COMPOSITION :

Each capsule contains : Esomeprazole Magnesium trihydrate equivalent to Esomeprazole 20 mg, 40 mg (as enteric coated pellets)

DESCRIPTION :

Esoprax (Esomeprazole) is the S-isomer of omeprazole, where it specifically inhibits the enzyme H+/ K+ - ATPase (the acid pump) in the

parietal cell of stomach and hence inhibits both basal and stimulated acid secretion. The absorption of esomeprazole is rapid with peak

plasma levels occurring approximately 1 - 2 hours after dose. Food intake both delays and decreases the absorption of esomeprazole

although this has no significant influence on the effect of esomeprazole on intragastric acidity. Esomeprazole is 97% bound to plasma

protein and metabolized in the liver , 80% of an oral dose is excreted as metabolites in the urine and the remainder in the faeces, less than

1% of the parent drug is found in urine. The elimination half- life is 1.3 hours.

INDICATIONS & DOSAGE :

• Gastroesophageal Reflux Disease (GERD) :

- Treatment of erosive reflux esophagitis : 40 mg once daily for 4 weeks. An additional 4 weeks treatment is recommended for patients in

whom esophagitis has not healed or who have persistent symptoms.

- Long term management of patients with healed esophagitis to prevent relapse : 20 mg once daily.

- Symptomatic treatment of gastroesophageal reflux disease (GERD) : 20 mg once daily in patients without esophagitis . If symptoms

control has not been achieved after four weeks, the patient should be investigated. Once symptoms have resolved, subsequent symptom

control can be achieved using an on demand regimen taking 20 mg once daily when needed.

• In combination with an appropriate antibacterial therapeutic regimen for the eradication of Helicobacter pylori :

Healing of Helicobacter pylori associated duodenal ulcer and prevention of relapse of peptic ulcers in patients with Helicobacter pylori

associated ulcers : 20 mg Esoprax with 1 g amoxicillin and 500 mg clarithromycin all twice daily for 7 days.

• Treatment of Zollinger Ellison syndrome : The recommended initial dose is 40 mg of Esomeprazole twice daily . The maintenance dose

ranges between 80 – 160 mg daily .If the dose is above 80 mg , the dose should be divided and given twice daily.

• Impaired renal function : Dose adjustment is not required, but in patients with severe renal insufficiency, 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.

RESTRICTIONS ON USE :

Contraindications

Known hypersensitivity to Esomeprazole or substituted benzimidazoles.

Precautions

- Caution should be taken in the presence of any symptoms as significant unintentional weight loss, recurrent vomiting, dysphagia,

haematemesis or malaena and when gastric ulcer is suspected or present, malignancy should be excluded as treatment with Esomeprazole

may alleviate symptoms and delay diagnosis.

- Absorption of vitamin B12 may be reduced during treatment with Esomeprazole for long time , so caution should be taken in patients with

reduced body stores of vitamin B12.

- Treatment with Esomeprazole may cause hypomagnesaemia, so monitoring of Magnesium plasma levels should be done before initiating

the treatment or during treatment with Esomeprazole in patients expected to be on prolonged treatment with Esomeprazole ,patients who

are taking Digoxin with Esomeprazole or taking medicines that may cause hypomagnesaemia.

- Caution should be taken in patients at risk of osteoporosis or elderly , taking Esomeprazole for long time or in high doses may increase the

risk of osteoporosis, and they should have an adequate intake of calcium and vitamin D.

Use in pregnancy and lactation

Caution should be excercised when prescribing to pregnant women ,and it should not be used during breast feeding.

DRUG INTERACTIONS :

- The absorption of Ketoconazole and Itraconazole can be decreased during treatment with Esomeprazole.

- The plasma concentration of Tacrolimus , Methotrexate, diazepam, citalopram, imipramine, clomipramine, cisapride and phenytoin may

be increased and a dose reduction could be needed if coadministered with Esomeprazole, whereas the plasma concentration of clopidogrel

is decreased .

- Co- administration with CYP3A4 inhibitors such as clarithromycin increase the plasma concentration of Esomeprazole , whereas

CYP3A4 inducers such as rifampicin decrease its concentration.

- The co-administration of Esomeprazole with atazanavir is not recommended and is contraindicated with nelfinavir.

ADVERSE EFFECTS :

- The most common adverse effects include : Headache, abdominal pain, diarrhoea, flatulence, nausea, vomiting and constipation.

- Uncommon adverse effects include : Dermatitis, pruritus, urticaria, dizziness and dry mouth.

STORAGE INSTRUCTIONS :

- Store below 30°C, in a dry place. Protect from light.

- Close the bottle tightly after each use.

- Discard three months from the date of opening.

PRESENTATIONS :

Esoprax 20 mg capsule : Pack of 14 capsules and pack of 10 strips x 10 capsules.

Esoprax 40 mg capsule : Pack of 14 capsules and pack of 10 strips x 10 capsules.