Indication
Esomeprazole is indicated:
Treatment of Gastroesophageal Reflux Disease (GERD)
Healing of erosive esophagitis
Maintenance of healing of erosive esophagitis
Symptomatic Gastroesophageal Reflux Disease (GERD)
Reduction of NSAID-associated gastric ulcer
H. pylori eradication (Triple therapy)
Zollinger-Ellison syndrome
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Pharmacology
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
Tablet or Capsule:
Healing of erosive esophagitis: 20 mg or 40 mg once daily for 4 to 8 weeks. The majority of patients are healed within 4 to 8 weeks. For patients who do not heal after 4-8 weeks, an additional 4-8 weeks treatment may be considered.
Maintenance of healing of erosive esophagitis: 20 mg once daily. Controlled studies did not extend beyond six 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.
H.pylori eradication (Triple therapy): Esomeprazole 20 mg twice daily for 10 days, Amoxicillin 1000 mg Twice daily for 10 days and Clarithromycin 500 mg twice daily for 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).?ÿ
Interaction
Esomeprazole appears to be a selective inhibitor of the cytochrome P450 mono-oxygenase system, there may be an effect on hepatic clearance, but there have been no reports to date of clinically relevant interactions. There is some uncertainty over the effect of Esomeprazole on the oral combined contraceptive pill. Physiological changes similar to those found with omeprazole are likely to take place because of the reduction in gastric acid which is likely to influence the bacterial colonization of the stomach and duodenum and also vitamin B12 absorption.
Contradiction
Esomeprazole is contraindicated in those patients who have known hypersensitivity to any other components of the formulation.
Side Effect
Side effects reported with Esomeprazole include headache, diarrhea and abdominal pain.
Pregnancy
US FDA pregnancy category of Esomeprazole is C. So, Esomeprazole should be avoided in pregnancy and lactation unless the potential benefits to the other outweigh the possible risks to the fetus.
Precaution
Exclude the possibility of malignancy when gastric ulcer is suspected and before treatment for dyspepsia. When using in combination with antibiotic, refer to the prescribing information of the respective antibiotics.
Overdose
Storage
Keep in dry place and away from light and heat. Keep out of the reach of children.