Indications of Esomep 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 Esomep 20

ACI Limited

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.

Esomeprazole binds to plasma proteins 97 percent of the time. Over a concentration range of 2 20 mmol/L, plasma protein binding remains constant. In healthy volunteers, the apparent volume of distribution at steady state is around 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 creates the hydroxy and desmethyl metabolites, is responsible for the majority of esomeprazole metabolism. The sulphone metabolite is formed by CYP3A4, which is responsible for the remaining proportion.

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 dose of esomeprazole is eliminated in the urine as inactive metabolites, with the remainder detected in the feces as inactive metabolites.

Dosage & Administration

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.

Interaction of Esomep 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.

The principal Esomeprazole metabolizing enzyme, CYP2C19, may be harmed by Esomeprazole. When Esomeprazole 30 mg and diazepam, a CYP2C19 substrate, were given together, diazepam clearance was reduced by 45 percent. Increased diazepam plasma levels have been seen up to 12 hours following dosage. Gastric acid secretion is inhibited by esomeprazole. As a result, Esomeprazole may interfere with the absorption of medications whose bioavailability is influenced by gastrointestinal pH. (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 Esomep 20

Headache, diarrhoea, nausea, flatulence, abdominal pain, constipation, and dry mouth are the most common side effects reported with Esomeprazole. When compared to short-term treatment, there is no difference in the categories of linked adverse events noticed with maintenance treatment up to 12 months.

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: A symptomatic response to esomeprazole medication does not rule out the possibility of gastric cancer.

Esomeprazole pills should be taken at least one hour before meals, according to the manufacturer’s instructions. One tablespoon of applesauce can be put to an empty bowl for patients who have trouble swallowing capsules, and the Esomeprazole capsules can be opened and the pellets carefully spilled into the applesauce. The pellets should be combined with applesauce and quickly eaten. The applesauce should not be too hot, and it should be mushy enough to consume without chewing.

Therapeutic Class

Proton Pump Inhibitor

Storage Conditions

Do not store at temperatures above 30°C. Keep out of children’s reach.

Generic of Esomep 20

Esomeprazole Magnesium Trihydrate