Naproxen (brand name: Aleve , Naprosyn , and many others) is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid class together with ibuprofen) that relieves pain, fever, swelling, and stiffness. This is a selective COX inhibitor, usually sold as a sodium salt. It is available in direct release and extended release formulations. Naproxen is generally safe for use in breastfeeding mothers.
Common adverse effects of naproxen include central nervous system effects (eg headache and headache), blood effects (eg bruising), allergic reactions (eg rash), and gastrointestinal complaints (eg heartburn and stomach). It has an intermediate risk of stomach ulcers compared to other drugs in the same class (NSAID). NSAIDs appear to increase the risk of serious cardiovascular events, although this risk appears to be less with naproxen than with other NSAIDs. Serious drug interactions can occur in combination with other drugs that affect blood, or with drugs that also increase the risk of ulcers.
As an NSAID, naproxen uses anti-inflammatory action by reducing the production of inflammatory mediators called prostaglandins. It is extensively metabolized by the liver into an inactive metabolite. There have been several studies to show a person's genetic impact on the risk of naproxen-induced stomach ulcers.
Video Naproxen
Medical use
Medical use of Naproxen is associated with its mechanism of action as an anti-inflammatory compound. Naproxen is used to treat various inflammatory conditions and symptoms caused by excessive inflammation, such as pain and fever (naproxen has a fever reliever, or antipyretic, in addition to anti-inflammatory activity). In particular, not all drugs that reduce fever are anti-inflammatory compounds (such as paracetamol). The sources of inflammatory pain that can respond to naproxen's anti-inflammatory activity are conditions such as migraine, osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, and bursitis.
Due to the mechanism of anti-inflammatory action, one would not expect naproxen to be useful in treating the cause of non-inflammatory pain (eg, diabetic nerve pain).
Naproxen is used as a "bridge therapy" in over-the-counter medicines to wean patients from other drugs.
Available formats
Naproxen is available both as a direct release and as an extended release tablet. Extended release formulations (sometimes called "sustained release," or "coated enteric") take longer to apply than an immediate release formulation, and therefore are less useful when pain relief is desirable. Extended release formulations are more useful for chronic, or long-lasting, conditions, where long-term pain relief is desired.
Specific population
Pregnancy and lactation
A small amount of naproxen is excreted in breast milk. However, adverse effects are rare in breastfed infants of mothers taking naproxen.
Diagnostics
Naproxen has been used to distinguish between communicable fevers and fever associated with tissue or neoplastic disease. Although the literature can not be inferred, it is thought that naproxen may help distinguish between infection fever and neoplastic fever with its efficacy in reducing them; in some studies, naproxen reduces neoplastic fever much better than reducing infectious fever. This information is potentially used to identify the etiology of a patient's fever, which can be complex in cancer patients (who are often at high risk for infection in the first place).
Maps Naproxen
Adverse effects
Common side effects include dizziness, drowsiness, headache, rash, bruising, and gastrointestinal disorders. Severe use is associated with an increased risk of end-stage renal disease and renal failure.
Gastrointestinal side effects
Like other non-COX-2 selective NSAIDs, naproxen can cause gastrointestinal problems, such as heartburn, constipation, diarrhea, ulcers and gastric bleeding. Naproxen should be taken with food to reduce the risk of gastrointestinal side effects. People with a history of ulcers or inflammatory bowel disease should consult a physician before taking naproxen. In the US, naproxen is sold with a box warning about the risk of gastrointestinal ulceration or bleeding. Naproxen poses an intermediate risk of abdominal ulcers compared to low-risk ibuprofen, and indomethacin, which are at high risk. To reduce the risk of gastric ulcers, it is often combined with proton pump inhibitors (drugs that reduce the production of stomach acid) during their long-term treatment with pre-existing abdominal ulcers or a history of gastric ulcers during NSAIDs.
Cardiovascular side effects
Selective and non-selective COX-2 NSAIDs have been associated with an increase in the number of serious and potentially fatal cardiovascular events, such as myocardial infarction and stroke. Naproxen, however, is associated with the smallest overall cardiovascular risk. Cardiovascular risk should be considered when prescribing nonsteroidal anti-inflammatory drugs. The drug has about 50% of the risk of stroke associated with ibuprofen, and is also associated with a decrease in the number of myocardial infarcts compared with the control group.
One study found that high-dose naproxen induced complete suppression of platelet thromboxane throughout the dosing interval and did not appear to increase the risk of cardiovascular disease (CVD), whereas non-aspirin high dose NSAID regimens had only a temporary effect on COX platelets. 1 and is associated with a small but definite vascular danger. In contrast, naproxen was associated with higher rates of upper gastrointestinal bleeding complications compared with other NSAIDs.
Interactions
Drug interactions
Naproxen can interact with antidepressants, lithium, methotrexate, probenecid, warfarin and other blood thinners, heart medications or blood pressure, including diuretics, or steroidal drugs such as prednisone.
NSAIDs such as naproxen can disrupt and reduce the effectiveness of SSRI antidepressants, as well as increase the risk of bleeding greater than the risk of individual bleeding from both classes of agents when taken together. Naproxen is not contraindicated in the presence of SSRIs, although concurrent drug use should be performed with caution.
Drug-food interactions
Alcohol consumption increases the risk of gastrointestinal bleeding when combined with NSAIDs such as naproxen in a dose-dependent manner (ie, the higher the dose of naproxen, the higher the risk of bleeding). The highest risk for people who are heavy drinkers.
Pharmacology
Action mechanism
Naproxen works by reversibly inhibiting both COX-1 and COX-2 enzymes as non-selective coxibs. This results in inhibition of prostaglandin synthesis. Prostaglandins act as signaling molecules inside the body, inducing inflammation. Thus, by inhibiting COX-1/2, naproxen induces an anti-inflammatory effect.
Pharmacokinetics
Naproxen is a minor substrate of CYP1A2 and CYP2C9. It is extensively metabolized in the liver to 6-O-desmethylnaproxen, and both the parent drug and the desmethyl metabolite undergo further metabolism for each conjugated acylglucuronide metabolite. Analysis of two clinical trials showed that the time of naproxen reached peak plasma concentration occurred between 2-4 hours after oral administration, although naproxen sodium reached peak plasma concentrations within 1-2 hours.
Pharmacogenetic
Pharmacogenetic naproxen has been studied in an effort to better understand its side effects. In 1998, small pharmacokinetic studies (PK) failed to show that differences in the patient's ability to clean naproxen from the body could explain the difference in risk of patients experiencing the adverse effects of serious gastrointestinal bleeding when taking naproxen. However, the study failed to explain the differences in CYP2C9 activity, a drug metabolic enzyme responsible for clearing naproxen. Studies of the association between CYP2C9 genotype and induced NSAID-induced bleeding gastrointestinal have shown that genetic variants in CYP2C9 that reduce major CYP2C9 substrate cleansing (such as naproxen) increase the risk of NSAID-induced gastrointestinal bleeding, especially for homozygous defect variants.
As of October 2017, there is no recommendation for routine CYP2C9 testing for naproxen.
Chemistry
Naproxen is a member of the 2-arylpropionate (profen) family of NSAIDs. Free acid is a white, odorless, white-colored crystalline substance. It is fat soluble and practically insoluble in water. It has a melting point of 152-155 Â ° C.
Synthesis
Naproxen has been manufactured industrially by Syntex ranging from 2-naphthol as follows:
Society and culture
Brand name
Naproxen and naproxen sodium are marketed under various brand names, including: Synflex, Aleve, Accord, Anaprox, Antalgin, Apranax, Feminax Ultra, Flanax, Inza, Maxidol, Midol Extended Relief, Nalgesin, Naposin, Naprelan, Naprogesic, Naprosyn, Narocin, Pronaxen , Proxen, Soproxen, MotriMax, and Xenobid. It is also available as a combination of naproxen/esomeprazole magnesium in delayed release tablets under the brand name Vimovo.
Access restricted
Syntex first marketed naproxen in 1976 as a prescription drug Naprosyn. They first marketed naproxen sodium under the brand name Anaprox in 1980. It remains the only drug prescribed in most parts of the world. In the United States, the Food and Drug Administration (FDA) approved it as an over-the-counter (OTC) drug in 1994. OTC preparations in the US are mainly marketed by Bayer HealthCare under the brand name Aleve and generic store brand formulations in 220 mg tablets. In Australia, the 275 mg sodium naproxen package is pharmaceutical drug Schedule 2, with a maximum daily dose of five tablets or 1375 mg. In the UK, 250 mg of naproxen was approved for OTC sales under the Feminax Ultra trademark in 2008, for the treatment of primary dysmenorrhea in women aged 15 to 50 years. In the Netherlands, 220 mg and 275 mg tablets are available at the OTC drugstore, 550 mg only OTC in pharmacies. Aleve became available freely in most provinces in Canada on July 14, 2009, but not British Columbia, Quebec or Newfoundland and Labrador; it later became OTC available in British Columbia in January 2010.
Research
Naproxen may have antiviral activity against influenza. In particular, it blocks the RNA binding groove of the viral nucleoproteins, preventing the formation of the ribonucleotoprotein complex - thus taking the viral nucleoprotein out of the circulation.
Veterinary use
Use in horses
Naproxen is administered orally to the horse at a dose of 10 mg/kg, and has been shown to have a wide margin of safety (no toxicity when administered at 3 times the recommended dose of 42 days). It is more effective for miositis than commonly used NSAID phenylbutazone, and has shown excellent results for the treatment of rhabdomyolysis during activity, muscle damage, but less commonly used for musculoskeletal disease.
References
External links
- CID 1302 from PubChem
- EINECS number 244-838-7
- MedlinePlus Information about naproxen
- FDA Drug Prescription Information at drugs.com
- The FDA statement on Naproxen, released December 20, 2004
- Alzheimer's Disease Anti-Inflammatory Prevention Trial
- Forbes article (revealing the point of view that the risk of a heart attack or stroke is too exaggerated)
- NSAIDs for Which Heart Disease Patients? - Medscape
- US. National Drug Library: Drug Information Portal - Naproxen
- Aleve Med Daily
- Naproxen is bound to proteins in GDP
Source of the article : Wikipedia
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