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If pK
a
of the drug equals pH of the environment, then 50%
of the drug will be ionized.
Ka
H B
BH
AH
H A
Ka
B) Filtration
Molecules do not penetrate across
membrane but through pores or paracellular
channels (different from diffusion).
Depends on gradient and size of the
molecule.
MW < 100 (urea, lithium, methanol).
B) Bulk flow
Fast movement through inter-cellular pores.
Transport across endothelia extravasation (except brain).
Driven by hydrostatic and oncotic pressure.
e.g. glomerular filtration through fenestrations in
capillaries of the glomerulus.
C) Facilitated transports
Mediated by a carrier.
These carriers are:
specific
saturable (T
max
)
inhibitable (competition)
Includes: active transport and facilitated
diffusion.
C) Active transport
Mediated by a carrier.
Energy-dependent (in the form of ATP).
Can run against the concentration gradient.
Is saturable (Tmax) and inhibitable (competition).
Runs in one direction only.
Substrates: mostly endogenous molecules or compounds
with structural similarity (levodopa, a-methyldopa).
Example: active tubular secretion and reabsorption
C) Facilitated diffusion
Mediated by a carrier.
Is not energy-dependent (in contrast to active transport).
Driven by concentration gradient.
Is saturable (Tmax) and inhibitable (competition).
D) Transport of ion pairs
E.g.: absorption of quarternary ammonium compounds
from GIT.
Formation of neutral complex (with endogenous mucin)
> passive diffusion > dissociation.
E) Endocytosis
Cellular uptake of
molecules.
Useful in controlled
delivery/gene therapy.
Physiologically:
transport of IgG from
mother to fetus.
E) Endocytosis
transport of IgG from
mother to fetus
F) Efflux ABC transporters
Efflux transporter
pumping lipophilic drugs
out of cell.
Important role in:
chemotherapy (resistance)
pharmacokinetics (affects
absorption, distribution,
elimination).
E.g. P-glycoprotein, BCRP, MRP
Extracellular space
Intracellular space