The Drugs are the important to the daily usage To the any type of the problem in the stomach

1. Gastric proton pump inhibitor
Presented By-
Antriksh M.Rathod
Final year B-Pharm

2. Content
Introduction
Mechanism of action
Classification of PPIs
Drugs of PPIs
 Omeprazole
 Lansoprazole
 Rabeprazole
 Pantoprazole

3.  Introduction
 They are the class of drugs which are used to control the
gastric acidity and duodenal ulcer
 These agents are of benzimidazole class which selectively
inhibit the functioning of proton pump by getting
accumulated in the parietal cell- membrane
 All the PPI contain a sulphonyl group in a bridge between
substituted benzimidazole pyridine rings.

4.  Mechanism of Action
• The H+ -K+ -ATPase proton pump of the apical membrane of parietal cell
is the mediator acid secretion .The newer substituted benzimidazole are
used in peptic ulcer.
• The PPIs have a sulphinyl group in
a bridge between substituted
benzimidazole and pyridine rings.
• These agents are chemically stable and
lipid –soluble weak bases without
inhibitory activity at neutral pH.
• Here the drugs become protonated & trapped.The protonated agent re-
arranges for producing sulphuric & sulphonamide , which covalently
interacts with sulphhydral groups of cysteine at critical sites in the extra
cellular domain of the H+ -K+ -ATPase.Thus it irreversibly inhibits gastric
acid secretion

5.  Classification
Proton pump inhibitor are classified as follows:-
Drugs X R1 R2 R3 R4
Omeprazole CH OCH3 CH3 CH3 CH3
Esomeprazole CH OCH3 CH3 CH3 CH3
Tenatoprazole N OCH3 CH3 CH3 CH3
Lansoprazole CH H CH3 CH2CF3 H
Rabeprazole CH H CH3 (CH2)3OCH3 H
Pantoprazole CH OCHF2 OCH3 CH3 H

6. Drugs of Proton pump inhibitor
Omeprazole
Omeprazole inhibits the proton pump and decreases the
amount of acid produced in the stomach.
• Mechanism of Action
Omeprazole suppresses gastric acid secretion by inhibiting H+ -K+ -
ATPase the gastric parietal cell .Thus by acting specifically on the proton
pump it block the final step in acid production, and reduces gastric acidity.
Uses
o In duodenal ulcer
o In gastric ulcer
o In pathological hypersecretory conditions
N
H
N
S N
O
O
O

7. Lansoprazole
Lansoprazole is a substituted benzimidazole prodrug having the selective
and irreversible proton pump inhibitor activity. It prevents the
production of acid in the stomach.
• Mechanism of action
It suppresses gastric acid secretion by inhibiting the H+ -K+ -ATPase
enzyme system at the secretory surface of gastric parietal cell.
It has higher oral bioavailability, faster onset of action and slightly longer
t1/2 (Half life) than omeprazole. Dose should be reduced in liver disease.
Uses
o In acid –reflux disorders & peptic ulcer
disease.
o It is used for H. pylori eradication
o It is used in combination with NSAIDs for preventing
gastrointestinal bleeding
N
H
N
S
O
N
O

8. Rabeprazole
Rabeprazole is an antiulcer drug that blocks the H+ -K+ -ATPase of
the coating gastric cells . It also inhibits the dose –dependent oppresses
basal and stimulated gastric acid secretion.
• Mechanism of Action
Rabeprazole is an anti-secretory compound. It is a substituted benzimidazole
proton-pump inhibitor that suppresses gastric acid secretion by inhibiting the
H+ -K+ -ATPase enzyme system at the secretory surface of gastric parietal
cell . Since this enzyme system is the acid (proton) pump in the parietal cell ,
rabeprazole is considered the gastric acid –pump inhibitor which inhibits the
final step of acid production
Uses
o In GERD , In severe erosive esophagitis
o In Zollinger-Ellison syndrome , Systemic mastocytosis & multiple
endocrine adenomas , In duodenal ulcer , In daytime or night time heartburn.
N
H
N
S N
O
O
O

9. Pantoprazole
Pantoprazole is a first generation PPI.
It is also used for treating other disorders where in gastric acid secretion
needs to be reduced.
pantoprazole is available in many forms, such as a delayed – release oral
capsule, and intravenous injection
• Mechanism of action
Pantoprazole suppresses the final step in gastric acid production by
formation a covalent bond to two sites of the (H+,K+) -ATPase
enzyme system at the secretory surface of the gastric parietal cell.
This effect is dose-related and leads to inhibition of both basal and
stimulated gastric acid secretion irrespective of the stimulus

10. Uses
o Pantoprazole injection is given to patients having GERD and history of
erosive esophagitis for short-treatment (7-10 days). It is given as an
alternate to pantoprazole delayed-release tablet in patients who are not
able to swallow the tablets.
o It is used in the treatment of pathological hypersecretory condition
related to Zollinger-Ellison syndrome or other neoplastic condition.
o Pantoprazole delayed-release oral suspension is used for short-term
treatment of erosive esophagitis related to GERD.
o It is also used to promote the healing of erosive esophagitis and
decrease the relapse rates of daytime and night time heartburn
symptoms in adult patients of GERD.
N
H
N
S N
O O
O
F
F
O