A nonsteroidal anti-inflammatory drug (NSAID) used to treat pain, menstrual cramps, inflammatory diseases such as rheumatoid arthritis, and fever.
A nonselective COX inhibitor.
Oral agent, available in immediate and delayed release formulations.
Onset of effects is within an hour and last for up to twelve hours.
Trade names Aleve, Naprosyn.
Pregnancy category US: C (Risk not ruled out)
OTC
Bioavailability 95% by mouth.
Protein binding 99%.
Metabolism by Liver
Elimination half-life12–17 hours.
Excretion by Kidney
Common side effects include: dizziness, headache, bruising, allergic reactions, heartburn, and stomach pain.
Severe side effects include: an increased risk of heart disease, stroke, gastrointestinal bleeding, and stomach ulcers.
The heart disease risk may be lower than with other NSAIDs.
It is not recommended in people with renal disease.
Use is not recommended in the third trimester of pregnancy.
It manifests its anti-inflammatory action by reducing the production of inflammatory mediators called prostaglandins, and is metabolized by the liver to inactive metabolites.
It is used to treat inflammatory conditions and symptoms that are due to excessive inflammation, such as pain and fever.
Migraine, osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, and bursitis are inflammatory conditions that may be responsive to Naproxen.
It is not useful in treating non-inflammatory causes of pain.
It is available as both an immediate release and as an extended release tablet.
Extended release formulations are more useful for the treatment of chronic, or long-lasting, conditions.
Small amounts of the drug are excreted in breast milk: adverse effects are uncommon in infants breastfed from mother taking naproxen.
Common adverse effects include dizziness, drowsiness, headache, rash, bruising, and gastrointestinal upset.
Major use is associated with increased risk of end-stage renal disease and kidney failure.
About 3% of patients have muscle cramps in the legs.
It can cause gastrointestinal problems: heartburn, constipation, diarrhea, ulcers and stomach bleeding.
Should be taken with food to decrease the risk of gastrointestinal side effects.
Has boxed warnings about the risk of gastrointestinal ulceration or bleeding.
It has an intermediate risk of stomach ulcers compared with ibuprofen, which is low-risk, and indomethacin, which is high-risk.
It is often combined with a proton-pump inhibitor during long-term treatment of those at risk of stomach ulcers.
It is associated with the smallest overall cardiovascular risks of NSAIDs, with roughly 50% of the associated risk of stroke compared with ibuprofen, and was also associated with a reduced number of myocardial infarctions compared with control groups.
In a study of high-dose naproxen it was found to induce near-complete suppression of platelet thromboxane and appeared not to increase cardiovascular disease (CVD) risk.
Other non-aspirin high-dose NSAID regimens had only transient effects on platelet COX-1 and were associated with a small but definite vascular hazard.
It isnassociated with higher rates of upper gastrointestinal bleeding complications compared with other NSAIDs.
It may interact with antidepressants, lithium, methotrexate, probenecid, warfarin and anticoagulants, heart or blood pressure medications, including diuretics, or steroid medicines.
It increases the risk of bleeding.
Alcohol consumption increases the risk of gastrointestinal bleeding when combined with NSAIDs.
It works by reversibly inhibiting both the COX-1 and COX-2 enzymes as a non-selective coxib.
It inhibits prostaglandin synthesis.
Prostaglandins act by inducing inflammation.
Thus, by inhibiting COX-1/2, it induces an anti-inflammatory effect.
It is a minor substrate of CYP1A2 and CYP2C9.
It is extensively metabolized in the liver.
Its time to peak plasma concentration occurs between 2–4 hours after oral administration, though naproxen sodium reaches peak plasma concentrations within 1–2 hours.
Genetic variants in CYP2C9 that reduce the clearance of major CYP2C9 substrates like naproxen increase the risk of NSAID-induced gastrointestinal bleeds, especially for homozygous defective variants.
In some studies, it reduced neoplastic fevers better than it reduced infectious fevers.
In patients with gout, naproxen was associated with similar pain relief, fewer side effects and lower use of other analgesics compared to low-dose colchicine.
Naproxen should be considered ahead of low-dose colchicine in primary care on the grounds of effectiveness, safety and cost.