ROZAIMAH ZAIN-HAMID

HASANUL ARIFIN
Department of Pharmacology and Therapeutics Faculty of Medicine, Universitas Sumatera Utara

Pharmacokinetic
Site of action/ receptor binding drug free drug Tissue depot free drug binding drug

SYSTEMIC CIRCULATION

Absorption

free drug

Excretion

binding drug

metabolite

Biotransformation
RZH HA - Faculty of Medicine - USU

What is drug absorption?

RZH HA - Faculty of Medicine - USU

Drug absorption Drug Through the biologic membrane

(>>>phospholipids & protein)

Systemic circulation Drug bioavailability AUC (Area Under the Curve)

RZH HA - Faculty of Medicine - USU

Drug bioavailability

RZH HA - Faculty of Medicine - USU

Pharmacokinetic
Bioavailability AUC
The fraction of the dose which reaches the systemic circulation in unchanged form depend on:
Drug absorption First pass metabolism
RZH HA- Faculty of Medicine - USU

FACTORS AFFECTING BIOAVAILABILITY

Gut lumen
Drugs in gut

Portal circ.
Drug absorbed intact

Liver

Systemic circ.
Drug absorbed intact and escaping first-past metab.

60 100 80 60 20

Drug extracted first-past

RZH HA- Faculty of Medicine - USU

Drug mechanism through the biologic membrane

RZH HA - Faculty of Medicine - USU

Drug absorption Through the biologic membrane

Passive diffusion Facilitated diffusion Active transport Pinocytosis

RZH HA - Faculty of Medicine - USU

 Passive diffusion
Through the biologic membrane Higher conc. lower conc.
(the process requiring no direct expenditure of energy by biologic system)
RZH HA - Faculty of Medicine - USU

 Facilitated diffusion
Through the biologic membrane Higher conc. lower conc.
(the process is limited by the availability of carrier)
RZH HA - Faculty of Medicine - USU

 Active transport
Through the biologic membrane Lower conc. higher conc.
(the process requiring cellular energy)
RZH HA - Faculty of Medicine - USU

 Pinocytosis
Through the biologic membrane

The process of engulfing particles or dissolved materials by local invagination of cell membrane (vesiculation)
(the process requiring of cellular energy)
RZH HA - Faculty of Medicine - USU

JENIUS TERDIRI DARI 1 % ILHAM & 99 % KERINGAT/ KERJA KERAS

RZH HA - Faculty of Medicine - USU

Factors influence drug absorption

RZH HA - Faculty of Medicine - USU

Factors influence drug absorption

Physical propeties Chemical properties

RZH HA - Faculty of Medicine - USU

Physical properties

Size of drugs particle Route of drug administration Surface area for absorption Blood circulation on site of absorption
RZH HA - Faculty of Medicine - USU

Physical properties
Drugs diffuse down concentration

The concentration are equal in all parts of the body

RZH HA - Faculty of Medicine - USU

Chemical properties

Lipid solubility of the drug Degree of ionization

pKa of the drug

RZH HA - Faculty of Medicine - USU

Chemical properties of drugs

1. Unionized lipid soluble drugs pass most readily through biologic membrane
2. Ionized drugs or low lipid solubility drugs are relatively impermeable to biologic membrane
RZH HA - Faculty of Medicine - USU

The lipid solubility and degree of ionization of the drug, regulate its absorption, distribution and elimination

these same properties are major determinant of drug selectivity, intensity and duration of action
RZH HA - Faculty of Medicine - USU