Products
The fixed combination of naproxen (500 mg) with esomeprazole (20 mg) is approved in the form of coated tablets (Vimovo, AstraZeneca AG). The drug was registered in many countries in May 2011. Naproxen is contained in the core, and esomeprazole is contained in the coating of the tablet.
Structure and properties
Naproxen (C14H14O3, Mr = 230.3 g/mol) is a white powder that is practically insoluble in water. It was developed as an analog of ibuprofen and is commercially available as an -enantiomer. Esomeprazole is the -enantiomer of omeprazole (C17H19N3O3S, Mr = 345.4 g/mol) and is present in the drug as magnesium esomeprazole trihydrate, a white powder that is sparingly soluble in water.
Effects
Naproxen (ATC M01AE52) is analgesic, antipyretic, and anti-inflammatory. Esomeprazole reduces secretion of gastric acid by irreversibly inhibiting the proton pump in the occupant cells of the stomach. It is added to the combination as a “gastric protector” to protect the mucosa from the adverse effects of naproxen and reduce the risk of developing a gastric or intestinal ulcer. The fixed combination may potentially increase adherence to therapy because only a single tablet needs to be taken. A disadvantage is less flexibility in dosing and choice of active ingredients. Naproxen is included in the combination because it is thought to have a lower cardiovascular risk, unlike other NSAIDs.
Indications
For the treatment of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. The drug is not recommended for acute pain because absorption and onset of action are delayed.
Dosage
According to the drug label. The drug is taken twice daily with water at least 30 minutes before meals.
Contraindications
For complete precautions, see the drug label.
Adverse effects
Clinical trials have confirmed that the risk of developing intestinal ulcers is reduced when esomeprazole is used in combination. Gastrointestinal side effects also occur less frequently.
