Mash D C, Kovera C A, Pablo J, Tyndale R F, Ervin F D, Williams I C, Singleton E G, Mayor M
Department of Neurology, University of Miami School of Medicine, Florida 33136, USA.
Ann N Y Acad Sci. 2000 Sep;914:394-401. doi: 10.1111/j.1749-6632.2000.tb05213.x.
Ibogaine is an indole alkaloid found in the roots of Tabernanthe Iboga (Apocynaceae family), a rain forest shrub that is native to western Africa. Ibogaine is used by indigenous peoples in low doses to combat fatigue, hunger and thirst, and in higher doses as a sacrament in religious rituals. Members of American and European addict self-help groups have claimed that ibogaine promotes long-term drug abstinence from addictive substances, including psychostimulants and opiates. Anecdotal reports attest that a single dose of ibogaine eliminates opiate withdrawal symptoms and reduces drug craving for extended periods of time. The purported efficacy of ibogaine for the treatment of drug dependence may be due in part to an active metabolite. The majority of ibogaine biotransformation proceeds via CYP2D6, including the O-demethylation of ibogaine to 12-hydroxyibogamine (noribogaine). Blood concentration-time effect profiles of ibogaine and noribogaine obtained for individual subjects after single oral dose administrations demonstrate complex pharmacokinetic profiles. Ibogaine has shown preliminary efficacy for opiate detoxification and for short-term stabilization of drug-dependent persons as they prepare to enter substance abuse treatment. We report here that ibogaine significantly decreased craving for cocaine and heroin during inpatient detoxification. Self-reports of depressive symptoms were also significantly lower after ibogaine treatment and at 30 days after program discharge. Because ibogaine is cleared rapidly from the blood, the beneficial aftereffects of the drug on craving and depressed mood may be related to the effects of noribogaine on the central nervous system.
伊博格碱是一种吲哚生物碱，存在于原产于西非的热带雨林灌木——伊博格（夹竹桃科）的根部。伊博格碱在低剂量时被当地居民用于对抗疲劳、饥饿和口渴，而在高剂量时则作为宗教仪式中的圣礼使用。美国和欧洲成瘾者自助组织的成员声称，伊博格碱能促进对包括精神兴奋剂和阿片类药物在内的成瘾物质的长期戒毒。轶事报告证明，单剂量的伊博格碱可消除阿片类药物戒断症状，并在较长时间内减少对药物的渴望。伊博格碱治疗药物依赖的所谓疗效可能部分归因于一种活性代谢物。伊博格碱的大多数生物转化是通过CYP2D6进行的，包括伊博格碱的O-去甲基化生成12-羟基伊博格胺（去甲伊博格碱）。个体受试者单次口服给药后获得的伊博格碱和去甲伊博格碱的血药浓度-时间效应曲线显示出复杂的药代动力学特征。伊博格碱已显示出在阿片类药物解毒以及药物依赖者准备进入药物滥用治疗时的短期稳定方面具有初步疗效。我们在此报告，伊博格碱在住院戒毒期间显著降低了对可卡因和海洛因的渴望。伊博格碱治疗后以及项目出院后30天，抑郁症状的自我报告也显著降低。由于伊博格碱从血液中清除迅速，该药物对渴望和抑郁情绪的有益后效应可能与去甲伊博格碱对中枢神经系统的作用有关。
