Products
Naproxen has been approved in many countries since 1975 and is commercially available in the form of film-coated tablets (e.g., Apranax, Proxen, generics). Other dosage forms such as the suppositories and the juice are no longer available. Drugs with a deep dose have been available over the counter since 1999 (Aleve with 200 mg naproxen as 220 mg naproxen sodium). The brand name Aleve is derived from English meaning to relieve or relieve. In 2011, a fixed-dose combination with the gastric protector esomeprazole was released (Vimovo).
Structure and properties
Naproxen (C14H14O3, Mr = 230.3 g/mol) exists as an acid as a white crystalline powder that is practically insoluble in water. It is also present in drugs in the form of the salt naproxen sodium, which is more soluble in water and is absorbed more rapidly because of its rapid release. Methoxynaphthylpropionic acid was developed as an analogue of ibuprofen and is sold exclusively as an -enantiomer.
Effects
Naproxen (ATC M01AE02) has analgesic, antipyretic, and anti-inflammatory properties. Unlike many other NSAIDs, it has a long half-life, a long duration of action of about 8-12 hours, and is reported to have a comparatively better cardiovascular profile. Its effects are based on inhibition of prostaglandin synthesis through nonselective inhibition of cyclooxygenases 1 and 2.
Indications
Naproxen is used to treat pain, fever, and inflammatory conditions of various causes, for example, back pain, arthritis, muscle and joint pain, gout, menstrual cramps, colds, influenza, headache, and toothache. Because of the possible adverse effects, only a short treatment period of 3 days is intended for self-medication.
Dosage
According to the drug label. The single dose for self-medication in adults is 200-400 mg, and the maximum daily dose is 600 mg, calculated as naproxenum. This corresponds to a maximum of 3 tablets per day. Single doses up to a maximum of 1000 mg and daily doses up to 1250 mg are administered on medical prescription. Taking with meals may slow absorption but does not affect the extent.
Contraindications
- Hypersensitivity, including to other NSAIDs
- 3rd trimester of pregnancy
- Gastrointestinal ulcers,
- Active bleeding
- Blood formation disorders
- Inflammatory bowel disease
- Severe liver, kidney or heart dysfunction.
Full precautions can be found in the drug label.
Interactions
Interactions have been described with antacids, cholestyramine, albumin-binding drugs, anticoagulants, antiplatelet agents, phenytoin, sulfonamides, sulfonylureas, glucocorticoids, SSRIs, ciclosporin, probenecid, methotrexate, NSAIDs, diuretics, furosemide, lithium, and beta-blockers, among others.
Adverse effects
The most common potential adverse effects include central disturbances such as headache, dizziness, fatigue, and digestive disturbances such as dyspepsia, nausea, heartburn, abdominal pain, diarrhea, constipation, and vomiting. Occasionally, dizziness, hearing disorders, ringing in the ears, breathing disorders, asthma, skin reactions, and kidney dysfunction occur. Very rarely, severe side effects are possible, such as blood count disorders, hypersensitivity reactions, central and psychiatric disorders, visual disturbances, cardiovascular disorders, gastrointestinal ulcers, gastrointestinal bleeding, and renal insufficiency.
