Non-steroidal anti-inflammatory analgesic
Naproxen sodium is a non-steroidal anti-inflammatory analgesic drug which is more tolerable to human, belonging to the phenylpropionic acid compounds. It plays anti-inflammatory effect by inhibiting prostaglandin synthesis.It is absorbed rapidly after oral administration and the plasma reached the peak concentration within 2 to 4 hours. Food has little effect on the rate of absorption. Naproxen and plasma protein are highly binded(99%); the plasma concentration is between 23~40mcg/ml. The metabolic process is demethylation and then combining with glucuronide; the elimination half-life is 12 to 15 hours, mainly excreted by the urine. Clinical application is to relieve a variety of mild to moderate degree of pain, such as tooth extraction and other postoperative pain, primary dysmenorrhea and headache. It is also used for rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, juvenile arthritis, tendinitis, bursitis and acute gouty arthritis; it also plays a role in arthritis pain, swelling and activity restricted symptom. Psoriatic arthritis and Reiter's syndrome can also be treated with this product. Compared with ibuprofen, fenoprofen, aspirin, sulindac and indomethacin, the symptom relief effect was similar, but the incidence and severity of adverse reactions in the gastrointestinal and neurological systems were low. In addition, this product is also the same as aspirin which can inhibit platelet aggregation and prolong bleeding time; but the effect is reversible, and can be restored after stopping.
Naproxen sodium and plasma protein binding rate is high (99%), and other protein-binding drugs can be replaced by its joint out. Therefore, the acceptance of these drugs (such as oral anticoagulants, sulfonylurea, hydantoins) people should observe the interaction effects. At the same time the application of probenecid, naproxen can increase the plasma concentration, half-life period. Magnesium hydroxide, aluminum can make this product absorption rate slightly lower; sodium bicarbonate can make it higher.
Uses
Used as anti-inflammatory analgesic
Chemical Properties
White Powder
Uses
An anti-inflammatory, analgesic, antipyretic. A non-steroidal anti-inflammatory
Uses
Naproxen (Aleve, Anaprox) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively
Uses
A cyclooxygenase inhibitorNaproxen sodium acts as a nonselective inhibitor of Cox-1 and Cox-2. It serves as an anti-inflammatory agent with analgesic and antipyretic properties. Further, it is used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea and acute gout.
Definition
ChEBI: The sodium salt of naproxen.
brand name
Aleve (Bayer); Anaprox (Roche);Naprelan (Stat Trade).
General Description
Naproxen sodium (NS) is a sodium salt of propionic acid derivative and demonstrates analgesic, anti-pyretic, and anti-inflammatory properties. It exhibits efficiency in being used as an indomethacin in the treatment of acute musculoskeletal disorders. It belongs to the group of nonsteroidal anti-inflammatory drugs (NSAIDS) and acts by inhibiting the activity of both the cyclooxygenase enzymes, COX-1 & COX-2 and further blocking the synthesis of certain prostaglandins. It is administered in the treatment of ankylosing spondylitis, osteoarthritis, rheumatoid disorders, acute gout, mild to moderate pain, tendonitis, bursitis, dysmenorrhea, fever, and migraine headache. Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
Biological Activity
Non-selective cyclooxygenase (COX) inhibitor that displays anti-inflammatory, antipyretic and analgesic effects. Has a neuroprotective role against colchicine-induced cognitive impairment and oxidative stress.
Biochem/physiol Actions
Cyclooxygenase (Prostaglandin H synthase 1 and 2) inhibitor.
References
[1]. mendias cl, tatsumi r and allen re. role of cyclooxygenase-1 and -2 in satellite cell proliferation, differentiation, and fusion. muscle nerve, 2004, 30(4):497-500.
[2]. hinz b, cheremina o, besz d, et al. impact of naproxen sodium at over-the-counter doses on cyclooxygenase isoforms in human volunteers. int j clin pharmacol ther, 2008, 46(4):180-6.
[3]. sances g, martignoni e, fioroni l, et al. naproxen sodium in menstrual migraine prophylaxis: a double-blind placebo controlled study. headache, 1990, 30(11):705-9.
[4]. tavolari s, bonafè m, marini m, et al. licofelone, a dual cox/5-lox inhibitor, induces apoptosis in hca-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade. carcinogenesis, 2008, 29(2):371-80.
