Summary
Summary ADMET
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Summary of all the lectures from the masters course Drug Discovery and Safety at the VU. Summary is handwritten on an Ipad and in English. Grade: 8.6
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Sum ADMETMary
Lecture 1 :
Absorption
-
Routes of administration
-
topica 1 :
10cal exposure
circulatory System
:c
System
-
:
-
enter A1 : GIT
GIT
paren ter A1 :
avoiding
-
-
Absorption depends OM
-
physicochemical properties drug
-
Physiological Properties site of absorption
-
Administration environment
-
GIT : stomach
-
Limited absorption
Hydro lytic enzymes
-
-
mucusproducedsurfaceiiningep.itheli al cells
•
GIT : smalt in testine
-
duodenum jejunum and ileum .
-
absorptie in
-
first site metabolisch
bite acids
soiubiiity enhanced
by
-
-
Main cells involved in absorption : en
terocytes
Mechanism s of
drug absorption
-
trans or paraCellular passive diffusion
-
-
-
Active transport
endocytoseis
-
-
passie diffusion
and
-
baiano between
soiubiiity permeability
Fick S first 19W
'
-
DQ
It = D ✗
P ✗ S ✗
Linear process
-
-
Non - saturatie
,•
Facilitated diffusion
-
Michaelis Menten
DA
☒
= -
VIII
-
saturated process
- de
pendant on number of channels or carriers
para Cellular transport
-
tight junction 5
-
-
occludins and Claudia
Claudine
Leak Vs
tight
-
.
↳
depends on tissue
-
smal/
hydrophilic molecules
-
Active transport
primary
:
ATP required to transport against conc gradient
-
.
Secondary :
Movement of ions clown gradient couped with
-
molecules againstgradient
substratespecii ty-efr.lu/:widesubstratespecifity
-
uptake : narrow
Nat / kt ATPase at basoiateralside as
driving Force
-
Nat wat
-1
gklc .
je
µV
nemen
-
""°" """
-0¥ 2kt
basoeterai
Kt (l
-
3 nat
.
ABC ( ATP
binding cassette)
-
transporter
physiological role
-
-
cholesterol and lipid transport
antigen presentation
-
-
mitochondria1 iron homeostaseis
ij
, primary active transport
-
-
Ex porters
In
enterocy.es
-
api (al side :
transport EO lumen
-
-
baso lateral side : transport to bood
-
ABC transporters
associated proteinS CMRPS)
muitidrug resistance
-
-
-
anionic drugs
glutathione. giucuronate.sulfateconjugal.es
-
breast Cancer resistance protein ( BCRP)
-
hydrophobiccationslanions-sulfatedconjugates-p-giy.co
large
-
Pgp)
protein (MDRI /
-
hydrophobic cationic drugs
-
often have aromatic rings and Ntr 4
-
MW >
400 . pka
>
4 .
N t 0 38
SLC ( 5014te Carrier ) transporter
•
Secondary active
-
Physiological role s
-
glucose transport
-
-
ami no acid transport
-
SK example
-
0 AT I
-
Organic anion transporter
-
basoiateral uptake of an NS into tubular ep cells
.
-
in teracts with a lot of drugs
-
OAT 3
-
suipate - and giucuronides-eroidconjugal.es
-
OCTI / 2
-
Organic Cation transporter
-
uni porters
OCT 1 Ii ver OCT 2 :
Kidney
-
:
,
-
OCTN 1 / 2
Cati on and Carriere transporter
Organic
-
-
MATE 1 12
, and
Multi
drug to✗in extrusion transporter
-
-
proton -
Cati on anti Porter
-
OATPS
-
Organic anion transportîng polypeptide
and
uptake of bulky hydro phobic ani ons
-
↳
bilesalts.steroidconjugat.es ,
hormones
Efflux transporters rate of uptake
mag regulatie so
C p 450s
'
are not saturated
-
B( S absorption
-
I :
high 501 .
t
high perm .
I : 10W 501 t
high perm
-
. .
-
☒ :
high 501 . + 10W Perm .
-
IV : 10W SOI .
t 10W Perm .
PAMPA ( parallel artificial membrane per
meabiiity assa )
-
sive diffusion over Micro porosus filter
pas
-
-
high throughput and cheap
-
(en based assays
-
( acoz (human colon adenocarcinooma)
-
MDCK cells ( Carine distal tubular)
-
polarized Mondayer of cells
presence of drug transporters
-
A →
BL BL - A :
passive diffusion
-
=
-
Active transport cel based
MDCK HEK 293 LLC PKI
-
-
. .
-
Cen limes transfected with transporter
-
use of inhibitor for certain transporters
Uptake as
says
-
-
Concentration increasesinsideceus
-
cells then Iysed -
Measure compound
when cells do not form continent
Necessary Mondayer
-
ij ij
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