2.PROTON PUMP INHIBITOR. UNIT 01 # PMC-1# SEM 5TH

PROTON PUMP INHIBITOR# STRUCTURES WITH IUPAC NAMES# USES

1. PROTON PUMP INHIBITOR Mrs. Sandhya Sujeetkumar Ahire Pharmaceutical Chemistry

2. DEFINATION Drugs which are used to reduce or inhibited gastric acid production and secretion are known as PPI. More potent and longer duration of action as H 2 antagonist. Act irreversibly blocking H + / K + ATPase enzyme of gastric parietal cells.

3. All the proton pump inhibitor contain sulphinyl gr in bridge between substituted Benz imidazole and pyridine ring. Under influence of proton it get charged into sulphuric acid and sulphonamide that react covalently with SH gr of cysteine of the H + / K + ATPase enzyme inactive it irreversibly and thereby blocks gastric acid secretion especially when 2 mole of omeprazole react with 1 mol of enzymes. MECHANISM

4. PROTON PUMP INHIBITION BY OMEPRAZOLE

5. MEDICAL USES : Peptic ulcers Stress gastritis ulcers Dyspepsia Stress gastritis Barrett's oesophagus Gastroesophangeal reflux disease

6. GENERAL STRUCTURE :

7. 1.Omeprazole : protype member of substituted Benz imidazole which inhibit the final common step in gastric acid secretion. Clinical uses: Treatment of peptic ulcer, stress ulcer, bleeding peptic ulcer, gastroesophageal reflux disease, aspiration pneumonia. Dose : 20mg once daily(peptic ulcer)

8. 2. R abeprazole: Newer PPI Due to high pKa it is more rapidly converted to the active species. Fastest acid suppression cause. Clinical use : Gastric hyper secretory disorders. Dose : 20mg once daily.

9. 3.LANSOPRAZOLE: proton pump inhibitor Racemic 1:1 mix of enantiomers dexlansoprazole and levolansoprazole. Clinical use : Used to treatment and prevention of stomach , duodenum, NSAID induced gastric ulcers, gastroesophageal reflux disease. Dose : 15-30mg once daily.

10. 4. PANTOPRAZOLE: Newer H + / K + ATPase inhibitor similar in potency and clinical efficacy to omeprazole . More acid stable and has higher oral bioavailability. Clinical uses: Zollinger-ellison syndrome Bleeding peptic ulcer Prophylaxis of acute stress ulcers.

11. Draw structure of cimetidine and ranitidine What is PPI ? Draw structure of any 2. Mechanism of action for PPI. Questioned ask in examination

12. Thank you