Diclofenac: A Comprehensive Pharmacological and Clinical Review

1. Introduction to Diclofenac

1.1. Overview and Summary

Diclofenac is a well-established phenylacetic acid derivative classified as a non-steroidal anti-inflammatory drug (NSAID).[1] It is primarily utilized for the management of signs and symptoms associated with various arthritic conditions, including osteoarthritis and rheumatoid arthritis.[1] Its therapeutic applications extend to ankylosing spondylitis and a range of other painful states, such as menstrual cramps (primary dysmenorrhea) and acute migraine attacks.[2] The pharmacological profile of diclofenac is characterized by its potent anti-inflammatory, analgesic (pain-relieving), and antipyretic (fever-reducing) activities.[3]

The broad spectrum of indications for diclofenac underscores its efficacy in conditions where prostaglandins play a significant pathogenic role. Prostaglandins are key mediators in inflammation, pain sensitization, and fever development. By inhibiting their synthesis, diclofenac offers relief across a diverse array of clinical scenarios. Its utility in both chronic inflammatory diseases like arthritis and acute painful conditions such as migraines highlights its versatility as a therapeutic agent.[1] This versatility is a direct consequence of its fundamental mechanism of action as an NSAID, which targets the cyclooxygenase (COX) enzymes responsible for prostaglandin production. However, this same mechanism also underpins its potential for adverse effects, particularly concerning the gastrointestinal and cardiovascular systems, which are significant enough to warrant boxed warnings from regulatory authorities like the U.S. Food and Drug Administration (FDA).[3] The widespread and long-standing use of diclofenac implies a considerable clinical impact in pain and inflammation management. Concurrently, this extensive use necessitates a comprehensive understanding and careful consideration of its