Source: Health Products Regulatory Authority (ZA) Revision Year: 2022 Publisher: Biotech Laboratories (Pty) Ltd, Ground Floor, Block K West, Central Park, 400 16th Road, Randjespark, Midrand 1685, South Africa
Category and class: A.3.1 Antirheumatics (anti-inflammatory agents)
Pharmacotherapeutic group: Acetic acid derivatives and related substances
ATC code: M01AB05
Diclofenac is a nonsteroidal anti-inflammatory compound (NSAID) with analgesic, antipyretic and anti-inflammatory activities. It causes decreased formation of prostaglandins and thromboxanes through inhibition of the activity of the enzyme cyclo-oxygenase. Prostaglandins play a major role in the causation of inflammation, pain and fever and the inhibition of prostaglandin synthesis may have an important bearing on diclofenac’s mechanism of action. Diclofenac inhibits platelet aggregation in vitro.
In addition, diclofenac appears to reduce intracellular concentrations of free arachidonate in leukocytes, perhaps by altering the release or uptake of the fatty acid.
Diclofenac is well absorbed after oral administration. Therapeutic plasma concentrations occur about ½ hour after administration of MOTIFINE.
There is a substantial first-pass effect (only 50% of diclofenac is available systemically).
Diclofenac is extensively bound to plasma proteins (99%) and its plasma half-life for the terminal elimination phase is 1 to 2 hours.
Diclofenac is metabolised in the liver by a cytochrome P450 isozyme of the CYP2C subfamily and excreted in the form of glucuronide and sulphate conjugates. Approximately 60% of the administered dose is excreted via the kidneys in the form of metabolites and less than 1% in unchanged form. The remainder of the dose is excreted via the bile in metabolised form.
Following rapid gastric passage, the enteric coated pellet component of MOTIFINE ensures quick availability of the active component in the blood stream. The sustained release pellets cause a delayed release of the active component, which means one single daily dose is usually sufficient.
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