Pharmacy

Sunday 13 December, 23:26

NSAIDs: efficacy and safety

Current recommendations for the use of NSAIDs

NSAIDs: efficacy and safety

Non-steroidal anti-inflammatory drugs or NSAIDs (such as aspirin, ibuprofen, naproxen and meloxicam) are among the most widely used medicines in the world, because of their anti-inflammatory and analgesic effects.

 

NSAIDs are characterized by the common basic property to inhibit the pro-inflammatory enzyme cyclooxygenase (COX), although they greatly differ in their efficacy and safety. COX enzyme exists as two isoforms, COX-1 (constitutive isoenzyme) and COX-2 (inducible isoenzyme). While COX-1 is responsible for the synthesis of prostaglandins involved in normal homeostatic processes of the kidney, gut (e.g. gastric cytoprotection), endothelium and platelets, COX-2 is induced in response to inflammatory stimuli and is responsible for the production of prostaglandins involved in the generation of pain and inflammation.

 

Based on their selectivity to inhibit the COX isoenzymes, NSAIDs are divided into two broad categories: 1) traditional nonselective NSAIDs (tNSAIDs, such as aspirin), that inhibit both COX-1 and COX-2; 2) selective COX-2 inhibitors (such as celecoxib and rofecoxib).

 

Despite of their efficacy in relieving pain and inflammation, the chronic use of tNSAIDs is associated with, among other dangers, a significant risk of gastrointestinal adverse effects, such as bleeding, ulcers and perforation. The ulcerogenic effects of traditional nonselective NSAIDs are due to their inhibition of COX-1 in the gastric mucosa.

 

That’s why pharmacological research has focused on the development of new, more selective NSAIDs (namely selective COX-2 inhibitors), in order to circumvent these relative disadvantages. However serious concerns have been recently raised about the potential cardiovascular toxicity (dose- and duration-related) of COX-2 inhibitors, which is just due to the selective inhibition of COX-2 isoenzyme.

 

In the light of this new finding, the current recommendations for the use of NSAIDs may be summarized schematically as follow:

 

1) due to the potential serious adverse effects associated with chronic use, both tNSAIDs and COX-2 inhibitors should be prescribed with the lowest therapeutic dose and for the shortest therapy duration

 

2) COX-2 inhibitors should not be prescribed for the treatment of cardiovascular high-risk patients (e.g. patients with a history of stroke or congestive heart failure)

 

3) treatment with tNSAIDs alone in patients under 65 years of age is appropriate, if they don’t have gastrointestinal risk factors

 

4) patients above 65 years of age and patients with gastrointestinal risk factors should receive a combination of tNSAIDs and gastrointestinal protectors (such as proton pump inhibitors and antacids) or, alternatively, selective COX-2 inhibitors

 

By Chiara De Carli 

Category: Pharmacy


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