Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0184567 (acute pain)
 3,962 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

: The beneficial actions of non-steroidal anti-inflammatory drugs (NSAIDs) have been associated with inhibition of cyclooxygenase-2 (COX-2), whereas some of their adverse effects are associated mainly with inhibition of COX-1. Selective COX-2 inhibitors reduce the risk of gastrointestinal adverse events, but increase the risk of thromboembolic events pointing to importance of optimal COX-1/COX-2 inhibition in drug safety. We compared the effects of acetylsalicylic acid, ibuprofen, nabumetone and nimesulide on COX-1 and COX-2 pathways in healthy volunteers in an ex vivo set-up using single oral doses commonly used to treat acute pain. In a randomized, double-blind four-phase cross-over study, 15 healthy volunteers were given orally a single dose of either acetylsalicylic acid 500 mg, ibuprofen 400 mg, nabumetone 1 g or nimesulide 100 mg. Blood samples were drawn before and 1, 3, 6, 24 and 48 hr after the drug for the assessment of COX-1 and COX-2 activity. COX-1 activity was measured as thromboxane(2) production during blood clotting and COX-2 activity as endotoxin-induced prostaglandin E(2) synthesis in blood leucocytes. The data show that after a single oral dose these four NSAIDs have different profiles of action on COX-1 and COX-2. As expected, acetylsalicylic acid appeared to be COX-1-selective and ibuprofen effectively inhibited both COX-1 and COX-2. Nabumetone showed only a slight inhibitory effect on COX-1 and COX-2. Nimesulide caused almost complete suppression of COX-2 activity and a partial reduction of COX-1 activity. This confirms the relative COX-2 selectivity of nimesulide.
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PMID:Effects of nimesulide, acetylsalicylic acid, ibuprofen and nabumetone on cyclooxygenase-1- and cyclooxygenase-2-mediated prostanoid production in healthy volunteers ex vivo. 1915 49

Osteoarthritis is one of the most common joint diseases and is a major cause of chronic disability in the elderly, second only to cardiovascular disease. Although, in addition to important nonpharmacological measures, paracetamol is recommended as first-line therapy in osteoarthritis because of its analgesic efficacy and tolerability profile, its efficacy is often disappointing and the more recent guidelines from the European League Against Rheumatism (EULAR) highlight how NSAIDs may be a valid alternative in patients with an inadequate response to paracetamol. The American College of Rheumatology (ACR) 2000 guidelines state that NSAIDs may even be used as initial treatment in patients with osteoarthritis of the knee and moderate-to-severe pain and inflammation. Data from several clinical studies suggest that NSAIDs provide superior analgesia to paracetamol. Little evidence is available to distinguish one NSAID from another in terms of efficacy, whilst their gastrointestinal (GI) tolerability profile remains a main concern and a key discriminating factor in selecting a NSAID. Nimesulide is a NSAID with a multi-factorial mode of action which is particularly suitable in the symptomatic treatment of states characterised by acute pain, such as osteoarthritis flares. In particular, its proven efficacy, a fast onset of the analgesic action, its protective effect against the degradation of cartilage and a demonstrated low incidence of gastrointestinal adverse events compared with other NSAIDs make it a particularly valuable option in the symptomatic treatment of patients with joint osteoarthritis.
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PMID:Applying the evidence in osteoarthritis: strategies for pain management. 2339 87