MedChem - Antiulcer drugs

Gastric acid secretion

H+/K+ ATPase mechanism

Proton pump

Omeoprazole (definition & mechanism)

First PPI discovered. Short half life but irreversible binding (S-S bond formation with proton pump, can be cleaved by glutathione reducatse).

Hepatic metabolism: demethylation & oxydation to sulfone

Omeoprazole (mechanism)

Prazanes (definition, mechanism and 1 example)

potassium-competitive acid blockers (aka acid pump antagonists). They reversible and competitively inhibit the acid secretion by binding to the K+ binding site.

Linaprazan

Helicobacter pylori (definition)

Gram negative flagellate acidophilic bacterium. It is able to survive in gastric mucus due to presence of urease and CA, acting as buffer.

It generates toxic metabolites, leading to gastritis, ulcer and gastric cancer?

Most people are infected but have a good immune systeme/bacteria equilibrium.

Helicobacter pylori (membrane structure)

Helicobacter pylori (therapy)

Triple therapy: 2 antibiotics (e.g. amoxicillin, clarithromycin + 1 antiacid (omeoprazole)