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SEMINAR ON PROTON PUMP
INHIBITORS.
SUBMITTED BY AVS.PRAVEEN KUMAR
07P25R0005.UNDER THEGUIDENCE OF
Mr. K.SURENDRAAssistant professor,M.Pharm,RAO’S COLLEGE OF PHARMACY
PEPTIC ULCER. INTRODUCTION:
DEFINITION: Formation of sores or
erosions in the lining of stomach and duodenum are referred as peptic ulcers.
Ulcers are known to be caused whenever there occurs an imbalance b/n the protective factors.
Use of non steroidal anti-inflammatory drugs (NSAIDS). Pathologic hypersecretory disorders.
Esophageal ulcers.Gastric Ulcers.Duodenal Ulcers.Stress-induced Ulcers.Marginal or anastomotic Ulcers.Drug or NSAID-induced Ulcers.
The common signs & symptoms of peptic ulcer
• Pain after 2-3 hours of food consumption.• Heart burn and indigestion.• Belching (expulsion of gas).• Nausea, vomiting, loss of appetite and weight loss.• Black tarry stools.• Pain in the abdomen with the burning sensation.• Blood vomiting and pain during night time.
DIAGNOSIS
Endoscopy.
X-rays of Upper GI tract.
Gastric secretory studies show hyperchlorhydria.
Hemorrhage or bleeding. Penetration or spreading.Gastric perforation.Gastric outlet obstruction & Shock.
COMPLICATIONS
ANTI ULCER DRUGS DEFINITION
Anti ulcer drugs are medicines used to treat ulcers in
the stomach and the upper part of small intestine.
Anti secretory agents are the drugs that are used to
suppress or reduce the gastric acid secretion.
1.Reduction Of gastric acid:a)H2 Anti Histamines Cimetidine Ranitidine Pantaprazole
b) Proton Pump Inhibitors.Omeprazole Lansoprazole Pantoprazole Rabeprazole
c) Anti cholinergics a)Pirenzapine b)Propanthelinec)Oxyphenonium
d) Prostaglandin Analogues Misoprostil Enprostil
2) Neutralization of gastric acid
a) SystemicSodium bicarbonate (NaHCO3)
b) Non-Systemic Magnesium hydroxideMagnesium trisilicateAluminum hydroxide gelMagaldrate calcium
3) Ulcer protective SucralfateColloidal bismuth sub citrate 4)Ulcer HealingCarbenoxolone sodium
5)Anti-H.pylori drugs
AmoxicillinClarithromycinMetronidazoleTinidazoleTetracycline
PROTON PUMP INHIBITORS DRUG OF CHOICEOMEPRAZOLE
ESOMEPRAZOLE
LANSOPRAZOLE
PANTOPRAZOLE
RABEPRAZOLE
Omeprazole. The proton pump inhibitor
OMEPRAZOLE
OMEPRAZOLE.
Systematic (IUPAC) name
6-methoxy-2-((4-methoxy-3,5-dimethylpyridin-2-yl) methylsulfinyl)-1H-benzo[d]imidazole
Chemical data
Formula C17H19N3O3S
Mol. mass 345.4 g/molPharmacokinetic data
Bioavailability 35–60%Metabolism Hepatic (CYP2C19, CYP3A4)Half life 1 - 1.2 hoursExcretion 80% Renal
20% FaecalTherapeutic considerations
Routes Oral, IV
PHARMACO KINETICSABSORPTION
The absorption of omeprazole takes place in the small intestine and is usually completed within 3–6 hours. The systemic bioavailability of omeprazole after repeated dose is about 60%.Plasma protein binding is about 95%.
DISTRIBUTION
Distribution of the drug is wide and about 95% of the drug is bound to proteins.
METABOLISM
Omeprazole. Sulphenic acid.
Enzyme inhibitor complex. Sulphenamide.
Omeprazole under goes rapid first pass metabolism & systemic hepatic metabolism by cytochrome P450,(CYP2C19 and CYP3A4).
The plasma half life of the drug is 0.5 to 1 hour
EXCRETION:
Urine : 80%
Faeces : 20%
PHYSIOLOGY OF HCL SECRETION
MECHANISM OF ACTION OF OMEPRAZOLE
Omeprazole belongs to the 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 system selectively at the secretory surface of the gastric parietal cells.
Adverse reactions CNS Manifestations CVS Manifestations Endocrinal Manifestations Gastrointestinal Manifestations
Drug interactions Omeprazole decreases plasma concentrations of Atazanavir. Omeprazole increases plasma concentrations of Crabamazepine, Tacrolimus, Diazepam. Omeprazole effects are reduced incase of Amino glutethimide.
CONTRA INDICATIONS
Omeprazole 20 mg, Capsules
Omeprazole 10 mg, Capsules
OMEZ :10, 20, 40,mg capsules. PROTOLOC :20, 40,mg capsules.
MARKETED PRODUCTS
OTHER DRUGSPANTOPRAZOLE
LANSOPRAZOLE
ESOMEPRAZOLE
RABEPRAZOLE
CONCLUSION • Proton pump inhibitors are the first class drugs in the treatment of peptic ulcer and other gastro intestinal disorders.
• Mainly the drug omeprazole have less side effects when compared to other drugs in this class. So this drug is used very commonly in treating gastric disorders.
• PPI use is not driven by secondary care admission.
• Most patients prescribed a therapeutic rather than maintenance dose.
REFFERENCE
Essentials of medical pharmacology, by KD. Thripathi.Pharmacology & pharmaco therapeutics, by R.S. satoshkar.Text book of medical pharmacology, by Padmaja uday kumar.Pharmacology & clinical pharmaco kinetics, by G. Kutzung.Www. Proton pump inhibitor wikipedia, the free encyclopedia.