Esomeprazole, sold under the brand name Nexium or among others,[ is a medication which reduces gastric acid.][ It is used to treat gastroesophageal reflux disease, peptic ulcer, and Zollinger–Ellison syndrome.][
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Common side effects include headache, constipation, dry mouth, and abdominal pain.[ Serious side effects may include angioedema, Clostridioides difficile infection, and pneumonia.][ Use in pregnancy appears to be safe, while safety during breastfeeding is unclear.][ It works by blocking H+/K+-ATPase in the of the stomach.]
It was patented in 1993 and approved for medical use in 2000.[ In 2022, it was the 122nd most commonly prescribed medication in the United States, with more than 5million prescriptions.][ the United Kingdom]
Medical use
The primary uses of esomeprazole are gastroesophageal reflux disease, treatment and maintenance of erosive esophagitis, treatment of duodenal ulcers caused by H. pylori, prevention of gastric ulcers in those on chronic NSAID therapy, and treatment of gastrointestinal ulcers associated with Crohn's disease.
Gastroesophageal reflux disease
Gastroesophageal reflux disease (GERD) is a condition in which the digestive acid in the stomach comes in contact with the esophagus. The irritation caused by this disorder is known as heartburn.
Duodenal ulcers
Esomeprazole is combined with the antibiotics clarithromycin and amoxicillin (or metronidazole instead of amoxicillin in penicillin-hypersensitive patients) in a 10-day eradication triple therapy for Helicobacter pylori. Infection by H. pylori is a causative factor in the majority of Peptic ulcer.
Efficacy
A 2006 meta analysis concluded that compared to other proton pump inhibitors, esomeprazole confers a modest overall benefit in esophageal healing and symptom relief. When broken down by disease severity, the benefit of esomeprazole relative to other proton pump inhibitors was negligible in people with mild disease (number needed to treat 50), but appeared more in those with severe disease (number needed to treat 8).
Adverse effects
Common side effects include headache, diarrhea, nausea, flatulence, decreased appetite, constipation, dry mouth, and abdominal pain. More severe side effects are severe allergic reactions, chest pain, dark urine, fast heartbeat, fever, paresthesia, persistent sore throat, severe stomach pain, unusual bruising or bleeding, unusual tiredness, and yellowing of the eyes or skin.
Proton pump inhibitors may be associated with a greater risk of hip fractures
Long-term use of proton pump inhibitors in patients treated for Helicobacter pylori has been shown to dramatically increase the risk of gastric cancer.
Acute tubulointerstitial nephritis is a possible adverse reaction when using proton pump inhibitors.
Interactions
Esomeprazole is a enzyme inhibitor of the enzyme CYP2C19, and may therefore drug interaction with drugs that depend on it for drug metabolism, such as diazepam and warfarin; the concentrations of these drugs may increase if they are used concomitantly with esomeprazole.
Drugs that depend on stomach pH for absorption may interact with esomeprazole; drugs that depend on an acidic environment (such as ketoconazole or atazanavir) will be poorly absorbed, whereas drugs that are broken down in acidic environments (such as erythromycin) will be absorbed to a greater extent than normal.[
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Pharmacokinetics
Single 20 to 40mg oral doses generally give rise to peak plasma esomeprazole concentrations of 0.5-1.0mg/L within 1–4 hours, but after several days of once-daily administration, these levels may increase by about 50%. A 30-minute intravenous infusion of a similar dose usually produces peak plasma levels on the order of 1–3mg/L. The drug is rapidly cleared from the body, largely by urinary excretion of pharmacologically inactive metabolites such as 5-hydroxymethylesomeprazole and 5-carboxyesomeprazole. Esomeprazole and its metabolites are analytically indistinguishable from omeprazole and the corresponding omeprazole metabolites unless chiral techniques are employed.
Dosage forms
Esomeprazole is available as delayed-release capsules in the United States or as delayed-release tablets in Australia, the United Kingdom, and Canada (containing esomeprazole magnesium) in strengths of 20 and 40mg, as delayed-release capsules in the United States (containing esomeprazole strontium) in a 49.3mg strength (delivering the equivalent of 40mg of esomeprazole,
The combination naproxen/esomeprazole magnesium (brand name Vimovo) is used for the prevention of gastric ulcers associated with chronic NSAID therapy. Vimovo is available in two dosage strengths: 500/20mg and 375/20mg. Clinical trials of naproxen/esomeprazole demonstrated an incidence of GI ulcer in 24% of patients on naproxen (alone) versus 7% on naproxen/esomeprazole.
Multiple-unit pellet system
Esomeprazole capsules, as well as Losec/Prilosec tablets, are formulated as a "multiple-unit pellet system" (MUPS). Essentially, the capsule consists of extremely small enteric-coated granules (pellets) of the esomeprazole formulation inside an outer shell. When the capsule is immersed in an aqueous solution, as happens when the capsule reaches the stomach, water enters the capsule by osmosis. The contents swell from water absorption, causing the shell to burst, and releasing the enteric-coated granules. For most patients, the multiple-unit pellet system is of no advantage over conventional enteric-coated preparations. Patients for whom the formulation is of benefit include those requiring nasogastric tube feeding and those with difficulty swallowing (dysphagia).
Society and culture
Global distribution
In 2010, AstraZeneca announced a co-promotion agreement with Daiichi Sankyo to distribute Nexium in Japan.
Economics
Between the launch of esomeprazole in 2001 and 2005, the drug netted AstraZeneca about $14.4billion.[Financial impact information:
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Controversy
There has been some controversy about AstraZeneca's behaviour in creating, patenting, and marketing the drug. Esomeprazole's successful predecessor, omeprazole, is a mixture of two mirror-imaged molecules (esomeprazole which is the S-enantiomer, and R-omeprazole); critics said the company was trying to "Evergreening" its omeprazole patent by patenting the pure esomeprazole and aggressively marketing to doctors that it is more effective than the mixture.
Brand names
Generic versions of esomeprazole magnesium are available worldwide.[ It is available over-the-counter under the brand name Nexium in the United States]
Veterinary use
Injection formulations of esomeprazole are used for gastroprotection in veterinary medicine. In goats administered the drug by intravenous or subcutaneous injection rapid elimination was noted.
Other uses
Esomeprazole can be used as a parasiticide.
Further reading
