Pharmacology: Mechanism of Action: Diclofenac, a phenylacetic acid derivative, is a non-steroidal anti-inflammatory drugs (NSAIDs). As with other NSAIDs drug, its mode of action is not known but may be related to its ability to inhibit prostaglandin synthesis. It has been proposed that NSAIDs may act through inhibition of cyclo-oxygenase-1 and cyclo-oxygenase-2 and that inhibition of Cox-1 is associated with adverse gastrointestinal effects while inhibition of Cox-2 is associated with anti-inflammatory activity. Both Cyclo-oxygenase-1 and -2 are involved in biosynthesis of prostaglandin that plays a major role in the pathogenesis of inflammation, pain and fever.
Pharmacokinetics: Axcel Diclofenac-50 Tablet is in a pharmaceutical formulation that resists dissolution in the low pH of gastric fluid but allows a rapid release of drug in the higher pH-environment of the duodenum. Diclofenac is rapidly absorbed from the gastrointestinal tract. Although orally administered diclofenac is almost completely absorbed, due to the first-pass metabolism, only about 50% of the absorbed dose is systemically available. At therapeutic concentration, it is more than 99% bound to plasma protein. Diclofenac penetrates synovial fluid where concentrations may persist even when plasma concentrations fall; diclofenac has been detected in breast milk. The minimal plasma half-life is about 1 to 2 hours. It is metabolised in the liver and excreted in the form of glucuronide and sulphate conjugates mainly in the urine (about 35%) but also in the bile (about 35%).
Sign Out