Exium is indicated:

• To relieve from chronic heartburn symptoms and other symptoms associated with GERD
• For the healing of erosive esophagitis
• For maintenance of healing of erosive esophagitis
• In combination with amoxicillin and clarithromycin for eradication of Helicobacter pylori infection in patients with duodenal ulcer disease.
• Zollinger-Ellison Syndrome
• Acid related Dyspepsia
• Duodenal & Gastric ulcer

Oral dosage form-

• Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The majority of patients are healed within 4 to 8 weeks. For patients who don’t heal after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. Maintenance of Healing of Erosive
• Esophagitis: 20 mg Once Daily (Clinical studies did not extend 6 months).
• Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
• Helicobacter Pylori eradication: Triple Therapy to reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg Twice Daily for 10 days.
• Zollinger-Ellison Syndrome: The dose is 20-80 mg once daily. The dosage should be adjusted individually and treatment continued as long as clinically indicated.
• Acid-related Dyspepsia: 20-40 mg once daily for 2-4 weeks according to the response.
• Duodenal ulcer: 20 mg once daily for 2-4 weeks. Gastric ulcer: 20-40 mg once daily for 4-8 weeks.

IV Injection or IV infusion:

GERD with Erosive Esophagitis–
Adult Patients (≥18 years):

• 20 mg or 40 mg once daily
• IV Injection: >3 Minutes, IV Infusion: 10-30 minutes

Pediatric Patients (1 year to 17 years)

• Body weight <55 kg: 10 mg Once daily
• Body Weight ≥55 kg: 20 once daily
• 1 month to <1 year: 0.5 mg/kg once daily
• IV Infusion: 10-30 minutes

Risk reduction of rebleeding of Gastric or Duodenal Ulcers following therapeutic endoscopy in adults–
Adult Patients (≥18 years)

• 80 mg
• IV Infusion: 30 minutes, followed by a continuous infusion of 8 mg/h for a total treatment duration of 72 hours.

Tablet or capsule: should be swallowed whole and taken one hour before a meal.

Oral Suspension: Whole contents of the packet should be taken into a small glass containing 15 ml. of water. The mixer should be stirred well and leave 2 to 3 minutes to thicken. Stir again and drink within 30 minutes. If any medicine remains after drinking, add more water, stir, and drink immediately. If the suspension is to be administered through a nasogastric or gastric tube, the volume of water in the syringe should be 15 ml. & immediately shake the syringe and leave 2 to 3 minutes to thicken. Shake the syringe and inject it through the nasogastric or gastric tube into the stomach within 30 minutes. An appropriately sized syringe should be used. Shake and flush any remaining contents from the nasogastric or gastric tube into the stomach.

IV Injection: Solution for injection is prepared by adding 5 ml of 0.9% Sodium Chloride for intravenous injection into the vial containing the dry powder. The reconstituted solution for injection is clear and colorless to very slightly yellow. IV injection must be administrated intravenously over a period of at least 3 minutes. Prepared solution must be used within 12 hours of preparation and can be exposed to normal indoor lighting at a maximum of 30°C.

Exium is extensively metabolized in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that Exium is not likely to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with drugs metabolized by these CYP enzymes would be expected. Drug interaction studies have shown that Exium does not have any clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.

Exium may potentially interfere with CYP2C19, the major Exium metabolizing enzyme. Co-administration of Exium 30 mg and diazepam, a CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam. Increased plasma levels of diazepam have been observed 12 hours after dosing and onwards. Exium inhibits gastric acid secretion. Therefore, Exium may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).

Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do not seem to change the pharmacokinetic profile of Exium.

Combination Therapy with Clarithromycin: Co-administration of Exium, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of Exium and 14-hydroxyclarithromycin.

Esomeprazole is contraindicated in-patient with known hypersensitivity to any of the formulation.

The most frequently occurring adverse events reported with Exium include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth. There are no difference in types of related adverse events seen during maintenance treatment upto 12 months compared to short term treatment.

There are no adequate and well-controlled studies in pregnant women. Animal studies have revealed no teratogenic effects. The excretion of esomeprazole in milk has not been studied. Breast-feeding should be therefore be discontinued if the use of esomeprazole is considered essential.

General: Symptomatic response to therapy with Exium does not preclude the presence of gastric malignancy.

Information for patients: Exium capsules should be taken at least one hour before meals. For patients who have difficulty swallowing capsules, one tablespoon of applesauce can be added to an empty bowl and the Exium capsules can be opened, and the pellets inside the capsule carefully emptied onto the applesauce. The pellets should be mixed with the applesauce and then swallowed immediately. The applesauce used should not be hot and should be soft enough to be swallowed without chewing. The pellets should not be chewed or crushed. The pellet/applesauce mixture should not be stored for future use. Antacids may be used while taking Exium.

Paediatric Use: Safety and effectiveness in paediatric patients have not been established.

Geriatric Use: No overall differences in safety and efficacy have been observed between the elderly and younger individuals, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out

Hepatic Insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency, a dose of 20 mg once daily should not be exceeded.

Renal Insufficiency: The Pharmacokinetics of Exium in patients with renal impairment are not expected to be altered relative to healthy volunteers as less than 1% of Exium is excreted unchanged in the urine.

A single oral dose of Exium at 510 mg/kg (about 103 times the human dose on a body surface area basis), has been lethal to rats. The major signs of acute toxicity are reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions. There have been no reports of overdose with Exium. No specific antidote for Exium is known. Since Exium is extensively protein bound, it is not expected to be removed by dialysis. In the event of overdosage, treatment should be symptomatic and supportive. As with the management of any overdose, the possibility of multiple drug ingestion should be considered.

Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture. Keep out of reach of children.

Molecular Formula :	C17H19N3O3S
Chemical Structure :