CN103588671A - 癌性疼痛治疗药物 - Google Patents
癌性疼痛治疗药物 Download PDFInfo
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Abstract
本发明属于医药技术领域,涉及一种癌性疼痛治疗药物,本发明还涉及含有该药物的组合物。
Description
技术领域
本发明属于生物医药领域,具体涉及一种癌性疼痛治疗药物。
背景技术
疼痛是最常见的肿瘤相关症状之一,疼痛的定义是“与实际或潜在的组织损伤或类似损伤相关联的感觉和情绪体验”。癌性疼痛是指癌症、癌症相关性病变及抗癌治疗所致的疼痛。癌性疼痛常为慢性痛。疼痛是癌症患者的常见症状,约1/4新诊断的癌症患者,1/3正在接受治疗的癌症患者和3/4晚期癌症患者合并疼痛,癌症疼痛患者可能生存数月或数年,如果得不到恰当的止痛治疗,患者将长期忍受疼痛的折磨,并极大影响他们的活动、睡眠、心情以及整体生活质量,癌痛动摇着患者的人格完整性,支配着他们的自我意识,引起内心深处持久的极度痛苦。癌性疼痛患者在精神、社会心理、生活方式上所感受到的痛苦、焦虑往往超过疾病本身所造成的疼痛。
世界卫生组织(WHO)1982年组织姑息治疗专家、癌性疼痛专家制定了缓解癌性疼痛的全球指南,即著名的三阶梯止痛疗法,尽管20余年过去了,三阶梯的基本原则仍被广泛接受。WHO确定了以阿片类镇痛药为中心的疼痛治疗的国际基准,按照此基准的治疗法成为了癌性疼痛治疗的主流。轻度疼痛:首选三阶梯的第一阶梯以阿司匹林为代表的非甾体抗炎药(Nonsteroidal Antiinflammatory Drugs,NSAIDs);中度疼痛:首选弱阿片类药物(以可卡因为代表),并可合用非甾体类抗炎药;重度疼痛:首选强阿片类药物(以吗啡为代表),并可同时合用非甾体类抗炎药。但是,已知非阿片类镇痛药NSAIDs容易发生胃肠损害或肾损害等副作用。还知道阿片类镇痛药吗啡作为代表性的副作用有便秘、恶心、呕吐等,还有由于突然中止给药或减少给药量而带来戒断症状。另外,在癌性疼痛中也包含神经源性疼痛,由于其是末梢神经或中枢神经受到伤害而发生的疼痛,所以阿片类效果有限。另外,在吗啡慢性给药时,胆囊收缩素或神经肽Y等抗阿片类物质增强,致使吗啡的镇痛效果下降,形成镇痛耐药性。所以需要开发出副作用少的镇痛药来代替现有的非阿片类及阿片类镇痛药。
发明内容
本发明的目的是为了弥补市场上产品的不足,提供一种癌性疼痛治疗药物,化学名为:7S,8R,17S-三羟基-4Z,9E,11E,13Z,15E,19Z-二十二碳六烯-N-异丁基酰胺,结构式为:
本发明的癌性疼痛治疗药物可以与一种或多种药用辅料制成药学上可接受的任一剂型。
具体实施方式
实施例1.缓解癌性疼痛药效的评价
动物建模:动物麻醉后,左侧后肢剪毛,75%乙醇消毒股骨及胫骨处皮肤,膝关节处沿着股直肌肌腱方向切一长约0.5~1.0cm的皮肤切口,小心暴露髌骨,先用一次性无菌1mL注射器针头在髌骨沿股骨长轴方向穿刺打孔,然后换上10μL注射器进入股骨骨髓腔,缓慢注入10μL的Lewis小鼠肺癌细胞溶液(含3×105个细胞)至股骨。注射完毕后用骨腊封住针孔,清洗创口,皮肤缝合。假手术组动物左侧髌骨注入等体积的生理盐水,其余操作同模型组,空白组不进行任何处理。
评价指标:用小鼠热板法测量热刺激痛阈,先将热板温度恒定在(50±1)℃,然后将小鼠放置在热板上,待出现舔后足时所需要的时间值(s)即为该动物的痛阈值,每只小鼠测3次,间隔5min,取3次均值作为该动物的热刺激痛阈值(筛选基础痛阈在10~30s的动物用于实验)。
给药方法和结果:造模第8天开始给药,连用7d。造模第14天,治疗组热刺激痛阈明显延长,与模型组比较有显著性差异(P<0.05),见表1。
表1.癌痛各组小鼠不同时间点热刺激痛阈的变化
与模型组同时间点比较ΔP<0.05
结论:表1数据充分表明本发明的癌性疼痛治疗药物具有良好的防治癌性疼痛的作用。
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Citations (5)
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US20040116408A1 (en) * | 2002-08-12 | 2004-06-17 | Serhan Charles N. | Resolvins: biotemplates for novel therapeutic interventions |
US20060293288A1 (en) * | 2005-01-07 | 2006-12-28 | Serhan Charles N | Use of resolvins to treat gastrointestinal diseases |
WO2008063772A2 (en) * | 2006-10-13 | 2008-05-29 | The Brigham And Women's Hospital Inc. | Resolvin d series and protectin d1 mitigate acute kidney injury |
WO2011034887A2 (en) * | 2009-09-15 | 2011-03-24 | The Brigham And Women's Hospital, Inc. | A method for treating neuropathic pain |
CN103193643A (zh) * | 2013-04-01 | 2013-07-10 | 史克勇 | Resolvin D1衍生物在癌性疼痛中的应用 |
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- 2013-10-28 CN CN201310537668.5A patent/CN103588671A/zh active Pending
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
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US20040116408A1 (en) * | 2002-08-12 | 2004-06-17 | Serhan Charles N. | Resolvins: biotemplates for novel therapeutic interventions |
US20060293288A1 (en) * | 2005-01-07 | 2006-12-28 | Serhan Charles N | Use of resolvins to treat gastrointestinal diseases |
WO2008063772A2 (en) * | 2006-10-13 | 2008-05-29 | The Brigham And Women's Hospital Inc. | Resolvin d series and protectin d1 mitigate acute kidney injury |
WO2011034887A2 (en) * | 2009-09-15 | 2011-03-24 | The Brigham And Women's Hospital, Inc. | A method for treating neuropathic pain |
CN103193643A (zh) * | 2013-04-01 | 2013-07-10 | 史克勇 | Resolvin D1衍生物在癌性疼痛中的应用 |
Non-Patent Citations (1)
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Application publication date: 20140219 |