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What Is Ibogaine
Buy Iboga root bark (iboga, ibogaine, Tabernanthe) ; Iboga is a shrub indigenous to central west Africa, especially Gabon, Cameroon and Congo. The shrub grows up to 1.5–2 m in height, has yellowish or pinkish flowers, and produces sweet pulpy fruits without any psychoactive alkaloids. The root bark contains about 6% of indole alkaloids: these include ibogaine, ibogaline, ibogamine, and tabernanthine, in the proportions 80%, 15% and 5% respectively for the first three listed. Ibogaine’s chemical formula is C20H26N2O; its molecular mass is 310.433 g/mol. It possesses two distinct chiral centers, thereby generating four stereoisomers.
Apart from extraction from the iboga plant, ibogaine hydrochloride can be semi-synthesized from voacangine, another plant alkaloid which acts as a precursor. Total synthesis of ibogaine was first described in a US patent in 1956 (Janot and Goutarel, 1957), and a decade later Büchi et al. (1966) published a detailed paper on its complete synthesis. Over the years, additional methods of synthesis have been achieved (Frauenfelder, 1999).
Introduction
Ibogaine (12-methoxyibogamine, NIH 10567, Endabuse) is one of the psychoactive indole alkaloids found in the West African shrub,Tabernanthe iboga. For over a century, both extracts of T. iboga and its constituent alkaloids, including ibogaine, have been used as medicinals (1). What make this alkaloid of particular interest to contemporary pharmacology are anecdotal observations indicating that ibogaine possesses “antiaddictive” properties. Thus, ibogaine (6-25 mg/kg, in humans) has been claimed to attenuate both dependence and withdrawal symptoms to a variety of abused dmgs including opiates, alcohol, nicotine, and psychostimulants (2–9). Preclinical studies demonstrating that ibogaine reduces self-administration of both cocaine and morphine, and attenuates the symptoms of morphine withdrawal, are consistent with these claims [reviewed in Popick and Glick (10) ]. This chapter reviews the pharmacological properties of ibogaine and related alkaloids. Since our last comprehensive review (11), more than a hundred new reports on the pharmacological actions of ibogaine and ibogaine-like alkaloids have appeared. The chemistry of ibogaine has been reviewed by Taylor in this series (12,13).
History of Ibogaine
Ibogaine has been used in some countries for many centuries. In the mid-1800s Ibogaine was used in Gabon, Africa in initiation rights of the Bwiti religion. When boys would come of age, usually around age 9–12, it was tradition to have them ingest large amounts of the root and, once they got through the day or two long “trip,” they were thought to be adult men. During this 24-hour period they were cared for by older members of the community who would stay awake by chewing on Ibogaine roots. It was known even then that when using Ibogaine at the hallucinogenic level, suffocation and other side effects could be risks. Buy Iboga root bark
Ibogaine (12-methoxyibogamine, NIH 10567, Endabuse) is one of the psychoactive indole alkaloids found in the West African shrub,Tabernanthe iboga. For over a century, both extracts of T. iboga and its constituent alkaloids, including ibogaine, have been used as medicinals. What make this alkaloid of particular interest to contemporary pharmacology are anecdotal observations indicating that ibogaine possesses “antiaddictive” properties. Thus, ibogaine (6-25 mg/kg, in humans) has been claimed to attenuate both dependence and withdrawal symptoms to a variety of abused dmgs including opiates, alcohol, nicotine, and psychostimulants. Preclinical studies demonstrating that ibogaine reduces self-administration of both cocaine and morphine, and attenuates the symptoms of morphine withdrawal, are consistent with these claims. Buy Iboga root bark
Side effects
Side effects observed immediately on administration of large dose of Ibogaine include ataxia (difficult coordination of muscles in motion), xerostomia (dry mouth), followed by nausea, and vomiting. These symptoms may last between 4 and 24 h. Ibogaine may be given by enema to avoid the vomiting that causes loss of medication dose. Psychiatric medications are contraindicated because of adverse interaction with Ibogaine. Buy Iboga root bark
Ventricular ectopy could present with low ventricular ejection fraction which is a hallmark of systolic heart failure. It has been observed in a minority of patients during Ibogaine therapy. QT-interval prolongation and ventricular tachycardia after large dose was reported in the New England Journal of Medicine. Clinical supervision of the use of Ibogaine in treatment of addiction is highly recommended, while self-treatment should be discouraged because of adverse side effects that could result in fatality. Buy Iboga root bark
Global Use:
Ibogaine use is legal in Canada. In 2002, Marc Emery opened the Iboga Therapy House in Vancouver, Canada. The therapy house offers Ibogaine treatments with blood monitoring and electrocardiogram, complemented with posttreatment follow-up.
Ibogaine is legal in Mexico as well. “Awakening in the Dream House” is an integrative Ibogaine addiction therapy center in Mexico. The author’s conversation with Rocky Caravelli, the manager of the therapy center, focused on side effect management to prevent or minimize fatalities. He disclosed that a “safe therapeutic dose and clinical monitoring are the essence of a successful treatment.” Buy Iboga root bark
Pain and Addiction
The roots of iboga (Tabernanthe iboga (Apocynaceae)) are used throughout central Africa to induce a hallucinogenic experience that serves as a rite of passage into adulthood and which also can treat female sterility. These hallucinations are claimed to render insight as to the causes of sterility, and to facilitate contact with a villager’s ancestors. The indole alkaloid ibogaine as well as its metabolite noribogaine are now under investigation by Deborah Mash at the University of Miami Brain Bank for treatment of chronic pain and to help deal with addiction. Initial clinical trials in St. Kitts with heroin addicts have been highly successful (Mash et al., 2000). The Miami biotech firm DEMERx is seeking FDA approval for an ibogaine treatment for chronic pain.
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Toxicology
The perennial rainforest shrub T. iboga, commonly known as iboga, is native to central western Africa. The plant reaches about 1.5–2 m in height and has yellowish or pinkish flowers that turn into sweet fruits which do not contain psychoactive alkaloids. The plant is a sacrament and symbol of power in the Bwiti religion, with the roots used in religious ceremonies as a ‘bridge to the ancestors.’ In small amounts (up to 5 mg kg−1), the root is chewed by locals to reduce hunger and fatigue, but larger amounts (10 mg kg−1 or greater) will cause hallucinations and have even caused death. Buy Iboga root bark
The root bark contains about 6% indole alkaloids: primarily ibogaine (12-methoxyibogamine), and also tabernanthine, ibogaline, and ibogamine.
Ibogaine is a noncompetitive antagonist at α3β4 nicotinic receptors and a sigma2 receptor agonist, increases ribonucleic acid expression of glial-cell-line-derived neurotrophic factor, is a weak agonist on the serotonin 5HT2A receptor, and is a weak N-methyl-d-aspartate receptor antagonist. The major metabolite, noribogaine (12-hydroxyibogamine), is a potent serotonin reuptake inhibitor and is also a moderate kappa and weak mu opioid receptor full agonist. Ibogaine has also been used to treat dependency on alcohol and illicit drugs, although its efficacy is questionable. Buy Iboga root bark
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