Diclofenac Case Study

2.3.1.1 DICLOFENAC

It is a non-steroidal anti- inflammatory drug (NSAID) used for the treatment of inflammation and can also be used as an analgesic. It is supplied as or contained in medication under a variety of trade names. Inhibition of prostaglandin production is the primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action. It also appears to exhibit bacteriostatic activity by inhibiting bacterial DNA synthesis (Bhalaet al., 2013). It also affects the function of polymorphonuclear leukocytes in vitro, thereforereducing superoxide toxic radical formation, chemotaxis, oxygen-derived free radical generation and neutral protease production(Mahgoub, 2002). According to a report from an experimental animal models, diclofenac suppress inflammation induced by various phlogistic agents(Al-Tuwaijri and Mustafa, 1992). Other side effects may include gastrointestinal disorders when administered by oral route andcutaneous lesions by intramuscular injection (Lopes et al., 2006;

EETsepoxyeicosatrienoicacids;FLAP-5-lipoxygenase-activatingprotein; HETEshydroxyeicosatetraenoicacids; HPETE - hydroxyperoxyeicosatetraenoic acid; 12-KETE-12-ketoeicosatetraenoic acid; LOX- lipoxygenase; LT- leukotriene; PG- prostaglandin; TXA2-thromboxane A2 (Howard, 2006).

2.5 CYCLOOXYGENASE PATHWAY

This enzymemetabolizearachidonic acid to endoperoxide intermediate to produce prostaglandins and thromboxanes. The cyclooxygenase active site (CAS), transformarachidonic acid to prostaglandin G2 (PGG2) and the Peroxidase active site (PAS) converts PGG2 to PGH2. PGH2 serve as precursor for many bioactive prostanoids, that areformed by the action of tissue isomerases. The prostanoidsinclude PGF2α, PGI2, PGE2, PGD2and TxA2. Synthesis of individual prostanoids iscatalyzedby specific synthases and they possess distinct biological functions (Davies et al., 2002; Rocca, 2006).

2.5.1. ISOFORMS OF