Diclofenac injectable indications

The first-line agents in the treatment of rheumatoid arthritis are non-steroidal anti-inflammatory drugs such as diclofenac. Diclofenac and indometacin, another NSAID, tend to have similar activity hov/ever, indometacin has a higher incidence of side-effects and therefore diclofenac is more appropriate for initial treatment. Sodium aurothiomalate is classified as a disease-modifying antirheumatic drug and is used as a second-line treatment in rheumatoid arthritis, but has been superseded by methotrexate, administered v/eekly. Paracetamol is often indicated in the management of osteoarthritis. Local intra-articular injections of dexamethasone may be administered for the relief of soft-tissue inflammatory conditions. 

Figure 6.43 H spectrum of diclofenac glucuronide obtained after single trapping from a 100 pi injection of female urine 4 h after dosage of 50 mg of diclofenac. The spectrum was recorded using a cryogenic flow probe at 600 MHz. The spectrum indicates that the sensitivity is sufficient to run aU two-dimensional experiments needed for structure elucidation. Reproduced from [82] with permission from Elsevier.

Because the older formulation of diclofenac for parenteral injection was approved in the UK decades ago and marketed there continuously since, with ample experience as to its safety and efficacy, the regulatory pathway for approval of the new formulation in that country as an essentially similar product was relatively straightforward. The new formulation was approved and has been marketed in the UK since late 2007 for parenteral use, 75 mg every 12 hours as needed for the treatment of acute moderate to severe pain. This dose, dosing interval, and indication are the same as for the earlier formulation. Other European submissions are planned and our new formulation of injectable diclofenac is currently under clinical development in the USA. Because no injectable diclofenac has previously been approved in the USA, the US clinical development program has been more comprehensive than that in the UK, including clinical trials that have assessed various doses and dose intervals in several pain models and in subjects ranging from healthy normal subjects to post-surgical patients, and patients with renal or hepatic insufficiency. 

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