Trumeprazole

Omeprazole.

Each capsule contains: Omeprazole USP 20 mg.

Pharmacology: Pharmacodynamics: Mechanism of Action: Omeprazole suppress gastric acid secretion by specific inhibition of the H⁺/K⁺ ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton)pump within the gastric mucosa, Omeprazole is characterized as the gastric pump inhibitor as it blocks the final step of acid production.
Site and Mechanism of Action: Omeprazole is a weak base and is concentrated and converted to the active form in the acid environment of the intracellular canaliculi within the parietal cell, where it inhibits the enzyme H⁺, K⁺-ATPase- the acid pump. This effect on the final step of the gastric acid formation process is dose-dependent and provides for effective inhibition of both basal acid secretion and stimulated acid secretion irrespective of the secretagogue.
Omeprazole has no effect on acetylcholine or histamine receptors and no clinically significant pharmacodynamic effects have been observed other than those explained by the effect of omeprazole on acid secretion. Effect of Helicobacter pylori: Helicobacter pylori is associated with acid peptic disease including duodenal and gastric ulcer in which about 95% and 70% of patients, respectively, are infected with this bacterium. H. pylori is the major factor in development of gastritis and ulcers in such patients.
Recent evidence also suggest a causative link between H. pylori and gastric carcinoma.
Other Effects Related to Acid Inhibition: During long-term treatment, gastric glandular cysts have been reported in a somewhat increased frequency. These changes are physiological consequence of pronounced inhibition of acid secretion, are benign and appear to be reversible.
Pharmacokinetics: Absorption and Distribution: Omeprazole is acid-labile and is administered as enteric granules in capsules. Absorption takes place in the small intestine and usually completed within 3-6 hours. The systemic bioavailability of omeprazole from a single-oral dose is approximately 35%. After repeated once-daily administration, the bioavailability increases to about 60%. Concomitant intake of food has no influence in the bioavailability. The plasma protein-binding of omeprazole is about 95%.
Elimination and Metabolism: The average half-life of the terminal phase of the plasma concentration-time curve is approximately 40 mins. 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) but not to the actual plasma concentration at a given time.
Omeprazole is entirely metabolized, mainly in the liver. Identified metabolites in the plasma are the sulfone, the sulfide and hydroxyomeprazole, these metabolites having no significant effect on acid secretion. About 80% of the metabolites are excreted in the urine and the rest in the feces. The 2 main urinary metabolites are hydroxyomeprazole and corresponding carboxylic acid.
The systemic bioavailability of omeprazole is not significantly altered in patients with reduced renal function. The area under the plasma concentration-time curve is increased in patients with impaired liver function, but no tendency to accumulation of omeprazole has been found.

Duodenal and Gastric ulcer.
Treatment of Gastroesophageal Reflux Disease (GERD).
Treatment of Heartburn and other symptoms associated with GERD.
Erosive Esophagitis.
Treatment hypersecretory conditions (Zollinger-Ellison syndrome, multiple endocrine adenomas and systemic mastocytosis).

Route of Administration: Usually administered orally. The usual dose for healing reflux oesophagitis is 20 to 40 mg once daily for 4 to 8 weeks; thereafter maintenance therapy can be continued with 20 mg once daily.
In the management therapy can be continued with 20 mg once daily.
In the management of peptic ulcers a single daily dose of 20 mg, or 40 mg in severe cases, is recommended usually for 4 weeks in patients with duodenal ulcer and for 8 weeks in those with gastric ulcers. Treatment for longer periods is not yet recommended; therefore omeprazole is not used for long-term maintenance.
The initial recommended dosage for patients with the Zollinger-Ellison syndrome is 60 mg once daily, but doses in the range 20 to 120 mg daily may be used; doses above 80 mg should be divided and given twice daily.
In such patients treatment with omeprazole is continued as required to keep the condition under control.

Delayed release capsules are contraindicated in patients with known hypersensitivity to any components of the formulation.

Serious allergic reactions including angioedema, anaphylaxis and dermatologic reactions including Stevens Johnson's syndrome and toxic epidermal necrolysis have been reported rarely in patients on Azithromycin therapy.

Before giving omeprazole to patients with gastric ulcers the possibility of malignancy should be excluded since omeprazole may mask symptoms and delay diagnosis.
Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long term with omeprazole.
Should be taken before eating. Patients should be cautioned that the capsule should not be opened, chewed or crushed and should be swallowed as a whole.

The adverse effects reported most frequently with omeprazole have been diarrhoea, skin rashes, headache; they have sometimes been severe enough to require discontinuation of treatment.
Body as a whole: fever, pain, fatigue, malaise, abdominal swelling.
Cardiovascular: Chest pain or angina, tachycardia, bradycardia, palpitation, elevated blood pressure, peripheral edema.
Gastrointestinal: Pancreatitis, anorexia, irritable colon, flatulence, fecal discoloration, esophageal candidiasis, mucosal atrophy of the tongue, dry mouth.
Hepatic: Mild and rarely marked elevations of liver function test ALT (SGPT), AST (SGOT), alkaline phosphatase and bilirubin (jaundice).
Metabolic/Nutritional: Hyponatremia, hypoglycemia, weight gain.
Musculoskeletal: Muscle cramps, myalgia, muscle weakness, joint pain, parenthesis, leg pain.
Nervous System/Psychiatric: Psychic disturbances, including depression, aggression, hallucinations, confusion, insomnia, nervousness, tremors, apathy, somnolence, anxiety.
Respiratory: Epistaxis, pharyngeal pain.
Skin: Rash.

Omeprazole inhibits the metabolism of drugs metabolised and may increased plasma concentrations of diazepam, phenytoin, and warfarin. Because of its long lasting inhibition of gastric acid secretion, Omeprazole may interfere with the absorption of drugs where gastric pH is important (e.g. Ketoconazole, Ampicillin esters, Iron salts).

Store at a temperature not exceeding 30°C. Protect from light.

Antacids, Antireflux Agents & Antiulcerants

A02BC01 - omeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).

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