iMax 20Capsule

Indications of iMax 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 iMax 20

Delta Pharma Ltd.

Pharmacology

Esomeprazole is a proton pump inhibitor that inhibits gastric acid secretion by specifically inhibiting ATPase H + / K + in gastric parietal cells. Esomeprazole (omeprazole isomer) is the first unique optical isomer of proton pump inhibitors, which provides better acid control than racemic proton pump inhibitors.

Absorption: Esomeprazole capsules contain enteric-coated granules of esomeprazole magnesium. After oral administration, the peak plasma level (Cmax) appears at approximately 1.5 hours (Tmax). As the dose increased, Cmax increased proportionally, and the area under the plasma concentration-time curve (AUC) increased from 20 mg to 40 mg. With repeated administration once a day, the systemic bioavailability is approximately 90%, compared to 64% for a single administration. Compared with fasting conditions, AUC after a single dose of esomeprazole reduced food intake by 3353b. Esomeprazole should be taken at least one hour before meals.

Distribution: The binding rate of esomeprazole to plasma protein is 97%. The binding to plasma proteins is constant within the concentration range of 20 mmol/L. The steady state apparent volume of distribution of healthy volunteers is approximately 16 L.

Metabolism: Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. Esomeprazole metabolites lack antisecretory activity. The main part of the metabolism of esomeprazole is dependent on the CYP2C19 isoenzyme which forms the hydroxyl and demethylated metabolites. The remaining amount depends on CYP3A4 which forms the sulfone metabolite.

Excretion: The plasma elimination half-life of esomeprazole is about 1 to 1.5 hours. Less than 1% of the parent drug is excreted in the urine. Approximately 80% of the oral dose of esomeprazole is excreted in the urine as inactive metabolites, and the rest is in the feces as inactive metabolites.

Antimicrobial combination therapy: esomeprazole magnesium 40 mg once a day, clarithromycin 500 mg twice a day, and amoxicillin 1000 mg twice a day for 7 days. Compared with esomeprazole treatment alone, the average steady-state AUC and Cmax of esomeprazole during the triple therapy period increased by 70% and 18%, respectively. The pharmacokinetic parameters of clarithromycin and amoxicillin were similar during triple therapy and during the administration of each drug alone. However, compared to treatment with clarithromycin alone, the mean AUC and C of 14-hydroxy clarithromycin increased by 19% and 22%, respectively, during the triple treatment period. This increased exposure to 14-hydroxy clarithromycin is considered to be of no clinical significance.

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.

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.

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 iMax 20

Esomeprazole is extensively metabolised in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that esomeprazole is unlikely to inhibit CYP 1A2, 2A6, 2C9, 2D6, 2E1, and 3A4. Clinically relevant interactions with drugs metabolized by these CYP enzymes are not expected. Drug interaction studies have shown that esomeprazole has no clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin, or amoxicillin.

Esomeprazole may interfere with CYP2C19, the main enzyme that metabolizes esomeprazole. Coadministration of esomeprazole 30 mg and diazepam (a CYP2C19 substrate) resulted in a 45% increase in diazepam clearance. An increase in the plasma concentration of diazepam was observed 12 hours after administration and thereafter. Esomeprazole inhibits gastric acid secretion. Therefore, esomeprazole may interfere with drug absorption, where gastric pH is an important determinant of bioavailability (eg, ketoconazole, iron salts, and digoxin).

Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine does not appear to change the pharmacokinetic characteristics of esomeprazole.

Clarithromycin combination therapy: Co-administration of esomeprazole, clarithromycin, and amoxicillin resulted in increased plasma levels of esomeprazole and 14-hydroxylamithromycin.

Contraindications

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

Side Effects of iMax 20

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

Pregnancy & Lactation

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

Precautions & Warnings

Esomeprazole is extensively metabolised in the liver by CYP2C19 and CYP3A4. In vitro and in vivo studies have shown that esomeprazole is unlikely to inhibit CYP 1A2, 2A6, 2C9, 2D6, 2E1, and 3A4. Clinically relevant interactions with drugs metabolized by these CYP enzymes are not expected. Drug interaction studies have shown that esomeprazole has no clinically significant interactions with phenytoin, warfarin, quinidine, clarithromycin, or amoxicillin.

Esomeprazole may interfere with CYP2C19, the main enzyme that metabolizes esomeprazole. Coadministration of esomeprazole 30 mg and diazepam (a CYP2C19 substrate) resulted in a 45% increase in diazepam clearance. An increase in the plasma concentration of diazepam was observed 12 hours after administration and thereafter. Esomeprazole inhibits gastric acid secretion. Therefore, esomeprazole may interfere with drug absorption, where gastric pH is an important determinant of bioavailability (eg, ketoconazole, iron salts, and digoxin).

Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine does not appear to change the pharmacokinetic characteristics of esomeprazole.

 Clarithromycin combination therapy: Co-administration of esomeprazole, clarithromycin, and amoxicillin resulted in increased plasma levels of esomeprazole and 14-hydroxylamithromycin.

Therapeutic Class

Proton Pump Inhibitor

Storage Conditions

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

Generic of iMax 20

Esomeprazole Magnesium Trihydrate