INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo OMEZ 10 (capsule)
OMEZ 20 (capsule)

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

OMEZ 10 (capsule)
OMEZ 20 (capsule)

COMPOSITION
OMEZ 10: Each capsule contains
omeprazole 10 mg
OMEZ 20: Each capsule contains omeprazole 20 mg

PHARMACOLOGICAL CLASSIFICATION
A.11.4.3 Medicines acting on gastro-intestinal tract.

PHARMACOLOGICAL ACTION
Pharmacodynamics
Omeprazole is a specific inhibitor of the gastric proton pump in the parietal cell and thus reduces the secretion of gastric acid. Reversible control of gastric acid secretion is produced with single daily doses of omeprazole.
Omeprazole is a weak base, which is concentrated in the intracellular canaliculi of the parietal cell. Due to the acidic environment in these cells, omeprazole is converted to the active form, where it acts as an inhibitor of the enzyme H+, K+ -ATPase – the proton pump. There is a dose-dependency on this final step in the formation of gastric acid, which provides for effective inhibition of the secretion of both basal acid and stimulated acid irrespective of the secretatory enhancer.
Omeprazole has no pharmacological effect on acetylcholine, histamine or gastrin receptors.
Effect on gastric secretion
When omeprazole is given daily as a single oral dose, the gastric acid secretion is inhibited with a maximum effect reached within four days of treatment. In patients with duodenal ulcers, a mean decrease of approximately 80% in intragastric acidity is then maintained over a 24 hour period, with the mean decrease in peak acid output after pentagastrin stimulation being approximately 70%, twenty-four hours after initiating treatment with omeprazole.
Pharmacokinetics
Due to the acid lability of omeprazole, the oral formulation consists of enteric-coated granules in capsules. Omeprazole is usually completely absorbed from the small intestine within three to six hours.
After a single oral dose, the systemic bioavailability of omeprazole is approximately 35%, which can be increased to about 60%, after repeated once-daily administration. The simultaneous intake of food has no influence on the bioavailability. Omeprazole is approximately 95% bound to plasma proteins.
The average terminal phase half-life of the plasma concentration-time curve is approximately forty minutes. There is no change in half-life during treatment. The inhibition of acid secretion is related to the area under the plasma concentration-time curve (AUC) and not to the actual plasma concentration at a given time.
Omeprazole is completely metabolised, mainly in the liver. The sulphone, the sulphide and hydroxy-omeprazole are the metabolites detected in plasma. These metabolites are inactive and have no significant effect on acid secretion.
Approximately 80% of the metabolites are excreted in the urine and the balance in the faeces. The two main metabolites in the urine are hydroxy-omeprazole and the corresponding carboxylic acid.
There is no significant change in the systemic bioavailability of omeprazole in patients with impaired renal function. Although the area under the plasma concentration-time curve is increased in patients with reduced liver function, no apparent accumulation of omeprazole has been found.

INDICATIONS
OMEZ is indicated for the treatment of:
duodenal ulcer,
gastric ulcer,
reflux oesophagitis and,
Zollinger-Ellison syndrome.
If duodenal ulcers are associated with Helicobacter pylori, the concomitant use of omeprazole and suitable antibiotics may be beneficial.

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

DOSAGE AND DIRECTIONS FOR USE
The capsule must be kept intact and swallowed whole.
Duodenal Ulcer
  20 mg once daily for 2 –4 weeks.
  In some duodenal ulcer patient’s refractory to other treatment regimes, 40 mg once daily may be effective.
  The usual maintenance dose is 10 to 20 mg once daily.
  In demonstrated Helicobacter pylori associated duodenal ulcer, concomitant use of omeprazole and suitable antibiotics may be beneficial.
Gastric Ulcer and Reflux Oesophagitis
  A dosage of 20 mg once daily for 4 –8 weeks is recommended.
  In some patients with gastric ulcer or reflux oesophagitis refractory to other treatment regimes, OMEZ 40 mg once daily may be effective.
  In patients with severe or symptomatic recurrent reflux oesophagitis treatment can be continued with OMEZ at a dosage of 20 mg once daily.
Zollinger-Ellison Syndrome
  An initial dosage of 60 mg once daily is recommended. The dosage should be adjusted to the individual requirements of each patient and treatment continued as long as is clinically required.
  More than 90% of patients with severe disease have been maintained on daily doses of 20 mg to 120 mg. If doses required are higher than 80 mg daily, it should be divided into twice daily regimens.
Pediatrics
  The safety and efficacy of omeprazole in children have not been established.
Elderly
  No dose adjustment is required in the elderly.
Impaired Renal Function
  No dose adjustment is required in patients with reduced renal function.
Impaired Hepatic Function
  Due to an increase in the bioavailability plasma half-life of omeprazole in patients with impaired hepatic function a daily dose of 20 mg is generally adequate.
  The long-term safety of omeprazole in patients with renal and hepatic impairment has not been established.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS
The most commonly reported side-effects are: Nausea/vomiting, headache, diarrhoea, constipation, abdominal pain and flatulence, rash and/or pruritis, dizziness, paraesthesia, somnolence, insomnia, vertigo, increased liver enzymes and malaise.
The following have occurred in a few cases:
Skin: Photosensitivity, erythema multiforme, alopecia.
Central and peripheral nervous system: Arthralgia, muscular weakness, myalgia, reversible mental confusion, agitation, depression and hallucinations, mostly in severely ill patients.
Gastrointestinal: Dry mouth, stomatitis and gastrointestinal candidiasis.
Hepatic: Encephalopathy in patients with pre-existing severe liver disease; hepatitis with or without jaundice, hepatic failure. Increases in liver enzymes have been observed.
Endocrine: Gynaecomastia.
Haematologic: Leukopenia and thrombocytopenia.
Other: Hypersensitivity reactions e.g. urticaria, angioedema, fever, bronchospasm and interstitial nephritis. Increased sweating, peripheral oedema, blurred vision and taste disturbance.
Other effects related to acid inhibition:
During long term treatment gastric glandular cysts have been reported to occur more frequently. These changes are benign and seem to be reversible and are a physiological consequence of pronounced inhibition of acid secretion.
If a gastric ulcer is suspected, the possibility of malignancy should be excluded as treatment may mask the symptoms and delay diagnosis.

INTERACTIONS
Omeprazole can prolong the elimination of medicines which are metabolised by oxidation in the liver e.g. warfarin, diazepam and phenytoin.
Patients receiving warfarin or phenytoin concomitant with omeprazole, should be monitored closely as a reduction in dosages of warfarin or phenytoin may be required.
It was however shown in patients on concurrent omeprazole treatment at a daily dosage of 20 mg and continuous phenytoin treatment, that the simultaneous use of these two medications did not influence the blood concentration of phenytoin. Concomitant treatment with omeprazole 20 mg daily also did not alter coagulation time in patients on long-term treatment with warfarin.
There is a possibility of interactions with medicines metabolised via the cytochrome P450 enzyme system, although no interactions with propranolol, metoprolol, theophylline, lignocaine, quinidine and amoxycillin have been recorded.
No interaction with food or the concurrent administration of antacid medications have been found.
The plasma concentrations of both omeprazole and clarithromycin may be increased during concomitant treatment with these medicines.
An increase of approximately 10% in the bioavailability of digoxin was recorded in healthy volunteers due to the increase in intragastric pH when omeprazole and digoxin are administered concurrently.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
See Side-effects and Special Precautions.
Treatment is symptomatic and supportive.

IDENTIFICATION
OMEZ 10: Off-white to pale yellow elliptical to spherical pellets filled in a hard gelatin capsule with opaque lavender coloured cap and opaque yellow coloured body. “Omeprazole 10 mg”imprinted with black ink on cap and “R158” imprinted with black ink, on body.
OMEZ 20: Off-white to pale yellow elliptical to spherical pellets filled in a hard gelatin capsule with opaque lavender coloured cap and opaque iron grey coloured body. “Omeprazole 20 mg”imprinted with black ink on cap and “R158”imprinted with black ink, on body.

PRESENTATION
OMEZ 10: Blister packing containing 30 capsules.
OMEZ 20: Blister packaging containing 30 capsules

STORAGE INSTRUCTIONS
Store below 25°C. Protect from light and moisture.
Store the blisters in the outer carton until required for use.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBERS
OMEZ 10 (capsule) : 34/11.4.3/0299
OMEZ 20 (capsule) : 34/11.4.3/0300

NAME AND BUSINESS ADDRESS OF THE APPLICANT
Dr. Reddy’s Laboratories (Pty) Ltd.
3rd Floor, TA Bank Building
160 Jan Smuts Avenue
Rosebank, 2196

DATE OF PUBLICATION OF THIS PACKAGE INSERT
17 August 2000

New addition to this site: March 2006
Source: Pharmaceutical Industry

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