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misoprostol
parietalna
celica
1
Proglumid
H3C
N O
H3C
HO
NH
O
O
- zaviralec gastrina
- zaviralec holecistokinina
misoprostol
parietalna
celica
2
Pirenzepin
O
H
N
N N
O
N
N
CH3
Selektivni antagonist muskarinskih M1 receptorjev
misoprostol
parietalna
celica
3
Misoprostol
O
O
CH3
O
H3C OH
CH3
HO
misoprostol
za profilakso ulkusa pri terapiji z NSAID
Sukralfat
4
Mehamizem izlo anja klorovodikove kisline
misoprostol
parietalna
celica
H+/K+ - ATPaza
proti
gradientu
A general model of cation motive ATPases illustrating the cytoplasmic, membrane and extramembranal sectors. The dominant
region is the cytoplasmic domain, but transport occurs across the membrane domain as illustrated schematically.
5
H+/K+ - ATPaza
6
Omeprazol kot predzdravilo
7
Razvoj omeprazola in esomeprazola
patentni
problemi!
toksi nost,
vgradnja v obro
metabolit,
ni patentno atrofija ne zavira
zaš iten š itnice absorpcije joda
višji pKa
Esomeprazole magnesium
Launched 2000
8
9
Sinteza
omeprazola
(I)
Sinteza
omeprazola
(II)
Polonovski-jeva
premestitev
10
Sinteza
omeprazola
(V)
Sinteza
omeprazola
(VI)
11
Ti(OPr)4, H2O2, (-)-dietil D-tartrat
Penicillium frequetans
Rhodobacter capsulatus
12
Sinteza lansoprazola
Sinteza pantoprazola
13
Sinteza pantoprazola
14
Sinteza rabeprazola
15