Esomeprazole; Uses, Dosage, Side Effects, Interactions, Pregn

Esomeprazole
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Esomeprazole is the S-isomer of omeprazole, with gastric proton pump inhibitor activity. In the acidic compartment of parietal cells, esomeprazole is protonated and converted into the active achiral sulfenamide; the active sulfenamide forms one or more covalent disulfide bonds with the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting its activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production. H+/K+ ATPase is an integral membrane protein of the gastric parietal cell.

or

The active ingredient in the proton pump inhibitor (esomeprazole magnesium) Delayed-Release Capsules for oral administration and (esomeprazole magnesium) For Delayed-Release Oral Suspension is bis(5-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole-1-yl) magnesium trihydrate. Esomeprazole is the S-isomer of omeprazole, which is a mixture of the S- and R- isomers. (Initial U.S. approval of esomeprazole magnesium: 2001). Its molecular formula is (C17H18N3O3S)2 Mg x 3 H2O with molecular weight of 767.2 as a trihydrate and 713.1 on an anhydrous basis. The structural formula is

Mechanism of Action of Esomeprazole

Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. The S- and R-isomers of omeprazole are protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.

Or

Esomeprazole is a substituted benzimidazole which inhibits the secretion of hydrochloric acid in the stomach by specific blockade of the proton pumps of the parietal cells. Esomeprazole is converted to its active form in the acidic environment in the parietal cells where it inhibits the H+, K+-ATPase enzyme, i.e. the final stage in the production of hydrochloric acid in the stomach. The inhibition is dose-dependent and affects both basal and stimulated acid secretion. In most patients, freedom from symptoms is achieved within 2 weeks. As with other proton pump inhibitors and H2 receptor inhibitors, treatment with esomeprazole reduces acidity in the stomach and thereby increases gastrin in proportion to the reduction in acidity. The increase in gastrin is reversible. Since esomeprazole binds to the enzyme distal to the cell receptor level, it can inhibit hydrochloric acid secretion independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect is the same whether the product is given orally or intravenously.

Indications of Esomeprazole

Esomeprazole  is used to treat conditions caused by too much acid production in the stomach, such as

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Therapeutic Indications of Esomeprazole

  • Anti-Ulcer Agents; Proton Pump Inhibitors
  • Although evidence currently is limited, proton-pump inhibitors have been used for gastric acid-suppressive therapy as an adjunct in the symptomatic treatment of upper GI Crohn’s disease, including esophageal, gastroduodenal, and jejunoileal disease.
  • Esomeprazole magnesium is used for the long-term treatment of pathologic GI hypersecretory conditions. Efficacy for this indication was established in an open-label study in a limited number of patients with previously diagnosed pathologic GI hypersecretory conditions (e.g., Zollinger-Ellison syndrome, idiopathic gastric acid hypersecretion); patients received total daily dosages of esomeprazole ranging from 80 mg-240 mg.
  • Esomeprazole magnesium is used for reducing the occurrence of gastric ulcers associated with chronic nonsteroidal anti-inflammatory agent (NSAIA) therapy in patients at risk for developing these ulcers, including individuals 60 years of age or older and/or those with a documented history of gastric ulcers.
  • Efficacy for this indication was established in two 6-month randomized, controlled studies in patients receiving chronic therapy with either a prototypical NSAIA or a selective cyclooxygenase-2 (COX-2) inhibitor; individuals enrolled in these studies were considered to be at risk for developing NSAID-associated ulcers because of their age (60 years or older) and/or a history of documented gastric or duodenal ulcer within the previous 5 years, but they had no evidence of gastric or duodenal ulcers on endoscopic examination at the start of the studies.
  • Esomeprazole magnesium is used in combination with amoxicillin and clarithromycin (triple therapy) for short-term (10 days) treatment of patients with H. pylori infection and duodenal ulcer disease (active duodenal ulcer or a history of duodenal ulcer within the preceding 5 years).
  • Efficacy of esomeprazole-based triple therapy for H. pylori eradication was established in 2 controlled studies in patients with documented H. pylori infection and at least one endoscopically verified duodenal ulcer (or documented history of duodenal ulcer disease in the preceding 5 years).
  • At 4 weeks after treatment, H. pylori eradication rates were substantially higher in patients receiving triple therapy (esomeprazole 40 mg once daily, amoxicillin 1 g twice daily, and clarithromycin 500 mg twice daily) for 10 days than in those receiving dual therapy (esomeprazole 40 mg daily and clarithromycin 500 mg twice daily) or monotherapy with esomeprazole 40 mg daily for 10 days.
  • Esomeprazole magnesium is used for short-term (4-8 weeks) treatment of diagnostically confirmed erosive esophagitis in patients with gastroesophageal reflux disease (GERD). The drug also is used as maintenance therapy following the healing of erosive esophagitis to reduce recurrence of the disease.
  • In addition, esomeprazole is used for short-term (4-8 weeks) treatment of symptoms (e.g., heartburn) of GERD in patients without erosive esophagitis. In infants, esomeprazole is used for short-term (up to 6 weeks) treatment of erosive esophagitis due to acid-mediated GERD.

Contra-Indications of Esomeprazole

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Taking a proton pump inhibitor such as esomeprazole may increase your risk of bone fracture in the hip, wrist, or spine. This effect has occurred mostly in people who have taken the medicine long term or at high doses, and in those who are age 50 and older. It is not clear whether esomeprazole is the actual cause of an increased risk of fracture.

Dosage of Esomeprazole

Strengths:  2.5 mg; 5 mg;10 mg; 20 mg; 40 mg;  & 20 mg ,40 mg I.V Injection

Gastroesophageal Reflux Disease

  • Esomeprazole Magnesium: 20 mg orally once a day
  • Duration of therapy: 14 days (over-the-counter [OTC] formulations); 4 weeks (prescription formulations)
  • Esomeprazole Strontium: 24.65 mg orally once a day
  • Duration of therapy: 4 weeks

GERD with Erosive Esophagitis , Esomeprazole Sodium

  • IV injection: 20 mg or 40 mg once a day, over no less than 3 minutes

Erosive Esophagitis

Esomeprazole magnesium

  • Healing: 20 to 40 mg orally once a day
  • Duration of therapy: 4 to 8 weeks
  • Maintenance: 20 mg orally once a day

Esomeprazole strontium

  • Healing: 24.65 to 49.3 mg orally once a day
  • Duration of therapy: 4 to 8 weeks
  • Maintenance: 24.65 mg orally once a daily

Helicobacter pylori Infection

Esomeprazole Magnesium

  • Triple therapy: 40 mg orally once a day, taken concomitantly with amoxicillin and clarithromycin
  • Duration of therapy: 10 days

Esomeprazole Strontium

  • Triple therapy: 49.3 mg orally once a day, taken concomitantly with amoxicillin and clarithromycin
  • Duration of therapy: 10 days

NSAID-Induced Gastric Ulcer

  • Esomeprazole Magnesium: 20 mg to 40 mg orally once daily
  • Duration of therapy: Up to 6 months
  • Esomeprazole Strontium: 24.65 mg to 49.3 mg orally once a day
  • Duration of therapy: Up to 6 months

Zollinger-Ellison Syndrome

  • Esomeprazole Magnesium: 40 mg orally twice a day
  • Esomeprazole Strontium: 49.3 mg orally twice a day

Pediatric Gastroesophageal Reflux Disease

Esomeprazole Magnesium

  • 1 to 11 years: 10 mg once a day
  • Duration of therapy: Up to 8 weeks
  • 12 to 17 years: 20 mg once a day
  • Duration of therapy: 4 weeks
Esomeprazole Sodium
GERD with Erosive Esophagitis
  • 1 month to less than 1 year: 0.5 mg/kg IV infused over 10 to 30 minutes
1 to 17 years
  • fainting
  • Less than 55 kg: 10 mg IV infused over 10 to 30 minutes
  • 55 kg or more: 20 mg IV infused over 10 to 30 minutes

Recommended Dosage Schedule for 

IndicationDoseFrequency
Gastroesophageal Reflux Disease (GERD)
  Healing of Erosive Esophagitis20 mg or 40 mgOnce Daily for 4 to 8 Weeks*
  Maintenance of Healing of Erosive Esophagitis20 mgOnce Daily†
  Symptomatic Gastroesophageal Reflux Disease20 mgOnce Daily for 4 Weeks‡
Pediatric GERD 12 to 17-Year-Olds
Healing of Erosive Esophagitis Symptomatic GERD20 mg or 40 mgOnce Daily for 4 to 8 Weeks
20 mgOnce Daily for 4 Weeks
1 to 11-Year-Olds §
Short-term Treatment of Symptomatic GERD10 mgOnce Daily for up to 8 Weeks
Healing of Erosive Esophagitis
  weight < 20 kg10 mgOnce Daily for 8 Weeks
  weight ≥ 20 kg10 mg o r 20 mgOnce Daily for 8 Weeks
1 month to < 1 year old¶
Erosive esophagitis due to acid-mediated GERD
  weight 3 kg to 5 kg2.5 mgOnce Daily for up to 6 Weeks
  weight > 5 kg to 7.5 kg5 mgOnce Daily for up to 6 Weeks
  weight > 7.5 kg to 12 kg10 mgOnce Daily for up to 6 Weeks
Risk Reduction of NSAID-Associated Gastric Ulcer20 mg or 40 mgOnce Daily for up to 6 months†
H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence
Triple Therapy:
  NEXIUM40 mgOnce Daily for 10 Days
  Amoxicillin1000 mgTwice Daily for 10 Days
  Clarithromycin500 mgTwice Daily for 10 Days
Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome40 mgTwice Daily
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Side Effects of Esomeprazole

The most common

More common

Rare

Drug Interactions of Esomeprazole

Esomeprazole may interact with following drugs, supplements, & may change the efficacy of the drug

Pregnancy Catagory of Esomeprazole

FDA Pregnancy Category C

Pregnancy

A moderate amount of data on pregnant women (between 300-1000 pregnancy outcomes) indicate no malformative or fetal/ neonatal toxicity of esomeprazole.Animal studies have shown reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of esomeprazole during pregnancy.

Lactation

Animal studies have shown excretion of esomeprazole in breast milk. There is insufficient information on the excretion of esomeprazole in human milk but excretion into human milk has been reported. A risk to the newborns/infants cannot be excluded. Therefore, a decision on whether to discontinue breastfeeding or to discontinue/abstain from esomeprazole therapy should take into account the benefit of breastfeeding for the child and the benefit of esomeprazole therapy for the woman. There was no evidence of impaired fertility following the administration of  esomeprazole in animal studies

References

esomeprazole

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