布洛芬的发现、作用机制和安全性。

K D Rainsford
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引用次数: 0

摘要

布洛芬是20世纪50年代和60年代一个长期研究项目的产物,该项目旨在开发一种治疗类风湿性关节炎的“超级阿司匹林”,它与目前的替代药物一样有效,但更安全。1964年,在几种有希望的化合物在临床阶段被证明令人失望之后,布洛芬被选中进行开发,人们发现它的半衰期很短,而且具有特殊的胃肠道耐受性。布洛芬于1966年在英国推出,1974年在美国推出,并于1983年在英国和次年在美国获得非处方药许可,成为第一种非甾体抗炎药(NSAID)。布洛芬是一种非环加氧酶选择性非甾体抗炎药,但最近的证据表明,额外的抗炎特性是由于白细胞活性的调节,减少细胞因子的产生,抑制自由基和信号转导。布洛芬也可在背角发挥中枢镇痛作用。布洛芬未来的作用可能包括预防某些癌症和阿尔茨海默病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Discovery, mechanisms of action and safety of ibuprofen.

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.

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