Abstract
Oxaprozin (3-(4,5-difeniloksazol-2-yl)propanoic acid) is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of numerous inflammatory musculoskeletal diseases, including rheumatoid arthritis, osteoarthritis, tendonitis, ankylosing spondylitis and bursitis. It is the first representative member of the diaryl-substituted heterocyclic compounds, which have found clinical use as selective cyclooxygenase-2 (COX-2) inhibitors. U.S. Food and Drug Administration (FDA) approved its official use in 1992. Both anti-inflammatory and analgesic properties of oxaprozin are mainly due to the potent inhibition of COX. However, oxaprozin-induced benefits might be also regulated by other COX-independent pathways. It has been shown that oxaprozin induced direct proapoptotic effects in CD40L-treated human monocytes independently of COX inhibition. It also has several advantages in the treatment of inflammatory diseases in comparison to other NSAIDs such as aspirin, naproxen, indomethacin and phenylbutazone, which enabled oxaprozin to become one of the most used NSAIDs in America. Oxaprozin, as other members of the group of NSAIDs, can cause gastrointestinal complications, but significantly lower due to relatively high pKa value. In this paper, importance of oxaprozin in the treatment of arthritis and its pharmacokinetic properties were described, therewith its activity and side effects were compared with other commercially available anti-inflammatory drugs.
Highlights
Elektron-akceptorski efekat cijano grupe povećava kiselost α-vodonika na ugljenikovom atomu i na taj način olakšava transfer protona sa α-ug
The importance of oxaprozin in the treatment of arthritis and its pharmacokinetic properties were described, therewith its activity and side effects were compared with other commercially available anti-inflammatory drugs
Summary
Derivati propanske kiseline sa analgetskim i antipiretičkim svojstvima su nesteroidni anti-inflamatorni lekovi (NSAIL). Širok spektar NSAIL koristi se u kliničkoj praksi za lečenje inflamatornih bolesti, uključujući osteoartritis, reumatoidni artritis i ankilozirajući spondilitis, kao i za prevenciju infarkta miokarda i Alchajmerove bolesti [1,2,3,4,5]. Pokazano je da su NSAIL inhibitori u sintezi prostaglandina, koji inhibiraju jedan od glavnih enzima u inflamatornoj kaskadi, ciklooksigenazu (COX), koja postoji u dva izomorfna oblika, COX-1 i COX-2 [6,7]. Oksaprozin (Wy-21,743; 3-(4,5-difeniloksazol-2-il)propanska kiselina [11]; CAS-21256-18-8) (slika 1), prvi je reprezentativni član diaril-supstituisanih heterocikličnih jedinjenja, koji je našao kliničku upotrebu kao selektivni COX-2 inhibitor [12]. Oksaprozin je dugodelujući NSAIL koji se koristi za lečenje brojnih inflamatornih mišićnoskeletnih bolesti, uključujući reumatoidni artritis, osteoartritis, upale tetiva, postoperativnih bolova zuba, ankilozirajući spondilitis i burzitis [13,14,15].
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