Esomeprazole is a medication that belongs to a class of drugs called proton pump inhibitors (PPIs).
It is commonly used to treat conditions such as gastroesophageal reflux disease (GERD), stomach ulcers, and excessive stomach acid production.
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.
Esomeprazole works by reducing the amount of acid produced in the stomach, which helps to relieve symptoms such as heartburn, acid reflux, and indigestion.
It can also help promote the healing of stomach ulcers.
Esomeprazole works by inhibiting the enzyme in the stomach known as the proton pump, which is responsible for producing acid.
By reducing the amount of acid produced, esomeprazole helps to relieve symptoms such as heartburn, acid reflux, and the healing of stomach ulcers.
As with any medication, there may be potential side effects associated with esomeprazole. Common side effects include headache, nausea, diarrhea, abdominal pain, and dry mouth. However, not everyone experiences side effects and they are usually mild.
It’s important to inform your healthcare provider of any existing medical conditions, allergies, or other medications you are taking before starting esomeprazole to avoid any potential drug interactions or complications.
If you have any further questions or concerns about esomeprazole, it is always best to consult with your healthcare provider or pharmacist, as they can provide you with specific and personalized advice based on your individual situation.
Trade name Nexium
Pregnancy category AU: B3
Routes of administration By mouth, intravenous
Drug class Proton pump inhibitor
Bioavailability 50 to 90%
Metabolism Liver (CYP2C19, CYP3A4)
Elimination half-life 1–1.5 hours
Excretion
80% Kidney
20% Feces
It is used to treat gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome.
Effectiveness is similar to other proton pump inhibitors (PPIs).
Common side effects include headache, constipation, dry mouth, and abdominal pain.
Serious side effects may include angioedema, Clostridium difficile infection, and pneumonia.
Use in pregnancy appears to be safe, while safety during breastfeeding is unclear.
Esomeprazole works by blocking H+/K+-ATPase in the parietal cells of the stomach.
Esomeprazole reduces the production of digestive acids, thus reducing their effect on the esophagus in GERD.
Esomeprazole is combined with the antibiotics clarithromycin and amoxicillin in a 10-day eradication triple therapy for Helicobacter pylori.
The benefit of esomeprazole relative to other proton pump inhibitors is negligible in people with mild disease but appeared more in those with severe disease.
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 jaundice,
Proton pump inhibitors may be associated with a greater risk of hip fractures and Clostridium difficile-associated diarrhoea.
Patients are frequently administered the drugs in intensive care as a protective measure against ulcers, but this use is also associated with a 30% increase in occurrence of pneumonia.
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.
Esomeprazole is a competitive inhibitor of the enzyme CYP2C19, and may therefore interact with drugs that depend on it for metabolism: diazepam and warfarin, and may increase if they are used concomitantly with esomeprazole.
Clopidogrel (Plavix) is an inactive prodrug that partially depends on CYP2C19 for conversion to its active form; inhibition of CYP2C19 blocks the activation of clopidogrel, thus reducing its effects.
Drugs that depend on stomach pH for absorption may interact with esomeprazole; drugs that depend on an acidic environment, such as ketoconazole, 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.
Single 20 to 40 mg oral doses generally give rise to peak plasma esomeprazole concentrations of 0.5-1.0 mg/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 1–3 mg/L.
Esomeprazole 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.