NSAIDs

NSAIDs are widely used for reducing inflammation, analgesia, and reducing fever.

  • NSAIDs can be administered systemically (oral, IV, suppository), or locally (gel, ointment).
  • The combination of two systemic NSAIDs is contraindicated.

Mechanism of action

They work by inhibiting the activity of COX and LOX enzymes, which reduces the production of prostaglandins and leukotrienes, leading to a reduction in inflammation.

  • There are three isoforms of the COX enzyme, with the important ones being COX-1 and COX-2.
  • COX-1 enzyme is important for many physiological processes required for the maintenance of homeostasis, while COX-2 is mostly involved in inflammation.

Selectivity and examples

There are a variety of groups of NSAIDs, and they are generally classified based on whether they are non-selective (deactivate both COX-1 and COX2), or selective (higher affinity to COX-2).

Examples for non-selective NSAIDs:

  • Paracetamol (500mg, max 4g/day)
  • Ibuprofen (200mg, max 1200mg/day)
  • Diclofenac (50mg, max 150mg/day)
  • Naproxen (max 1500mg/day)
  • Piroxicam (max 20mg/day)

Selective COX-2 inhibitors (COXIBs) have a significantly reduced risk for gastric ulcers but they have a higher risk of cardiovascular adverse effects, and some of them have been withdrawn due to that (for example, VIOXX).

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