Each enteric coated tablet contains : Esomeprazole Magnesium Trihydrate equivalent to Esomeprazole 20 mg and 40 mg.
The active ingredient esomeprazole magnesium Trihydrate is bis (5-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl] sulfinyl]-1H-benzimidazote-1-yl) magnesium trihydrate. Esomeprazole is the S-isomer of omeprazole, which is a mixture of the S- and R- isomers. Its molecular formula is (C17H18N3O3S)2Mg x 3 H2O with molecular weight of 767.2 as a trihydrate and 713.1 on an anhydrous basis.
Excipients/Inactive Ingredients: Esomeprazole Tablets 20 mg: Mannitol, Light Magnesium Oxide, Hydroxy Propyl Cellulose (L-Substituted HPC (LH11)), Isopropyl Alcohol, Magnesium Stearate, Purified Talc, Colloidal Anhydrous Silica, Ethyl Cellulose, Hydroxy Propyl Methyl Cellulose (E-15), Macrogol 6000, Titanium Dioxide, Dichloromethane, Acryl Ezee White (93058751) (Purified Talc, Methacrytic Acid Copolymer Type C, Titanium Dioxide, Triethyl Citrate, Colloidal Anhydrous Silica, Sodium Bicarbonate, Sodium Lauryl Sulfate), Iron Oxide Red, Iron Oxide Yellow, Purified Water.
Esomeprazole Tablets 40 mg: Mannitol, Light Magnesium Oxide, Hydroxy Propyl Cellulose (L-Substituted HPC (LH11)), Isopropyl Alcohol, Magnesium Stearate, Purified Talc, Colloidal Anhydrous Silica, Ethyl Cellulose, Hydroxy Propyl Methyl Cellulose (E-15), Macrogol 6000, Titanium Dioxide, Dichloromethane, Acryl Ezee White (93058751) (Purified Talc, Methacrylic Acid Copolymer Type C, Titanium Dioxide, Triethyl Citrate, Colloidal Anhydrous Silica, Sodium Bicarbonate, Sodium Lauryl Sulfate]. Iron Oxide Red & Purified Water.
Pharmacology: Pharmacodynamics: Mechanism of Action: Esomeprazole is a proton pump inhibitor. It is the S-isomer of omeprazole and reduces gastric acid secretion through a specific targeted mechanism of action. It is a specific inhibitor of the acid pump in the parietal cell. Both the R- and S-isomer of omeprazole have similar pharmacodynamic activity.
Esomeprazole is a weak base and is concentrated and converted to the active form, in the highly acidic environment of the secretory canaliculi of the parietal cell, where it inhibits the enzyme H+K+-ATPase - the acid pump and inhibits both basal and stimulated acid secretion.
Pharmacokinetics: Absorption and Distribution: Esomeprazole is acid labile and is administered orally as enteric-coated granules. In vivo conversion to the R-isomer is negligible. Absorption of esomeprazole is rapid, with peak plasma levels occurring approximately 1-2 hours after dose. The absolute bioavailability is 64% after a single dose of 40 mg and increases to 89% after repeated once-daily administration. For 20 mg esomeprazole, the corresponding values are 50% and 68%, respectively. The apparent volume of distribution at steady state in healthy subjects is approximately 0.22 L/kg body weight. Esomeprazole is 97% plasma protein bound.
Food intake both delays and decreases the absorption of esomeprazole although this has no significant influence on the effect of esomeprazole on intragastric acidity.
Metabolism and Excretion: Esomeprazole is completely metabolised by the cytochrome P450 system (CYP). The major part of the metabolism of esomeprazole is dependent on the polymorphic CYP2C19, responsible for the formation of the hydroxy- and desmethyl metabolites of esomeprazole. The remaining part is dependent on another specific isoform, CYP3A4, responsible for the formation of esomeprazole sulphone, the main metabolite in plasma.
The parameters as follows reflect mainly the pharmacokinetics in individuals with a functional CYP2C19 enzyme, extensive metabolisers.
Total plasma clearance is about 17 L/h after a single dose and about 9 L/h after repeated administration. The plasma elimination half-life is about 1.3 hours after repeated once-daily dosing. The pharmacokinetics of esomeprazole has been studied in doses up to 40 mg b.i.d. The area under the plasma concentration time curve increases with repeated administration of esomeprazole. This increase is dose-dependent and results in a more than dose proportional increase in AUC after repeated administration. This time- and dose-dependency is due to a decrease of first pass metabolism and systemic clearance probably caused by an inhibition of the CYP2C19 enzyme by esomeprazole and/or its sulphone metabolite. Esomeprazole is completely eliminated from plasma between doses with no tendency for accumulation during once-daily administration.
The major metabolites of esomeprazole have no effect on gastric acid secretion. Almost 80% of an oral dose of esomeprazole is excreted as metabolites in the urine, the remainder in the faeces. Less than 1% of the parent drug is found in urine.
Esomeprazole tablets are indicated for: Gastro-Oesophageal Reflux Disease (GORD): treatment of erosive reflux oesophagitis; long-term management of patients with healed oesophagitis to prevent relapse; symptomatic treatment of gastro-oesophageal reflux disease (GORD).
In combination with an appropriate antibacterial therapeutic regimen for the eradication of Helicobacter pylori and healing of Helicobacter pylori associated duodenal ulcer and prevention of relapse of peptic ulcers in patients with Helicobacter pylori associated ulcers.
Patients requiring continued NSAID therapy: Healing of gastric ulcers associated with NSAID therapy; Prevention of gastric and duodenal ulcers associated with NSAID therapy, in patients at risk.
Prolonged treatment after IV induced prevention of rebleeding of peptic ulcers.
Treatment of Zollinger Ellison Syndrome.
Adults and adolescents from the age of 12 years: Gastro-Oesophageal Reflux Disease (GORD): treatment of erosive reflux oesophagitis: 40 mg once daily for4 weeks.
An additional 4 weeks treatment is recommended for patients in whom oesophagitis has not healed or who have persistent symptoms.
long-term management of patients with healed oesophagitis to prevent relapse: 20 mg once daily.
symptomatic treatment of gastro-oesophageal reflux disease (GORD): 20 mg once daily in patients without oesophagitis. If symptom control has not been achieved after four weeks, the patient should be further investigated. Once symptoms have resolved, subsequent symptom control can be achieved using 20 mg once daily. In adults, an on demand regimen taking 20 mg once daily, when needed, can be used. In NSAID treated patients at risk of developing gastric and duodenal ulcers, subsequent symptom control using an on demand regimen is not recommended.
Adults: In combination with an appropriate antibacterial therapeutic regimen for the eradication of Helicobacter pylori and healing of Helicobacter pylori associated duodenal ulcer and Prevention of relapse of peptic ulcers in patients with Helicobacter pylori associated ulcers: 20 mg esomeprazole with 1 g amoxicillin and 500 mg clarithromycin, all twice daily for 7 days.
Patients requiring continued NSAID therapy: Healing of gastric ulcers associated with NSAID therapy: The usual dose is 20 mg once daily. The treatment duration is 4-8 weeks.
Prevention of gastric and duodenal ulcers associated with NSAID therapy in patients at risk: 20 mg once daily.
Prolonged treatment after IV induced prevention of rebleeding of peptic ulcers: 40 mg once daily for 4 weeks after IV induced prevention of rebleeding of peptic ulcers.
Treatment of Zollinger Ellison Syndrome: The recommended initial dosage is esomeprazole 40 mg twice daily. The dosage should then be individually adjusted and treatment continues as long as clinically indicated. Based on the clinical data available, the majority of patients can be controlled on doses between 80 and 160 mg esomeprazole daily. With doses above 80 mg daily, the dose should be divided and given twice-daily.
Children below the age of 12 years: Esomeprazole should not be used in children younger than 12 years since no data is available.
Impaired renal function: Dose adjustment is not required in patients with impaired renal function. Due to limited experience in patients with severe renal insufficiency, such patients should be treated with caution.
Impaired hepatic function: Dose adjustment is not required in patients with mild to moderate liver impairment. For patients with severe liver impairment, a maximum dose of 20 mg esomeprazole should not be exceeded.
Elderly: Dose adjustment is not required in the elderly.
There is very limited experience to date with deliberate overdose. The symptoms described in connection with 280 mg were gastrointestinal symptoms and weakness. Single doses of 80 mg esomeprazole were uneventful. No specific antidote is known. Esomeprazole is extensively plasma protein bound and is therefore not readily dialyzable. As in any case of overdose, treatment should be symptomatic and general supportive measures should be utilised.
Esomeprazole is contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted benzimidazoles. Hypersensitivity reactions, e.g., angioedema and anaphylactic shock, have been reported with esomeprazole use.
In the presence of any alarm symptom (e.g. 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 esomeprazole may alleviate symptoms and delay diagnosis.
Patients on long-term treatment (particularly those treated for more than a year) should be kept under regular surveillance.
Patients on on-demand treatment should be instructed to contact their physician if their symptoms change in character. When prescribing esomeprazole for on-demand therapy, the implications for interactions with other pharmaceuticals, due to fluctuating plasma concentrations of esomeprazole should be considered.
When prescribing esomeprazole for eradication of Helicobacter pylori, possible drug interactions for all components in the triple therapy should be considered. Clarithromycin is a potent inhibitor of CYP3A4 and hence contraindications and interactions for clarithromycin should be considered when the triple therapy is used in patients concurrently taking other drugs metabolised via CYP3A4 such as cisapride.
This medicinal product contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
Treatment with proton pump inhibitors may lead to slightly increased risk of gastrointestinal infections such as Salmonella and Campylobacter.
Co-administration of esomeprazole with atazanavir is not recommended. If the combination of atazanavir with a proton pump inhibitor is judged unavoidable, dose clinical monitoring is recommended in combination with an increase in dose of atazanavir to 400 mg with 100 mg of ritonavir, esomeprazole 20 mg should not be exceeded.
Effects on ability to drive and use machines: No effects have been observed.
Esomeprazole, clinical data on exposed pregnancies are insufficient. With the racemic mixture omeprazole, data on a larger number of exposed pregnancies from epidemiological studies indicate no malformative nor foetotoxic effect.
Animal studies with esomeprazole do not indicate direct or indirect harmful effects with respect to embryonal/fetal development: Animal studies with the racemic mixture do not indicate direct or indirect harmful effects with respect to pregnancy, parturition or postnatal development. Caution should be exercised when prescribing to pregnant women. It is not known whether esomeprazole is excreted in human breast milk. No studies in lactating women have been performed. Therefore, Esomeprazole should not be used during breast-feeding.
Nursing Mothers: Esomeprazole has not been adequately studied in nursing women.
Esomeprazole, like other PPIs, is well tolerated. The most common side effects are Headache, abdominal pain, diarrhoea, flatulence, nausea/vomiting, constipation. Nervousness, abnormal heartbeat, muscle pain, weakness, leg cramps and water retention occur infrequently.
The decreased intragastric acidity during treatment with esomeprazole, might increase or decrease the absorption of drugs if the mechanism of absorption is influenced by gastric acidity. In common with the use of other inhibitors of acid secretion or antacids, the absorption of ketoconazole and itraconazole can decrease during treatment with esomeprazole.
Esomeprazole inhibits CYP2C19, the major esomeprazole metabolising enzyme. Thus, when esomeprazole is combined with drugs metabolised by CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin etc., the plasma concentrations of these drugs may be increased and a dose reduction could be needed. This should be considered especially when prescribing esomeprazole for on-demand therapy. It is recommended to monitor the plasma concentrations of phenytoin when treatment with esomeprazole is introduced or withdrawn.
Esomeprazole has been shown to-have no clinically relevant effects on the pharmacokinetics of amoxicillin, quinidine or warfarin.
Store below 30°C in a dry place.
Protect from light and moisture.
A02BC05 - esomeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
EC tab 20 mg x 10 x 10's. 40 mg x 10 x 10's.
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