Tanasescu S, Lévesque H, Thuillez C
Service de pharmacologie, CHU de Rouen-Boisguillaume, France.
Rev Med Interne. 2000 Mar;21 Suppl 1:18s-26s. doi: 10.1016/s0248-8663(00)88721-4.
Aspirin (acetylsalicylic acid) is the best-known salicylate and belongs to the non steroid anti-inflammatory drug class. Despite wide use being made since more than 100 years, knowledge about mechanism of action and therapeutic issues continually evolves. The main mechanism of action is prostaglandin synthesis inhibition. This is achieved through inhibition of prostaglandin endoperoxide synthase (PGHS) or cyclooxygenase (COX) synthesis. Most of the therapeutic uses of aspirin are explained by this mechanism. Nevertheless aspirin uses change as time goes by: if the main one during the first fifty years was an analgesic, anti-pyretic and anti-inflammatory one, the last fifty years saw aspirin being used mainly as an anti-thrombotic agent, in primary and secondary thrombo-embolic prevention. Better knowledge of mechanism of action points today at, on one hand, more selective and therefore better tolerated molecules, and, on the other hand, at new therapeutic applications, such as anti-cancer and neurodegenerative diseases prevention.
阿司匹林(乙酰水杨酸)是最知名的水杨酸盐,属于非甾体抗炎药类别。尽管阿司匹林已被广泛使用了100多年,但有关其作用机制和治疗问题的认识仍在不断发展。其主要作用机制是抑制前列腺素合成。这是通过抑制前列腺素内过氧化物合酶(PGHS)或环氧化酶(COX)的合成来实现的。阿司匹林的大多数治疗用途都可以用这一机制来解释。然而,随着时间的推移,阿司匹林的用途也在发生变化:如果说在最初的五十年里其主要用途是止痛、退热和抗炎,那么在过去的五十年里,阿司匹林主要被用作抗血栓药物,用于一级和二级血栓栓塞预防。如今,对作用机制的深入了解一方面指向了更具选择性、因而耐受性更好的分子,另一方面也指向了新的治疗应用,如抗癌和预防神经退行性疾病。