Keep out of reach of children.
Read the directions carefully before use.
For prescription only.
QUALITATIVE AND QUANTITATIVE COMPOSITION:
Active ingredient:
Esomeprazole (as gastro-resistant pellets containing esomeprazole magnesium trihydrate) ......................................................... 40 mg
Excipients: q.s ……………………………. 1 tablet
Gastro-resistant hard capsule.
Product description: A hard, purple capsule containing off-white, gastro-resistant pellets.
Box of 2 blisters x 10 capsules.
Box of 3 blisters x 10 capsules.
Esomeprazole 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. 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.
Absorption of esomeprazole is rapid, with peak plasma levels occurring approximately 1-2 hours after dose. The bioavailability increases proportionally when the dose is increased. At repeated once-daily dosing with 40 mg, the systemic bioavailability is approximately 89% compared to 68% after a single dose of 20 mg. Esomeprazole absorption is delayed and decreased by food. The AUC after administration of a single 40 mg dose of esomeprazole is decreased by 43% to 53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.
Esomeprazole is 97% plasma protein bound. Esomeprazole is extensively metabolised by the cytochrome P450 system, CYP2C19 isoenzyme, responsible for the formation of the inactive hydroxy- and desmethyl metabolites. The remaining part is metabolized through CYP3A4, responsible for the formation of esomeprazole sulphone.
The plasma elimination half-life is about 1.3 hours. Almost 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, the remainder in the faeces. In patients with severe hepatic insufficiency the AUCs were 2 to 3 times higher than in the patients with normal liver function. Reduction of esomeprazole dosage should be considered in such patients.
Caution should be taken in those who are operating machinery, driving, working at height, and other cases because the drug is likely to cause vertigo, dizziness.
The drug does not affect pregnant women and nursing mothers. However, as other drugs, caution should be exercised when using the drug for these objects.
Gastric acid suppression during treatment with esomeprazole might increase gastric pH, which affects the bioavailability of pH-dependent drugs, including ketoconazole, itraconazole, erlotinib, iron salts, digoxin.
Esomeprazole inhibits CYP2C19, the major esomeprazole metabolising enzyme. Thus, when esomeprazole is combined with active substances metabolised by CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin etc., the plasma concentrations of these active substances may be increased and a dose reduction could be needed.
Esomeprazole is metabolised by CYP2C19 and CYP3A4. Concomitant administration of esomeprazole and a CYP3A4 inhibitor, clarithromycin (500 mg b.i.d.), resulted in a doubling of the exposure (AUC) to esomeprazole. Concomitant administration of esomeprazole and a combined inhibitor of CYP2C19 and CYP3A4 may result in more than doubling of the esomeprazole exposure. The CYP2C19, CYP3A4 inhibitors and voriconazole increased omeprazole AUC by 280%. A dose adjustment of esomeprazole is not regularly required in either of these situations. However, dose adjustment should be considered in patients with severe hepatic impairment and if long-term treatment is indicated.
Common, ADR > 1/100
Systemic disorders: headache, dizziness, skin rash.
GI disorders: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, dry mouth.
Uncommon, 1/1000 < ADR < 1/100
Systemic disorders: fatigue, insomnia, drowsiness, rash, pruritis, paraesthesia
Eye disorders.
Rare, ADR < 1/1000
Systemic disorders: fever, sweating, peripheral oedema, photosensitivity, hypersensitivity reactions (including urticaria, angioedema, bronchospasm, anaphylactic shock).
CNS disorders: agitation, depression, reversible confusion, hallucinations.
Blood disorders: pancytopenia, leucocytosis, leucopenia, thrombocytopenia.
Liver disorders: increased liver enzymes, hepatitis, jaundice, liver failure.
GI disorders: taste disorders, stomatitis.
Metabolic disorders: hypomagnesemia, hyponatremia, porphyria.
Musculoskeletal disorders: arthralgia, myalgia, osteoporosis, fractures.
Urinary disorders: interstitial nephritis.
Endocrine disorders: gynaecomastia.
Skin disorders: bullous rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, dermatitis.
Decreased gastric acidity due to any means including proton pump inhibitors, increases gastric counts of bacteria normally present in the gastrointestinal tract.
Please inform your doctor of all undesirable effects upon drug administration.
Treatment of ADRs:
The drug should be discontinued if severe adverse effects occur.
OVERDOSE:
Symptoms: 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.
Management: 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.
Symptoms: 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.
Management: 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.
Store in dry places, not exceeding 30°C, protect from light.
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.
Treatment with proton pump inhibitors may lead to slightly increased risk of gastrointestinal infections such as Salmonella and Campylobacter.
Peptic ulcer.
Prevention and treatment of peptic ulcer associated with NSAID therapy.
Prevention and treatment of stress-induced ulcers.
Gastroesophageal reflux disease.
Zollinger-Ellison syndrome.
Bleeding from severe peptic ulcer after endoscopic therapy (prevention of rebleeding of peptic ulcer)
Hypersensitivity to esomeprazole, substituted benzimidazoles or to any of the excipients.
Esomeprazole should not be used concomitantly with nelfinavir.
The drug should be taken at least 1 hour before a meal and concurrently given with an antacid to relieve pains if necessary.
Adult dosage:
- Healing of Helicobacter pylori associated peptic ulcer:
The recommended oral dosage is 20 mg twice daily for 7 days or 40 mg once daily for 10 days.
- Healing of gastric ulcers associated with NSAID therapy or prevention of stress-induced ulcers: The recommended oral dosage of 20 mg once daily for 4-8 days.
- Treatment of erosive esophagitis associated gastroesophageal reflux disease:
The recommended oral dosage of esomeprazole is 40 mg once daily for 4 weeks. An additional 4-week course of treatment may be considered if needed.
Or the recommended oral dosage is 20 - 40 mg once daily for 4-8 weeks. An additional 4- to 8-week course of treatment is recommended for patients in whom esophagitis has not healed.
- For maintenance therapy following healing of erosive esophagitis or for treatment of symptomatic GERD in patients without erosive esophagitis, the recommended oral dosage is 20 mg once daily.
- Treatment of Zollinger-Ellison syndrome:
The recommended initial dosage is 40 mg twice daily.
The recommended control dose is 80 mg once to twice daily or 120 mg twice daily.
Pediatric dosage:
- Gastroesophageal reflux disease:
Children 1-11 years of age weighing 10 kg and more: oral dose of 10 mg once daily for 8 weeks.
- Erosive esophagitis: The dosage is based on body weight:
10 - 20 kg: oral dose 10 mg once daily for 8 weeks;
≥ 20 kg: oral dose of 10-20 mg once daily for 8 weeks;
Children ≥ 12 years of age: as adult dose.
Patients with impaired hepatic function:
- Mild and moderate hepatic impairment: No dosage adjustment.
- Severe hepatic impairment: maximum of 20 mg daily.
Patients with impaired renal function and elderly: Dose adjustment is not required.
Note:
- With dosage of 20 mg and 10 mg: It is recommended to switch to another suitable product.
Or as directed by the physician.
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