Review of Diclofenac and Evaluation of its Place in Therapy as a Nonsteroidal Antiinflammatory Agent

Abstract

Diclofenac sodium is a nonsteroidal antiinflammatory drug (NSAID) that has been used in 120 countries since its introduction in Japan in 1974. It is currently the eighth largest-selling drug and the most frequently used NSAID in the world. Diclofenac, a phenylacetic acid derivative, is a potent inhibitor of cyclooxygenase enzyme activity, and may also interact with the lipoxygenase enzyme pathway, and with the release and reuptake of arachidonic acid. Diclofenac is almost completely absorbed, highly protein-bound, penetrates well into synovial fluid, and is extensively metabolized. Comparative studies have shown that diclofenac is at least equivalent in efficacy to aspirin and other NSAID when used for the treatment of rheumatic diseases such as rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis. Diclofenac also possesses potent analgesic properties. Clinical trials suggest that diclofenac has a favorable side-effect profile, excellent patient tolerability, and a lower patient dropout rate when compared with aspirin and other NSAID.

Decrease in Efficacy and Potency of Nonsteroidal Anti-Inflammatory Drugs by Chronic Δ9-Tetrahydrocannabinol Administration

“…When efficacy remains the same, however, there is a decrease in potency. Diclofenac is reported to have a potency greater than all the NSAIDs tested (Skoutakis et al, 1988), which is in agreement with our observations. In fact, diclofenac was so potent that the ED 50 in animals given chronic THC was lethal in our chronic vehicle (1:1:18) animals.…”

Il-1β and Reactive Oxygen Species Differentially Regulate Neutrophil Directional Migration and Basal Random Motility in a Zebrafish Injury–Induced Inflammation Model

“…These phenotypes share some common features with human inflammatory disorders, and thus, the Tg(hsp70: m il-1b_eGFP;lyz:DsRed2) hkz10t;nz50 transgenic line could be used as an animal model for developing new therapeutic strategies for the treatment and prevention of human inflammatory disorders. To provide proofof concept evidence to support such a notion, we tested whether the treatment of Tg(hsp70: m il-1b_eGFP;lyz:DsRed2)hkz10t; nz50 embryos with diclofenac and dexamethasone, two antiinflammatory drugs commonly used for clinical treatment of human inflammatory disorders (27,53,54), could reduce the inflammation. Result showed that anti-inflammatory treatment with diclofenac and dexamethasone significantly reduced the number of abnormal distributed neutrophils in heat shock-treated Tg(hsp70: m il-1b_eGFP;lyz:DsRed2)hkz10t;nz50 embryos (Fig.…”

Antinociceptive and gastro-protective effect of the ethanolic extract of the flowering top of Anthocephalus Cadamba Roxb

“…Diclofenac, a non-steroidal anti-inflammatory drug (NSAID), is commonly employed in the treatment and/or management of rheumatoid arthritis, osteo-arthritis and ankylosing spondylitis (Eddy and Leimback, 1953;Siraux, 1977) and for its anti-inflammatory and analgesic effects (Brooks et al, 1980). Diclofenac reduces inflammation, swelling and arthritic pain by inhibiting prostaglandins synthesis and/or production (Skoutakis et al, 1988;Todd and Sorkin, 1988;Small, 1989). It is known that non-steroidal anti-inflammatory drugs usually do not increase the pain threshold in normal tissues, whereas local anesthetics and narcotics do (Ferreira et al, 1978).…”