ONIVERSIlY Of JORDAN

Faculty OF Medicine
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LECTURE NO: II

_ DONE BY: ZAIJ. D> ~MJ

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 By the name of allah

**Type of receptors:
We have 4 types of receptors in every human body.
Receptor: kind of protein among the target and the drug.

1. ligand-gated ion channel:

Ligand means agonist
In this case the interaction between the drugs (agonist) and
receptor causes opening of ion channel.
e.g:
1. Nicotinic receptor
2. Acetyl choline receptor
Location: nervous system
Effect: within milliseconds

2. G-protein coupled receptors

Initiate effects through activation of guanine nucleotide binding
protein
GTP-7 GDP -7 Adenylate cyclase -7 ATP -7 cyclic AMP (2 nd
messenger)
Kinases -7 protein phosphorylation
e.g:
1. muscarinic receptors
2. acetyl choline receptors
3. B- adrenoreceptors
Location: cell membrane
Effect: within seconds
B-adrenoreceptors: leads to glycogen and fat metabolism in liver,
fat and muscle cells

3. Kinase-like receptors
It causes -7 protein phosphorylation -7 Genes transcription -7
protein synthesis -7 cellular effects

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So its action becomes clear after few hours
e.g: insulin, growth factors, cytokines receptors

4. Nuclear receptors
Location: cytoplasm or in nucleus
Effect: after days
e.g: steroid receptors
drugs that don't fit the drug-receptor modal (drugs don't act
through receptors)

the kind of drugs react with their target

such as:
1. osmotic diruretic
2. antacids which give to patient suffering from acidity, in this case
the interaction between acid (mainly HCI) and alkaline (base)
directly without receptors.

The biological Targets could be:

1. Ion channel in our body (e.g: Na+ channel)
2. enzymes
Human body full of enzymes that react with certain type of drugs
3. macromolecules (e.g: DNA, RNA and special proteins)
The interaction between the drug and DNA cause mutation in the
cell.
4. cell membrane carriers:
Certain drugs can't enter the cell without interation with carriers in
cell membrane.

Pharmacokinetics:
The action of human body on the drugs (unlike
pharmacodynamics)
Co: concentration reaction outside
Ci: concentration reaction inside
T: time
As we see all these factors affecting affecting absorption

ADVICE:
Don't sit beside a smoker, because in milliseconds the smoke will
go from lungs to blood (this occur rapidly because large area
of absorption)

Drugs classified to:

1. weak acidic drugs (such as aspirin)
pKa= 3.5
suppose it carries a negative charge
pKa is calculated by:
pKa= pH + Log (concentration of unionized molecules/ cone of
ionized m)
increase in ionization decrease in absorption increases clearly, the
absorption increases when the unionized concentration increase.

2. weak basic drugs (such as Diazepam)

Suppose to carry positive charge (pKa- 3.3)
Calculated by:
pKa = pH + log (cone of ionized! cone of unionized)

3. neutral drugs (don't carry any charge)

Mechanism of drug transport across membranes
1. passive diffusion ,<-

Down their cone gradient (from high to low cone)

Molecule must be: .
1. unionized
2. small
3. lipid soluble
Rate of diffusion depends on: lipid-water solubility
Process of pharmakinetics, for example:
1. absorption
2. distribution
3. metabolism
4. elimination

N.B: the same drugs could be in many forms so at certain time of

illness, we give certain form (depends on worsening)

1. drug absorption
The passage of the drug from it's site of administration in to the
blood except LV. application (because it gives to blood directly so
there is no absorption)

Cell membrane:
It is a barrier that face the entery of drugs from outside to inside
the cell.

Biomolecular lipid layer (so the drugs suppose to be lipid soluble,

unionized and small in size) we can test if the drug can cross cell
membrane or not by buffer with HCl or acetate and shake it this
will give colored drug then we observe if the drug goes to HCl
layer of water layer
If it goes to HCllayer so it can pass lipid layer.
We can use other organic solvent like octanol with buffer which
we called lipid water portion coefficient value which indicate lipid
solubility of drugs

Absorption rate depends on Fick's law'"

M= PA (Co - Ci) T
W
M: amount of uncharged molecule
A: area of cell membrane ( very important, that's why absorption
occurs in intestine more than ~bsorption occurs in stomach)
P: permeability
2. filtration
Depend on size of molecule (small enough to cross the pores)
Driven by gradient pressure

I want to dedicate this sheet to all my colleagues.

Zydon khrissat

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