Esomeprazole

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[edit] BRAND NAMES

[edit] STRUCTURE

Esomeprazole.jpg

S-enantiomer of Omeprazole

[edit] MECHANISM OF ACTION

Esomeprazole is a proton pump inhibitors. it decreases the amount of acid produced in the stomach by inhibition of H+/K+ ATPase located in the luminal membrane of gastric parietal cells

[edit] INDICATIONS

  • Treatment of Gastroesophageal reflux disease (GERD)
  • To prevent ulcer caused by NSAIDs.
  • Treatment of ulcer caused by H. Pylori bacteria.
  • Pathological hypersecretory conditions, including Zollinger-Ellison syndrome.

[edit] DOSAGE

  • Gastroesophageal Reflux Disease:
    • Adults: 20-40mg/day for 4 to 8 weeks
    • 12 to 17 Year Olds: 20-40mg/day for up to 8 weeks
    • 1 to 11 Year Olds: 10-20mg/day for up to 8 weeks
    • In infants 1 month to less than 1 year:
      • 3-5 kg: 2.5 mg once daily for up to 6 Weeks
      • 5-7,5 kg: 5 mg once daily for up to 6 Weeks
      • 7,5-12 kg: 10 mg once daily for up to 6 Weeks
  • Risk Reduction of NSAID Associated Gastric Ulcer: 20-40mg/day for up to 6 months
  • H. pylori Eradication (Triple Therapy): Esomeprazole (40 mg) once daily + Amoxicillin (1000 mg) Twice Daily + Clarithromycin (500 mg) Twice Daily for 10 days
  • Zollinger-Ellison syndrome: 40 mg twice daily

[edit] CONTRAINDICATIONS

Patients with known hypersensitivity to PPIs (angioedema and anaphylaxis have occurred)

[edit] WARNINGS AND PRECAUTIONS

  • Symptomatic response to therapy does not rule out the presence of gastric malignancy
  • PPI therapy may be associated with increased risk of Clostridium difficile associated diarrhea.
  • Bone Fracture: Long-term and multiple daily dose PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist or spine.
  • Hypomagnesemia has been reported rarely with prolonged treatment with PPIs.

[edit] INTERACTIONS

  • Clopidogrel: Avoid concomitant use of Esomeprazole with clopidogrel, due to a reduction in plasma concentrations of the active metabolite of clopidogrel. When using Esomeprazole consider alternative antiplatelet therapy.
  • Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg, ketoconazole, iron salts, erlotinib, and digoxin)
  • Combined inhibitor of CYP2C19 and CYP3A4 may raise esomeprazole levels
  • Concomitant use of Esomeprazole and St. John’s wort or rifampin can substantially decrease Esomeprazole concentrations.
  • Concomitant use of Esomeprazole and atazanavir or nelfinavir is not recommended because the plasma concentrations and therapeutic effects of those antiretroviral drugs may be reduced.
  • Esomeprazole may increase the plasma levels of saquinavir. Dose reduction of saquinavir should be considered.
  • Methotrexate: Concomitant use of Esomeprazole and methotrexate may increase and prolong the serum levels of methotrexate and/or its metabolite. In high-dose methotrexate administration, a temporary withdrawal of Esomeprazole may be considered in some patients.
  • Warfarin: Patients treated with PPIs and warfarin concomitantly may need to be monitored for increases in INR and prothrombin time.
  • Cilostazol: May increase systemic exposure of cilostazol and an active metabolite. Consider dose reduction
  • Tacrolimus: May increase serum levels of Tacrolimus

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US), Esomeprazole should be used during pregnancy only if clearly needed.
  • Nursing mothers: a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

In adults, the most frequently reported adverse reactions with Esomeprazole include headache, diarrhea, nausea, flatulence, dry mouth, abdominal pain and constipation.

In pediatric patients 1 to 17 years of age, the most frequently reported adverse reactions with Esomeprazole include headache, diarrhea, abdominal pain, nausea, and somnolence

In pediatric patients 1 month to less than 1 year of age: Abdominal pain, regurgitation, tachypnea and increased ALT.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Heartburn/Gastritis/Gastric ulcer/Duodenal ulcer/Gastroesophageal reflux
H2 antagonists Famotidine   Nizatidine   Ranitidine (Zantac)
Proton-pump inhibitors Dexlansoprazole (Dexilant)   Esomeprazole (Nexium)   Lansoprazole (Prevacid)   Omeprazole (Losec, Prilosec)   Omeprazole/Sodium bicarbonate (Zegerid)   Pantoprazole (Controloc, Pantecta, Pantoloc, Protonix) (  Rabeprazole (Aciphex, Pariet)
Prostaglandins Misoprostol (Cytotec)
Other drugs Alginic acid   Magaldrate   Sucralfate
Combination Regimens Bismuth Subcitrate Potassium/Metronidazole/Tetracycline (Pylera)   Lansoprazole/Amoxicillin/Clarithromycin (Prevpac)