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AGIO PHARMACEUTICALS LTD,
A-38, Nandjyot Industria/ Estate, Kurla-Andheri Road, Safedpool, Mumbai-400 072, India
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Capsules (NRN: -): Each hard gelatin Capsule contains Omeprazole B.P. 20 mg (Asenteric coated pellets) Approved colours used in capsule shell
Pack Size: 2 strips containing 10 capsules each are packed in a primary carton along with the Pack Insert
Omeprazole is a specific inhibitor of the gastric proton pump in the parietal cell and thus reduces the secretion of gastric acid. Reversible control of gastric acid secretion is produced with single daily doses of omeprazole. Omeprazole is a weak base, which is concentrated in the intracellular canaliculi of the parietal cell.
Due to the acidic environment in these cells, omeprazole is converted to the active form, where it acts as an inhibitor of the enzyme H+, K+ -ATPase - the proton pump. There is a dose dependency on this final step in the formation of gastric acid, which provides for effective inhibition of the secretion of both basal acid and stimulated acid irrespective of the secretatory enhancer.
When omeprazole is given daily as a single oral dose, the gastric acid secretion is inhibited with a maximum effect reached within four days of treatment. In patients with duodenal ulcers, a mean decrease of approximately 80% in intragastric acidity is then maintained over a 24-hour period, with the mean decrease in peak acid output after pentagastrin stimulation being approximately 70%, twenty-four hours after initiating treatment with omeprazole.
Due to the acid lability of omeprazole, the oral formulation consists of enteric-coated granules in capsules. Omeprazole is usually completely absorbed from the small intestine within three to six hours. After a single oral dose, the systemic bioavailability of omeprazole is approximately 35% which can be increased to about 60%, after repeated once-daily administration.
The simultaneous intake of food has no influence on the bioavailability. Omeprazole is approximately 95% bound to plasma proteins. The average terminal phase half-life of the plasma concentration-time curve is approximately forty minutes There is no change in half-life during treatment. The inhibition of acid secretion is related to the area under the plasma concentration-time curve (AUC) and not to the actual plasma concentration at a given lime.
Omeprazole is completely metabolised mainly in the liver. The sulphone, the sulphide and hydroxy omeprazole are the metabolites detected in plasma. These metabolites are inactive and have no significant effect on acid secretion. Approximately 80% of the metabolites are excreted in the urine and the balance in the faeces.
The two main metabolites in the urine are hydroxy-omeprazole and the corresponding carboxylic acid. There is no significant change in the systemic bioavailability of omeprazole in patients with impaired renal function. Although the area under the plasma concentration-time curve is increased in patients with reduced liver function, no apparent accumulation of omeprazole has been found.
Omeprazole is indicated in the treatment of:
• Duodenal Ulcer.
• Gastric Ulcer
• Zollinger-Ellison syndrome.
• Reflux oesophagitis
If duodenal ulcers are associated with Helicobacter pylori, the concomitant use of omeprazole and suitable antibiotics may be beneficial.
Hypersensitivity to any of the ingredients in this product.
Decreased gastric acidity due to any means, including proton-pump inhibitors, increases gastric counts of bacteria normally present in the gastrointestinal tract. Treatment with acid-reducing drugs may lead to a slightly increased risk of gastrointestinal infections, such as Salmonella and Campylobacter.
For severely ill children, who require long-term treatment with Omeprazole, and may have borderline levels or body stores of B12, it may be advisable to monitor serum B12 levels during long-term treatment.
Omeprazole can prolong the elimination of medicines which are metabolised by oxidation in the liver, e.g. warfarin, diazepam and phenytoin Patients receiving warfarin or phenytoin concomitant with omeprazole, should be monitored closely as a reduction in dosages of warfarin or phenytoin may be required.
It was however shown in patients on concurrent omeprazole treatment at a daily dosage of 20 mg and continuous phenytoin treatment, that the simultaneous use of these two medications did not influence the blood concentration of phenytoin. Concomitant treatment with omeprazole 20 mg daily also did not alter coagulation time in patients on long-term treatment.
There is a possibility of interactions with medicines metabolised via the cytochrome P450 enzyme system, although no interactions with propranolol, metoprolol, theophylline, lignocaine, quinidine and amoxicillin have been recorded. No interaction with food or the concurrent administration of antacid medications has been found.
The plasma concentrations of both omeprazole and clarithromycin may be increased during concomitant treatment with these medicines An increase of approximately 10% in the bioavailability of digoxin were recorded in healthy volunteers due to the increase in intragastric pH when omeprazole and digoxin are administered concurrently.
PREGNANCY and LACTATION:
Safety in pregnancy and lactation has not been established
The most commonly reported side effects are Nausea, vomiting. headache, diarrhoea, constipation, abdominal pain and flatulence, rash and/or pruritus, dizziness, paraesthesia, somnolence, insomnia, vertigo, increased liver enzymes and malaise.
Dosage & Administration
A daily 20 mg dose is recommended for treatment of duodenal and gastric ulcer and reflux oesophagitis 40 mg/day may be required in patients with conditions poorly responsive to histamine H2 receptor antagonist therapy.
Recurrence of reflux oesophagitis has been successfully prevented with daily 20 or 40 mg dose while a 10 mg daily dose appears promising in patients with duodenal ulcer.
In patients with Zollinger-Ellison syndrome, omeprazole 60 mg/day is recommended initially with individual adjustment to maintain target gastric acid output. Dosage adjustment is not necessary in elderly patients or in patients with renal or hepatic impairment.
Store below 25°C, protect from light & moisture