Omed/Omed 20

Omed/Omed 20

omeprazole

Manufacturer:

Medhaus

Distributor:

Medhaus
Full Prescribing Info
Contents
Omeprazole.
Description
Omed: Each combi pack contains: 1 Vial of Sterile lyophilized Omed contains: Omeprazole USP 40 mg, Excipients q.s.
1 Ampoule of Sterile Water for Injection containing: Water for Injection USP 10 mL.
Omed 20: Each capsule contains: Omeprazole 20 mg.
Action
Pharmacology: Omed: Pharmacological Actions: Omeprazole belongs to a class of antisecretory compounds, known as 'proton pump inhibitors' which are substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+ K+ ATPase enzyme system, the acid (proton) pump of the gastric parietal cell.
After intravenous administration of omeprazole, the onset of the antisecretory effect occurs within one hour, with the maximum effect occurring within two hours. A single dose of 40 mg of Omeprazole given intravenously has similar effect on intragastric acidity over a 24-hour period as repeated oral dosing with 20 mg once daily. Although the plasma half-life of omeprazole is very short (50 minutes), the antisecretory effect lasts longer due to prolonged binding to the parietal H+ K+ ATPase enzyme. When the drug is discontinued, secretory activity returns gradually, over 3 to 5 days. The inhibitory effect of omeprazole on acid secretion is dose-related and increases with repeated once daily dosing, reaching a plateau after four days.
Mechanism of Action: Omeprazole is activated at an acidic pH to a sulphenamide derivative that binds irreversibly to H+ K+ ATPase enzyme, an enzyme system found at the secretory surface of the parietal cells, it thereby inhibits the final transport of hydrogen ions (via exchange with potassium ions) into the gastric lumen thus inhibiting acid secretion. Omeprazole inhibits both basal and stimulated acid secretion irrespective of the stimulus.
Pharmacokinetic Profile:The apparent volume of distribution of omeprazole in healthy subjects and in patients with renal insufficiency is almost similar. The volume of distribution is slightly decreased in the elderly and in patients with hepatic insufficiency. The plasma protein binding of omeprazole is about 95%. The average half-life of the terminal phase of the plasma concentration time curve following intravenous administration of omeprazole is approximately 40 minutes. Omeprazole is completely metabolized by the cytochrome P450 system, mainly in the liver. No metabolite has been found to have any effect on gastric acid secretion. Almost 80% of an intravenous dose of Omeprazole is excreted as metabolites in the urine, and the remainder is found in the faeces, primarily originating from biliary secretion.
Omed 20: Pharmacokinetics: Absorption is rapid, with peak plasma levels of Omeprazole occurring within 0.5 to 3.5 hours. Peak plasma concentrations and AUC are approximately proportional to doses up to 40 mg, but because of a saturable first-pass effect, a greater than linear response in peak plasma concentration and AUC occurs with doses greater than 40 mg. Absolute bioavailability (compared to intravenous administration) is about 30-40% at doses of 20-40 mg, due in large part to presystemic metabolism. In healthy subjects, the plasma half-life is 0.5 to 1 hour, and the total body clearance is 500-600 mL/min. Protein binding is approximately 95%. The bioavailability of Omeprazole increases slightly upon repeated administration of Omeprazole. Following single dose oral administration of a buffered solution of Omeprazole, little if any unchanged drug was excreted in urine. The majority of the dose (about 77%) was eliminated in urine as at least six metabolites. Two were identified as hydroxyOmeprazole and the corresponding carboxylic acid. The remainder of the dose was recovered in feces. This implies a significant biliary excretion of the metabolites of Omeprazole. These metabolites have very little or no antisecretory activity. In patients with chronic hepatic disease, the bioavailability increased to approximately 100% compared to an I.V. dose, reflecting decreased first-pass effect, and the plasma half-life of the drug increased to nearly 3 hours compared to the half-life in normals of 0.5-1 hour. Plasma clearance average 70 mL/min, compared to a value of 500-600 mL/min in normal subjects. In parents with chronic renal impairment, whose creatinine clearance ranged between 10 and 62 mL/min/1.73 m2 the disposition of Omeprazole was very similar to that in healthy volunteers, although there was a slight increase in bioavailability. Because urinary excretion is a primary route of excretion of Omeprazole metabolites, their elimination slowed in proportion to the decreased creatinine clearance. The elimination rate of Omeprazole was somewhat decreased in the elderly, and bioavailability was increased. Omeprazole was 76% bioavailable when a single 40 mg oral dose of Omeprazole (buffered solution) was administered to healthy elderly volunteers, versus 58% in young volunteers given the same dose. Nearly 70% of the dose was recovered in urine as metabolites of Omeprazole and no unchanged drug was detected. The plasma clearance of Omeprazole was 250 mL/min (about half that of young volunteers) and its plasma half-life averaged one hour, about twice that of young healthy volunteers.
Indications/Uses
Omed: Omeprazole (Omed) is indicated primarily for the treatment of Zollinger-Ellison syndrome, and may also be used for the treatment of gastric ulcer, duodenal ulcer and reflux oesophagitis.
Omed 20: It is used in conditions where inhibition of gastric acid secretion may be beneficial, including aspiration syndrome, dyspepsia, gastro-esophageal reflux disease, peptic ulcer disease and the Zollinger-Ellison syndrome.
Dosage/Direction for Use
Omed: Patients who are unable to take oral medication, e.g in severely ill patients with reflex oesophagitis, duodenal ulcer or gastric ulcer. Omeprazole 40 mg bolus is recommended once daily for up to 5 days.
Administration: Omeprazole 40 mg I.V. injection should be administered intravenously only and should not be given by any other route.
Injection: For I.V. injection, reconstitute one sterile single dose vial of Omeprazole (Omed) injection with 10 mL of sterile water for Injection USP (without preservative) to make 10 mL solution containing 4 mg/mL of Omeprazole approximately.
The reconstituted solution of Omeprazole (Omed) injection having 4 mg/mL of Omeprazole approximately is stable for 4 hrs when stored in original vial in a cool place.
The reconstituted solution of Omeprazole (Omed) injection should not be used if it contains visible particulate matter.
Infusion: For I.V. infusion, reconstitute one sterile single dose vial of Omeprazole (Omed) injection with 10 mL of sterile water for Injection USP (without preservative) to make 10 mL solution containing 4 mg/mL of Omeprazole approximately. Subsequently add 10 mL of reconstituted solution containing 4 mg/mL of Omeprazole approximately, to 90 mL of Sodium Chloride Injection (Containing 0.9% w/v Sodium Chloride) or 90 mL of Dextrose Injection (Containing 5% w/v Dextrose) or 90 mL of Mannitol Injection (containing 5% w/v of Mannitol) to make 100 mL solution of 0.4 mg/mL of Omeprazole approximately. No other solution should be used for infusion. The resultant infusion should be given intravenously over a period of 20-30 minutes. The prepared infusion solution should be used within 3 hours of preparation and any unused portion should be discarded. The infusion solution having Omeprazole should not be refrigerated.
The diluted infusion solution of Omeprazole (Omed) injection having 0.4 mg/mL of Omeprazole approximately in infusion fluids are stable up to 4 hrs when stored in a cool place and protect from light. The diluted infusion solution containing Omeprazole sodium should not be used if they contain visible particulate matter.
Omed 20: Acid-related Dyspepsia: 10 or 20 mg daily for 2 to 4 weeks.
Gastro-esophageal reflux Disease: 20 mg daily for 4 weeks up to 8 weeks if not fully healed.
Peptic Ulcer disease: 20 mg daily, or 40 mg in severe case, 4 weeks for duodenal ulcer and 8 weeks for gastric ulcer.
Zollinger-Ellison Syndrome: 60 mg daily, adjusted as required. The majority of patients are effectively controlled by dose in the range 20 to 120 mg daily, but doses up to 120 mg 3 times daily.
Acid Aspiration: 40 mg in the evening before the surgery, further 40 mg up to 6 hours before the procedure.
Or as prescribed by the physician.
Overdosage
Omed: There is no sufficient information available on deliberate over dosage with Omeprazole. However, doses up to 400 mg have not resulted in severe symptoms. Therefore, treatment of over dosage should be symptomatic and supportive. In clinical trials, intravenous doses up to 270 mg/day and up to 650 mg over a three-day period have been given without any dose related adverse effects.
Contraindications
Omed: Patients who are hypersensitive to Omeprazole or any of the inactive ingredients of Omeprazole are contraindicated to use Omeprazole intravenous injection.
Omed 20: Omeprazole is contraindicated in patients with known hypersensitivity to the component of the formulation.
Special Precautions
Omed: Use in Patients with Impaired Liver Function: Dosage reduction may be required in patients with impaired liver function as Omeprazole is extensively metabolized in the liver and its elimination rate is prolonged in such patients when compared to normal persons. The daily dose of 10-20 mg is recommended in patients with severe liver disease.
Use In Patients with Impaired Kidney Function: It is not necessary to adjust the dose of omeprazole in patients with renal insufficiency.
Use in Pregnancy and Lactation: There is no adequate data on the safety of Omeprazole in pregnant women. Animal studies have revealed no teratogenic effect, but reproduction studies have revealed reduced lifter weights. However, to avoid the risk of developing the undesirable effects, Omeprazole should not be recommended in pregnancy unless its use is essential.
It is not known whether Omeprazole is secreted into human milk. Breast feeding should therefore be discontinued if the use of Omeprazole is considered essential.
Use in Children: The safety and effectiveness of Omeprazole Sodium Injection in children have not been established.
Use in Elderly: It is not necessary to adjust the dose of Omeprazole in elderly patients. However, a slight decrease in elimination rate and an increase in bioavailability are likely to occur in such patients.
Use In Pregnancy & Lactation
Omed: There is no adequate data on the safety of Omeprazole in pregnant women. Animal studies have revealed no teratogenic effect, but reproduction studies have revealed reduced lifter weights. However, to avoid the risk of developing the undesirable effects, Omeprazole should not be recommended in pregnancy unless its use is essential.
It is not known whether Omeprazole is secreted into human milk. Breast feeding should therefore be discontinued if the use of Omeprazole is considered essential.
Adverse Reactions
Omed: The adverse effects reported most frequently with omeprazole have been gastrointestinal disturbances, in particular diarrhea, constipation, abdominal pain, nausea and vomiting and flatulence. Skin rash, pruritus and urticaria have also been reported, usually resolving after discontinuation of treatment.
Central nervous system disorders reported so far include paresthesia, dizziness, light-headedness and feeling faint, all of these usually resolved on cessation of therapy. Somnolence, insomnia, and vertigo have been reported rarely. Reversible mental confusion, agitation, depression and hallucinations have occurred predominantly in severely ill patients.
Other adverse events reported rarely include arthralgias and myalgia, blurred vision, taste disturbances, peripheral edema, hyponatremia, blood disorders including agranulocytosis, leucopenia, thrombocytopenia, pancytopenia, anaphylactic shock, malaise, fever, bronchospasm, encephalopathy in patients with preexisting severe liver disease, hepatitis with or without jaundice, rarely hepatic failure and interstitial nephritis which has resulted in acute renal failure.
Omed 20: The most common side effects are diarrhea, skin rashes, and headache. Other adverse effects reported rarely include arthralgia, and myalgia, blood disorders including leucopenia and thrombocytopenia, interstitial nephritis, and hepatotoxicity.
Drug Interactions
Omed: The potential for metabolic interactions between Omeprazole and other drugs is very limited. However, as Omeprazole inhibits hepatic microsomal drug metabolism (cytochrome P450 enzyme system), the elimination of other drugs that require hepatic metabolism via the cytochrome P450 system or that are highly extracted by the liver may be decreased during concurrent use with Omeprazole. This effect may result in delayed elimination, increased blood concentrations of diazepam, phenytoin and anticoagulants such as warfarin (monitoring of blood concentrations, or prothrombin time for anticoagulants, is recommended as a guide to dosage adjustment may be necessary during Omeprazole therapy).
Omeprazole, by increasing gastric pH, has the potential to affect the bioavailability of any medication for which absorption is pH-dependent and also Omeprazole may prevent the degradation of acid labile drug. Therefore, concurrent use of itraconazole and Ketoconazole with Omeprazole may result in reduced absorption of these drugs.
Omeprazole has no influence on any other relevant isoforms of CYP, as shown by the lack of metabolic interaction with substrates for CYP1A2 (caffeine, phenacetin, theophylline), CYP2C6 (S-warfarin, piroxicam, phenacetin, theophylline), CYP2D6 (metoprolol, propranolol), CYP2E1 (ethanol), and CYP3A (cyclosporine, lidocaine, quinidine, estradiol, erythromycin, budesonide).
Omed 20: The following drugs should not be used: atazanavir, cilostazol, cyclosporine, diazepam, disulfiram, phenytoin, voriconazole, warfarin, ampicillin, azole antifungals (e.g. ketoconazole), iron supplements.
Caution For Usage
Omed: Incompatibilities: Infusions with low pH should not be used for diluting OMED Injection as fading & discoloration of solution can occur.
Storage
Omed: Store at temperatures not exceeding 25°C.
Shelf-life: 24 months.
Omed 20: Store at temperatures not exceeding 30°C.
Protect from light.
ATC Classification
A02BC01 - omeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Presentation/Packing
Omed: Lyophilized powd for inj (vial + 10 mL amp diluent) 40 mg x 10 mL x 1's.
Omed 20: Cap 20 mg x 24's.
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