Indications of Opton 20

Esomeprazole 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

Pharmaceutical Name of Opton 20

Beximco Pharmaceuticals Ltd.

Pharmacology

Esomeprazole is a proton pump inhibitor that inhibits the H+/K+-ATPase in the gastric parietal cell, suppressing gastric acid output. The first single optical isomer of a proton pump inhibitor, esomeprazole (S-isomer of omeprazole), provides superior acid control than racemic proton pump inhibitors.

Esomeprazole capsules contain an enteric-coated pellet version of esomeprazole magnesium for improved absorption. Peak plasma levels (Cmax) occur roughly 1.5 hours after oral dosing (Tmax). When the dose is increased, the Cmax increases correspondingly, and the area under the plasma concentration-time curve (AUC) increases thrice from 20 to 40 mg. The systemic bioavailability with repeated once-daily doses is around 90%, compared to 64% after a single dose. When compared to fasting conditions, the AUC following a single dosage of esomeprazole is reduced by 33-53 percent after food ingestion. At least one hour before meals, esomeprazole should be consumed.

Dosage

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.

Injection: The recommended adult dose is 40 mg Esomeprazole given once daily by intravenous injection (not less than 3 minutes) or intravenous infusion (10 to 30 minutes). Esomeprazole IV injection should not be administered concomitantly with any other medications through the same intravenous site. Treatment with Esomeprazole IV injection should be discontinued as soon as the patient is able to resume treatment with Esomeprazole delayed-release capsules. Safety and effectiveness in paediatric patients have not been established.

Administration

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

Direction for use of Delayed-Release 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.

Esomeprazole IV Injection: Esomeprazole IV should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 5 ml of the solvent (WFI) provided. After reconstitution, the injection should be given slowly over a period of at least 3 minutes. The solution should be used within 12 hours of reconstitution when stored at room temperature up to 30°C. No refrigeration is required. The reconstituted solution should not be used if it contains visible particulate.

Interaction of Opton 20

CYP2C19 and CYP3A4 substantially metabolize esomeprazole in the liver. Esomeprazole does not appear to inhibit CYPs 1A2, 2A6, 2C9, 2D6, 2E1, or 3A4 in vitro or in vivo investigations. There should be no clinically significant interactions with medicines processed by these CYP enzymes. Esomeprazole has no clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin, or amoxicillin, according to drug interaction studies.

Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole metabolizing enzyme. Co-administration of Esomeprazole 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. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).

Contraindications

In patients who have a history of hypersensitivity to any of the formulations, esomeprazole is not recommended.

Side Effects of Opton 20

The most frequently occurring adverse events reported with Esomeprazole 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.

Pregnancy & Lactation

In pregnant women, there are no sufficient and well-controlled trials. No teratogenic effects have been found in animal investigations. Esomeprazole excretion in milk has not been studied. If the use of esomeprazole is thought necessary, breastfeeding should be terminated.

Precautions & Warnings

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

Information for patients: Esomeprazole 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 Esomeprazole 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 esomeprazole.

Therapeutic Class

Proton Pump Inhibitor

Storage Conditions

Store in a dry area at a temperature of not more than 30°C. Light and dampness should be avoided. Keep out of children’s reach.

Generic of Opton 20

Esomeprazole Magnesium Trihydrate