FARMAKOKINETIKA KLINIK (1)

(Program MFK)

BUDI SUPRAPTI
 PHARMACOKINETICS

Application of kinetics to pharmacon (drug and poison)

The science of the quantitative analysis between organism

and drug

The purpose of pharmacoknetics is to study the time course

of drug and metabolit concentrations and amounts in
biological fluids, tissue and excreta, and also pharmacological
response, and to construct suitable models
PHARMACOKINETIC

The science of kinetics of drug absorption, distribution

and elimination (i.e. excretion and metabolism)

 Using mathematical model and statistic

Drug distribution and elimination  drug disposition

 CLINICAL PHARMACOKINETICS

The application of pharmacokinetics methods to the

safe and effective therapeutic management of
individual patient.

To optimized dosing strategies – individually

Based on px’s desease state and px’s-specific cond.
 muldisciplinary approach

POPULATION PHARMACOKINETICS
The study of pharmacokinetic differences of drugs
in various populations groups
drug/product development
individualization
MODEL FARMAKOKINETIKA

MODEL : A hypothesis using mathematical terms to describes

quantitative relationships concisely

Mathematical models that represent the system of interest

and “can be used to explore the structure and behaviour
of the system (Wastney et.al., 1997)

PREDICTIVE CAPABILITY
 the proper selection and development of mathematical
function that parameterize the essential factor governing
the kinetic process
MODEL FARMAKOKINETIKA

PHARMACOKINETIC PARAMETERS
 Fitting the model to the experimental data

 dose
 time of administration
 time of sampling
VARIOUS OF COMPARTMENT MODEL
PHARMACOKINETIC PARAMETER

ka – absorption rate constant

tmax – time to peak concentration
Cmax – maximum concentration
Vd – volume of distribution
Cl – Clearance
ClR – renal clearance
Clh – hepatic clearance
k– elimination rate constant
Ke – urinary excretion rate constant
t1/2 – half life
 BIOPHARMACEUTICS

TOXICOKINETICS PHARMACOGENETICS

PHARMACOKINETICS CHRONO-
THERAPEUTIC
PHARMACOKI-
DRUG
NETICS
MONITORING

INVOLVED IN INVOLVED IN DRUG

PRACTICAL DELIVERY
THERAPEUTICS TECHNOLOGY
INVOLVED IN
TARGETING OF DRUG
THE USE OF PHARMACOKINETIC KNOWLEDGE

•Est. of rates of abs., dist., metab., urinary excretion

•Bioavailability-bioequivalence.
•Pred. of blood level after multiple doses based on single dose
•Design of improved drugs
•Optimize Dosage regimen of specific drugs
•Pred. of appropriate dosage reg. for indiv. Patient
•Relating pharmacologic response to drug conc. in plasma,
other biological fluid
•Est. the possible accumulation of drugs and/or metabolite
•The effect of food on absorption of drugs
•Describe the change of physiologic or diseases affect the ADME
of drug
THE USE OF PHARMACOKINETIC KNOWLEDGE (cont.)

•Pharmacogenetics
param.to analyze constributions of genetic and
enviroment effects
 metab/dist.- genetic control
•Studies of mech. of absorption, excretion
•Studies of site of metabolism
•Effect of protein binding on drug distribution
•The cause of capacity limited metabolism of a drug if exist
•Elucidating drug interactions
•Toxicology
Determining the cause of toxicity of a drug
Determining how to reduce or avoid toxicity