Omeprazole Sodium for Injection

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Omeprazole sodium lyophilized powder for injection contains omeprazole sodium, and its' chemical name is 5-methoxy-2-[[(4-methoxy-3, 5-dimethyl-2-pyridinyl) methyl] sulfinyl]-1H-benzimidazole hydrate, and the chemical structure is:

Molecular formular: is C17H18NaN3O3S·H2O,

Molecular weight:385.41.

Omeprazole sodium lyophilized powder for injection is a white or almost white loose masses or powders.

Omeprazole sodium for injection, a racemic mixture of two active enantiomers, reduces gastric acid secretion through a highly targeted mechanism of action. It is a specific inhibitor of the acid pump in the parietal cell. It is rapid acting and provides control through reversible inhibition of gastric acid secretion with once daily dosing.

Intravenous omeprazole produces a dose dependent inhibition of gastric acid secretion in humans. In order to immediately achieve a similar reduction of intragastric acidity as after repeated dosing with 20 mg orally, a first dose of 40 mg intravenously is recommended. This results in an immediate decrease in intragastric acidity and a mean decrease over 24 hours of approximately 90%.

The inhibition of acid secretion is related to the area under the plasma concentration-time curve (AUC) of omeprazole and not to the actual plasma concentration at a given time.

No tachyphylaxis has been observed during treatment with omeprazole.
 

Distribution

The apparent volume of distribution in healthy subjects is approximately 0.3 L/kg and a similar value is also seen in patients with renal insufficiency. For elderly patients and in patients who is with hepatic insufficiency, the volume of distribution is decreased slightly. The plasma protein binding of omeprazole is about 95%.

Metabolism and excretion

The average half-life of the terminal phase of the plasma concentration-time curve following IV administration of omeprazole is approximately 40 minutes. The total plasma clearance is 0.3 to 0.6 L/min. 

It is completely metabolised by the cytochrome P450 system (CYP), basically in the liver. The major part of its metabolism is dependent on the polymorphically expressed, specific isoform CYP2C19 (S-mephenytoin hydroxylase),which is responsible for the formation of hydroxyomeprazole, the major metabolite in plasma. On the basis of this, as a result of competitive inhibition, there is a potential for metabolic drug-drug interactions between omeprazole and other substrates for CYP2C19.

By now there is no metabolite that has been found to have any effect on gastric acid secretion. Nearly 80% of an intravenously given dose is excreted as metabolites in the urine, and the remainder is found in the faeces, primarily originating from bile secretion.

The elimination of omeprazole is unchanged in patients with reduced renal function. The elimination half-life is increased in patients with impaired liver function, but any accumulation with once daily dosing was showed on omeprazole.

Indications:

Omeprazole sodium for injection is substituted indicated primarily for the treatment of Zollinger-Ellison syndrome, and also be used for the treatment of gastric ulcer, duodenal ulcer and reflux oesophagitis when oral medication is inappropriate.

I.V infusion: dissolve the contents in 100ml of 0.9% sodium chloride or 100ml of 5% glucose injection, the duration of the injection process should be persist 20 minutes to 30minutes or exceed the length.

When oral medication in the treatment gastric ulcer, duodenal ulcer and reflux oesophagitis is inappropriate, 40mg of omeprazole sodium daily is recommended.

Zollinger-Ellison syndrome the recommended initial dose of omeprazole sodium for injection given intravenously 40mg daily. It may be required higher daily doses and the dose should be adjusted individually. When doses exceed 60 mg per day, the dose should be divided and given twice a day.

Omeprazole sodium for injection is well tolerated and adverse reaction have generally been mild and reversible. The following events have been reported in clinical trials or reported from routine uses. but in many cases a relationship to treatment with omeprazole has not been established

The following definitions of frequencies are used:

Common ≥1/100

Uncommon ≥1/1,000 and <1/100

Rare <1/1,000

Common

Central and peripheral nervous system: Headache

Gastrointestinal Diarrhoea, constipation, abdominal pain, nausea/vomiting and flatulence

Uncommon

Central and peripheral nervous system:

Dizziness, paraesthesia, somnolence, insomnia and vertigo

Hepatic: Increased liver enzymes

Skin: Rash, dermatitis and/or pruritis. Urticaria

Other: Malaise

Rare:

Central and peripheral nervous system: Reversible mental confusion, agitation, aggression, depression and halluncinations, predominantly in severely ill patients

Endocrine: Gynaecomastia

Gastrointestinal: Dry mouth, stomatitis and gastrointestinal candidiasis

Haematological: Leukopenia, thrombocytopenia, agranulocytosis and pancytopenia

Hepatic: Encephalopathy in patients with pre-existing severe liver disease; hepatitis with or without jaundice, hepatic failure

Musculoskeletal: Arthralgia, muscular weakness and myalgia

Skin: Photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN), alopecia

Other: Hypersensitivity reactions eg. angioedema, bronchospasm,fever, interstitial nephritis and anaphylactic shock.

Increased sweating, blurred vision,peripheral oedema, taste disturbance and hyponatraemia.

Isolated cases of critically ill patients who have received omeprazole intravenous injection, especially at high doses,was reported for irreversible visual impairment has been reported in..

Contraindication:known hypersensitivity to omeprazole.

Warning And Precautions:In the presence of any alarm symptom (e.g. significant unintentional weight loss, recurrent vomiting, dysphagia, haematemesis or melena) and when gastric ulcer is suspected or present, the possibility of malignancy should be excluded as treatment may alleviate symptoms and delay diagnosis.

Use In Pregnancy And Lactation

Results from animal studies indicate no adverse effects of omeprazole on pregnancy or on the health of the fetus/newborn child. Omeprazole arenot commonly advisedly to used during pregnancy and nurses.

Omeprazole is excreted in breast milk but is not likely to influence the child when therapeutic doses are used.

Effects on ability to drive and use machines

Omeprazole is not likely to affect the ability to drive or use machines.

Children:There is no experance with omeperazole in children.

Elderly: No need to adjustment on dose for elderly, and directed by the pharmacist

Drug Interactions

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