ABSORPTION OF DRUGS

ISHAQ ARSHAD
PHARMACOKINETICS
 PHARMACOKINETICS :means what the
body does to the drug. It includes,
 Absorption,Distribution, metabolism and

elimination of drug.
 ABSORPTION
 Transfer of drug from the site of

administration to the bloodstream.

 Mechanisms of absorption from the
GI tract
 Depending on the chemical properties,
drugs can be absorbed from the GI tract
by:
 1.Passive diffusion
 2.Facilitated diffusion
 3.Active transport
 4.Endocytosis
Passive diffusion
Drug moves from an area of high
concentration to lower concentration.
1.It does not involve a carrier.
2.It is not saturable.
3.Water-soluble drugs penetrate cell
membrane through aqueous channels or
pores.
4.Lipid-soluble drugs move across cell
membranes due to solubility in the
membrane lipid bilayer.
Facilitated diffusion
Drugs can enter cell through specialized
trans- membrane carrier proteins that
facilitate the passage of large molecules.
This process is known as facilitated
diffusion.
1-It does not require energy.
2-Can be saturated,
3-It may be inhibited by compounds that
compete for the carrier.
Active transport
1. Drugs move against a concentration
gradient, from lower concentration to
higher concentration.
1- It is energy dependent which is
provided by ATP.
2- This process is saturable.
3-It is selective
4-It is competitively inhibited by co-
transported substances
 Endocytosis and exocytosis
Endocytosis involves engulfment of a drug by the
cell membrane and transport into the cell by
pinching off the drug filled vesicle. Exocytosis is
the reverse of endocytosis.
1. It is used to transport drugs of exceptionally
large size across the cell membrane.
2. Vitamin B12 is transported across the gut wall
by endocytosis, whereas certain
neurotransmitters (norepinephrine) are
transported by exocytosis.
Factors AFFECTING absorption

1-Effect of pH on drug absorption:

1. Ionized drugs are water-soluble and

cannot cross the membrane.

2. Unionized drugs are lipid-soluble and

can cross the membrane.
Factors AFFECTING absorption

2-Blood flow to the absorption site:

1. Intestine receive more blood than

stomach so absorption in intestines is
more.

2. Shock severely reduces blood flow to the

skin therefore minimizing absorption from
subcutaneous ( S/C) route
Factors AFFECTING absorption

3-Total surface area available for

absorption:

Intestines have a surface area of about

1000 times that of stomach containing
microvilli so the absorption from the
intestines is more efficient.
Factors AFFECTING absorption
4-Contact time at the absorption surface:
1.In diarrhea drug moves through GIT very
quickly so it is not well absorbed.
2. Delay of transport of drug from stomach
to intestines delays rate of absorption.
3.Drug taken with food is absorbed more
slowly.
Factors AFFECTING absorption
P-glycoprotein:
1. P-glycoprotein is a transmembrane protein that
pumps drugs out of the cells.

2. It is found throughout the body specially in

liver ,kidneys ,brain capillaries, placenta and intestines.

3. Where there is more P-glycoprotein drug absorption

is reduced.

4. It is also related with multidrug resistance.