Last Updated on June 3, 2023
Esomeprazole is a proton pump inhibitor that is used to treat acid reflux and other related conditions. It is available both in prescription and over-the-counter forms. For people who want to buy esomeprazole over the counter in the UK, there are several options available. One of the most common places to purchase this medication is at a pharmacy. Many pharmacies throughout the UK carry esomeprazole and other over-the-counter medications.
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What is esomeprazole?
The active ingredient esomeprazole is a proton pump inhibitor and is used to treat heartburn and regulate stomach acid. It works in the same way as omeprazole, but is slightly more effective. Here you will find everything you need to know about esomeprazole: how it works, how to use it and possible side effects.
How does esomeprazole work?
Esomeprazole is taken by mouth and is dissolved in the intestines and absorbed into the blood. It then travels through the blood vessels to the stomach lining, which produces stomach acid: The main component of stomach acid – hydrochloric acid – is released in the form of positively charged particles (protons) and negatively charged particles (chloride ions) from certain mucosal cells in the stomach. The mucosal cells use a special protein to ‘pump’ the protons across the cell membrane. Esomeprazole inhibits this protein and therefore the proton pump. This makes it a proton pump inhibitor.
Esomeprazole can only develop its inhibitory effect when it reaches the stomach lining and meets existing gastric acid – it is activated by
mirror image of omeprazole
The active ingredient omeprazole, a proton pump inhibitor, is also chemically defined, but is made up of individual particles that behave like mirror images of each other. By way of comparison: A person’s hands are the same, just mirror images. These two different types of substance are called enantiomers. Often, one enantiomer is more effective, less harmful or otherwise advantageous than the other.
This was the case with esomeprazole, an enantiomer of omeprazole. The other enantiomer of omeprazole can only be broken down in the body by a specific enzyme in the liver (CYP2C19). About three percent of the population hardly has this enzyme, which is why the so-called omeprazole enantiomer would quickly accumulate in the blood after repeated dosing with it.
Esomeprazole, on the other hand, can also be broken down by a second enzyme (CYP3A4), which ensures reliable elimination. However, the two enantiomers of omeprazole do not differ in their effect on the stomach lining.
Pharmacokinetics and metabolism of esomeprazole
Esomeprazole reaches peak blood levels approximately one to two hours after oral administration. It binds to the proton pump in the stomach lining and exerts its inhibitory effect there. The free drug circulating in the blood is completely broken down in the liver by the enzymes mentioned. Approximately one and a half hours after taking esomeprazole, the blood level is halved.
When is esomeprazole used?
The active ingredient esomeprazole is used for the following conditions:
- to treat heartburn (GERD – gastroesophageal reflux disease)
- to protect the stomach during long-term use of certain painkillers (NSAIDs such as aspirin/acetylsalicylic acid)
- in combination with antibiotics for the treatment of gastric bacterial infections (Helicobacter pylori)
- for the treatment of Zollinger-Ellison syndrome, a condition associated with increased acid production in the stomach
Depending on the underlying condition, esomeprazole may be used for a short or long time.
How esomeprazole is used?
Esomeprazole is taken in the form of enteric-coated tablets or capsules. Gastroresistance means that the active ingredient is only released in the intestine, where it can be absorbed into the blood. This absorption is particularly good if the medication is taken on an empty stomach (usually in the morning). Depending on the severity of the condition, twenty to forty milligrams of esomeprazole may be taken daily.
An intravenous formulation of esomeprazole is also available for patients with swallowing difficulties. Alternatively, tablets labelled “MUPS” (multiple unit pellet system) are dispersed in water and then drunk or administered via a feeding tube.
What are the side effects esomeprazole?
Tens to hundreds of people experience bloating, nausea and vomiting as side effects when taking esomeprazole.
In one hundred to one thousand patients, esomeprazole side effects include fluid retention in the arms and legs, insomnia, dizziness and vertigo, paresthesia, fatigue, dry mouth, increased liver enzymes, and skin reactions such as itching and redness. There may also be an increased risk of bone fractures, especially in older people and those on long-term treatment.
What should I watch for while taking esomeprazole?
As esomeprazole inhibits the production of stomach acid, it may alter the absorption of other drugs that are taken in dependence on stomach acid. Concerns about certain antifungal drugs (ketoconazole, itraconazole) and cancer drugs (erlotinib) – their intake may be reduced by concomitant use of esomeprazole.
Conversely, the intake of digoxin and other drugs by the heart may be increased by taking esomeprazole.
Concurrent use of drugs that are metabolised in the liver by the same enzymes as esomeprazole may interfere with the breakdown of either the proton pump inhibitor or the other drug. As a result, blood levels of esomeprazole or other drugs may increase or decrease.
In the case of protease inhibitors used to treat HIV (atazanavir, nelfinavir), blood levels may decrease with concurrent use of esomeprazole, whereas they may increase with other protease inhibitors (saquinavir, ritonavir).
Blood levels of methotrexate (for cancer and rheumatism), tacrolimus (used to suppress the immune system), diazepam (a sedative) and phenytoin (an anticonvulsant) also increase when esomeprazole is taken together.
As a precaution, the use of esomeprazole with anticoagulants such as warfarin and clopidogrel should also be monitored.
Pregnancy and lactation
Taking esomeprazole during pregnancy was studied in trials of omeprazole. There were no side effects. However, the use of esomeprazole during pregnancy should be medically assessed and used with caution.
It is not known whether esomeprazole is excreted in human milk, so the drug should not be used while breast-feeding.
Esomeprazole can be used in young people from the age of twelve and in older patients. Patients with severe liver impairment may need a lower dose.
How to get esomeprazole?
As well as pharmacies and online retailers, some supermarkets and health food stores in the UK sell esomeprazole over the counter. These stores may offer generic versions of the medication at a lower price than the brand name version. It’s important to read labels carefully and make sure you’re buying the right medication for your condition. If you’re not sure which product to buy, ask a pharmacist.
Since August 2014, small packs containing a maximum of 14 tablets containing 20 milligrams of active ingredient for the treatment of heartburn are no longer available on prescription in Germany. Higher doses, larger packs and products with other uses are still only available on prescription.
How long has esomeprazole been on the market?
Esomeprazole has been marketed by the pharmaceutical company AstraZeneca since 2001. It was introduced shortly before the patent on omeprazole, also from AstraZeneca, expired.