Ibogaine and the inhibition of acetylcholinesterase (original) (raw)
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Archives of Clinical Psychiatry (São Paulo)
Background: Therapeutic properties of ibogaine in the treatment of addiction are attracting both clinicians and patients to its use. Since ibogaine is not an authorized medicine, the quality of these products is not always known, increasing the probability of adverse reactions. Objective: This study collects different types of iboga-derived samples from treatment providers, vendors and online buyers to analyse their content. Methods: Analysis of iboga products (n = 16) was performed using gas chromatography and mass spectrometry methods (GC/MS). Products included Iboga root bark, Total Alkaloids (TA), Purified Total Alkaloids (PTA HCl), ibogaine hydrochloride (ibogaine HCl) and one Voacanga africana root bark. Results: The content of ibogaine was highly variable, ranging from 0.6% to 11.2% for products sold as iboga root bark, from 8.2% to 32.9% for products sold as TA, 73.7% for one sample sold as PTA and from 61.5% to 73.4% for products sold as ibogaine HCl. One sample did not show any iboga alkaloids. Other alkaloids and unknown substances were found in almost all samples. Discussion: The purity of iboga products is highly variable. These results should be taken into consideration by suppliers and users, especially regarding correct dosing to avoid overdose, as well as potential interactions with other substances.
Ibogaine in the Treatment of Substance Dependence
Ibogaine is a psychoactive alkaloid derived from Tabernanthe iboga, a plant used in initiatory rituals in West Central Africa. Largely because of ibogaine's status as a Schedule I substance in the U.S., the development of ibogaine's use in the treatment of drug addiction took place outside conventional clinical and medical settings. This article reviews the history of ibogaine's use in the treatment of drug addiction, and discusses progress made towards, and obstacles blocking, the establishment of controlled clinical trials of ibogaine's efficacy. Preclinical research has generally supported anecdotal claims that ibogaine attenuates withdrawal symptoms and reduces drug cravings. Concerns about ibogaine's safety, as well as a dearth of solid data from human studies, have hampered progress in its development as an approved medication. This article outlines major findings from preclinical studies, discusses concerns about ibogaine's safety, and details previous and ongoing research on ibogaine's use as an anti-addictive treatment for humans.
IBOGAINE is a potentially hallucinogenic indole alkaloid with anecdotal antiaddictive properties against multiple drugs of abuse. Medical literature concerning the administration of this substance to humans is sparce. Ibogaine HCL (20-25 mg/kg) was administered orally to five subjects addicted to cocaine and/or opiates. Subjects underwent continuous intensive medical, neurologic and electroencephalographic observation. Movement-induced nausea and vomiting was seen in several subjects, all developed transient ataxia, and several experienced visual hallucinosis. No general medical, EKG or EEG abnormalities were seen. No subjects experienced withdrawal symptoms 24 hours after treatment, and two subjects were free of withdrawal or craving one week after treatment.
Psychopharmacology, 1996
The purported efficacy of ibogaine for the treatment of drug dependence may be due in part to an active metabolite. Ibogaine undergoes first pass metabolism and isO-demethylated to 12-hydroxyibogamine (12-OH ibogamine). Radioligand binding assays were conducted to identify the potency and selectivity profiles for ibogaine and 12-OH ibogamine. A comparison of 12-OH ibogamine to the primary molecular targets identified previously for ibogaine demonstrates that the metabolite has a binding profile that is similar, but not identical to the parent drug. Both ibogaine and 12-OH ibogamine demonstrated the highest potency values at the cocaine recognition site on the 5-HT transporter. The same rank order (12-OH ibogamine > ibogaine), but lower potencies were observed for the [3H]paroxetine binding sites on the 5-HT transporter. Ibogaine and 12-OH ibogamine were equipotent at vesicular monoamine and dopamine transporters. The metabolite demonstrated higher affinity at the kappa-1 receptor and lower affinity at the NMDA receptor complex compared to the parent drug. Quantitation of the regional brain levels of ibogaine and 12-OH ibogamine demonstrated micromolar concentrations of both the parent drug and metabolite in rat brain. Drug dependence results from distinct, but inter-related neurochemical adaptations, which underlie tolerance, sensitization and withdrawal. Ibogaine’s ability to alter drug-seeking behavior may be due to combined actions of the parent drug and metabolite at key pharmacological targets that modulate the activity of drug reward circuits.
A narrative review of the pharmacological, cultural and psychological literature on ibogaine
Journal of Psychedelic Studies
Ibogaine is a psychoactive alkaloid contained in the West African plant Tabernanthe iboga. Although preliminary, evidence suggests that ibogaine could be effective in the treatment of certain substance use disorders, specifically opioid use disorder. This narrative review concentrated on the pharmacological, cultural and psychological aspects of ibogaine that contribute to its reputed effectiveness with a specific focus on the ibogaine state of consciousness. Although the exact pharmacological mechanisms for ibogaine are still speculative, the literature highlighted its role as an NMDA antagonist in the effective treatment of substance use disorders. The cultural aspects associated with the use of ibogaine pose questions around the worldview of participants as experienced in the traditional and western contexts, which future research should clarify. From a psychological perspective, the theory that the ibogaine state of consciousness resembles REM sleep is questionable due to eviden...