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Logo ALTOSEC 40 mg/10 mL

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

ALTOSEC 40 mg/10 mL
(powder and solvent for injectable solution)

COMPOSITION:
Each vial of powder contains Omeprazole (as a sodium salt) equivalent to 40 mg Omeprazole.
Each ampoule of solvent for injection contains 5.25 mg citric acid monohydrate, 4.2 g polyethylene glycol 400 and water for injection.

PHARMACOLOGICAL CLASSIFICATION:
A 11.4.3 Medicines acting on gastro-intestinal tract - other

PHARMACOLOGICAL ACTION:
Omeprazole is an inhibitor of the gastric proton pump (H+, K+ATPase)
It inhibits both basal and stimulated gastric acid secretion by parietal cells, whether induced by acetylcholine, gastrin or histamine.
Omeprazole has no effect on acetylcholine, histamine or gastrin receptors.
Effects on Gastric Secretion
Omeprazole infusion produces an immediate decrease in intra-gastric acidity and a mean decrease over 24 hours of approximately 90%
Pharmacokinetics:
Omeprazole is more than 95% bound to plasma proteins. Clearance from the circulation is by hepatic metabolism with a plasma half life of 30 to 90 minutes. Hepatic metabolism occurs primarily via the cytochrome P450 (CYP) isoform (CYP2C19). The inactive metabolites are excreted mainly in the urine (80%) whilst the remaining 20% are excreted via faeces. The average half-life of the terminal phase of the plasma concentration-time curve is approximately 40 minutes. There is no change in plasma half-life during treatment. The inhibition of acid secretion is related to the area under the plasma concentration-time curve (AUC) and not the actual plasma concentration at a given time.
The systemic bioavailability of omeprazole is unchanged 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.

INDICATIONS:
Altosec 40 mg/10 mL is indicated for the short-term treatment of duodenal ulcer, gastric ulcer, reflux oesophagitis, and Zollinger-Ellison syndrome when oral therapy is regarded inappropriate or contra-indicated, for up to 5 days.

CONTRA-INDICATIONS:
Hypersensitivity to any of the ingredients.
Safety in pregnancy and lactation has not been established.

WARNINGS:
Symptomatic response to Altosec 40 mg/10 mL therapy does not preclude the presence of gastric ulcer or malignancy or a malignant disease of the oesophagus. The administration of Altosec 40 mg/10 mL in this situation may delay diagnosis (see Special Precautions).
Hepatic impairment may require a reduction in dose (see DOSAGE AND DIRECTIONS FOR USE).
THERE IS VERY LIMITED EXPERIENCE WITH THE USE OF ALTOSEC 40 mg/10 mL IN CHILDREN.
THE LONG-TERM SAFETY OF ALTOSEC 40 mg/10 mL IN PATIENTS WITH RENAL AND/OR HEPATIC IMPAIRMENT HAS NOT BEEN ESTABLISHED.
THIS MEDICINE MAY LEAD TO DROWSINESS AND IMPAIRED CONCENTRATION THAT MAY BE AGGRAVATED BY THE SIMULTANEOUS INTAKE OF ALCOHOL OR OTHER CENTRAL NERVOUS SYSTEM DEPRESSANT. PATIENTS SHOULD BE ADVISED, PARTICULARLY AT THE INITIATION OF THERAPY, AGAINST TAKING CHARGE OF VEHICLES OR MACHINERY OR PERFORMING POTENTIALLY HAZARDOUS TASKS WHERE LOSS OF CONCENTRATION COULD LEAD TO ACCIDENTS.

INTERACTIONS:
Altosec 40 mg/10 mL is metabolised via the hepatic P450 cytochrome enzyme system, which may affect the metabolism of other medications metabolised by these enzymes when given concomitantly. The elimination of diazepam, warfarin and phenytoin may be prolonged when Altosec 40 mg/10 mL is given concomitantly. Monitoring of INR and phenytoin serum levels is recommended and dosage reductions may be necessary when Altosec 40 mg/10 mL is given concomitantly.
There is a possible interaction of Altosec 40 mg/10 mL with digoxin and a 10% increase in digoxin bioavailability may be expected.
There may be interactions with other medicines, which are also metabolised via the cytochrome P450 enzyme system.

PREGNANCY AND LACTATION:
Safety in pregnancy and lactation has not been established (see CONTRAINDICATIONS)

DOSAGE AND DIRECTIONS FOR USE:
The intravenous formulation is indicated for short-term use when oral therapy is regarded as inappropriate or contra-indicated.
In Zollinger-Ellison syndrome the dosage should be individually adjusted and higher doses may be indicated.
When doses exceed 60 mg daily, the dose should be divided and given twice daily.
Children:
Safety and efficacy of omeprazole in children has not been established.
Elderly:
No dose adjustment is necessary in the elderly.
Impaired Renal Function:
No dose adjustment is required in patients with impaired renal function.
Impaired Hepatic Function:
As bioavailability and plasma half-life of omeprazole are increased in patients with impaired hepatic function, a daily dose of 10-20 mg is generally sufficient.
The long-term safety of Altosec 40 mg/10 mL in patients with renal and hepatic impairment has not been established.
Altosec 40 mg/10 mL is for intravenous administration only and must not be given by any other route. Altosec 40 mg/10 mL powder for injectable solution should only be dissolved in the solvent provided. No other solvents for I.V. injection should be used. Do not use if any particles are present in the reconstituted solution. After reconstitution outside validated aseptic conditions, use within 4 hours of preparation and any unused portion should be discarded. The duration of administration should be over 5 minutes.
Preparation:
Steps 1 to 5 should be done in immediate sequence:
1) With a syringe draw 10 mL of solvent from the ampoule.
2) Add approximately 5 mL of the solvent to the vial with freeze dried omeprazole.
3) Withdraw as much air as possible from the vial back into the syringe in order to reduce positive pressure; this will make it easier to add the remaining solvent.
4) Add the remaining solvent into the vial. Make sure that the syringe is empty.
5) Rotate and shake the vial to ensure all the freeze-dried omeprazole has dissolved.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Side-effects:
Gastro-intestinal:
Frequent: Abdominal pain or colic
Less frequent: Diarrhoea (severe enough to require discontinuation of therapy in some cases), constipation, nausea, vomiting, flatulence, acid regurgitation.
Has been reported, but frequency unknown: Dry mouth, stomatitis, oesophageal candidiasis, taste disturbances, benign reversible gastric glandular cysts, and increased gastrointestinal bacteria.
Haematological:
Less frequent: Pancytopenia, thrombocytopenia, agranulocytosis, and leucopenia.
Skin and appendages:
Less frequent: Skin rash, itching
Toxic epidermal necrolysis (TEN), Stevens-Johnson Syndrome, erythema multiforme.
Has been reported, but frequency unknown: Urticaria, photosensitivity, bullous eruption, angioedeme, alopecia and pruritus.
Endocrine:
Has been reported, but frequency unknown: Hyponatraemia
Respiratory:
Has been reported, but frequency unknown: Bronchospasm
Neurological:
Less frequent: Headache (severe enough to require discontinuation of therapy in some cases), dizziness, somnolence.
Has been reported, but frequency unknown: Vertigo, insomnia, reversible mental confusion, aggression, hallucinations, agitation, malaise, parasthaesias, fever, and depression, have occurred, predominantly in severely ill patients.
Cardiovascular:
Has been reported, but frequency unknown: Peripheral oedema
Genitourinary:
Has been reported, but frequency unknown: Interstitial nephritis, gynaecomastia
Vision:
Has been reported, but frequency unknown: Blurred vision
Hepatic:
Has been reported, but frequency unknown: Raised liver enzymes, hepatitis with or without jaundice and hepatic encephalopathy
Musculoskeletal:
Less frequent: Asthenia
Has been reported, but frequency unknown: Arthralgia and myalgia
Hypersensitivity reactions:
Has been reported, but frequency unknown: Hypersensitivity with anaphylaxis
Other:
Has been reported, but frequency unknown: Taste disturbance, aggression, increased sweating, malaise and fever
Special Precautions:
Effects related to acid inhibition
During long-term treatment, gastric glandular cysts have been reported in increased frequency. These physiological changes result from pronounced inhibition of gastric acid secretion. Decreased gastric acidity increases gastric counts of bacteria normally present in the gastro-intestinal tract. Treatment with Altosec 40 mg/10 mL may lead to an increased risk of gastro-intestinal infections such as Salmonella and Campylobacter.
In the presence of symptoms such as significant unintentional weight loss, recurrent vomiting, dysphagia, haematemesis, or melaena, and when gastric ulcer is suspected or present, malignancy should be excluded, as treatment with Altosec 40 mg/10 mL may alleviate symptoms and delay diagnosis.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Blurred vision, confusion, diaphoresis, flushing, headache, malaise, nausea, and tachycardia have been reported from over-dosage with omeprazole. There is no specific antidote for overdose with omeprazole.
TREATMENT IS SYMPTOMATIC AND SUPPORTIVE.
Due to extensive protein binding, omeprazole is not readily dialysable.
Patients in whom overdose is confirmed or suspected should be referred for medical practitioner/doctor consultation.

IDENTIFICATION:
Vial: A white lyophilised powder.
Ampoule: A limpid, colourless liquid free from visible particulate matter.
Reconstituted Solution: Clear, colourless to slightly yellow solution, practically free of particles.

PRESENTATION:
Altosec 40 mg/10 mL is available in pack sizes of 1's and is a combination pack comprising of a:
Vial: A colourless, type III, glass vial with a grey, bromobutyl rubber stopper and white polypropylene cap with an aluminum frame.
Ampoule: A colourless, type I, glass ampoule.
Both the vial and ampoule are packed together in a plastic tray, which is placed in an outer carton.

STORAGE INSTRUCTIONS:
Store below 25ºC. Protect from light.
Keep the vial and ampoule in the outer carton.
Reconstituted solution: After reconstitution outside validated aseptic conditions, use within 4 hours of preparation and any unused portion should be discarded.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER:
Vial (Lyophilised powder): A40/11.4.3/0192
Ampoule (Solvent): A40/11.4.3/0431

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION:
PHARMACARE LIMITED
Building 12
Healthcare Park
Woodlands Drive
Woodmead
Sandton
2148

DATE OF PUBLICATION OF THE PACKAGE INSERT:
15 November 2005

New addition to this site: September 2010
Source: Pharmaceutical Industry

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