Rofecoxib, a non-steroidal anti-inflammatory drug (NSAID), is known to have a lower risk of gastrointestinal (GI) side effects compared to traditional NSAIDs [1]. This is primarily due to its selective inhibition of the cyclooxygenase-2 (COX-2) enzyme, which plays a crucial role in inflammation and pain, while having minimal impact on the COX-1 enzyme that protects the stomach lining [2].
The GI protective effect of rofecoxib can be attributed to the following factors:
1. Reduced gastric acid secretion: Rofecoxib does not stimulate gastric acid secretion, unlike traditional NSAIDs that increase acid production, leading to gastric ulcers and other GI complications [3].
2. Preservation of gastroprotective prostaglandins: By selectively inhibiting COX-2, rofecoxib preserves the function of COX-1, which is responsible for producing prostaglandins that protect the stomach lining [4]. This results in a lower risk of developing gastric ulcers and other GI side effects.
3. Decreased platelet aggregation: Rofecoxib has a weaker effect on platelet aggregation compared to traditional NSAIDs, which can reduce the risk of GI bleeding and other cardiovascular events [5].
In summary, rofecoxib's GI protective effects stem from its selective COX-2 inhibition, which results in reduced gastric acid secretion, preserved gastroprotective prostaglandins, and decreased platelet aggregation.
Sources:
[1] DrugPatentWatch.com - Rofecoxib
[2] Nissen, S. E., & Wolski, K. (2007). Effect of rofecoxib on cardiovascular events and gastrointestinal safety: a meta-analysis. Archives of internal medicine, 167(7), 669-675.
[3] Silverstein, F. E., Faich, G. H., Goldstein, J. L., & Simon, L. S. (2000). Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis: a randomized controlled trial. JAMA, 284(10), 1247-1255.
[4] Vane, J. R., & Botting, R. M. (1998). Cyclooxygenase inhibitors. Pharmacological Reviews, 50(1), 47-79.
[5] Catella-Lawson, F., Reilly, M. P., Kapoor, S., & Rosenberg, J. (2001). Cyclooxygenase-2 inhibitors and cardiovascular risk: a statement for healthcare professionals from the American Heart Association. Circulation, 104(21), 2441-2443.