Indications of Esotac 40

Esomeprazole is prescribed for the following conditions:

• 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 Esotac 40

Navana Pharmaceuticals Ltd.

Pharmacology

Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole (S-isomer of omeprazole) is the first single optical isomer of proton pump inhibitor, provides better acid control than racemic proton pump inhibitors.

Esomeprazole capsules include an enteric-coated pellet version of esomeprazole magnesium for improved absorption. Peak plasma levels (Cmax) occur around 1.5 hours after oral dosing (Tmax). When the dosage is increased, the Cmax increases proportionately, and the area under the plasma concentration-time curve (AUC) increases thrice from 20 to 40 mg. The systemic bioavailability with repeated once-daily dosage is around 90%, compared to 64% after a single dose. When compared to fasting circumstances, 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.

Distribution: Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 20 mmol/L. The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.

Esomeprazole is extensively processed by the cytochrome P450 (CYP) enzyme system in the liver. Esomeprazole’s metabolites have no anti-secretory properties. The CYP2C19 isoenzyme, which generates the hydroxy and desmethyl metabolites, is responsible for the majority of esomeprazole metabolism.

Esomeprazole has a plasma elimination half-life of approximately 1–1.5 hours. In the urine, less than 1% of the parent medication is eliminated. Approximately 80% of an oral dosage of esomeprazole is eliminated in the urine as inactive metabolites, with the remaining detected in the feces as inactive metabolites.

Antimicrobial Conjunction Therapy: Esomeprazole magnesium 40 mg once day is administered for 7 days in combination with clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily. When compared to treatment with Esomeprazole alone, the mean steady-state AUC and Cmax of Esomeprazole rose by 70% and 18%, respectively, during triple combination therapy. When compared to treatment with clarithromycin alone, the mean AUC and Cmax for 14-hydroxyclarithromycin are raised by 19% and 22%, respectively, following triple combination therapy. This rise in 14-hydroxyclarithromycin exposure is not thought to be clinically meaningful.

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 Esotac 40

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.

Increased diazepam plasma levels have been reported up to 12 hours following treatment. Gastric acid secretion is inhibited by esomeprazole. As a result, Esomeprazole may interfere with the absorption of medicines whose bioavailability is influenced by stomach pH. (e.g., ketoconazole, iron salts and digoxin).

Oral contraceptives, diazepam, phenytoin, or quinidine appear to have no effect on Esomeprazole’s pharmacokinetic profile.

Clarithromycin in Combination Therapy: When esomeprazole, clarithromycin, and amoxicillin are given together, the plasma levels of esomeprazole and 14-hydroxyclarithromycin rise.

Contraindications

It is contraindicated in patients with known hypersensitivity to Esomeprazole or t0 substituted benzimidazoles

Side Effects of Esotac 40

The safety of Esomeprazole was evaluated worldwide in over 10000 patients (aged l8-84 years). ln clinical trialsthemost frequently occurring adverse events were headache, diarrhoea, nausea, flatulence, abdominal pain andconstipation. Rareiy dermatitis, pruritis, urticaria, dizziness and dry mouth reported.

Pregnancy & Lactation

Pregnancy FDA  approved pregnancy category B.Nursing molhetsThere are no data on the excretion of Esomeprazole into human milk’

Precautions & Warnings

General: The existence of stomach cancer does not prevent symptomatic response to esomeprazole treatment.

Esomeprazole pills should be taken at least one hour before meals, according to the manufacturer’s instructions. One spoonful of applesauce can be poured to an empty bowl for patients who have trouble swallowing capsules, and the Esomeprazole capsules can be opened and the pellets carefully placed over the applesauce.

Therapeutic Class

Proton Pump Inhibitor

Storage Conditions

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

Generic of Esotac 40

Esomeprazole Magnesium Trihydrate