NSAIDS inhibit COX, thereby inhibiting prostaglandin synthesis
SALICYLIC ACID PROPIONIC ACID OTHERS SELECTIVE COX-2 ANALGESIC
DERIVATIVES DERIVATIVES INHIBITORS ONLY
Aspirin Ibuprofen Diclofenac Etoricoxib
Naproxen Indomethacin Celecoxib Paracetamo
Nabumetone Lumiracoxib l
Mechanism of action:
ANALGESIC action
Peripheral actions predominate
Associated with anti-inflammatory action
Results from inhibition of prostaglandin synthesis in inflamed tissues
Prostaglandins potentiate the pain caused by inflammatory mediators
Anti-inflammatory action:
Attenuates inflammation (NOT abolish)
Rheumatoid arthritis
Not alter the course of the disease
Anti-pyretic action:
Aspirin prevents temperature-raising effects of IL-1
Prevent ↑ in brain prostaglandins levels
On COX:
Enzymes with a long channel (wider in COX2)
Block the channel by binding to arginine halfway down (hydrogen bonds)
Reversibly inhibits enzyme by preventing access of arachidonic acid
Aspirin acetylates enzyme at serine 530 (irreversible)
PARACETAMOL:
↓ Cytoplasmic peroxide tone
Peroxide: activate haem enzyme ferryl form
SALICYLIC ACID PROPIONIC ACID OTHERS SELECTIVE COX-2 ANALGESIC
DERIVATIVES DERIVATIVES INHIBITORS ONLY
Aspirin Ibuprofen Diclofenac Etoricoxib
Naproxen Indomethacin Celecoxib Paracetamo
Nabumetone Lumiracoxib l
Mechanism of action:
ANALGESIC action
Peripheral actions predominate
Associated with anti-inflammatory action
Results from inhibition of prostaglandin synthesis in inflamed tissues
Prostaglandins potentiate the pain caused by inflammatory mediators
Anti-inflammatory action:
Attenuates inflammation (NOT abolish)
Rheumatoid arthritis
Not alter the course of the disease
Anti-pyretic action:
Aspirin prevents temperature-raising effects of IL-1
Prevent ↑ in brain prostaglandins levels
On COX:
Enzymes with a long channel (wider in COX2)
Block the channel by binding to arginine halfway down (hydrogen bonds)
Reversibly inhibits enzyme by preventing access of arachidonic acid
Aspirin acetylates enzyme at serine 530 (irreversible)
PARACETAMOL:
↓ Cytoplasmic peroxide tone
Peroxide: activate haem enzyme ferryl form
