Source: Υπουργείο Υγείας (CY) Revision Year: 2016 Publisher: Medililink Pharmaceuticals Ltd, 30 Armenias Street, 2003 Strovolos, Nicosia, Cyprus, Tel.: +357 22319282, Fax: +357 22319290
Pharmacotherapeutic group: Non‑steroidal anti‑inflammatory and anti‑rheumatic agents; Acetic acid derivatives and related substances
ATC code: M01AB05
Diclofenac is a non‑steroidal anti‑inflammatory/anti‑rheumatic agent, which has proved effective by inhibiting prostaglandin synthesis in the usual inflammation models in animal studies. In human beings diclofenac reduces pain, swelling and fever which are caused by inflammation. Diclofenac also inhibits platelet aggregation caused by ADP and collagen.
After oral administration of the usual gastroresistant pharmaceutical forms diclofenac is fully absorbed distal to the stomach. Maximum plasma levels are attained, depending on the duration of the passage through the stomach, after 1-16 hours, the mean being after 2-3 hours. After IM administration, maximum plasma levels are attained after 10-20 minutes; after rectal administration after about 30 minutes. Orally administered diclofenac is subject to a marked first‑pass effect; only 35-70% of the active substance absorbed reaches the post‑hepatic circulation unchanged. About 30% of the active substance is eliminated in metabolised form with the faeces.
About 70% is excreted by the kidneys after hepatic metabolic conversion (hydroxylation and conjugation) as pharmacologically inactive metabolites. The elimination half‑life, which is largely independent of liver and renal function, is about 2 hours. Plasma protein binding is about 99%.
Non‑clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and reproduction toxicity, which is greater than the risks already described in other sections of the Information for Healthcare Professionals.
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