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CM2001 > PED2001 pharmacokinetics > Flashcards

PED2001 pharmacokinetics Flashcards

1
Q

pharmacokinetics - what thew body does to a drug

A

absorption
distribution
metabolism excretion

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2
Q

what are clinical pharmacokinetics

A

the application of pharmacokinetic principles to individual patients

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3
Q

what is pharmacodynamics

A

what the drug does to the body

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4
Q

what is the general order of ADME

A

site of administration - absorption
plasma - distribution, metabolism/excretion
urine/faeces

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5
Q

what are the route of administration of drugs

A

intravenous
oral
intramuscular
subcutaenous
transdermal
inhaled
intrathecal
sublingual
rectal
vaginal

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6
Q

what are the ways of gathering drug administered data

A

oral
IV

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7
Q

what are the ways of gathering blood sample taken data

A

separation of plasma
ultrafiltration
derivatisation

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8
Q

what are the ways of gathering analysis data

A

HLPC - UV detection (microg/ml)
HPLC - fluorescence detection (ng/ml)
LC-MS - mass specific detection (pg/ml)
atomic absorption spectrometry

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9
Q

what is concentration-time profile

A

schematic representation of the relationship between drug exposure, toxicity and response

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10
Q

what are the main types of pharmacokinetics data analysis

A

non compartmental analysis
compartmental
population PK models
physiologically based

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11
Q

what are the PK terms of the straight line PK principles

A

C=-K.T + C0
- c = concentration
- t= time
- k = rate constant
- C0 = concentration at time zero
- negative symbol indicating loss of drug with time

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12
Q

what are elimination rates

A

most commonly need to predict how a drug concentration in the plasma with change with time

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13
Q

what is a zero order process

A

elimination of a constant amount of drug per unit of time (independent of drug concentration)

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14
Q

what is a first order process

A

involve a constant proportion of drug eliminated in a defined time period
ln c = ln c0 - K.T

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15
Q

What is included in absorption

A
  • transfer of a exogenous compound from site of administration into systemic circulation
  • in general lipid-soluble compounds cross cell membranes more easily and are more rapidly absorbed
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16
Q

what are the parameters of absorption

A

CMax - maximum concentration of compounds after administration
TMAX - time at which Cmax is reached

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17
Q

how do you calculate AUC

A

sum all the component trapezoid areas to obtain the total AUC
AUC = Ct/K

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18
Q

how can we calculate bioavailability (F)

A

AUC oral/AUC x dose i.v./dose oral
% in urine as parent compound after oral dosing/ % in urine as parent compound after intravenous dosing

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19
Q

what does distribution depend on

A

its ability to cross cell membranes
blood flow to individual tissies
extent of its plasma protein binding

19
Q

what is the free drug hypothesis

A

only free drug can exhibit pharmacological effect
unbound drug is free to diffuse through membrane and interact with receptors

19
Q

how does protein binding affect distribution

A

greater binding to tissue proteins will result in a larger volume of distribution

20
Q

what is the distribution parameter of volume distribution

A

a dilution factor which represents the relationship between the amount of compound in the body and the plasma concentration

21
Q

what is the relevance of Vd estimates for distribution

A

plasma protein binding = lower Vd
tissue binding = higher Vd

22
Q

What is the equation for Vd

A

plasma volume of drug + apparent tissue volume of drug (fraction unbound in plasma/ fraction unbound in tissue)

23
Q

how do physiochemical properties effect mechanism of elimination

A

volatile gases are eliminated by exhalation
water-soluble compounds are often eliminated to some degree unchanged in the urine
lipid-soluble compound typically undergo metabolism to more water-soluble metabolites that are then excreted in the urine and/or bile

24
Q

how can we calculate clearance

A

total CL = hepatic CL + renal CL + all other CL

25
Q

why is a half life an elimination parameter

A

it takes 5 half lives for a compound to reach stead-state after chronic exposure

26
Q

what is the relationship between CL, Vd and t1/2

A

CL/Vd = K
t1/2 = 0.693/k

27
Q

what is one compartment model

A

linear processes assumed
all tissues/organs lumped into one compartment
v= volume of distribution
k = elimination rate constant

28
Q

what is 2 compartment model

A

assumes body doesn’t conform to one compartment
two compartment models do not represent specific tissues or fluid but may represent a group of similar tissues or fluid
processes of distribution and elimination

29
Q

what is the central compartment

A

blood
heart
lungs
liver
kidneys

30
Q

what are the features of population pharmacokinetic models

A

intensive and sparse sampling
computationally intensive
longer analysis time
allows provision for PK/PD modelling

31
Q

what are the ads of individual PK

A

simple
robust
model-independent
user friendly software
rapid

32
Q

what are the disadvantages of individual PK

A

assume linear PK
model-independent
single analysis, cannot address multiple doses
study design often limits analysis

33
Q

what are the advantages of population PK

A

robust
provides structural model for PK/PD
any administratuion schedule/route
linear and non-linear PK supported
descriptive and predictive
studies can be pooled

34
Q

what are the disadvantages of population PK

A

less rapid
less user friendly software
more expertise required for analysis

35
Q

what is PBPK

A

composed of a series of compartments representing organs or tissues whose drug concentration are assumed to be uniform

36
Q

what are the advantages of PBPK

A

can be used to extrapolate in vivo situations from in vivo or even animal data
allow estimation of drug time course in any organ/tissue of interest incorporated in the model
allow stimulation of different dosing regimens, large-scale clinical trials, drug interactions, parent and metabolite pharmacokinetics

37
Q

what can the PBPK model approach be used for

A

stimulation of clinical trials without need for clinical data
estimation of tissue specific drug concentrations
assessment of potential for drug-drug interactions

38
Q

what is the role of PK in drug development

A

idea
in silico
in vitro
in vivo
in man
in clinic
treatment

39
Q

what is allometric scaling

A

small animals can tolerate relative larger doses due to more rapid drug clearance
longer half life in human equates to increased tissue exposure
limitations in terms of available volumes of blood for studies

40
Q

what is PK/PD relationship

A

correlations investigated between [crizotinib] plasma and ALK/MET inhibition
rate limiting distribution of crizotinib from peripheral blood to target tumour
PK/PD model developed to provide EC50 values for ALK and MET inhibition
ALK is a better target

41
Q

what are the beneficial characteristics for drugs with potential for TDM

A

variable or unpredictable relationship between dose and resulting plasma drug concentrations
ability to correlate measured drug concentrations with efficacy and/or toxicity
availability of reliable and clinically feasible assays

42
Q

what are the clinical applications of TDM

A

cardiovascular disease
HIV/AIDs
epilepsy
infections/septicemia
respiratory disease

43
Q

what is the rationale for TDM in oncology

A

narrow therapeutic window between systemic exposure for toxicity and response for most established anticancer agent
large degree of inter patient variability in drug disposition at a given dosage for vast majority of anticancer drugs

44
Q
A

CM2001 (13 decks)

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