation

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24
Q

bioavailability equation

A

F=amount of drug reaching systemic circulation/total amount of drug dose

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25
Q

extraction ratio

A

provides a direct measurement of drug removal from the liver following oral administration of a drug

26
Q

extraction ratio equation

A

=(drug concentration in the blood entering the liver-drug conc. leaving the liver)/ drug conc. in the blood entering the liver

27
Q

extraction ratio represents

A

the amount of drug that is removed by the liver before it is available for systemic circulation

28
Q

Modified released characteristics compared to IR

A

Tmax longer
Cmax reduced
AUC identical

29
Q

Steady-state equation

A

(Cpss)=(dose x F x S)/(Tau x Cl)

30
Q

What does S represent

A

represents the fraction of the administered dose which is the active drug when administered as a salt or ester formulation

31
Q

S equation

A

S=MW of parent drug/total weight

32
Q

factors affecting drug distribution

A

cardiac output
regional blood flow
membrane permeability
tissue volume
Regional physiological pH changes
disease states altering physiological factors

33
Q

solute carriers

A

Oligopeptide transporter
Organic anion transporter protein
Organic cation transporter

34
Q

ATP-Binding Cassette

A

MDR1 or P-glycoprotein

35
Q

distribution constant equation

A

Kd=organ blood flow (Q)/ [volume of the organ (V) x Ratio drug concentration (R)]

36
Q

large Q does what to distribution time

A

decreases distribution time

37
Q

large tissue volume (V) does what to distribution time

A

increases distribution time
-longer time needed to fill a larger volume

38
Q

partition coefficient

A

physical property that measures the ratio of the solubility of the drug in the oil phase to the solubility in the aqueous phase

39
Q

partition coefficient equation

A

Log P= Log (Coil/Cwater)

40
Q

R ratio

A

concentration in tissue/concentration in plasma

41
Q

higher R-value indicates

A

increase in time to equilibration between tissue and plasma

42
Q

larger R-value associated with

A

larger Vd
slower Kd
longer t1/2
tissue affinity and binding to proteins within myocardium

43
Q

limiting processes of drug distribution

A

concentration gradient
membrane thickness
membrane surface area
lipid solubility/partition coefficient
diffusion constant

44
Q

perfusion limited distribution

A

rate of drug delivery from circulation to the tissue is largely dependent upon blood flow to that tissue

45
Q

perfusion limited distribution rate-limiting step

A

blood flow

46
Q

permeability limited distribution

A

drug distribution is limited by the slow diffusion of the drug across the membrane in the tissue

47
Q

volume of distribution

A

indicator of the extent of drug distribution into the body fluids and tissues

48
Q

volume of distribution equation

A

Vd=dose/drug concentration in system after equilibrium

49
Q

loading dose equation

A

=Vd(desired Cp)/(F x S)

50
Q

smaller Vd from

A

high water solubility
increased plasma protein binding
decreased tissue binding

51
Q

larger Vd from

A

high lipid solubility
decreased plasma protein binding
increased tissue binding

52
Q

percent protein binding equation

A

={total drug concentration-Cp(unbound)/total drug conc.} x 100

53
Q

factors that affect protein binding

A

drug concentration
affinity of the protein for the drug
The concentration of the circulating protein
The number of binding sites available
presence of disease or altered physiologic state
presence of other protein-bound drugs
physicochemical properties of the drug

54
Q

elimination

A

irreversible drug removal from the body results from the processes of metabolism and excretion

55
Q

two major organs involved in the elimination

A

kidneys and liver

56
Q

drug clearance

A

removal of drug from a volume of plasma or blood in a given time

57
Q

Compartmental model clearance equation

A

Clt= Vd x Ke

58
Q

physiological model clearance equation

A

Clorgan=Q x ER

59
Q

factors affecting clearance

A

body weight, SA and comp.
cardiac output
organ function
drug-drug interactions
extraction ratio
genetics
plasma protein binding

60
Q

clearance equation

A

= dose x F x S/Tau x average Cpss

61
Q

steady state

A

as the rate of elimination approaches the rate of administration, the max and min concentrations will reach an equilibrium when no additional accumulation will occur

kinetics (2 decks)

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