COMPOSITIONS AND METHODS FOR ENHANCING ANALGESIC POTENCY OF COVALENTLY BOUND-COMPOUNDS, ATTENUATING ITS ADVERSE SIDE EFFECTS, AND PREVENTING THEIR ABUSE
申请人:Kirk Randal J.
公开号:US20100144645A1
公开(公告)日:2010-06-10
The invention generally relates to compositions and methods with covalently bound compounds, such as controlled substances covalently attached to a chemical moiety, and opioid antagonists or covalently bound opioid antagonists to enhance analgesic potency and/or attenuate one or more adverse effects of covalently bound compounds, including adverse side effect(s) in humans such as nausea, vomiting, dizziness, headache, sedation (somnolence), physical dependence or pruritis. This invention relates to compositions and methods for selectively enhancing the analgesic potency of a covalently bound compound and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of a covalently bound compound. The methods of the invention comprise administering to a subject an analgesic or sub-analgesic amount of a covalently bound compound and an amount of excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of a covalently bound compound and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of covalently bound compound. The invention also relates to the addition of covalently-bound opioid antagonists to the compositions containing covalently bound compounds such that if the compositions are subjected to manipulation by illicit chemists, the opioid antagonist is released effectively reducing or eliminating the euphoric effect of the covalently bound compounds.
本发明通常涉及具有共价结合化合物的组合物和方法,例如将受控物质共价附着到化学基团上,以及阿片拮抗剂或共价结合的阿片拮抗剂,以增强镇痛效力和/或减轻共价结合化合物的一个或多个不良反应,包括在人类中的不良副作用,如恶心、呕吐、头晕、头痛、镇静(嗜睡)、身体依赖或瘙痒。本发明涉及组合物和方法,用于选择性增强共价结合化合物的镇痛效力,并同时减轻与共价结合化合物的给药相关的抗镇痛作用、过敏症、过度兴奋、身体依赖和/或耐受效应。本发明的方法包括向受试者注射镇痛剂或亚镇痛剂量的共价结合化合物,以及有效增强共价结合化合物的镇痛效力和减轻共价结合化合物的抗镇痛作用、过敏症、过度兴奋、身体依赖和/或耐受效应的兴奋性阿片受体拮抗剂,例如纳曲酮或纳尔美芬。本发明还涉及向含有共价结合化合物的组合物中添加共价结合的阿片受体拮抗剂,以便如果组合物被非法化学家操作,阿片受体拮抗剂会被有效释放,从而减少或消除共价结合化合物的欣快效应。