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.