Leveprazole

White powder.
Each vial contains: Omeprazole Sodium BP equivalent to Omeprazole 40 mg.
Each ampoule contains: Sterile Water for Injection BP 10 mL (diluent).

Pharmacology: Pharmacodynamics: Omeprazole is a proton pump inhibitor that belongs to a class of antisecretory compounds, the substituted benzimidazoles. It suppresses 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 has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production.
This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion.
Pharmacokinetics: Distribution: The apparent volume of distribution in healthy subjects is approximately 0.3 L/kg body weight. Omeprazole is 97% plasma protein bound.
Elimination: Total plasma clearance is about 30 to 40 L/h after a single dose. The plasma elimination half-life of Omeprazole is usually shorter than one hour both after single and repeated once-daily dosing. Omeprazole is completely eliminated from plasma between doses with no tendency for accumulation during once-daily administration. Almost 80% of a dose of Omeprazole is excreted as metabolites in the urine, the remainder in the feces, primarily originating from bile secretion.
Special populations: Hepatic impairment: The metabolism of Omeprazole in patients with liver dysfunction is impaired, resulting in an increased AUC. Omeprazole has not shown any tendency to accumulate with once-daily dosing.
Renal impairment: The pharmacokinetics of Omeprazole, including systemic bioavailability and elimination rate, are unchanged in patients with reduced renal function.
Older people: The metabolism rate of Omeprazole is somewhat reduced in elderly subjects (75 to 79 years of age).

Used in conditions where inhibition of gastric acid secretion may be beneficial, including aspiration syndromes, dyspepsia, gastroesophageal reflux disease, peptic ulcer disease and Zollinger-Ellison syndrome.

By intravenous injection over 5 minutes or by intravenous infusion over 20 to 30 minutes, prophylaxis of acid aspiration, 40 mg completed 1 hour before surgery.
Benign gastric ulcer, duodenal ulcer and gastroesophageal reflux, 40 mg once daily until oral administration is possible.
Severe peptic ulcer bleeding initial intravenous infusion of 80 mg then by continuous intravenous infusion, 8 mg/hr for 72 hours (then change to oral therapy).
Administration: Omeprazole 40 mg I.V. injection should only be administered intravenously. It should not be given by any other route.
Injection: For I.V. injection, each single dose vial containing lyophilized powder for Omeprazole 40 mg should be reconstituted with 10 mL of Sterile Water for Injection. The resulting concentration is 4 mg/mL of Omeprazole which should be given slowly (over a period of 5 minutes) as an intravenous injection.
Infusion: For I.V. infusion, the single dose vial should be dissolved in either 100 mL of Sodium Chloride injection (0.9% w/v) or 100 mL of Glucose intravenous infusion (5% w/v). No other solution should be used for the infusion. The infusion should be given over a period of 20 to 30 minutes. Or as prescribed by the physician.

Two cases of Omeprazole overdose were characterized by drowsiness, headache (possibly due to a metabolite) and tachycardia. Both patients recovered without specific treatment.
Intravenous doses of 270 mg given in a day and up to 650 mg over a three-day period in clinical trials did not show any dose-related adverse reactions. As in all cases where overdosing is suspected, treatment should be symptomatic and supportive.

Hypersensitivity to Omeprazole, other proton pump inhibitors or any component of the product.

Before giving Omeprazole or other proton pump inhibitors to patients with gastric ulcers, the possibility of malignancy should be considered since these drugs may mask symptoms and delay diagnosis. Omeprazole and other proton pump inhibitors should be used with caution in hepatic impairment.
Gastric malignancy should be excluded at initiation of treatment and at follow-up of gastric ulcer therapy.
Gastritis has been reported occasionally in gastric corpus biopsies from patients on long-term Omeprazole therapy.
The use of acid-suppressants such as Omeprazole may increase a patient's risk of community-acquired pneumonia.
Use in Asian Population: Consider dose reduction in Asian patients receiving long-term Omeprazole therapy for maintenance of healing of erosive esophagitis. The bioavailability of Omeprazole appears to be increased in these patients.
Use in Patients with Impaired Hepatic Function: Consider dose adjustment in patients with hepatic impairment especially in those requiring prolonged use since plasma half-life is increased in these patients.
Use in Patients with Impaired Renal Function: No dosage adjustment is necessary in patients with impaired kidney function.
Use in Pregnancy: See Use in Pregnancy & Lactation section for further information.
Use in Lactation: See Use in Pregnancy & Lactation section for further information.
Use in Children: There is limited experience with the use of Omeprazole IV in children.
Use in the Elderly: There is no difference in efficacy and safety observed between geriatric and younger patients. However, some elderly patients may exhibit increased sensitivity to the drug and may be at risk for potential side effects.

Use in Pregnancy: Omeprazole may be used in pregnant women. Epidemiological studies on Omeprazole have shown no adverse effects on pregnancy or on the health of the fetus/baby.
Use in Breastfeeding Mothers: Omeprazole is excreted in human milk. In rats, Omeprazole has been shown to be excreted in milk at low concentrations. Decision should be made whether to discontinue Omeprazole or breastfeeding since Omeprazole may cause potential serious adverse effects to the baby.

The adverse effects reported most frequently with Omeprazole and other proton pump inhibitors have been headache, diarrhea, and skin rashes; they have sometimes been severe enough to require stopping treatment. Other effects include pruritus, dizziness, fatigue, constipations, nausea and vomiting, flatulence, abdominal pain, arthralgia and myalgia, urticaria and dry mouth. Isolated cases of photosensitivity, bullous eruption, erythema multiforme, angioedema, and anaphylaxis have been reported. Effects on the CNS include occasional insomnia, somnolence, and vertigo; reversible confusional states, agitation, depression, and hallucinations have occurred in severely ill patients. Raised liver enzymes, and isolated cases of hepatitis, jaundice and hepatic encephalopathy, have been reported. Other adverse effects reported rarely or in isolated cases include paraesthesia, blurred vision, alopecia, stomatitis sweating, taste disturbances, peripheral edema, malaise, hyponatremia, blood disorders (including agranulocytosis, leukopenia, and thrombocytopenia), and interstitial nephritis.

Omeprazole and other proton pump inhibitors are metabolized by the cytochromes P450 system primarily by isoenzyme CYP2C19, and may alter the metabolism of some drugs metabolized by these enzymes. Omeprazole may prolong the elimination of diazepam, phenytoin, and warfarin. Omeprazole and other proton pump inhibitors can reduce the absorption of drugs such as ketoconazole, and possibly itraconazole, whose absorption is dependent on acid gastric pH with voriconazole, the plasma concentration of both drugs may be increased and a reduced dose of Omeprazole is recommended.

Direction for Reconstitution: Reconstitute with 10 mL of Sterile Water for Injection to provide a solution of 4 mg/mL of Omeprazole.

Store at temperatures 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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