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FARMAKOKINETIKA

Maya Dian Rakhmawatie, FK UNIMUS


The various phases of drug action
I. Pharmaceutical phase

Dose Disintegration of dosage form


Dissolution of active substance
(Pharmaceutical Drug available for
availability) absorption

II. Pharmacokinetics phase


Absorption, distribution, metabolisme,
Object excretion
(Biologival Drug available for
Result availability) action
III. Pharmacodynamic phase
Advantage Drug-receptor interaction Effect
DEFINITION

Pharmacokinetics is
* the study of rate processes involved in
the absorption, distribution, metabolism,
and excretion of drugs
* their relationship to the
pharmacological, therapeutic, or toxic
response in animal or humans
MEANING

1. Subject of kinetics  concerned  the


relationship between the movement of a
drug through the body and the processes
affecting it.
What the body does to the drug?
Not
What the drug does to the body?
2. It is a discipline which describes the
time-course of the movement of a drug
into, around, and out of the body
(fate of drug in the body).
INTO
Absorption D
Central

AROUND D D
Distribution Central Peripheral

OUT D D
Elimination
Central Peripheral

Pharmacokinetic parameters
• rates constant (How fast?)
• transferable concentration (How much?)
3.The uses of pharmacokinetic knowledge are to
describe, predict and control the
pharmacological, therapeutic and toxic response
of a drug
(describe what happens?).

Pharmacokinetics should use words beside


symbols and mathematical equations to express
and predict drug behavior.
4.There are two important basic concepts
(i.e. order kinetics and compartment model)
for describing the fate of drug in the body.
PROCESS OF THE STUDY
Dose (IV or EV) Subject/
Biological
System

Sampling

Assay

Plotting concentration vs time


Calculating parameters

Analysis & Application


Evaluation
NOTATIONS and THE MEANING in PHARMACOKINETICS

CONCENTRATION

C  concentration
C0  at time 0
Ct  at any certain time
Cmax  maximum concentration
Cmin  minimum concentration
Css  concentration at steady state
NOTATIONS and THE MEANING in PHARMACOKINETICS

VOLUME DISTRIBUTION

Vd  Volume distribution
Vd  Dose
Co
Influenced the amount of body fluid (hydrophilic /
hydrophobic), drug binding to proteins
NOTATIONS and THE MEANING in PHARMACOKINETICS

T ½ ELIMINATION

Time needed for drug levels in the blood is reduced to


half its original level
Short t ½ < 3 hour
Medium t ½ 3 – 6 h
Long t ½ 8 – 14 h
Very long t ½ > 14 h
NOTATIONS and THE MEANING in PHARMACOKINETICS

AREA UNDER CURVE (AUC)

AUC Model (Compartment Model)  Co/k


AUC Non Model (Trapezoid)  describes the drug
levels physiologically
NOTATIONS and THE MEANING in PHARMACOKINETICS

CLEARANCE (CL)

A parameter elimination, clearance of drugs from the


body fluid per unit time

Elimination of a drug changes according to the levels


of the drug in the body
JOURNEY FROM THE PLACE OF DELIVERY OF THE DRUG, THE
ACHIEVEMENT OF THE CIRCULATORY SYSTEM UNTIL THE
ONSET OF EFFECT
Per Oral Mouth

Gastric

Intestine
Lymphatic Intestinal Flora Rectal Bile
Intestinal Wall
Intra Peritoneal
liver
Iv, im, sc, buccal
Lungs inhalation

Central Compartment elimination

Periphery Compartment Effect


PLACE OF PHARMACOKINETICS
IN OTHER SPECIALITIES

Biophamaceutics Targeting of Drugs

Pharmacogenetics
First Past effect
TDM Pharmacokinetics

Practical Chronophar-
therapeutics Drug delivery macokinetics
technology
COMPARTEMENT MODELS

Simplify the structure of the body (animal or human)


complex into a simple mathematical model to explain the
concept of ADME
Compartment Models Non Compartment Models/
a. 1-compartment Physiology Models
b. 2-compartment To link the relationship between
dose, drug levels, and drug
disposition in the body tissues
2-compartment models

1-compartment models Piotrowski, JK. 1977. Retention and Excretion Kinetics


of Chemical Agents. Wiley Online Library
NARROW THERAPEUTIC RANGE

DRUG DISEASE/CONDITION THERAPEUTIC RANGE


(mg/L)
Salicylic acid Rheumatic fever 250 – 400

Valproic acid Epilepsy 40 – 100

Gentamycin Antibiotic 4 – 12

Digoxin Cardiac Dysfunction 0,01 – 0,02

Warfarin Thromboembolism 1- 4

Amitriptyline Depression 0,12 – 0,25

Dipiro et al, 2005 ; Rowland and Tozer, 2005


Orde Reactions

Orde-0
Any number of drugs, its elimination rate remains

Orde-1
Drug elimination velocity proportional to the amount of drug
remaining
REFFERENCES

1. Atlas of Pharmacology
2. Hakim, L. 2011. Farmakokinetik. Yogyakarta:
Bursa Ilmu
3. Another Pharmacology Handbooks

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