Naproxen

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[edit] BRAND NAMES

[edit] STRUCTURE

Naproxen.jpg

[edit] MECHANISM OF ACTION

Naproxen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and antirheumatic properties. Naproxen inhibits the enzyme, cyclooxygenase (COX), an early component of the arachidonic acid cascade, resulting in the reduced formation of prostaglandins and thromboxanes. Prostaglandins act as messenger molecules in the process of inflammation. The sodium salt of naproxen has been developed as a more rapidly absorbed formulation of naproxen for use as an analgesic.

[edit] INDICATIONS

  • temporarily reduces fever
  • temporarily relieves minor aches and pains due to:
    • minor pain of arthritis (Rheumatoid arthritis and osteoarthritis)
    • muscular aches
    • backache
    • dysmenorrhea (menstrual cramps)
    • headache
    • toothache
    • Acute gout
    • the common cold

[edit] DOSAGE

  • Naproxen sodium 220 mg (naproxen 200 mg):
    • Adults and children 12 years and older:
    • take 1 tablet every 8 to 12 hours while
    • for the first dose you may take 2 tablets within the first hour
    • do not exceed 2 tablets in any 8- to 12-hour period
    • do not exceed 3 tablets in a 24-hour period

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Naproxen or to any other NSAID
  • right before or after heart surgery

[edit] WARNINGS AND PRECAUTIONS

  • Naproxen sodium may cause a severe allergic reaction, especially in people allergic to aspirin
  • Stomach bleeding warning: NSAIDs may cause severe stomach bleeding, The chance is higher in: patients age 60 or older, history of stomach ulcers or bleeding problems, patients taking a blood thinning (anticoagulant) or steroid drug, patients taking another NSAIDs (aspirin, ibuprofen, or others), patients drinking 3 or more alcoholic drinks every day while on naproxen, patients taking Naproxen more or for a longer time than directed
  • Cardiovascular Risk: NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk
  • Hypertension: Use with caution in patients with hypertension (NSAIDs, can lead to onset of new hypertension or worsening of pre-existing hypertension)
  • Congestive Heart Failure and Edema: Fluid retention, edema, and peripheral edema have been observed in some patients taking NSAIDs. Naproxen should be used with caution in patients with fluid retention or heart failure.
  • NSAIDs should be used with caution in patients with a history of inflammatory bowel disease (ulcerative colitis, Crohn’s disease) as their condition may be exacerbated.

[edit] INTERACTIONS

  • Diuretics, ACE inhibitors or Beta blockers : concomitant use of diclofenac with diuretics or antihypertensive agents (e.g. beta blockers, angiotensin converting enzyme (ACE) inhibitors, Angiotensin Receptor Blockers (ARBs)) may cause a decrease in their antihypertensive effect and may increase the risk of renal dysfunction, especially in patients with pre-existing poor renal function. Therefore, the combination should be administered with caution and patients, especially the elderly, should have their blood pressure periodically monitored.
  • Lithium carbonate: If used concomitantly, Naproxen may raise plasma concentrations of lithium. Monitoring of the serum lithium level is recommended.
  • Methotrexate: Caution is recommended when NSAIDs, including Naproxen, are administered less than 24 hours before or after treatment with methotrexate, since blood concentrations of methotrexate may rise and the toxicity of this substance be increased.
  • Warfarin: Caution is recommended since concomitant administration could increase the risk of bleeding.
  • Selective serotonin reuptake inhibitors (SSRIs): Concomitant administration of systemic NSAIDs, including Naproxen, and SSRIs may increase the risk of gastrointestinal bleeding
  • Concomitant administration of some antacids (magnesium oxide or aluminum hydroxide) and sucralfate can delay the absorption of naproxen
  • Aspirin, Ibuprofen, other systemic NSAIDs or Corticosteroids: Concomitant administration of diclofenac and other systemic NSAIDs or corticosteroids is not recommended, because of the cumulative risks of inducing serious NSAID-related adverse events
  • NSAIDs inhibit platelet aggregation and have been shown to prolong bleeding time. Patients who have coagulation disorders or are receiving anticoagulation therapy (e.g. Heparin, Warfarin, Acenocoumarol) may be at incresed risk of bleeding.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Because of the known effects of nonsteroidal anti-inflammatory drugs on the fetal cardiovascular system (closure of ductus arteriosus), use during pregnancy (particularly late pregnancy) should be avoided.
  • Nursing Mothers: 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. Because of the possible adverse effects of prostaglandin-inhibiting drugs on neonates, use in nursing mothers should be avoided.

[edit] SIDE EFFECTS

The most frequently reported adverse experiences in approximately 1% to 10% of patients are:

  • Gastrointestinal: heartburn, abdominal pain, nausea, constipation, diarrhea, dyspepsia, stomatitis
  • Central Nervous System: headache, dizziness, drowsiness, lightheadedness, vertigo
  • Dermatologic: pruritus, skin eruptions, ecchymoses, sweating, purpura
  • Special Senses: tinnitus, visual disturbances, hearing disturbances
  • Cardiovascular: edema, palpitations
  • General: dyspnea, thirst


Serious side effects include:

  • heart attack
  • stroke
  • high blood pressure
  • heart failure from body swelling (fluid retention)
  • kidney problems including kidney failure
  • bleeding and ulcers in the stomach and intestine
  • low red blood cells (anemia)
  • life-threatening skin reactions
  • life-threatening allergic reactions
  • liver problems including liver failure
  • asthma attacks in people who have asthma

[edit] RELATED LINKS

NSAIDs: MOAs and Clinical Considerations

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Non-steroidal anti-inflammatory drugs (NSAIDs)
Non-selective (COX-1 and COX-2 inhibitors) Aceclofenac   Acetylsalicylic acid   Benzydamine   Diclofenac   Flurbiprofen   Ibuprofen   Indometacin   Ketoprofen   Ketorolac   Ketorolac   Lornoxicam   Mefenamic acid   Morniflumate   Nabumetone   Naproxen   Niflumic acid   Piroxicam   Tenoxicam
Relatively COX-2 selective Meloxicam   Nimesulide
COX-2 selective inhibitors (Coxibs) Celecoxib   Etoricoxib   Parecoxib
Ophthalmic NSAIDs Bromfenac (ophthalmic)   Diclofenac (ophthalmic)   Flurbiprofen (ophthalmic)   Ketorolac (ophthalmic)   Nepafenac (ophthalmic)
Veterinary use Carprofen   Deracoxib   Firocoxib   Mavacoxib   Robenacoxib
Antimigraine preparations
5 HT1 agonists (Triptans) Almotriptan (Almogran, Axert)   Eletriptan (Relpax)   Frovatriptan (Frova, Migard, Menatriptan)   Rizatriptan (Maxalt)   Sumatriptan (Imigran)   Zolmitriptan (Zomig)
Ergot alkaloids Dihydroergotamine   Ergotamine
NSAIDs/ Analgesics Indometacin   Acetylsalicylic acid (Aspirin)   Diclofenac (Voltaren)   Ibuprofen (Advil, Brufen, Dolgit, Nurofen)   Ketorolac (Toradol)   Naproxen (Naprosyn, Aleve)   Nimesulide   Paracetamol (Efferalgan, Panadol...)
Prophylaxis Cinnarizine (Stugeron, Stugeron forte)   Flunarizine (Sibelium)   Nifedipine (Adalat)   Pizotifen   Propranolol (Inderal)   Topiramate (Topamax)