1. Name Of The Medicinal Product
Boots Acid Reflux 10 mg Gastro-Resistant Tablets
Care Heartburn Relief 10 mg Tablets
Co-op Heartburn Relief 10 mg Tablets
Dexcel Heartburn Relief 10 mg Tablets
Galpharm Heartburn Relief 10 mg Tablets
Numark Heartburn Relief 10 mg Tablets
Sainsbury's Heartburn Relief 10 mg Tablets
Superdrug Heartburn Relief 10 mg Tablets
Tesco Heartburn Relief 10 mg Tablets
Unichem Heartburn Relief 10 mg Tablets
Vantage Pharmacy Heartburn Relief 10 mg Tablets
Lloydspharmacy Heartburn Relief 10mg Tablets
2. Qualitative And Quantitative Composition
Omeprazole 10 mg
For excipients, see section 6.1.
3. Pharmaceutical Form
Gastro-resistant tablets.
Brownish-pink, capsule-shaped film-coated tablets.
4. Clinical Particulars
4.1 Therapeutic Indications
Relief of reflux-like symptoms (e.g. heartburn) in patients aged 18 and over.
4.2 Posology And Method Of Administration
The tablets should be swallowed whole with plenty of liquid (e.g., water or fruit juice) prior to a meal. It is important that the tablets should not be crushed or chewed.
Initially the dosage is 20mg once daily.
Subsequently, symptomatic relief from heartburn can be achieved in some subjects by taking 10mg once daily, increasing to 20mg if symptoms return.
The lowest effective dose should always be used.
If no relief is obtained within two weeks then the patient should be referred to their doctor.
If continuous treatment for more than 4 weeks is required to relieve symptoms then the patient should be referred to their doctor.
4.3 Contraindications
Known hypersensitivity to omeprazole or to any of the other ingredients.
4.4 Special Warnings And Precautions For Use
Decreased gastric acidity, due to any means - including proton- pump inhibitors - increases gastric counts of bacteria normally present in the gastrointestinal tract. Treatment with acid-reducing drugs leads to a slightly increased risk of gastrointestinal infections such as salmonella or campylobacter.
Special warnings and precautions for patients taking non-prescription indigestion or heartburn remedies:
Patients should be referred to their doctor if:
• They have had to take an indigestion or heartburn remedy continuously for 4 or more weeks in order to control their symptoms
• They are aged over 45 years with new or recently changed symptoms
• They have unintentional weight loss, anaemia, gastrointestinal bleeding, dysphagia, pain on swallowing, persistent vomiting or vomiting with blood, epigastric mass, previous gastric ulcer or surgery, jaundice or any other significant medical condition (including hepatic and renal impairment).
Patients with long-term recurrent symptoms of indigestion or heartburn should see their doctor at regular intervals. Patients aged over 45 years taking any “over the counter” (OTC, non-prescription) indigestion or heartburn remedy on a daily basis should inform their pharmacist or doctor.
Patients should not take another “acid suppressor” e.g. H2 antagonist concomitantly.
Patients should consult their doctor before taking this product if they are due to have an endoscopy.
The Patient Information Leaflet will contain advice that the tablets will not provide immediate relief of symptoms.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
As with many indigestion and heartburn remedies, omeprazole may interact with other medications. Therefore, patients who are also taking other medications should first consult with either their pharmacist or doctor before taking omeprazole.
As omeprazole is metabolized in the liver through cytochrome P450 it can delay the elimination of diazepam, phenytoin and warfarin. Monitoring of patients receiving warfarin or phenytoin is recommended and a reduction of the warfarin or phenytoin dose may be necessary. However concomitant treatment with omeprazole 20 mg daily did not change the blood concentration of phenytoin in patients on continuous treatment with phenytoin. Similarly, concomitant treatment with omeprazole 20 mg daily did not change coagulation time in patients on continuous treatment with warfarin. Interactions with other medicinal products which are also metabolized via the cytochrome P-450 isoenzyme of group 2C cannot be excluded.
Due to the decreased intragastric acidity, the absorption of ketoconazole or itraconazole may be reduced during omeprazole treatment, as it is during treatment with other acid secretion inhibitors.
Concomitant use of omeprazole and cilostazol results in an increase in the plasma concentration of cilostazol, therefore concomitant use should be avoided. It is possible that omeprazole also increases the plasma-tacrolimus concentration, whereas voriconazole increases the plasma concentration of omeprazole.
Simultaneous treatment with omeprazole and digoxin in healthy subjects led to a 10% increase in the bioavailability of digoxin as a consequence of the increased intragastric pH.
Omeprazole as so far tested has no influence on the metabolism of the following substances: amoxycillin, antacids, quinidine, caffeine, ciclosporin, diclofenac, estradiol, lidocaine, metoprolol, naproxen, phenacetin, piroxicam, propranolol, theophylline.
Treatment with omeprazole may cause false negative results in 13C-Urea breath tests.
Alcohol and food do not affect the absorption of omeprazole.
4.6 Pregnancy And Lactation
This product should not be used during pregnancy or whilst breast feeding.
Pregnancy
There is no evidence on the safety of omeprazole in human pregnancy. Animal studies have revealed no teratogenic effect, but reproduction studies have revealed reduced litter weights. Avoid in pregnancy, unless there is no safer alternative.
Lactation
There is no information available on the passage of omeprazole into breast milk or its effects on the neonate. Breast-feeding should therefore be discontinued if the use of omeprazole is considered essential.
4.7 Effects On Ability To Drive And Use Machines
In rare cases, drowsiness has been reported. If affected, patients should not drive or operate machinery.
4.8 Undesirable Effects
Omeprazole is well tolerated and adverse reactions have generally been mild and reversible. The following have been reported as adverse events in clinical trials or reported from routine use but in many cases a relationship to treatment with omeprazole has not been established.
Skin and subcutaneous tissue disorders
Skin rash, urticaria and pruritus have been reported, usually resolving after discontinuation of treatment. In addition photosensitivity, bullous eruption, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, alopecia and increased sweating have been reported in isolated cases.
Musculoskeletal disorders
Arthritic and myalgic symptoms have been reported and have usually resolved when therapy is stopped.
Respiratory disorders
In isolated cases bronchospasm has been reported.
Gastrointestinal disorders
Diarrhoea has been reported and may be severe enough to require discontinuation of therapy. Constipation, abdominal pain, nausea/vomiting and flatulence have been reported. In isolated cases dry mouth, stomatitis and candidiasis have been reported.
Hepato-biliary disorders
Increases in liver enzyme have been observed. In isolated cases, encephalopathy in patients with pre-existing severe liver disease, hepatitis with or without jaundice and rarely hepatic failure.
Renal & urinary disorders
Interstitial nephritis which has resulted in acute renal failure has been reported in isolated cases.
Reproductive disorders
In isolated cases gynaecomastia and impotence have been reported.
Nervous system disorders
Headache has been reported which may be severe enough to require discontinuation of therapy. Rarely paraesthesia has also been reported. Taste disturbances have been reported in isolated cases.
Psychiatric disorders
In isolated cases reversible mental confusion, agitation, depression and hallucinations occurring predominantly in severely ill patients. Agression has also been reported in isolated cases.
Disorders of the eye
In isolated cases blurred vision has been reported.
Haematological
In isolated cases leucopenia, thrombocytopenia, agranulocytosis, hyponatraemia and pancytopenia have been reported.
Disorders of the ear
Vertigo has been reported.
Disorders of the immune system
Anaphylactic shock and angioedema have been reported in isolated cases.
General disorders
Dizziness, light-headedness and feeling faint have been associated with treatment, but all usually resolve on cessation of therapy. Somnolence and insomnia have also been reported. In isolated cases peripheral oedema, malaise and fever have been reported.
4.9 Overdose
There is no information available on the effects of overdosage in man. Beside ventilatory and circulatory control according to general guidelines on the treatment of intoxication no further direct therapeutic measures are indicated. Single oral doses of omeprazole of up to 400 mg have not resulted in any severe symptoms; elimination remained first order and no specific treatment was needed.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Omeprazole, a substituted benzimidazole, is a selective proton pump inhibitor which inhibits directly and in dose-dependent fashion the H+/K+-ATPase of the parietal cells of the stomach responsible for gastric acid secretion. By this selective intracellular attack, independently from membrane located receptors like histamine H2-, muscarine M1- or gastrineric receptors, omeprazole belongs to an independent class of inhibitors which block the terminal secretion process. By its mode of action, omeprazole reduces not only basal but also stimulus-induced acid secretion, independently of the kind of stimulus. Omeprazole thus increases the pH-value and reduces the secretory volume.
Oral dosing with 20 mg omeprazole once daily produces inhibition of gastric acid secretion within 1-2 hours of the first dose. The maximum effect is achieved within 4 days of starting treatment after which the degree of inhibition remains constant. The mean decrease in pentagastrin-stimulated peak acid output twenty-four hours after dosing is about 70%.
During long-term treatment an increased frequency of gastric glandular cysts have been reported. These changes are a physiological consequence of pronounced inhibition of acid secretion. The cysts are benign and appear to be reversible. No other treatment related mucosal changes have been observed in patients treated continuously with omeprazole for periods of up to 5 years.
Site and Mechanism of Action: Omeprazole is a weak base and is concentrated and converted to the active form by protonation in the acid environment of the intracellular canaliculi within the parietal cell, where it inhibits the enzyme, H+,K+-ATPase - the proton pump. This effect on the final step of the gastric acid formation process is dose-dependent and provides for effective inhibition of both basal acid secretion and stimulated acid secretion irrespective of the stimulus. All pharmacodynamic effects observed are explained by the effect of omeprazole on acid secretion.
5.2 Pharmacokinetic Properties
Absorption of omeprazole takes place in the small intestine and is usually completed within 3-6 hours. The systemic bioavailability of omeprazole from a single oral dose is approximately 35%. After repeated once-daily administration, the bioavailability increases to about 60%. Concomitant intake of food has no influence on bioavailability. The plasma protein binding of omeprazole is about 95%.
The average half-life of the terminal phase of the plasma concentration-time curve is approximately 40 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) but not to actual plasma concentration at a time.
Omeprazole is entirely metabolized, mainly in the liver. Identified metabolites in plasma are the sulphone, the sulphide and hydroxy-omeprazole; these metabolites have no significant effect on acid secretion. About 80% of the metabolites are excreted in the urine and the rest in the faeces. The two main urinary metabolites are hydroxy-omeprazole and the corresponding carboxylic acid.
The systemic bioavailability of omeprazole is not significantly altered 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.
Available data from children (1 year and older) suggest that the pharmacokinetics within the recommended doses is similar to those reported in adults. At steady state, lower plasma levels of omeprazole were seen in some children.
5.3 Preclinical Safety Data
Omeprazole is a well-established drug for which there are adequate published safety data. Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity or toxicity to reproduction.
Carcinogenic Potential: 2 years' carcinogenicity studies in rats (i.e., life-long treatment) showed development of ECL-cell-carcinoids; but rats which have been treated with high doses of omeprazole over a year have not shown any carcinoids in the later 1-year period. The mechanism for the build-up of the stomach carcinoids has been investigated very carefully and various studies lead to the conclusion that this is a secondary reaction due to the extreme increased serum gastrin levels of the rats during the treatment period. These changes are the result of sustained hypergastrinaemia secondary to acid inhibition and not from a direct effect of any individual drug. Similar development of ECL-cell-carcinoids was observed in rats subjected to partial fundectomy. ECL-cell-carcinoids were not seen in mice or dog studies.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Core
lactose monohydrate
sodium starch glycollate
sodium stearate
sodium stearyl fumarate
Enteric Coating
hydroxypropyl methylcellulose (HPMC) acetate succinate
talc
triethyl citrate
monoethanolamine
sodium lauryl sulphate
Sepisperse AP-3527 (containing:
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Polish
carnauba wax
6.2 Incompatibilities
Not applicable.
6.3 Shelf Life
2 years.
6.4 Special Precautions For Storage
Store in the original package. Do not store above 30°C.
6.5 Nature And Contents Of Container
Aluminium/aluminium blisters strips containing 7, 14 or 28 tablets, in a cardboard box.
6.6 Special Precautions For Disposal And Other Handling
Not applicable.
7. Marketing Authorisation Holder
Dexcel-Pharma Limited
7 Sopwith Way, Drayton Fields, Daventry, Northamptonshire NN11 8PB
United Kingdom
8. Marketing Authorisation Number(S)
PL 14017/0069
9. Date Of First Authorisation/Renewal Of The Authorisation
19 January 2004
10. Date Of Revision Of The Text
June 2011
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