Why the new ibuprofen might not be the ‘game changer’ it’s being made out to be

A new formulation of ibuprofen may allow people to take higher doses without experiencing the cardiovascular side effects associated with the drug, according to a new report in the experimental bioscience journal FASEB.

The researchers, from Imperial College London, used mice and rats to show that ibuprofen alginate is released into the bloodstream more quickly than the current formulations, likely providing faster pain relief.

The researchers made their discovery by measuring the blood pressure of live rats after blocking the protective effects of arginine in the body. The study revealed that ibuprofen arginine worked just like naturally occurring arginine to restore blood pressure to normal levels. The researchers say that arginine formulations of ibuprofen could act to negate the harmful cardiovascular consequences caused by high doses of these common anti-inflammatory painkillers.

The study’s lead author, Jane A. Mitchell, said: ‘While more experiments are required, our observations show that ibuprofen arginate provides, in one preparation, a COX-2 inhibitor and arginine supplement. Whilst remarkably simple, our findings are potentially game-changing in the pain medication arena.’

Instant analysis

Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used painkillers, such as ibuprofen and diclofenac, which work by blocking the action of cyclo-oxygenase (COX) family of enzymes. However, their mechanism of action has recently been cause for concern, as have been associated with the development of heart attacks (a blockage of one of the heart’s main blood vessels) and heart failure (an weakness of the heart’s muscular pumping action).

Indeed, an entire new class of NSAID’s (selective COX2 inhibitors) were withdrawn from sale due to this very association in 2004, known as the Vioxx scandal. Following on from previous work, demonstrating that asymmetric dimethylarginine (ADMA) was responsible for the toxic effects of the NSAIDs, the authors sought to use a different formulation of the same drug (ibuprofen arginate not ibuprofen sodium), which would reduce accumulation of ADMA and therefore be safer for patients, but still give the same pain control. In this study, experiments concluded that the alternative preparation was associated with apparently less negative cardiovascular effects.

However, this is a study on a small number of small animals, which looks at cells, blood vessels and blood pressure and for that reason, I think caution must be taken before referring to such findings as ‘game changing’ or ‘wonder drug’ as the authors and press release do respectively. Particularly as there has never been a study demonstrating NSAID’s improve survival, unlike aspirin, to which it is compared. Were the same findings to be reported in human participants, in a randomised control trial, comparing cardiovascular outcomes such as heart attacks or heart failure in a group taking ibuprofen arginate versus a group taking ibuprofen sodium, then this would be more telling. Furthermore, such a study would also need to comment on the efficacy of the NSAID’s in both groups – for example, are they equally as effective in controlling pain? To use the old cliché: more research is needed.

Research score: 2/5

DW