What is esomeprazole, and how does it work (mechanism of action)?
Esomeprazole is in a class of drugs called proton pump inhibitors (PPIs) which block the production of acid by the stomach. Other drugs in the same class include omeprazole
(Prilosec), lansoprazole (Prevacid), rabeprazole (Aciphex) and pantoprazole (Protonix). Chemically, esomeprazole is very similar to omeprazole. Proton pump inhibitors are used for the treatment of conditions such as stomach and duodenal ulcers, gastroesophageal reflux disease (GERD) and the Zollinger-Ellison syndrome which all are caused by stomach acid.
Esomeprazole, like other proton-pump inhibitors, blocks the enzyme in the wall of the stomach that produces acid. By blocking the enzyme, the production of acid is decreased, and this allows the stomach and esophagus to heal. Esomeprazole was approved by the FDA in February 2001.
What brand names are available for esomeprazole?
Nexium, Nexium 24HR, Nexium IV
Do I need a prescription for esomeprazole?
- Yes
– Nexium, Nexium IV - No – Nexium 24 hour
What are the side effects of esomeprazole?
Esomeprazole, like other PPIs, is well-tolerated. The most common side effects are
Nervousness, abnormal heartbeat, muscle pain, weakness, leg cramps, and water retention occur infrequently.
Proton pump inhibitors may increase the risk of
Clostridium difficile
infection. High doses and long-term use (1 year or longer) may increase the risk
of
osteoporosis-related fractures of the hip, wrist, or spine. Prolonged use
also reduces absorption of vitamin B12 (cyanocobalamin).
Long-term use of PPIs has also been associated with low levels of magnesium (hypomagnesemia).
Analysis of patients taking PPIs for long periods of time showed an increased
risk of heart attacks.
Therefore, it is important to use the lowest doses and shortest duration of
treatment necessary for the condition being treated.
What is the dosage for esomeprazole?
- For GERD, 20 or 40
mg of esomeprazole is given once daily for 4-8 weeks. In children ages 1-11, the dose is 10 or 20 mg daily. - For the treatment of H. pylori, 40 mg is administered once daily in combination with amoxicillin and clarithromycin for 10 days.
- Frequent heartburn is treated with 20 mg daily for 14 days.
- The dose for preventing NSAID-induced ulcers is 20 to 40 mg daily for 6 months.
- Zollinger-Ellison syndrome is treated with 40 mg twice daily.
Esomeprazole capsules should be administered one hour before meals, swallowed whole and should not be crushed or chewed. Patients with difficulty swallowing can open the capsule and mix the pellets with applesauce. The applesauce should not be hot and the pellets should not be chewed or crushed.
Which drugs or supplements interact with esomeprazole?
Esomeprazole potentially can increase the concentration in blood of diazepam
(Valium, Diastat) by decreasing the elimination of diazepam in the liver. Esomeprazole may have fewer drug interactions than omeprazole.
The absorption of certain drugs may be affected by stomach acidity. Therefore,
esomeprazole and other PPIs that reduce stomach acid also reduce the absorption and
concentration in blood of ketoconazole (Nizoral) and increase the absorption and
concentration in blood of digoxin (Lanoxin). This
may lead to reduced effectiveness of ketoconazole or increased digoxin toxicity,
respectively.
Through unknown mechanisms, esomeprazole may increase blood levels of
saquinavir (Invirase, Fortovase) and reduce blood levels of nelfinavir
(Viracept) and atazanavir
(Reyataz),
Therefore, nelfinavir or atazanavir should not be administered with
esomeprazole, and physicians should consider reducing the dose of saquinavir in order to avoid side effects from saquinavir.
Clopidogrel (Plavix) is converted to its active form by enzymes in the liver. Esomeprazole reduces the activity of these enzymes and potentially can reduce the activity of clopidogrel. Esomeprazole should not be used with clopidogrel.
Esomeprazole increases the concentration of
cilostazol (Pletal) and its metabolites. The dose of
cilostazol should be reduced from 100 mg twice daily to 50 mg twice daily when given with esomeprazole.
Esomeprazole may increase blood levels of methotrexate (Rheumatrex, Trexall) and tacrolimus (Prograf).
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Is esomeprazole safe to take if I’m pregnant or breastfeeding?
Use of esomeprazole in
pregnant women has not been adequately evaluated.
Esomeprazole has not been adequately studied in
nursing women.
What else should I know about esomeprazole?
What preparations of esomeprazole are available?
Capsules: 20
and 40 mg. Intravenous: 20 and 40 mg; Powder for Oral Suspension: 10 mg, 20 mg, 40 mg
How should I keep esomeprazole stored?
Store at room temperature, 15-30 C (59-86 F) in a tightly closed container.