过去50年新型镇痛药的进展：缺乏真正突破性的药物  

作　　者：Igor Kissin 

机构地区：[1]Department of Anesthesiology, Perioperative and Pain Medidne, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts

出　　处：《麻醉与镇痛》2012年第5期31-42,共12页Anesthesia & Analgesia

摘　　要：从1960年至2009年以来，有59种镇痛药被引入临床并使用至今。其中7种药物被认为具有新型的分子靶位；然而，只有一种，即舒马普坦，在促使多种作用于同一分子靶位的类似药物（曲普坦类）临床应用方面非常有效。在此期间，疼痛领域的出版物数量呈指数型增长。发表与疼痛相关的吗啡类研究论文在所有镇痛药中仍占主导地位。与疼痛机制相关的不同分子靶位的大量研究文章发表了数以千计，但这些努力仍然无法使具有足够有效的新型镇痛药产生质的飞跃，从而改变其在阿片类或非甾体抗炎药物论文中的比例。吗啡和阿司匹林，在一个多世纪之前就被用于疼痛治疗，尽管它们在许多领域（如神经病理性疼痛）的疗效有限，并存在许多严重不良反应，但仍然在生物医学出版物中占有优势。评估揭示，尽管大量的研究工作仍在深入，但镇痛药的研发缺乏真正突破性进展。应当探讨导致新型镇痛药明显缺乏的可能因素。Fifty-nine drugs identified as analgesics were introduced from 1960 to 2009 and remain in use. Seven can be regarded as having novel molecular targets; however, only one, sumatriptan, was sufficiently effective to motivate the introduction of many similar drugs acting at the same target （triptans）. Publication productivity in the area of pain grew exponentially during this period. Pain-related publications on morphine were dominant among other analgesics. Very intensive research efforts directed at diverse molecular targets related to pain mechanisms produced thousands of publications, but those efforts have not yet yielded new analgesics with sufficient effectiveness to change the share of publications on opioids or nonsteroidal antiinflammatory drugs. Morphine and aspirin, introduced for the treatment of pain more than a century ago, continue to dominate biomedical publications despite their limited effectiveness in many areas （e. g., neuropathie pain） and multiple serious adverse effects. The present assessment reveals the la＆ of real breakthroughs in analgesic drug development despite intense research efforts. Possible factors contributing to the apparent drought of novel analgesics are discussed.

关 键 词：药物论文 镇痛药 神经病理性疼痛 疼痛机制 分子靶位 严重不良反应 临床应用 2009年 

分 类 号：R969.3[医药卫生—药理学]