EXAM 1 Flashcards

(61 cards)

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
extraction ratio
provides a direct measurement of drug removal from the liver following oral administration of a drug
26
extraction ratio equation
=(drug concentration in the blood entering the liver-drug conc. leaving the liver)/ drug conc. in the blood entering the liver
27
extraction ratio represents
the amount of drug that is removed by the liver before it is available for systemic circulation
28
Modified released characteristics compared to IR
Tmax longer Cmax reduced AUC identical
29
Steady-state equation
(Cpss)=(dose x F x S)/(Tau x Cl)
30
What does S represent
represents the fraction of the administered dose which is the active drug when administered as a salt or ester formulation
31
S equation
S=MW of parent drug/total weight
32
factors affecting drug distribution
cardiac output regional blood flow membrane permeability tissue volume Regional physiological pH changes disease states altering physiological factors
33
solute carriers
Oligopeptide transporter Organic anion transporter protein Organic cation transporter
34
ATP-Binding Cassette
MDR1 or P-glycoprotein
35
distribution constant equation
Kd=organ blood flow (Q)/ [volume of the organ (V) x Ratio drug concentration (R)]
36
large Q does what to distribution time
decreases distribution time
37
large tissue volume (V) does what to distribution time
increases distribution time -longer time needed to fill a larger volume
38
partition coefficient
physical property that measures the ratio of the solubility of the drug in the oil phase to the solubility in the aqueous phase
39
partition coefficient equation
Log P= Log (Coil/Cwater)
40
R ratio
concentration in tissue/concentration in plasma
41
higher R-value indicates
increase in time to equilibration between tissue and plasma
42
larger R-value associated with
larger Vd slower Kd longer t1/2 tissue affinity and binding to proteins within myocardium
43
limiting processes of drug distribution
concentration gradient membrane thickness membrane surface area lipid solubility/partition coefficient diffusion constant
44
perfusion limited distribution
rate of drug delivery from circulation to the tissue is largely dependent upon blood flow to that tissue
45
perfusion limited distribution rate-limiting step
blood flow
46
permeability limited distribution
drug distribution is limited by the slow diffusion of the drug across the membrane in the tissue
47
volume of distribution
indicator of the extent of drug distribution into the body fluids and tissues
48
volume of distribution equation
Vd=dose/drug concentration in system after equilibrium
49
loading dose equation
=Vd(desired Cp)/(F x S)
50
smaller Vd from
high water solubility increased plasma protein binding decreased tissue binding
51
larger Vd from
high lipid solubility decreased plasma protein binding increased tissue binding
52
percent protein binding equation
={total drug concentration-Cp(unbound)/total drug conc.} x 100
53
factors that affect protein binding
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
elimination
irreversible drug removal from the body results from the processes of metabolism and excretion
55
two major organs involved in the elimination
kidneys and liver
56
drug clearance
removal of drug from a volume of plasma or blood in a given time
57
Compartmental model clearance equation
Clt= Vd x Ke
58
physiological model clearance equation
Clorgan=Q x ER
59
factors affecting clearance
body weight, SA and comp. cardiac output organ function drug-drug interactions extraction ratio genetics plasma protein binding
60
clearance equation
= dose x F x S/Tau x average Cpss
61
steady state
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