DRUG DISTRIBUTION
DRUG DISTRIBUTION
4. Miscellaneous
TISSUE PERMEABILITY OF DRUGS
Physicochemical Properties of drug
□ Molecular size,
□ pKa
Polar and hydrophilic drugs are less likely to cross the cell
membrane
Where,,,,,,,,
Nonpolar and hydrophobic drugs are more likely to cross
the cell membrane
EFFECTIVE KO/W = Fraction unionized x KO/W of unionized
at pH 7.4 drug
In case of polar drugs where permeability is the rate- limiting step in
the distribution , the driving force is the effective partition coefficient
of drug ……..that can be calculated by above formula
Lipoidal drug penetrate the tissue rapidly. Among Drugs
with same Ko/w but diff in ionization of blood pH.
Only drugs that bound to that blood components can’t pass through
this barrier Because of larger size of complex
B. PHYSIOLOGICAL BARRIERS
ex.
Phenytoin, methotrexate
later stage pregnancy affect physiological functions like
B. PHYSIOLOGICAL BARRIERS
6) Blood - Testis Barrier :-
It is the tight junction / barrier b/w neighboring sertoli cells that act
as blood-testis barrier .
It is defined as the volume of the blood that flows per unit time per
unit volume of the tissue.
Unit: ml/min/ml
b) Fat content
c) Skeletal muscles
d) Organ composition
e) Plasma protein
content
Pregnancy
Obesity
Diet
Disease states
a) AGE:-
Vd=X/C
Vd=X0 /Co
=i.v.
bolu
s
dose/
conc
Vd(area)=X0/KE(AUC)
entra
tion
of
For drug
drugs administered extravascularly:
in Vd(area) = FXo/KE(AUC)
plas
ma
for drugs
given as