Source: Health Products Regulatory Authority (ZA) Revision Year: 2021 Publisher: CIPLA MEDPRO (PTY) LTD, Building 9, Parc du Cap, Mispel Street, Bellville, 7530, RSA
A 3.1 Antirheumatics (anti-inflammatory agents)
Diclofenac is a non-steroidal 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.
Diclofenac is well absorbed after oral administration. Peak plasma concentrations are reached within approximately 1 hour. Administration with food slows the rate but does not alter the extent of absorption. 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 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 metabolites via the kidneys (approximately 60%) and faeces (approximately 30%). Less than 1% is excreted in unchanged form.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.