- Works by inhibiting the COX (cyclooxyrgenase) enzymes, which convert arachidonic acid to prostaglandin H2 (PGH2).
- PGH2, is converted to several other prostaglandins (which are mediators of pain, inflammation, and fever)
- Also converted to thromboxane A2 which stimulates platelet aggregation, leading to the formation of blood clots.
- Non-selective COX inhibition of 1 & 2.
- Antipyretic effects may be due to action on the hypothalamus = increased peripheral blood flow, vasodilation, and heat dissipation
Dr. David Lyness@Gas_Craic
Developed in the UK in 1960 - and released in 1969
Adverse effects include:
Nausea, dyspepsia, diarrhea, constipation, gastrointestinal ulceration/bleeding, headache, dizziness, rash, salt and fluid retention, and hypertension.
Infrequent adverse effects include oesophageal ulceration, heart failure, hyperkalemia, renal impairment, confusion, and bronchospasm.
DOSE - ADULT and CHILD over 12 years, 300–400 mg 3–4 times daily; increased if necessary to max. 2.4 g daily;
maintenance of 0.6–1.2 g daily may be adequate
Peak @ 1h
Analgesia, Anti-inflamatory, Anti-Pyretic
CVS risk of HTN & MI
Skin - bullous pemphigoid, can sensitise skin
USES: Rheumatoid Arthritis, post-op pain, non-articular MSK conditions: frozen shoulder (capsulitis), bursitis, tendonitis, tenosynovitis and low-back pain. Sprains & strains. Painful menstruation, osteoarthritis, dental pain, headaches and pain from kidney stones.
Can be used to close a PDA in a neonate!
Avoid in asthma, heart failure, liver failure, kidney disease, lupus, Crohn's & GI disease and alongside aspirin.
There is an analgesic ceiling dose of 400mg (1200mg daily)(i.e: 600mg will not confer additional ANALGESIA per dose)