Abstract

•Ibuprofen is nearing its golden anniversary (50 years) and remains among the most widely prescribed and frequently taken over-the-counter analgesic in the world. First developed in the United Kingdom by Boots Pure Drug Company, Limited,1 the drug evolved when scientist Stewart Adams sought to elucidate the anti-inflammatory effects of aspirin which seemed to him to be a clear advantage over acetaminophen.2 Adams and his colleague John Nicholson developed over 200 compounds and brought four to clinical trials with disappointing results. It was the fifth drug they tried that succeeded and came to market in 1969 in the United Kingdom and in 1974 in the United States.3 An anecdote told by Adams himself said that he took the first dose of the new drug himself to treat a hangover.1

•Despite lengthy clinical experience with ibuprofen, new safety concerns had been raised about its role in infections4 and its safety for COVID-19 patients.5 Ibuprofen is unique in the NSAID family in that it appears to block both cyclooxygenase (COX) 1 and COX 2 enzymes. The COX enzymes synthesize prostaglandins which are associated with the inflammatory cascade. Safety concerns related to COX-1 inhibition mainly involved gastrointestinal adverse events; the introduction of selective COX-2 inhibitors or coxibs likewise raised safety concerns, in particular relating to cardiovascular events. Almost all NSAIDS may be associated with elevating blood pressure but the safety profiles of various NSAIDs are unique. Ibuprofen’s position of balance “middle of the road” position as being neither strongly selective for COX-1 or COX-2 has afforded it a strong safety and tolerability profile.

•The authors sought to review safety data on ibuprofen at the half-century mark and to consider the advantages and disadvantages of this versatile and popular analgesic.