Subsyde-CR/Subsyde-M Mechanism of Action

Pharmacology: Subsyde-CR: Subsyde-CR contains the sodium salt of diclofenac, a nonsteroidal anti-inflammatory drug (NSAIDs). In pharmacologic studies, diclofenac has shown anti-inflammatory, analgesic and antipyretic effects. Inhibition of prostaglandin biosynthesis, which has been demonstrated in experiments, is considered to be fundamental to the mechanism of action of diclofenac. Prostaglandins play a major role in the pathogenesis of inflammation, pain and fever. In rheumatic diseases, diclofenac produces marked relief from signs and symptoms eg, pain at rest, pain on movement, morning stiffness and swelling of the joints as well as by an improvement in function. Subsyde-CR is particularly suitable for patients requiring a daily dosage of 100 mg.
Subsyde-M: Percutaneous anti-inflammatory analgesic.
Mode of Action: Diclofenac diethylamine is absorbed through the skin. It inhibits the enzyme cyclooxygenase and thus reduces the formation of prostaglandins. Moreover, it also decreases the arachidonic acid entering into the lipooxygenase pathway and the resultant effect is a decreased formation of leukotrienes. Prostaglandins and leukotrienes are the most powerful mediators of pain and inflammation. Subsyde-M gel thus provides a superior relief of pain, inflammation and swelling.
Pharmacokinetics: Absorption: Diclofenac is completely absorbed from the gastrointestinal tract. After administration of 100 mg Subsyde-CR, mean peak plasma concentrations of about 1.39 mcg/mL were reached at a mean of 4.38 hrs. Pharmacokinetic behaviour does not change after repeated administration of the drug. The area under the plasma concentration curve (AUC) is 18.87 mcg·hr/mL.
Distribution: More than 99% of diclofenac is reversibly bound to human plasma 2 albumin. As with other NSAIDs, diclofenac diffuses into and out of the synovial fluid. Diffusion into the joint occurs when plasma levels of diclofenac are higher than those in synovial fluid.
Metabolism and Excretion: Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulphate conjugates of the metabolites. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile.