PERAN PARAMETER FARMAKOKINETIK

DALAM TERAPI
Mata Kuliah : Farmakokinetik
Dosen Pengampu : Rovina Ruslami, dr., SpPD,
PhD

Oleh : Neni Anggraeni (130120150011)

Parameter farmakokinetika adalah besaran yang

diturunkan secara matematis dari model yang berdasarkan
hasil pengukuran kadar obat utuh atau metabolitnya dalam
darah, urin atau cairan hayati lainya. Parameter
farmakokinetik suatu obat ini dapat digunakan untuk
memperoleh gambaran dan mempelajari suatu kinetika
absorpsi, distribusi dan eliminasi didalam tubuh.

Volume Of Distribution
Volume of distribution (V) relates the amount of drug in the body to
the concentration of drug (C) in blood or plasma:

Volume distribusi dapat berubah karena umur, jenis kelamin, dan

penyakit
Obat yg terikat dgn protein plasma, sebagian besar obat berada
didalam darah maka volume distribusinya akan mempunyai batas
terendah. (warfarin & klorpropamid)

Clearance
Drug clearance principles are similar to the clearance concepts of renal
physiology. Clearance of a drug is the factor that predicts the rate of
elimination in relation to the drug concentration (C)

Clearance, like volume of distribution, may be defined with respect to blood

(CLb), plasma (CLp), or unbound in water (CLu), depending on where and
how the concentration is measured.

Clearance
Elimination of drug from the body may involve processes occurring in the
kidney, the lung, the liver, and other organs.

Clearance
Capacity-Limited Elimination
Most drug elimination pathways will become saturated if the dose and
therefore the concentration are high enough. When blood flow to an organ
does not limit elimination, the relation between elimination rate and
concentration (C) :

Half Life
Half-life (t1 /2) is the time required to change the amount of drug in the body
by one-half during elimination (or during a constant infusion).
The time course of drug in the body will depend on both the volume of
distribution and the clearance:

Bioaviability

A RATIONAL DOSAGE REGIMEN

A rational dosage regimen is based on the assumption that there is a target
concentration that will produce the desired therapeutic effect.
Penentuan Dosis berdasarkan :
Jumlah obat yang diberikan dalam satu
waktu
Cara pemberian
Jarak waktu diantara dua dosis
Lama waktu pemberian obat

Maintenance Dose
At steady state, the dosing rate (rate in) must equal the rate of elimination
(rate out). Substitution of the target concentration (TC) for concentration (C)
in equation predicts the maintenance dosing rate:

Maintance Dose = Dosing rate x Dosing interval

Loading Dose
The volume of distribution is the proportionality factor that relates the total
amount of drug in the body to the concentration; if a loading dose is to
achieve the target concentration

Efek Penyakit Terhadap Proses Farmakokinetik

Keadaan patologis dapat merubah semua parameter farmakokinetik
Umumnya kelainan hati dapat mengurangi clearance dan memprlama half time
obat. Tetapi pada obat-obat tertentu terjadi sebaliknya.
Contoh : tolbutamid pada penyakit hepaitis virus akut.
Perubahan farmakokinetik pada penyakit ginjal dapat diterangkan dengan
konsep clearance.
Cl ginjal = (Cl RF + Cl RS) x (1-FR)
Ekskresi ginjal di tentukan oleh Filtrasi, sekresi aktif, dan reabsorpsi.
Filtrasi : Volume cairan yg difiltrasi & konsentrasi obat yg tidak terikat didalam
plasma.