Esomeprazole

Esomeprazole Uses, Dosage, Side Effects, Food Interaction and all others data.

Esomeprazole is a PPI that suppresses gastric acid secretion by inhibiting H+/K+ ATPase in the gastric parietal cell. It is the S-isomer of omeprazole.

Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase at the secretory surface of the gastric parietal cell. By doing so, it inhibits acid secretion into the gsatric lumen. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.

Esomeprazole is the s-isomer of Omeprazole, which is a racemate of the S- and R-enantiomer. Esomeprazole has been shown to inhibit acid secretion to a similar extent as Omeprazole, without any significant differences between the two compounds in vitro.

PPIs such as esomeprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes.

Trade Name Esomeprazole
Availability Rx and/or OTC
Generic Esomeprazole
Esomeprazole Other Names (S)-omeprazole, Esomeprazol, Ésoméprazole, Esomeprazole, Esomeprazolum, Perprazole
Related Drugs amoxicillin, omeprazole, famotidine, pantoprazole, metronidazole, Nexium, Pepcid, Protonix, sucralfate, Prilosec
Weight 20mg, 40mg, 49.3mg, 10mg, 2.5mg, 5mg,
Type Oral Delayed Release Capsule, Oral Delayed Release Tablet, Oral Powder For Reconstitution, Delayed Release, Intravenous Powder For Injection, Injection, Capsule, Tablet
Formula C17H19N3O3S
Weight Average: 345.416
Monoisotopic: 345.114712179
Protein binding

Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 to 20 µmol/L.

Groups Approved, Investigational
Therapeutic Class Proton Pump Inhibitor
Manufacturer Mylan, Etercon Pharma, Ecomed Pharm Ltd, Ecomed Pharma Limited
Available Country United Kingdom, United States, Indonesia, Nigeria
Last Updated: September 19, 2023 at 7:00 am
Esomeprazole
Esomeprazole

Uses

Esomeprazole 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

Esomeprazole 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 Esomeprazole works

Esomeprazole 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

Esomeprazole 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 Esomeprazole 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 Esomeprazole 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 Esomeprazole 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 for up 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 Esomeprazole 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 Esomeprazole 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 Esomeprazole 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. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole 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 Esomeprazole.

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: Esomeprazole 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.

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 Esomeprazole is decreased by 43% to 53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.

Combination Therapy with Antimicrobials:

Esomeprazole 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 Esomeprazole in pregnant women. Therapeutic doses during pregnancy are unlikely to pose a substantial teratogenic risk. Esomeprazole should be used during pregnancy only if the potential benefit to pregnant women justifies the potential risk to the fetus.

Lactation: Esomeprazole 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

Esomeprazole 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 Esomeprazole were uneventful. Esomeprazole 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.

Innovators Monograph

You find simplified version here Esomeprazole

FAQ

What is Esomeprazole good for?

Esomeprazole reduces the amount of acid your stomach makes. It's used for heartburn, acid reflux and gastro-oesophageal reflux disease (GORD) - GORD is when you keep getting acid reflux. It's also taken to prevent and treat stomach ulcers.

What are the side effects of Esomeprazole?

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

  • Incidence not known
  • Blistering, peeling, or loosening of the skin
  • bloating
  • chills
  • constipation
  • cough
  • darkened urine
  • difficulty with swallowing
  • dizziness
  • drowsiness
  • fast heartbeat
  • fever
  • indigestion
  • joint or muscle pain
  • loss of appetite
  • mood or mental changes
  • muscle spasms (tetany) or twitching
  • nausea
  • pains in the stomach, side, or abdomen, possibly radiating to the back
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • red skin lesions, often with a purple center
  • red, irritated eyes
  • seizures
  • skin rash, hives, itching
  • sore throat
  • sores, ulcers, or white spots in the mouth or on the lips
  • tightness in the chest
  • trembling
  • unusual tiredness or weakness
  • vomiting
  • yellow eyes or skin


Is esomeprazole better than omeprazole?

Esomeprazole was well tolerated. In conclusion, esomeprazole 40 mg provides more effective acid control than twice the standard dose of omeprazole.

How long should you take Esomeprazole?

Esomeprazole is usually given for 4 to 8 weeks only. Your doctor may recommend a second course of treatment if you need additional healing time. Use this medicine for the full prescribed length of time, even if your symptoms quickly improve.

Can I take Esomeprazole after eating?

You can take Esomeprazole before or after food. If you forget to take a dose at your usual time, you can take it when you remember (unless it is nearly time for your next dose, in which case leave out the missed dose). Do not take two doses together to make up for a forgotten dose.

*** Taking medicines without doctor's advice can cause long-term problems.
Share