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DRUG NEWS

ANTI-INFLAMMATORY DRUGS - I N T R O D U C T I O N

Non-steroidal Anti-inflammatory Drugs (NSAIDs)


Non-steroidal anti-inflammatory drugs are medications which have analgesic, antipyretic and, with higher doses or used over a period of time, anti-inflammatory effects. The term "non-steroidal" is used to distinguish these drugs from steroids which have, among many others, an anti-inflammatory action. (1)

The most prominent members of this group of drugs are aspirin, ibuprofen, and naproxen partly because they are available over-the-counter in many areas. (1) Most NSAIDs act as non-selective inhibitors of the enzyme cyclooxygenase (Cox-1 and Cox-2) which catalyses the formation of prostaglandins and thromboxane which in turn promote inflammation, pain and fever, support the blood clotting function of platelets and protect the lining of the stomach from the damaging effects of acid. (2)

Cox-2 selective inhibitors form of NSAIDs directly targets Cox-2, thus inhibiting only the formation of prostaglandins responsible for inflammation and pain and sparing prostaglandins responsible for maintenance and protection of the gastrointestinal tract, thus reducing the risk of peptic ulceration. (3)

NSAIDs are used primarily to treat inflammation, mild to moderate pain, and fever. Specific uses include the treatment of headaches, arthritis, sports injuries, and menstrual cramps. Aspirin is used to inhibit the clotting of blood and prevent strokes and heart attacks in individuals at high risk. NSAIDs are also included in many cold and allergy preparations. (2)

The widespread use of NSAIDs is associated with many side effects. The main adverse effects are gastro-intestinal, cardiac and renal effects. The common gastro-intestinal adverse reactions include: nausea/vomiting, dyspepsia, gastric ulceration, bleeding and even ulcer perforation. (2)

As for cardiac adverse effects, NSAIDs (except of low dose aspirin) may increase the risk of potentially fatal heart attacks, thrombosis and stroke especially in case of Cox-2 inhibitors through the relative increase in thromboxane. This risk may increase with duration of use and in patients who have underlying risk factors for heart and blood vessel disease. Rofecoxib (commonly known as Vioxx) was voluntarily taken off the market by Merck & Co., Inc. in 2004 due to safety concerns of an increased risk of cardiovascular events in patients on Vioxx (2), (3) & (4). Also on April 2005, the FDA asked Pfizer to voluntarily remove Bextra (valdecoxib) from the market.

NSAIDs have renal adverse drug reactions due to changes in renal haemodynamics, ordinarily mediated by prostaglandins, leading to altered renal function which includes salt and fluid retention, hypertension and even renal impairment especially in combination with other nephrotoxic agents. (1)

On April 28, 2009 the FDA issued a warning on NSAIDs use and urged the pharmaceutical manufacturers to include warnings on all their over-the-counter painkillers and fever reducers containing NSAIDs and acetaminophen according to the new FDA rules. The purpose of the new labeling is to raise awareness of potential stomach bleeding from NSAIDs and liver damage from acetaminophen. (5)

References:

  • http://en.wikipedia.org/wiki/Non-steroidal_anti-inflammatory_drug (1)
  • www.medicinenet.com/nonsteroidal_antiinflammatorydrugs/article.htm# (2)
  • http://en.wikipedia.org/wiki/COX-2_inhibitor (3)
  • www.fda.gov/Drugs/Drugsafety/ (4)
  • www.bio-medicine.org/medicine-news-1/FDA-Adds-New-Label-Warnings-to-Over-the-counter-Painkillers-43912-1/ (5)
 
     
IOMS Newsletter - 12 August 2009  
Issue No. 002/09
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