Naproxen Sodium 500mg Best Pain Killer Best for Back Pain /Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout. Naproxen is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of naproxen is as a Cyclooxygenase Inhibitor. The chemical classification of naproxen is Nonsteroidal Anti-inflammatory Compounds.
Naproxen is a propionic acid derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities. Naproxen inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of naproxen. Naproxen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation.
Mechanism of Action of Naproxen
Naproxen has pharmacologic actions similar to those of other prototypical nonsteroidal anti-inflammatory agents (NSAIAs). The drug exhibits anti-inflammatory, analgesic, and antipyretic activity. The exact mechanisms have not been clearly established, but many of the actions appear to be associated principally with the inhibition of prostaglandin synthesis. Naproxen inhibits the synthesis of prostaglandins in body tissues by inhibiting cyclooxygenase; at least 2 isoenzymes, cyclooxygenase-1 (COX-1) and -2 (COX-2) (also referred to as prostaglandin G/H synthase-1 (PGHS-1) and -2 (PGHS-2), respectively), have been identified that catalyze the formation of prostaglandins in the arachidonic acid pathway. Naproxen, like other prototypical NSAIAs, inhibits both COX-1 and COX-2. Although the exact mechanisms have not been clearly established, NSAIAs appear to exert anti-inflammatory, analgesic, and antipyretic activity principally through inhibition of the COX-2 isoenzyme; COX-1 inhibition presumably is responsible for the drugs’ unwanted effects on GI mucosa and platelet aggregation.
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The anti-inflammatory, analgesic, and antipyretic effects of naproxen and other nonsteroidal anti-inflammatory agents (NSAIAs), including selective inhibitors of COX-2 (e.g., celecoxib, rofecoxib), appear to result from inhibition of prostaglandin synthesis. While the precise mechanism of the anti-inflammatory and analgesic effects of NSAIAs continues to be investigated, these effects appear to be mediated principally through inhibition of the COX-2 isoenzyme at sites of inflammation with subsequent reduction in the synthesis of certain prostaglandins from their arachidonic acid precursors. Naproxen stabilizes lysosomal membranes and inhibits the response of neutrophils to chemotactic stimuli. The drug does not possess glucocorticoid or adrenocorticoid-stimulating properties.
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Indications of Naproxen
- For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, tendinitis, bursitis, and acute gout. Also for the relief of mild to moderate pain and the treatment of primary dysmenorrhea.
- Fibromyalgia
- Pain due to road traffic accident.
- A headache
- Severe fever
- Chest pain
- A migraine headache
- Acute pain due to trauma
- Rheumatoid arthritis
- Osteoarthritis
- Ankylosing spondylitis
- Accidental pain
- Acute abdominal pain due to gastritis/appendicitis
- Pain due to the especially musculoskeletal system
- Lumbago
- Low back pain
- PLID
- Polyarthralgia
- Muscles stiffness in nerve diseases
- Morning stiffness
- Multiple joint pain
- Muscles stiffness in the spinal cord
- Periarthritis of scapulohumeral
- For the management of primary dysmenorrhea.
Therapeutic Indications of Naproxen
- Anti-Inflammatory Agents, Non-Steroidal; Cyclooxygenase Inhibitors; Gout Suppressants
- Naproxen and its salt are used to relieve postoperative pain (including that associated with dental surgery), postpartum pain, primary dysmenorrhea, pain following insertion of an intrauterine contraceptive device, orthopedic pain, headache (including a migraine), and visceral pain associated with cancer.
- Naproxen sodium also may be used for self-medication to provide temporary relief of minor aches and pains associated with the common cold, headache, toothache, muscular aches, and backache.
- Naproxen has been used in the symptomatic management of osteitis deformans (Paget’s disease of bone) and Bartter’s syndrome.
- When used in the treatment of rheumatoid arthritis or juvenile rheumatoid arthritis, naproxen has relieved pain and stiffness, reduced swelling, and improved mobility and grip strength. In the treatment of osteoarthritis, naproxen has relieved pain and stiffness and improved knee joint function.
- Naproxen appears to be the only palliative in these conditions and has not been shown to permanently arrest or reverse the underlying disease process. Naproxen sodium also may be used for self-medication to provide temporary relief of minor aches and pains associated with arthritis.
- Naproxen and naproxen sodium are used for anti-inflammatory and analgesic effects in the symptomatic treatment of rheumatoid arthritis, osteoarthritis, juvenile rheumatoid arthritis, and ankylosing spondylitis.
- Naproxen also is used in combination with lansoprazole for the symptomatic treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis in patients with a history of documented gastric ulcer who require continued use of an NSAIA.
- Naproxen and naproxen sodium are used to relieve mild to moderately severe pain. Conventional (immediate-release) and delayed-release (enteric-coated) tablets and suspension formulations of naproxen or naproxen sodium are used for anti-inflammatory and analgesic effects in the symptomatic treatment of rheumatoid arthritis, osteoarthritis, juvenile rheumatoid arthritis, and ankylosing spondylitis.
- Conventional (immediate-release) tablets and suspension formulations of naproxen or naproxen sodium also are used for the symptomatic treatment of tendinitis, bursitis, acute gout, pain, and primary dysmenorrhea. Suspension formulations of naproxen are preferred for the management of juvenile arthritis since this formulation provides maximum dosage flexibility. Because of the delayed-release properties of enteric-coated naproxen tablets, this formulation is not recommended for the management of acute pain.
- Extended-release naproxen sodium tablets are used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, tendinitis, bursitis, acute gout, mild to moderately severe pain, and primary dysmenorrhea. (Naproxen 250 mg is approximately equivalent to naproxen sodium 275 mg.) Naproxen sodium also may be used for self-medication for anti-inflammatory and analgesic effects to provide temporary relief of minor aches and pains, including those associated with arthritis, and of dysmenorrhea and for its antipyretic effect to reduce fever.
- Naproxen has been used effectively to relieve pain, fever, redness, swelling, and tenderness in patients with acute gouty arthritis.
- When used in patients with ankylosing spondylitis, naproxen has relieved night pain, morning stiffness, and pain at rest. In a limited number of controlled studies, the anti-inflammatory and analgesic effects of usual dosages of naproxen in the symptomatic treatment of ankylosing spondylitis were greater than those of placebo and comparable to those of usual dosages of aspirin or phenylbutazone (no longer commercially available in the US).
Contra-Indications of Naproxen
- Allergy to medicines called opioid antagonists (e.g. codeine, morphine);
- Active peptic ulcer
- Allergic to thiocolchicoside
- Asthma
- Pregnant
- Urticaria
- Concurrent peptic ulcer, or history of ulcer disease
- Allergy to indomethacin, aspirin, or other NSAIDs
- Patients with nasal polyps reacting with angioedema to other NSAIDs
- Children under 2 years of age (with the exception of neonates with patent ductus arteriosus)
- Some painkillers, including opioid painkillers;
- Hypnotic drugs;
- Psychotropic drugs;
- Used monoamine oxidase inhibitors (MAOIs) such as phenelzine or tranylcypromine
- Epilepsy;
- Addiction or are recovering from addiction to another medication.
- History of peptic ulcer disease,
- Gastrointestinal bleeding,
- Severe pre-existing renal and liver damage
- Caution: pre-existing bone marrow damage (frequent blood cell counts are indicated)
- Caution: bleeding tendencies of unknown origin
- Caution: Parkinson’s disease, epilepsy, psychotic disorders
- Patients who have a patent ductus arteriosus dependent heart defect (such as transposition of the great vessels)
- Significant hypertension (high blood pressure)
- Concomitant administration of lithium salts (such as lithium carbonate)
- History of gastric bypass surgery
- Renal impairment,Hepatic impairment.
- Alcohol intolerance,
- Renal impairment,
- Cerebrovascular bleeding,
- Heart failure,
- Coagulation disorders,
Dosage of Naproxen
Strengths: 250 mg , 275 mg; 500 mg; 375 mg; 375 mg, 125 mg/5 mL; 550 mg;
Ankylosing Spondylitis
Immediate Release Tablets and Suspensions
- 250 mg to 500 mg (naproxen) or 275 mg to 550 mg (naproxen sodium) orally twice a day
Controlled Release
- 750 mg to 1000 mg orally once a day
Delayed Release
- 375 mg to 500 mg orally twice a day
Osteoarthritis
Immediate Release Tablets and Suspension
- 250 mg to 500 mg (naproxen) or 275 mg to 550 mg (naproxen sodium) orally twice a day
Controlled Release
- 750 mg to 1000 mg orally once a day
Delayed Release
- 375 mg to 500 mg orally twice a day
Rheumatoid Arthritis
Immediate Release Tablets and Suspension
- 250 mg to 500 mg (naproxen) or 275 mg to 550 mg (naproxen sodium) orally twice a day
Controlled Release
- 750 mg to 1000 mg orally once a day
Delayed Release
- 375 mg to 500 mg orally twice a day
Acute Gout
Immediate Release Tablets and Suspension
- Initial dose: 750 mg (naproxen) or 825 mg (naproxen sodium) orally once on first day of attack
- Following initial dose: 250 mg (naproxen) or 275 mg (naproxen sodium) orally every 8 hours until attack subsides
Controlled Release
- 1000 mg to 1500 mg orally once on first day of attack, followed by 1000 mg orally once a day until attack subsides
Bursitis
Immediate Release (naproxen sodium)
- 550 mg orally once, followed by 275 mg orally every 6 to 8 hours or 550 mg orally every 12 hours as needed
- Maximum dose: Initial total daily dose not to exceed 1375 mg; thereafter, not to exceed 1100 mg/day
Controlled Release
- 1000 mg orally once a day
- For patients requiring additional analgesia, may increase to 1500 mg orally once a day for a limited time; thereafter, total daily dose should not exceed 1000 mg/day
Tendonitis
Immediate Release (naproxen sodium)
- 550 mg orally once, followed by 275 mg orally every 6 to 8 hours or 550 mg orally every 12 hours as needed
- Maximum dose: Initial total daily dose not to exceed 1375 mg; thereafter, not to exceed 1100 mg/day
Controlled Release
- 1000 mg orally once a day
- For patients requiring additional analgesia, may increase to 1500 mg orally once a day for a limited time; thereafter, total daily dose should not exceed 1000 mg/day
Dysmenorrhea
Immediate Release (naproxen sodium)
- 550 mg orally once, followed by 275 mg orally every 6 to 8 hours or 550 mg orally every 12 hours as needed
- Maximum dose: 1375 mg/day initial total daily dose; thereafter, not to exceed 1100 mg/day
Controlled Release
- 1000 mg orally once a day
- For patients requiring additional analgesia, may increase to 1500 mg orally once a day for a limited time; thereafter, total daily dose should not exceed 1000 mg/day
Over the Counter
- 220 mg orally every 8 to 12 hours while symptoms persist
- May take 440 mg orally once in the first hour if needed
- Maximum dose: 440 mg (in any 8 to 12 hour period); 660 mg (in any 24 hour period)
Pain
Immediate Release (naproxen sodium)
- 550 mg orally once, followed by 275 mg orally every 6 to 8 hours or 550 mg orally every 12 hours as needed
- Maximum dose: 1375 mg/day initial total daily dose; thereafter, not to exceed 1100 mg/day
Controlled Release
- 1000 mg orally once a day
- For patients requiring additional analgesia, may increase to 1500 mg orally once a day for a limited time; thereafter, total daily dose should not exceed 1000 mg/day
Over the Counter
- 220 mg orally every 8 to 12 hours while symptoms persist
- May take 440 mg orally once in the first hour if needed
- Maximum dose: 440 mg (in any 8 to 12 hour period); 660 mg (in any 24 hour period)
Fever
Over the Counter
- 220 mg orally every 8 to 12 hours while symptoms persisttake 440 mg orally once in the first hour if needed
- Maximum dose: 440 mg (in any 8 to 12 hour period); 660 mg (in any 24 hour period)
Pediatric Fever
Over the Counter
- 12 years or older: 220 mg orally every 8 to 12 hours while symptoms persist
- May take 440 mg orally once in the first hour if needed
- Maximum dose: 440 mg (in any 8 to 12 hour period); 660 mg (in any 24 hour period)
Pediatric Pain
Over the Counter
- 12 years or older: 220 mg orally every 8 to 12 hours while symptoms persist
- May take 440 mg orally once in the first hour if needed
- Maximum dose: 440 mg (in any 8 to 12 hour period); 660 mg (in any 24 hour period)
Pediatric Juvenile Rheumatoid Arthritis
Immediate Release Tablets and Suspension
- 2 years or older: 5 mg/kg orally twice a day
Side Effects of Naproxen
The most common
- GI disorders (e.g. dyspepsia, abdominal pain, nausea, vomiting, diarrhoea, flatulence, constipation,, ulcerative stomatitis, ),indigestion,
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Drowsiness and lightheadedness
- Nausea and vomiting
- joint pain
- Nausea and vomiting
- Severe stomach ache
- Severe diarrhea
- Vaginal thrush
- Skin rash
- Headache
- Chest pain
- Diarrhea or loose stools
- Difficulty with breathing
- Dizziness
- Heartburn
- Muscle pain
More common
- Abdominal or stomach pain,
- Chills or fever
- Headache,
- Joint or back pain
- Muscle aching or cramping
- Muscle pains or stiffness
- Chest pressure or squeezing pain in chest
- Excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- Constipation
- Diarrhoea
- Loss of muscle coordination
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Drowsiness
Rare
- Anxiety
- change in vision
- seizures
- abnormal or fast heart rate
- weight loss
- chest pain or tightness
- confusion
- cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats, fainting
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- hallucinations
- headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- muscle pains or stiffness
- chest pressure or squeezing pain in chest
- discomfort in arms, shoulders, neck or upper back
- pain or discomfort in the chest, upper stomach, or throat
- pale or blue lips, fingernails, or skin
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- unusual drowsiness, dullness, or feeling of sluggishness
Drug Interactions of Naproxen
Naproxen may interact with following drugs, supplements & may change the efficacy of drugs
- antacids (e.g., aluminum hydroxide, calcium carbonate, magnesium hydroxide)
- bisphosphonates (e.g., alendronate, etidronate, risedronate, zoledronic acid)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine,risperidone)
- angiotensin converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
- angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
- beta-adrenergic blockers (e.g., metoprolol, atenolol)
- baclofen
- barbiturates (e.g., butalbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- celecoxib
- cilostazol
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- clopidogrel
- corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- 5-ASA medications (e.g, sulfasalazine)
- glucosamine
- haloperidol
- heparin
- methotrexate
- multivitamins
- other non-steroidal anti-inflammatory medications (NSAIDs;e.g., diclofenac, ibuprofen, ketorolac, naproxen)
- Omega-3 fatty acids
- phenytoin
- phenobarbital
- pentoxifylline
- quinolone antibiotics (e.g., ciprofloxacin, ofloxacin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine,fluoxetine, paroxetine, sertraline)
- serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g., duloxetine, venlafaxine)
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- warferin
Pregnancy & Lactation of Naproxen
FDA Pregnancy Category C
Pregnancy
There are no adequate and well-controlled studies in pregnant women; data from observational studies regarding potential embryofetal risks of NSAID use in women in the first or second trimesters of pregnancy are inconclusive; NSAIDs inhibit prostaglandin synthesis, cause delayed parturition, and increase the incidence of stillbirth
Lactation
The naproxen anion has been found in the milk of lactating women at a concentration equivalent to approximately 1% of maximum naproxen concentration in plasma; developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed infant from therapy or from the underlying maternal condition
Before taking this medicine
Naproxen may also cause stomach or intestinal bleeding, which can be fatal. These conditions can occur without warning while you are using this medicine, especially in older adults.
You should not use naproxen if you are allergic to it, or if you have ever had an asthma attack or severe allergic reaction after taking aspirin or an NSAID.
Ask a doctor or pharmacist if it is safe for you to use this medicine if you have:
- heart disease, high blood pressure, high cholesterol, diabetes, or if you smoke;
- a history of heart attack, stroke, or blood clot;
- a history of stomach ulcers or bleeding;
- asthma;
- liver or kidney disease; or
- fluid retention.
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no ris.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
