Khriz Omeprazole

Omeprazole sodium.

Each vial contains Omeprazole (as sodium) 40 mg.

Pharmacology: Pharmacokinetics: Omeprazole is rapidly but variably absorbed after oral doses. Absorption is not significantly affected by food. Omeprazole is acid-labile and the pharmacokinetics of the various formulations developed to improve oral bioavailability may vary. The absorption of omeprazole also appears to be dose-dependent; increasing the dosage above 40 mg has been reported to increase the plasma concentrations in a non-linear fashion because of saturable first-pass hepatic metabolism. In addition, bioavailability is higher after long-term use.
Bioavailability of omeprazole may be increased in elderly patients, in some ethnic groups such as Chinese, and in patients with hepatic impairment, but is not markedly affected in patients with renal impairment.
On absorption, omeprazole is almost completely metabolised in the liver, primarily by the cytochrome P450 isoenzyme CYP2C19 to form hydroxy-omeprazole, and to a small extent by CYP3A4 to form omeprazole sulfone. The metabolites are inactive, and are excreted mostly in the urine and to a lesser extent in bile. The elimination half-life from plasma is reported to be about 0.5 to 3 hours. Omeprazole is about 95% bound to plasma proteins.

Omeprazole is a proton pump inhibitor. It suppresses secretion of gastric acid by inhibiting the enzyme system of hydrogen/potassium adenosine triphosphatase (H+/K+ ATPase), the 'proton pump' of the gastric parietal cell. It is used in conditions where inhibition of gastric acid secretion may be beneficial, including aspiration syndromes, dyspepsia, gastro-oesophageal reflux disease, peptic ulcer disease, and the Zollinger-Ellison syndrome.

In patients who are unsuited to receive oral therapy omeprazole sodium may be given on a short-term basis by intravenous infusion, in a usual dose equivalent to 40 mg of the base over a period of 20 to 30 minutes in 100 mL of sodium chloride 0.9% or glucose 5%. It may also be given by slow intravenous injection. Higher intravenous doses have been given to patients with Zollinger-Ellison syndrome.
For parenteral dosage in children the BNFC recommends an intravenous dose of 500 micrograms/kg (to a maximum of 20 mg) once daily in children aged 1 month to 12 years; this may be increased to 2 mg/kg (to a maximum of 40 mg) once daily if needed.
Administration in hepatic impairment: Bioavailability and half-life of omeprazole can increase in patients with hepatic impairment. UK licensed product information recommends that a maximum daily oral dose of 20 mg be used in these patients; a daily intravenous dose of 10 to 20 mg is considered sufficient.

Contraindicated in patients hypersensitive to the drug.

Proton pump inhibitors may increase the risk of gastrointestinal infections because of their acid suppressive effects.
Early toxicological studies identified carcinoid-like tumours of the gastric mucosa in rats given very high doses of omeprazole over long periods.
Before giving omeprazole or other proton pump inhibitors to patients with gastric ulcers the possibility of malignancy should be excluded since these drugs may mask symptoms and delay diagnosis. Omeprazole and other proton pump inhibitors should be used with caution in hepatic impairment and dose adjustment may be required.

Use in Pregnancy: It is not known to be harmful but should be used with caution during pregnancy.
Use in Lactation: Since omeprazole is excreted in human milk, caution should be exercised when administering this drug to a nursing mother.

Proton pump inhibitors are generally well tolerated, and adverse effects are relatively infrequent. The adverse effects reported most often with omeprazole and other proton pump inhibitors have been headache, diarrhoea, and skin rashes; they have sometimes been severe enough to require stopping treatment. Other effects include pruritus, dizziness, fatigue, constipation, nausea and vomiting, flatulence, abdominal pain, arthralgia and myalgia, urticaria, and dry mouth. Isolated cases of photosensitivity, bullous eruption, erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis have occurred.
Hypersensitivity reactions, including fever, bronchospasm, 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, hepatic failure, and hepatic encephalopathy, have been reported. Other adverse effects reported rarely include paraesthesia, blurred vision, alopecia, stomatitis, increased sweating, taste disturbances, peripheral oedema, malaise, hyponatraemia, blood disorders (including agranulocytosis, leucopenia, and thrombocytopenia), gynaecomastia, impotence, and interstitial nephritis.

Omeprazole and other proton pump inhibitors are metabolised by the cytochrome P450 system, primarily by isoenzyme CYP2C19, and to a smaller extent by CYP3A4. Inhibitors or inducers of these isoenzymes may affect exposure to omeprazole and other proton pump inhibitors. In turn, proton pump inhibitors may alter the metabolism of some drugs metabolised 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 dasatinib, ketoconazole, and itraconazole, whose absorption is dependent on an acid gastric pH. With voriconazole, the plasma concentration of both drugs may be increased. Other proton pump inhibitors may be similarly affected by voriconazole. Omeprazole and other proton pump inhibitors should not be used with atazanavir, as it substantially reduces exposure to atazanavir.

Directions for Reconstitution: Dissolve the powder in 5 mL of the accompanying diluent (Sterile Water for Injection).
Dilute in 100 mL of 0.9% sodium chloride solution or 5% glucose injection.
Use the product immediately after reconstitution.
Single dose. Discard any remaining portion.

Store at temperatures not exceeding 30°C. Keep the container in a dry place.
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).

Rx