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Kinetics
Exam 1
Question | Answer |
---|---|
Who is the father of pharmacoknetics? | Torsten Teorell |
bio availability is known as | rate and extent |
the assessment of effects of physiological and pathological conditions on drug ADME is known as | clinical PK |
Define CFLADMER | Chemistry Formulation liberation Absorption Distribution Metabolism Excretion Respons |
Define elimination | metabolism and excretion |
define disposition | Distribution, metabolism, and excretion |
By using PK, we can predict ? (3) | dose, dosing interval, target plasma concentration |
A SHORTER half life means a dose is given more or less frequent? | MORE |
Name the (3) crtical determinants of the in vivo performance, safety, and efficacy of the drug product | physiochemical characteristics of API Dosage form Route of admin |
The goal of engineering a drug is to have one that is _____ and gives the desired _________ _________-- | stable, therapeutic response |
acid drug in acidic medium is | unionized |
which route of administration goes directly into systemic circulation | Intravenous |
what is the sceince that examines the interrelationship of the physiochemical properties of the drug, the dosage form, and the route of admin on the rate and extent of systemic drug absorption | biopharmaceutics |
what is the primary concern in biopharmaceutics | bioavailability |
what is the study of techniological and fundamental aspects related to the formulation and fabrication of dosage forms | pharmaceutics |
what studies the physioloical and dosage form factors affecting the release and subsequent absorption of drugs from drug delivery systems | biopharmaceutics |
define in vitro | procedures employing test apparatus and equipment without involving lab animals or humans |
define in vivo | more complex involving human subjects or lab animals |
the science of the kinetics of ADME. Or fate of the drug in the body | pharmacokinetics |
drug distribution and elimination | drug disposition |
application of PK methods to drug therapy | clinical PK |
relationship between the drug concentration at the site of action and pharmacologic response. Or fate of body due to drug action | pharmacodynamic |
which graph is sigmoidal | pharmacodynamics |
PK/PD graph is used to predict | clinical doses |
application of PK principles to the design, conduct and interpretation of drug safety evaluation and used in validating dose related to exposure in animals | toxicokinetics and clinical toxicology |
TK data can be extrapolated to humans. T or F | true |
Define MTC | minimum toxic concentration |
define MEC | minimum effective concentration |
assumption when looking at a plasma level time curve | the drug concentration in plasma is in equilibrium with the tissues |
the minimum concentration of drug needed at the receptor to produce the desired pharmacological effect | MEC |
the concentration needed to just barely produce a toxic effect | MTC |
biopharmaceutic parameters that can be used to describe drug | C max, Tmax, AUC |
is it possible to sample drug at the biophase where the receptor resides | NO |
sampling drug concentrations in the plasma is a ______ measurement | direct |
sampling drug concentrations in the urine, saliva, CSF, feces, and milk are __________ measurements | indirect |
what describes the predictable relationship between plasma drug concentrations and concentrations at the receptor sites | kinetic homogeneity |
blood = | blood cells and plasma |
plasma = | serum and clotting factors |
are blood or plasma concentrations used in PK | plasma |
plasma samples have to go through an addition procedure in ordert o obtain the free drug level. T or F | True |
the major variability in the therapeutic outcomes is due to | pharmacokinetic variability |
a graph is NEVER required for data analysis . T or F | true |
A graph changes data. T or F | False |
a graph represents data in an easily comprehended, visual manner. T or F | true |
on semilog, which axis is typically log | Y axis |
on linear paper, both x and y axes are in logarithmic fashion. T or F | False, log-log paper |
Should you place trailing zeros after a decimal point? | no |
a leading zero should always be placed before the decimal point. T or F | True |
y=mx + b; define each letter | y= dependent variable m=slope x= independent variable b= intercept |
dependent variable axis | ordinate |
independent variable axis | abscissa |
slope is defined as | the change in y over the change in x |
on a semi long, when solving for slope, is the x or y as a ln | the Y variables |
what is the most common method in kinetics for determing the AUC for plasma concentration vs time date | trapezoidal rule |
log100= log10^2= ? | 2 |
log 1000= log 10 ^3= ? | 3 |
Natural log, base e=? | 2.72 |
log (a times b)= | log A + log B |
log (a/b) = | log A - log B |
log a^n = | n log a |
log e^x = | x |
if the data is plotted and it is a curved line, the slope is or is not constant | is NOT, its a function of X |
zero order processes are common in | chemical engineering |
first order processes are most common in | drugs and chemicals |
michaelis-menton processes are _____and is common in | mixed kinetics, drug metabolism and biochemistry |
michaelis menton kinetics is actuallly a combination of a first order process that turns into a zero order process at higher substrate concentrations. T or F | TRUE |
the rate of a reaction is proportional to the molar concentrations of the reactants each raised to power equal to the number of moelcules undergoing reaction | law of mass action |
In zero order, rate is _______ of concentration | independent |
in first order, rate is _____ of concentration | dependent |
first order depends on how many species | 1 |
a second order process depends on how many species | 2 |
most drugs undergo ______ order | first |
order refers to | the way in which concentration or the amount of drug/reactants influences the rate of a process |
zero order is a _____ administration | continuous |
zero order is only dependent of the _________ of the drug, not the concentration | administration |
for first order, the rate of the concentration vs. time is dependent on the | concentration |
for zero order, the units for rate constant are | mass/time or concentration/time |
for first order, the units for rate constant are | 1/time (ie. 0.5^-hr) |
usually only the parent drug is measured experimentally. T or F | True |
the rate of a reaction is determined experimentally by measureing the disappearance of _________ at given time intervals | the parent drug |
the rate is constant all the time in zero order kinetics. T or F | TRUE |
in zero order, the rate does depend on the amount of drug. T or F. | False, is does NOT |
zero order: it will always be eliminated at a FIXED rate. T or F | true |
Co = | initial concentration at time zero |
C= | concentration at time t |
k= | rate constant |
plotted data, get a straight, zero or first order? | zero |
T 1/2 equation for zero order is | Co/ 2K |
T1/2 equation for first order is | 0.693/ k |
we usually see zero order kinetics resulting from a | saturation of a system, carrier mediated transport, metabolic enzymes, sustained release drug systems, and constant rate infusions |
if a system becomes saturated, what order will it become | zero |
plot data, get straight line = | zero |
plot data, get concave up line | first |
plot semi log data, get concave down line | zero |
plot semi log data, get straight line | first |
how many half lives doe sit take for 100 % of drug to be removed | infinite |
most drugs are delivered as salts. T or F | true |
is the same salt always used between dosage forms? | no |
s value. the s stands for | salt and represents the fraction of the molecule that represents the active drug |
f stands for | bioavailability |
F is NEVER applied with intravenous dosing. T or F | True |
define F | its a function of the particular drug product, by a particular manufacturer given by a particular route and dosage form |
S applies to any dosing route. T or F | True |
S is a function of the | chemical salt, not who makes its or its dosage form |
how to find the amount of drub absorbed or reaching the systemic circulation | = (S)(F)(dose) |
when does S=1 | when a drug is adminstered in its parent or active form |
pharmacokinetic models can | summarize or compress data |
an assumption made in PK models is | plasma concentration of a drug is often assumed to be a reflection of its concentration at its site of action |
do PK parameters change with dose? | NO |
Does Vd change with dose? | NO |
what is a common type of model used in PK | compartmental model |
organs or tissues in which drug distribution is similar are grouped into a compartment. T or F | true |
which organs are typically in the Central | highly perfused organs |
does a compartment represent a specific tissue or fluid or a real physiologic or anatomic region? | NO |
is the mixing of a drug within a compartment assumed to be uniform, rapid and homogenous | YEs |
compartment models are based on linear or nonlinear assumptions? | linear |
should the simplest model be selected first? | yes |
lipophilic drugs are typically described by the _____ compartment | multi |
drugs (mostly polar molecules) are typically described by the ____ compartment | one |
selection of compartment model depends solely upon the _______ characteristics of a drug | DISTRIBUTION |
typically the ______ the drug distribution regardless of the route of admin, the greater the number of compartments required to characterize plazma conc. vs. time data and complex is equation | SLOWER |
Rapid distribution = ______ compartment | one |
a curve in a line represents | the transition from 1 compartment to the next |
no absorption phase is represented in what type of administration | intravenous |
a straight line suggests | instantaneous drug distribution |
two phases in a line suggests _____ compartment and ______distribution | two , slow |
alpha phase= | distribution |
beta phase= | post distribution |
which phase is more rapid | alpha |
which model has an absorption and elimination phase | one |
in a rapid absorption there is no ________ phase | absorption |
in a rapid equilibrium in body you have no _______ phase | distribution |
unless otherwise mentioned, always assume _______ order | first |
AUC represents | extend |
the unit for AUC is | time. concentration |
when is AUC directly proportional to the dose | linear conditions |
AUC= Co/ K OR | y intercept/ slope |
apparent volume of distribution defined | the value of the volume of distribution does NOT have a true physiological meaning |
Vd describeds distribution characteristics of the ___ | drug |
Vd= | dose/Do |
in a one compartment model, the Vd does not change from T=0 to infinite. T or F | true |
Vd is usually published in what units | L/kg |
Clearance defined | the apparent volume of bodily fluids cleared of drug per unit of time |
Cl= | D/AUC |
units for clearance | L/hr/kg or ml/min/kg |
Cl= | Vd x K |