Discovery, mechanisms of action and safety of ibuprofen.

Abstract

Ibuprofen was the product of a long research programme during the 1950s and 1960s to develop a 'super aspirin' for the treatment of rheumatoid arthritis which was as effective as current alternatives but safer. Selected for development in 1964 after several promising compounds had proved disappointing at the clinical stage, ibuprofen was found to have a short elimination half-life and exceptional gastrointestinal tolerability. Ibuprofen was introduced in the United Kingdom in 1966 and in the United States in 1974, and was the first non-steroidal anti-inflammatory drug (NSAID) licensed for over-the-counter use in the UK in 1983 and in the US the following year. Ibuprofen is a non-cyclo-oxygenase selective NSAID but recent evidence suggests additional anti-inflammatory properties are due to modulation of leucocyte activity, reduced cytokine production, inhibition of free radicals and signalling transduction. Ibuprofen may also exert a central analgesic action in the dorsal horn. Future roles for ibuprofen may include protection against certain cancers and Alzheimer's disease.