Ulcer 1
Ulcer 1
Ulcer 1
Michael Alwan
November 11, 2004
An Ulcer is …
Localized erosion in stomach or duodenum
Symptoms and Causes
Histamine 2 Receptors
Tagamet, Zantac, Pepcid, Axid
Proton Pump Inhibitors
Protonix, Prilosec, Prevacid, Aciphex, Nexium
Antibiotics
Clarithromycin, Amoxycillan, Tetracyclin
H2 Receptor
4-methylhistamine 4-methylhistamine
Conformation I Conformation II
Nα -Guanylhistamine
First partial agonist
First signs of antagonistic activity
Still allows partial conformational change
N α
-Guanylhistamine
Guanidine present in A.A. residue arginine
Carbon chain lengthened
Burimamide
Imidazole Ring Development
Metiamide
Cimetidine (Tagmet®)
Metiamide is toxic
Nitroguanidine and Cyanoguanidine showed
similar antagonistic activity
NO2>CN>OMe>CONH2>Ac>Ph>H
Cimetidine
(anTAGonist ciMETidine)
Rantidine (Zantaz®)
Rantidine
Famotidine (Pepcid®)
Famotidine
Nizatidine (Axid®)
Nizatidine
Proton Pump
H+/K+ ATPase
F-ATPase: in mitocondria and chloroplasts; make
ATP with proton gradient
V-ATPase: (vacuolar) hydrolyze ATP to generate
electrochemical gradient “Proton-Pump”
ATPase Animations
Proton Pump Inhibitors
Rabeprazole
Esomeprazole Mg
Lansoprazole
Pantoprazole Omeprazole
PPI Kinetic Data
Omeprazole UV spectra
Helicobacter pylori
Naturally found in stomach of many people
Can cause inflammation; leading to membrane erosion
Treatment
H2 anatagonist / PPI
Antibiotic against Helicobacter Pylori
Future
Increase activity, long-lasting effects
Questions?