Lecture 3- ADME Flashcards
permeation
movement of drug through barriers
aqueous/passive
no energy required: high to low conc
ficks law
“helps determine how well drugs can cross membranes” involves aqueous diffusion and passive diffusion of molecules down a conc. gradient
faster diffusion/absorption occurs when (ficks)
larger conc. gradients,
large area,
thin membrane
c1 (ficks law)
higher conc.
c2 (ficks law)
lower conc.
area (ficks law)
that diffusion is occurring
permeability coefficient (ficks)
measure of the mobility of drug mol. in the medium of diffusion path
thickness (ficks)
length of the diffusion path
the bigger the area, the thinner the membrane the ____ diffusion
faster diffusion
charged drugs are lipid ___ and water ____
insoluble, soluble
uncharged drugs are lipid ___ and water ___
soluble, insoluble
pKa
acid dissociation constant
HA
protonated acid, uncharged
A
unprotonated acid, charged
BH+
protonated base, charged
B
unprotonated base, uncharged
if pH equals pKa
50% protonated 50% unrpotonated
in order to cross membrane weak acids need to be _____ and weak bases need to be____; thus both are ____
protonated (acids)
unprotonated (bases)
both are uncharged
endocytosis
cell engulf
-occurs when substance is too large or insoluble or impemeant to cell by pinching it off
exocytosis
cell directs the contents of secretory vesicles out of the cell membrane, releasing a substance from the cell
volume distribution
how far the drug distributes out into body tissue; either bloodstream (SMALL) or out into tissues (HIGH vd)
Vd (L) equation
(D)amt of drug in body/conc. in plasma (C0)
a high VD indicates
out into tissues = lipophilic (fat lovin)
how can vd be decreased
plasma protein binding, dehydration
how can vd be increased
renal failure or liver failure