Question
Selective COX-2 inhibitors (merits and demerits).
Q8 4 marks Short Answers ★ ✓
Answer
Selective COX-2 inhibitors (Celecoxib, Etoricoxib) selectively inhibit the inducible COX-2 isoform responsible for inflammatory prostaglandin synthesis, while sparing constitutive COX-1, which maintains gastric mucosal protection and normal platelet thromboxane function.
Merits :
Substantially lower risk of GI ulceration/bleeding than non-selective NSAIDs, since gastroprotective COX-1-derived prostaglandins are spared.
No antiplatelet effect (COX-1/thromboxane A2 spared), so no added bleeding risk from platelet dysfunction.
Equivalent analgesic and anti-inflammatory efficacy to non-selective NSAIDs.
Demerits :
Increased cardiovascular (thrombotic) risk with prolonged use — COX-2 inhibition suppresses vascular endothelial prostacyclin (an antiplatelet, vasodilator mediator) without the offsetting COX-1/thromboxane suppression that non-selective NSAIDs provide, shifting the hemostatic balance toward thrombosis.
Some renal toxicity, similar to non-selective NSAIDs (both COX-1 and COX-2 contribute to renal prostaglandin-mediated blood flow autoregulation).
Higher cost than non-selective NSAIDs.
Rofecoxib was withdrawn from the market specifically for excess cardiovascular risk, a cautionary example for the whole class.
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