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Gastric Proton Pump
Inhibitor
B. Pharm Third Year
By- S. K. Dhawale
D. K. Patil Institute of Pharmacy, Sayal road loha,
Nanded.
Introduction
• Proton pump is an integral membrane protein in parietal cell of stomach.
• It pumps proton in stomach
• Hydrogen ions are generated within the parietal cells from dissociation of water.
• Hydroxyl ions formed in this process rapidly combines with CO2 to form
bicarbonate ions (HCO3)
• Bicarbonate is transported out of basolateral membrane in exchange of chloride.
• Hydrogen ion is pumped out of cell in lumen in exchange for potassium through
the action of proton pump.
• By using ATP an acidic hydrogen ion replaces a non acidic potassium ion
through the action of proton pump.
Ulcer
• Ulcer is kind of open wound followed by inflammation.
• Occurs both on outer skin of internal epithelium like surface of stomach or
inside mouth.
It occurs due to
• Infection of H. Pylori
• Due to increased concentration of stomach acid.
• Due to pressure on skin.
Clinical Uses of Proton pump Inhibitors
• Dyspepsia( reduction in thrust)
• Peptic ulcer disease
• Gastrointestinal reflux disorder
• Stress induced gastritis
• Zollinger Ellison Syndrome (tumors form in pancreas/ small intrestine)
Antiulcer Drug
• Drugs which are used to treat various kind of gastric ulcer, peptic ulcer or duodenal
ulcer.
• In gastric mucosa, Oxyntic glands are present which stimulate parietal cells to secret
about 2-3 liters of HCl in stomach.
• Gastric parietal cells do not store HCl.
• H+ ions and Cl- Ions are secreted separately into the stomach.
• The working of proton pump is controlled by various regulators.
• Histamine at H1 receptor.
• Gastrin at G receptor.
• Acetylcholine at M2 receptor.
• Prostaglandine.
• Somadostatin.
Antiulcer drugs Classification
1)Reduction of gastric acid secretion
H2 Antihistamine- Cimetidine, Ranitidine, Famotidine, Roxantidine
Proton pump inhibitors – Omeprazole, Pantoprazole, Rabeprazole, Esmoprazole
Anticholinergics – Piperazines, Propanthaline, Oxyphenonium
Prostaglandine Analogues – Misoprostol, Enprostil, Rioprostil.
2) Neuralization of gastric acid
Systemic – Sodium Bicarbonate, Sodium Citrate
Non- Systemic- Magnesium hydroxide, Aluminium Hydroxide, Calcium Carbonate.
3) Ulcer Protective
Sucralfate, Collidal bismuth subcitrate.
4) Ulcer beating drugs
Carbenoxolone sodium.
Some IMP structures of PPI
Lanseprazole
Pantoprazole
Omerazole
• The absorption of omeprazole takes place in the small intestine and completed
within 3-6hrs.
• Distribution of the drug is wide and about 95% of the drug is bound to
proteins
• The plasma half life of drug is 0.5-1hr
Mechanism of action:
Omeprazole belongs to category of anti secretory compound that act
primarily by suppressing the gastric acid secretion. This action is achieved by
inhibiting the H+/K+ ATPase enzyme selectively at the secretory surface of the
gastric parietal cells.
Synthesis of Omeprazole
Omerazole
Adverse Reaction:
• CNS manifestation
• CVS Manifestation
• Endocrinal Manifestation
• Gastrointestinal Manifestation
• Omeprazole have less side effects than other drugs in this class, so used
commonly in treating gastric disorders.

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Gastric Proton Pump Inhibitor

  • 1. Gastric Proton Pump Inhibitor B. Pharm Third Year By- S. K. Dhawale D. K. Patil Institute of Pharmacy, Sayal road loha, Nanded.
  • 2. Introduction • Proton pump is an integral membrane protein in parietal cell of stomach. • It pumps proton in stomach • Hydrogen ions are generated within the parietal cells from dissociation of water. • Hydroxyl ions formed in this process rapidly combines with CO2 to form bicarbonate ions (HCO3) • Bicarbonate is transported out of basolateral membrane in exchange of chloride. • Hydrogen ion is pumped out of cell in lumen in exchange for potassium through the action of proton pump. • By using ATP an acidic hydrogen ion replaces a non acidic potassium ion through the action of proton pump.
  • 3. Ulcer • Ulcer is kind of open wound followed by inflammation. • Occurs both on outer skin of internal epithelium like surface of stomach or inside mouth. It occurs due to • Infection of H. Pylori • Due to increased concentration of stomach acid. • Due to pressure on skin. Clinical Uses of Proton pump Inhibitors • Dyspepsia( reduction in thrust) • Peptic ulcer disease • Gastrointestinal reflux disorder • Stress induced gastritis • Zollinger Ellison Syndrome (tumors form in pancreas/ small intrestine)
  • 4. Antiulcer Drug • Drugs which are used to treat various kind of gastric ulcer, peptic ulcer or duodenal ulcer. • In gastric mucosa, Oxyntic glands are present which stimulate parietal cells to secret about 2-3 liters of HCl in stomach. • Gastric parietal cells do not store HCl. • H+ ions and Cl- Ions are secreted separately into the stomach. • The working of proton pump is controlled by various regulators. • Histamine at H1 receptor. • Gastrin at G receptor. • Acetylcholine at M2 receptor. • Prostaglandine. • Somadostatin.
  • 5. Antiulcer drugs Classification 1)Reduction of gastric acid secretion H2 Antihistamine- Cimetidine, Ranitidine, Famotidine, Roxantidine Proton pump inhibitors – Omeprazole, Pantoprazole, Rabeprazole, Esmoprazole Anticholinergics – Piperazines, Propanthaline, Oxyphenonium Prostaglandine Analogues – Misoprostol, Enprostil, Rioprostil. 2) Neuralization of gastric acid Systemic – Sodium Bicarbonate, Sodium Citrate Non- Systemic- Magnesium hydroxide, Aluminium Hydroxide, Calcium Carbonate. 3) Ulcer Protective Sucralfate, Collidal bismuth subcitrate. 4) Ulcer beating drugs Carbenoxolone sodium.
  • 6. Some IMP structures of PPI Lanseprazole Pantoprazole
  • 7. Omerazole • The absorption of omeprazole takes place in the small intestine and completed within 3-6hrs. • Distribution of the drug is wide and about 95% of the drug is bound to proteins • The plasma half life of drug is 0.5-1hr Mechanism of action: Omeprazole belongs to category of anti secretory compound that act primarily by suppressing the gastric acid secretion. This action is achieved by inhibiting the H+/K+ ATPase enzyme selectively at the secretory surface of the gastric parietal cells.
  • 9. Omerazole Adverse Reaction: • CNS manifestation • CVS Manifestation • Endocrinal Manifestation • Gastrointestinal Manifestation • Omeprazole have less side effects than other drugs in this class, so used commonly in treating gastric disorders.