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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
how do physiochemical properties effect mechanism of elimination
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
how can we calculate clearance
total CL = hepatic CL + renal CL + all other CL
25
why is a half life an elimination parameter
it takes 5 half lives for a compound to reach stead-state after chronic exposure
26
what is the relationship between CL, Vd and t1/2
CL/Vd = K t1/2 = 0.693/k
27
what is one compartment model
linear processes assumed all tissues/organs lumped into one compartment v= volume of distribution k = elimination rate constant
28
what is 2 compartment model
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
what is the central compartment
blood heart lungs liver kidneys
30
what are the features of population pharmacokinetic models
intensive and sparse sampling computationally intensive longer analysis time allows provision for PK/PD modelling
31
what are the ads of individual PK
simple robust model-independent user friendly software rapid
32
what are the disadvantages of individual PK
assume linear PK model-independent single analysis, cannot address multiple doses study design often limits analysis
33
what are the advantages of population PK
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
what are the disadvantages of population PK
less rapid less user friendly software more expertise required for analysis
35
what is PBPK
composed of a series of compartments representing organs or tissues whose drug concentration are assumed to be uniform
36
what are the advantages of PBPK
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
what can the PBPK model approach be used for
stimulation of clinical trials without need for clinical data estimation of tissue specific drug concentrations assessment of potential for drug-drug interactions
38
what is the role of PK in drug development
idea in silico in vitro in vivo in man in clinic treatment
39
what is allometric scaling
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
what is PK/PD relationship
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
what are the beneficial characteristics for drugs with potential for TDM
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
what are the clinical applications of TDM
cardiovascular disease HIV/AIDs epilepsy infections/septicemia respiratory disease
43
what is the rationale for TDM in oncology
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

CM2001 (13 decks)

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