Busson M
J Int Med Res. 1986;14(2):53-62. doi: 10.1177/030006058601400201.
Non-steroidal anti-inflammatory drugs (NSAIDs) have become the principal mode of therapy for rheumatic diseases and their use has continued to increase despite concern expressed recently regarding potential hazards (Figure 1). Prior to 1969, a limited number of NSAID drugs were available. Aspirin and indomethacin became the mainstay of treatment but tolerability, particularly gastric irritation, at doses necessary to control rheumatic symptoms limited the usefulness of these valuable agents. The pyrazolone, phenylbutazone, showed slightly better gastro-intestinal (GIT) tolerability but has since been associated with an increased risk of blood dyscrasiae and is now only available for restricted use in most countries. Ibuprofen was the first of a new breed of NSAIDs originally introduced into the United Kingdom in 1969. Chemically quite distinct from its forerunners it was the first of the propionic acid derivatives to be used in rheumatic practice. The propionics have since become the largest, single and most important group of NSAIDs accounting for 50% of NSAID prescriptions in the United Kingdom. It is estimated that over 100 million patients worldwide have received ibuprofen which is now available in over 100 countries throughout the world including all the major markets. Ibuprofen was developed directly as a result of the problems associated with the use of corticosteroids in the treatment of rheumatoid arthritis and also because of the gastro-intestinal irritation and general intolerability of the established NSAIDs, at that time. Ibuprofen was readily accepted because, unlike the previous drugs, its therapeutic efficacy was easily seen to outweigh the severity of its side-effects. Ibuprofen was the first new drug with the potency of aspirin but without its major disadvantages.
非甾体抗炎药(NSAIDs)已成为治疗风湿性疾病的主要方式,尽管最近有人对其潜在危害表示担忧,但它们的使用仍在持续增加(图1)。1969年之前,可用的NSAID药物数量有限。阿司匹林和吲哚美辛成为治疗的主要药物,但在控制风湿症状所需的剂量下,其耐受性,尤其是对胃部的刺激,限制了这些有价值药物的效用。吡唑酮类药物保泰松的胃肠道(GIT)耐受性稍好,但此后与血液系统疾病风险增加有关,现在在大多数国家仅可用于受限用途。布洛芬是1969年首次引入英国的新一代NSAIDs中的第一种。它在化学结构上与之前的药物有很大不同,是第一种用于风湿治疗的丙酸衍生物。此后,丙酸类药物已成为最大、单一且最重要的NSAIDs组,占英国NSAID处方的50%。据估计,全球有超过1亿患者使用过布洛芬,现在它在全球100多个国家都有销售,包括所有主要市场。布洛芬的研发直接源于在类风湿关节炎治疗中使用皮质类固醇所带来的问题,也源于当时已有的NSAIDs存在胃肠道刺激和普遍耐受性差的问题。布洛芬很容易被接受,因为与之前的药物不同,其治疗效果明显超过副作用的严重程度。布洛芬是第一种效力与阿司匹林相当但没有其主要缺点的新药。