E-Proton 40 mg Capsule (Enteric Coated Pellets)

Uses

E-Proton 40 mg Capsule (Enteric Coated Pellets) is used for:

• Treatment of Gastroesophageal Reflux Disease (GERD)
• Healing of Erosive Esophagitis
• Maintenance of Healing of Erosive Esophagitis
• Symptomatic Gastroesophageal Reflux Disease
• H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence
• Zollinger-Ellison Syndrome
• Acid Related Dyspepsia
• Duodenal and Gastric Ulcer

E-Proton 40 mg Capsule (Enteric Coated Pellets) is also used to associated treatment for these conditions: Duodenal Ulcer, Erosive Esophagitis, Gastro-esophageal Reflux Disease (GERD), Heartburn, Helicobacter Pylori Infection, NSAID Associated Gastric Ulcers, Stress Ulcers, Upper Gastrointestinal Hemorrhage, Zollinger-Ellison Syndrome, Acute benign gastric ulcers, Maintenance of healing Erosive esophagitis, Postendoscopy Bleeding

How E-Proton 40 mg Capsule (Enteric Coated Pellets) works

E-Proton 40 mg Capsule (Enteric Coated Pellets) exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect that persists longer than 24 hours.

Dosage

E-Proton 40 mg Capsule (Enteric Coated Pellets) dosage

Tablet:

Healing of erosive esophagitis: 20 mg or 40 mg once daily for 4 to 8 Weeks. For those patients who have not healed after 4-8 weeks of treatment, an additional 4-8 weeks course of E-Proton 40 mg Capsule (Enteric Coated Pellets) may be considered.

Long-term management of esophagitis: 20 mg once daily.

Symptomatic gastroesophageal reflux disease: 20 mg once daily for 4 weeks.

H. pylori eradication for treatment of duodenal ulcer:

Triple therapy: 20 mg E-Proton 40 mg Capsule (Enteric Coated Pellets) once daily with 500 mg Clarithromycin twice daily, and 1 g Amoxicillin twice daily for 7-10 days.

Injection:

The recommended adult dose in GERD with Erosive Esophagitis is either 20 or 40 mg E-Proton 40 mg Capsule (Enteric Coated Pellets) given once daily by intravenous injection (no less than 3 minutes) or intravenous infusion (10 to 30 minutes). Pediatric dose (1 to 11 years old):

• Short term treatment of symptomatic GERD: 10 mg once daily for up to 8 weeks.

Healing of erosive esophagitis:

• Weight <20 kg: 10 mg once daily for up to 8 weeks.
• Weight ≥20 kg: 10 mg or 20 mg once daily forup to 8 weeks.

Directions for reconstitution of solution: 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.

Preparations for Use and Administration of E-Proton 40 mg Capsule (Enteric Coated Pellets) 40 IV Injection: A solution for intravenous infusion is prepared by first reconstituting the contents of one vial with 5 ml of 0.9% Sodium Chloride and further diluting the resulting solution to a final volume of 50 ml. The resultant concentration after diluting to a final volume of 50 ml is 0.8 mg/ml.

• 20 mg dose: Withdraw 25 ml of the final solution and administer as an intravenous infusion over 10 minutes to 30 minutes.
• 10 mg dose: Withdraw 12.5 ml of the final solution and administer as an intravenous infusion over 10 minutes to 30 minutes.

Side Effects

In general, esomeprazole is well tolerated in both short and long term use. Adverse events reported with esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth.

Toxicity

Blurred vision, confusion, drowsiness, dry mouth, flushing headache, nausea, rapid heartbeat, sweating

Precaution

Symptomatic response to therapy with E-Proton 40 mg Capsule (Enteric Coated Pellets) does not preclude the presence of gastric malignancy. Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long-term with omeprazole, of which E-Proton 40 mg Capsule (Enteric Coated Pellets) is an enantiomer.

Interaction

Drug interaction studies have shown that Esomeparzole does not have any clinically significant interactions with Phenytoin, Warfarin, Quinidine, Clarithromycin or Amoxicillin. E-Proton 40 mg Capsule (Enteric Coated Pellets) inhibits gastric acid secretion. Therefore, E-Proton 40 mg Capsule (Enteric Coated Pellets) may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg, Ketoconazole, Iron salts and Dogoxin). Coadministration of oral contraceptives, Diazepam, Phenytoin or Quinidine did not seem to change the pharmacokinetic profile of E-Proton 40 mg Capsule (Enteric Coated Pellets).

Food Interaction

• Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

[Moderate] ADJUST DOSING INTERVAL: Food may interfere with the absorption of esomeprazole.

The manufacturer reports that the area under the concentration-time curve for esomeprazole following a single 40 mg dose was 33% to 53% lower when administered after food intake as opposed to during fasting conditions.

MANAGEMENT: E-Proton 40 mg Capsule (Enteric Coated Pellets) should be taken at least one hour before meals.

When administered to patients receiving continuous enteral nutrition, some experts recommend that the tube feeding should be interrupted for at least 1 hour before and 1 hour after the dose of esomeprazole is given.

E-Proton 40 mg Capsule (Enteric Coated Pellets) Drug Interaction

Moderate: levothyroxine, levothyroxineMinor: aspirin, aspirin, aspirin, aspirin, cyanocobalamin, cyanocobalaminUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, metoprolol, metoprolol, acetaminophen, acetaminophen, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

E-Proton 40 mg Capsule (Enteric Coated Pellets) Disease Interaction

Major: C. diffModerate: liver disease, bone fractures, hypomagnesemia

Volume of Distribution

The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.

Elimination Route

After oral administration, peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once-daily dosing with 40 mg, the systemic bioavailability is approximately 90% compared to 64% after a single dose of 40 mg. The mean exposure (AUC) to esomeprazole increases from 4.32 μmolhr/L on Day 1 to 11.2 μmolhr/L on Day 5 after 40 mg once daily dosing. The AUC after administration of a single 40 mg dose of E-Proton 40 mg Capsule (Enteric Coated Pellets) is decreased by 43% to 53% after food intake compared to fasting conditions. E-Proton 40 mg Capsule (Enteric Coated Pellets) should be taken at least one hour before meals.

Combination Therapy with Antimicrobials:

E-Proton 40 mg Capsule (Enteric Coated Pellets) magnesium 40 mg once daily was given in combination with Clarithromycin 500 mg twice daily and Amoxicillin 1000 mg twice daily for 7 days to 17 healthy male and female subjects. The mean steady state AUC and Cmax of esomeprazole increased by 70% and 18%, respectively during triple combination therapy compared to treatment with esomeprazole alone. The observed increase in esomeprazole exposure during co-administration with clarithromycin and amoxicillin is not expected to produce significant safety concerns.

Half Life

1-1.5 hours

Elimination Route

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

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies on the use of E-Proton 40 mg Capsule (Enteric Coated Pellets) in pregnant women. Therapeutic doses during pregnancy are unlikely to pose a substantial teratogenic risk. E-Proton 40 mg Capsule (Enteric Coated Pellets) should be used during pregnancy only if the potential benefit to pregnant women justifies the potential risk to the fetus.

Lactation: E-Proton 40 mg Capsule (Enteric Coated Pellets) is excreted in human milk. Thus, a decision should be taken to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

E-Proton 40 mg Capsule (Enteric Coated Pellets) is contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted Benzimidazoles.

Special Warning

Geriatric: Dosage adjustment is not necessary.

Pediatric: Safety and effectiveness in pediatric patients have not been established.

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: Dosage adjustment is not necessary.

Acute Overdose

There is no experience to data with deliverate overdose. Data are limited but single doses of 80 mg E-Proton 40 mg Capsule (Enteric Coated Pellets) were uneventful. E-Proton 40 mg Capsule (Enteric Coated Pellets) is extensively plasma protein bound and is therefore not readily dialyzable. As in any case of overdose, treatment should be symptomatic and general supportive measures should be utilised.

Storage Condition

Store between 15-30°C. Protect from light.

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