esomeprazole (Nexium)

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.

Nexium, Nexium 24HR, Nexium IV

• Yes - Nexium, Nexium IV
• No - Nexium 24 hour

Esomeprazole, like other PPIs, is well-tolerated. The most common side effects are

• diarrhea,
• nausea,
• vomiting,
• headaches,
• rash and
• dizziness.

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.

• 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.

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).

Use of esomeprazole in pregnant women has not been adequately evaluated.

Esomeprazole has not been adequately studied in nursing women.

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.