Grösch Sabine, Niederberger Ellen, Geisslinger Gerd
a Pharmazentrum frankfurt/ZAFES , Institut für Klinische Pharmakologie, Klinikum der Goethe-Universität Frankfurt , Frankfurt am Main , Germany.
b Fraunhofer Institute for Molecular Biology and Applied Ecology (IME), Project Group for Translational Medicine & Pharmacology (TMP) , Frankfurt/Main , Germany.
Expert Opin Investig Drugs. 2017 Jan;26(1):51-61. doi: 10.1080/13543784.2017.1260544. Epub 2016 Nov 20.
Non-steroidal anti-inflammatory drugs (NSAID) are the most commonly used drugs for the treatment of pain, inflammation and fever. Although they are effective for a huge number of users, their analgesic properties are not sufficient for several patients and the occurrence of side effects still constitutes a big challenge during long term therapy. Areas covered: This review gives an overview about the first and second generations of NSAIDs (COX1/2 non-selective, COX-2 selective), and their main side effects which gave still an urgent need for safer drugs and for the establishment of novel treatment strategies (improved safety, tolerability, patient convenience). The current developments of a possible third generation NSAID class comprise changes in the formulation of already approved drugs, combination therapies, dual cyclooxygenase-lipoxygenase inhibitors, NO- and HS-releasing NSAIDs, prostaglandin synthase inhibitors and EP receptor modulators, respectively. Literature search has been done with PubMed NCBI. Expert opinion: Currently, there is no newly developed drug that is superior to the already approved selective and non-selective NSAIDs. Several novel approaches show promising analgesic efficacy but side effects are still an important problem. Solutions might be constituted by combination therapies allowing administration of lower drug doses or by individualized therapies targeting molecules apart from COX, respectively.
非甾体抗炎药(NSAID)是治疗疼痛、炎症和发热最常用的药物。尽管它们对大量使用者有效,但对一些患者来说其镇痛特性并不充分,并且在长期治疗期间副作用的发生仍然是一个巨大挑战。涵盖领域:本综述概述了第一代和第二代NSAID(COX1/2非选择性、COX - 2选择性)及其主要副作用,这仍迫切需要更安全的药物并建立新的治疗策略(提高安全性、耐受性、患者便利性)。可能的第三代NSAID类药物的当前发展分别包括已批准药物的剂型变化、联合疗法、双环氧化酶 - 脂氧合酶抑制剂、释放NO和HS的NSAID、前列腺素合酶抑制剂以及EP受体调节剂。已通过PubMed NCBI进行文献检索。专家意见:目前,没有新开发的药物优于已批准的选择性和非选择性NSAID。几种新方法显示出有前景的镇痛效果,但副作用仍然是一个重要问题。解决方案可能分别由允许使用更低药物剂量的联合疗法或针对除COX之外的分子的个体化疗法构成。