Drug Detail:Esomeprazole (Esomeprazole (oral) [ ee-so-mep-ra-zol ])
Drug Class: Proton pump inhibitors
1. How it works
- Esomeprazole is an acid-suppressing agent that may be used to treat conditions associated with excessive stomach acid production, such as gastroesophageal reflux (GERD) and stomach ulcers.
- Esomeprazole reduces the production of stomach acid by irreversibly blocking the actions of an enzyme responsible for acid production, called H+/K+ ATPase (also known as the gastric proton pump). The proton pump is located in the parietal cells of the stomach wall. Both baseline gastric acid secretion and stimulated gastric acid secretion are affected.
- Esomeprazole allows damaged tissue in the esophagus, stomach, and duodenum to heal.
- Esomeprazole belongs to the class of medicines known as proton pump inhibitors (PPIs).
2. Upsides
- Effective at healing erosive esophagitis (a severe inflammation of the lining of the esophagus - the tube that carries food from the mouth to the stomach), and relieving symptoms of gastroesophageal reflux disease (GERD) (also known as heartburn). May be used for the short-term treatment of symptomatic GERD in people with or without erosive esophagitis.
- May be taken at the same time as NSAIDs to reduce the risk of NSAID-associated gastric ulcers in those people on continuous NSAID therapy who are at high risk (for example, age over 60 years or a previous history of gastric ulcer).
- May be used in conjunction with amoxicillin and clarithromycin (triple therapy) in people with Helicobacter pylori infection and duodenal ulcer disease.
- Useful in the treatment of hypersecretory conditions such as Zollinger-Ellison syndrome.
- The dosage of esomeprazole does not need adjusting in people with kidney disease.
- Available IV which may be a good short-term alternative to oral treatment in people with erosive esophagitis who are unable to take the drug orally. The safety and efficacy of IV esomeprazole has not been established beyond 10 days.
- Generic esomeprazole is available.
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3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- A headache, diarrhea or constipation, flatulence, nausea, abdominal pain, dry mouth, or drowsiness.
- May also interfere with some laboratory tests.
- PPIs (including esomeprazole) have been associated with an increased risk of osteoporosis-related fractures of the hip, wrist, or spine. People on high-dose or long-term therapy are more at risk.
- Has also been associated with other conditions such as lupus erythematosus and magnesium deficiency.
- Prolonged treatment (greater than 24-36 months) may cause vitamin B12 deficiency. The risk is greater in women, people aged less than 30, and with higher dosages.
- A dosage of 20mg esomeprazole should not be exceeded in people with severe liver disease.
- Administration of PPIs (such as esomeprazole), has been associated with acute interstitial nephritis, a severe inflammation of the kidneys. May occur on medication initiation or at any point of therapy. Symptoms include fever, rash, and generalized aches and pains. Discontinue esomeprazole and seek medical advice.
- Has been associated with a greater risk of Clostridium difficile-associated diarrhea. See your doctor if you develop diarrhea that does not improve.
- Esomeprazole should not be given with clopidogrel because it can reduce the activity of clopidogrel. Esomeprazole may also interact with several other medications, particularly those that induce the CYP2C19 or CYP3A4 hepatic enzymes such as St. John's Wort or rifampin. Esomeprazole can also reduce the absorption of drugs that are dependent on a certain gastric pH for their absorption.
- Usually, only up to 8 weeks of treatment is recommended. Controlled studies have not investigated use beyond 6 months; however, esomeprazole has been used long-term for the treatment of hypersecretory conditions such as Zollinger-Ellison syndrome.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Usually taken once daily.
- Take at least an hour before a meal.
- Swallow delayed-release capsules whole. In people who have difficulty swallowing, the capsule may be opened and the contents mixed with applesauce and swallowed immediately.
- See your doctor if you develop any unexplained fever, rash (particularly one that gets worse after you have been in the sun), new or worsening joint pain, persistent diarrhea, or generalized aches and pains.
- Also, see your doctor if you develop any muscle cramps, spasms, or weakness; jitteriness; abnormal heartbeat; dizziness; seizures; or any other symptoms of concern.
5. Response and effectiveness
- Peak effects happen within one and a half hours and effects can last for over 24 hours.
- Esomeprazole delayed-release capsules and esomeprazole for delayed-release oral suspension are bioequivalent (the same dosage has the same effect on the body).
- The effect of esomeprazole depends upon the dosage given (more acid is suppressed with 40mg capsules than with 20mg capsules); however, dosages above 40mg do not provide any more effect.
6. Interactions
Medicines that interact with esomeprazole may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with esomeprazole. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with esomeprazole include:
- antibiotics, such as cefuroxime
- antidepressants, such as citalopram, clomipramine, escitalopram, imipramine, St John's wort, or trimipramine
- antifungals, such as fluconazole, itraconazole, ketoconazole, or voriconazole
- attention deficit hyperactivity disorder (ADHD) medications (eg, dextroamphetamine, dexmethylphenidate, lisdexamfetamine, methylphenidate)
- benzodiazepines, such as diazepam
- bisphosphonates, such as alendronate, etidronate, or risedronate
- cancer treatments, such as bosutinib, dabrafenib, dasatinib, erlotinib, or pazopanib
- clopidogrel
- diuretics, such as bendroflumethiazide or furosemide
- epilepsy medications, such as carbamazepine, fosphenytoin, phenobarbital, or phenytoin
- hepatitis medications, such as boceprevir, ledipasvir, sofosbuvir, and telaprevir
- HIV medications (eg, atazanavir, indinavir, ritonavir, or saquinavir)
- iron supplements, such as ferrous fumarate, ferrous gluconate, or ferrous sulfate
- multivitamins
- nitrates (eg, amyl nitrate, isosorbide dinitrate, isosorbide mononitrate, or nitroglycerin)
- proton pump inhibitors (eg, lansoprazole, omeprazole, pantoprazole)
- quinidine
- statins, such as atorvastatin, lovastatin, or simvastatin
- warfarin or other anticoagulants, such as dabigatran
- others, such as cilostazol, cisapride, cyclosporine, dabigatran, delavirdine, diazepam, digoxin, enzalutamide, mesalamine, methotrexate, moclobemide, modafinil, mycophenolate mofetil, rifampin, or tacrolimus.
Note that this list is not all-inclusive and includes only common medications that may interact with esomeprazole. You should refer to the prescribing information for esomeprazole for a complete list of interactions.