Ibogaine
Encyclopedia
Ibogaine is a naturally occurring psychoactive
substance found in a number of plants, principally in a member of the Apocynaceae
family known as Iboga (Tabernanthe iboga). A hallucinogen with both psychedelic
and dissociative properties, the substance is banned in some countries; in other countries it is being used to treat addiction
to opiate
s, methamphetamine
and other drugs. Derivatives of ibogaine that lack the substance's hallucinogen properties are under development.
Ibogaine-containing preparations are used in medicinal and ritual purposes within Africa
n spiritual traditions of the Bwiti
, who claim to have learned it from the Pygmy
. Although it was first commonly advertised as having anti-addictive properties in 1962 by Howard Lotsof
, its western use predates that by at least a century. In France it was marketed as Lambarene, a medical drug used for dieting. Additionally, Freedom of Information Act documents released in the 1980s show that the U.S. Central Intelligence Agency
(CIA) studied the effects of ibogaine in the 1950s.
Ibogaine is an indole alkaloid that is obtained either by extraction from the iboga plant or by semi-synthesis from the precursor compound voacangine
, another plant alkaloid. A full organic synthesis of ibogaine has been achieved. The synthesis process is too expensive and challenging to be used to produce a commercially significant yield, primarily due to the need to conduct the synthesis in an anoxic environment.
While ibogaine's prohibition
in the U.S. has slowed scientific research into its anti-addictive properties, the use of ibogaine for drug treatment has grown in the form of a large worldwide medical subculture
. Ibogaine is now used by treatment clinics in 12 countries on six continents to facilitate detoxification and relief of chemical dependence to substances such as methadone, heroin, alcohol, powder cocaine, crack cocaine, and methamphetamine
, and to facilitate psychological introspection
and spiritual exploration.
'. Because of the ibogaine molecule's tryptamine core, ibogaine acts as an agonist for the 5-HT2A receptor
set like other psychedelic
tryptamine
s (such as DMT
and psilocybin
) and other serotonergic psychedelic
s like LSD and mescaline
. However what makes ibogaine's pharmacodynamic
properties and subjective experience unique from that of other psychedelic tryptamines and serotonergic psychedelics is that it also acts as a dissociative through antagonism of the NMDA receptor
set (like ketamine
) as well as acting as an agonist for the κ-opioid receptor
set, like the diterpenoid
compound salvinorin A
(found in Salvia divinorum
). Ibogaine's agonism to the κ-opioid receptors is thought to be what is responsible for ibogaine's well-documented anti-addictive properties, as salvinorin A exhibits a similar alleviation of withdrawal symptoms in individuals addicted to opiate
s and methamphetamine
.
DMT
and the dissociative ketamine
; see above) and an introspective phase (ostensibly the comedown).
The visual phase is characterized by open-eye visuals, closed-eye visuals, and dreamlike sequences. Objects may be seen as distorted, projecting tracers, or having moving colors or textures. When the eyes are closed, extremely detailed and vivid geometric and fractal visions may be seen. Subjective reports often include a movie-like recollection of earlier life experiences as well as dreamlike sequences with symbolism of one's present or anticipated future. Other effects in the visual phase may include laughing, sensations of euphoria or fear, and temporary short-term memory impairment. The visual phase usually ends after one to four hours, after which the introspective phase begins.
Ibogaine has been referred to as an oneirophrenic
(especially during the initial wave of psychedelic research following the discovery of LSD that occurred in late 1950s
and early 1960s
), referring to the dreamlike nature of its hallucinogenic effects. Ibogaine catalyzes an altered state of consciousness
reminiscent of dreaming while fully conscious and aware so that memories; life experiences; and issues of trauma can be processed in a subjective manner.
The introspective phase is typically reported to bring elevated mood, a sense of calm and euphoria, and a distinct intellectual and emotional clarity. Subjects often report being able to accomplish deep emotional and intellectual introspection into psychological and emotional concerns. It is also during this period that opioid addicts first notice the absence of withdrawal symptoms or cravings. The duration of the introspective phase is highly variable, usually lasting hours but sometimes lasting days.
, a difficulty in coordinating muscle motion which makes standing and walking difficult without assistance. Xerostomia
(dry mouth), nausea
, and vomiting may follow. These symptoms may be long in duration, ranging from 4 to 24 hours in some cases. Ibogaine is sometimes administered by enema
to help the subject avoid vomiting up the dose. Psychiatric medications are strongly contraindicated in ibogaine therapy due to adverse interactions. Some studies also suggest the possibility of adverse interaction with heart conditions. In one study of canine subjects, ibogaine was observed to increase sinus arrhythmia (the normal change in heart rate during respiration). Ventricular ectopy has been observed in a minority of patients during ibogaine therapy. It has been proposed that there is a risk of QT-interval prolongation following ibogaine administration. This risk was further demonstrated by a case reported in the New England Journal of Medicine
documenting prolonged QT interval and ventricular tachycardia
after initial use.
There are 12 documented fatalities that have been loosely associated with ibogaine ingestion. Exact determinations of the cause of death have proven elusive due to the quasi-legal status of ibogaine and the unfamiliarity of medical professionals with this relatively rare substance. No autopsy to date has implicated ibogaine as the sole cause of death. Causes given range from significant pre-existing medical problems to the co-consumption of drugs such as opiates which are potentiated by ibogaine. Also, because ibogaine is one of the many drugs that are partly metabolized by the cytochrome P450 complex, caution must be exercised to avoid foods or drugs that inhibit CP450, in particular foodstuffs containing bergamottin
or bergamot oil, common ones being grapefruit juice and Earl Grey tea
.
to opioid
s. An integral effect is the alleviation of symptoms of opioid withdrawal
. Research also suggests that ibogaine may be useful in treating dependence on other substances such as alcohol
, methamphetamine
, and nicotine
and may affect compulsive behavioral patterns not involving substance abuse or chemical dependence. However, researchers note that there remains a "need for systematic investigation in a conventional clinical research setting."
Proponents of ibogaine treatment for drug addiction have established formal and informal clinics or self-help groups in Canada
, Mexico
, the Caribbean
, Costa Rica
, the Czech Republic
, France
, Slovenia
, the Netherlands
, Brazil
, South Africa
, the United Kingdom
and New Zealand
, where ibogaine is administered as an experimental compound . Many users of ibogaine report experiencing visual phenomena during a waking dream state, such as instructive replays of life events that led to their addiction, while others report therapeutic shamanic visions that help them conquer the fears and negative emotions that might drive their addiction. It is proposed that intensive counseling, therapy and aftercare during the interruption period following treatment is of significant value. Some individuals require a second or third treatment session with ibogaine over the course of the next 12 to 18 months. A minority of individuals relapse completely into opiate addiction within days or weeks. A comprehensive article (Lotsof 1995) on the subject of ibogaine therapy detailing the procedure, effects and aftereffects is found in "Ibogaine in the Treatment of Chemical Dependence Disorders: Clinical Perspectives". Ibogaine has also been reported in multiple small-study cohorts to reduce cravings for methamphetamine.
There is also evidence that this type of treatment works with LSD
which has been shown to have therapeutic effect on alcoholism as far back as the 1960s. Both ibogaine and LSD appear to be effective at encouraging introspection and giving the user occasion to reflect on where their addiction came from while also occasioning an intense, transformative experience that can put established patterns of behaviour into perspective; ibogaine has the added benefit of preventing withdrawal effects.
analgesia. Further research was abandoned, and no additional data was ever published by Ciba researchers on ibogaine–opioid interactions. Almost 50 years later, Patrick Kroupa and Hattie Wells released the first treatment protocol for concomitant administration of ibogaine with opioids in human subjects, indicating ibogaine reduced tolerance to opioid drugs. Kroupa et al. published their research in the Multidisciplinary Association for Psychedelic Studies
Journal demonstrating that administration of low-"maintenance" doses of ibogaine HCl with opioids decreases tolerance. It should be noted however, that the potentiation action of ibogaine may make this a very risky procedure.
by Claudio Naranjo
, documented in his book The Healing Journey.
in 1901 by Dybowski and Landrin and independently by Haller and Heckel in the same year using T. iboga samples from Gabon
. In the 1930s, ibogaine was sold in France in 8 mg tablets under the name "Lambarene". The total synthesis of ibogaine was accomplished by G. Büchi in 1966. Since then, several further totally synthetic routes have been developed.
In the early 1960s, anecdotal reports appeared concerning ibogaine's effects. The use of ibogaine in treating substance use disorders in human subjects was first observed by Howard Lotsof
in 1962, for which he was later awarded in 1985. In 1969, Claudio Naranjo was granted a French patent for the use of ibogaine in psychotherapy.
Ibogaine was placed in US Schedule 1 in 1967 as part of the US government's strong response to the upswing in popularity of psychedelic substances, though iboga itself was scarcely known at the time. Ibogaine's ability to attenuate opioid withdrawal
confirmed in the rat was first published by Dzoljic et al. (1988). Ibogaine's use in diminishing morphine
self-administration in preclinical studies was shown by Glick et al. (1991) and ibogaine's capacity to reduce cocaine
self-administration in the rat was shown by Cappendijk et al. (1993). Animal model support for ibogaine claims to treat alcohol dependence
were established by Rezvani (1995).
The name "Indra extract", in strict terms, refers to 44 kg of an iboga extract manufactured by an unnamed European industrial manufacturer in 1981. This stock was later purchased by Carl Waltenburg, who distributed it under the name "Indra extract". Waltenburg used this extract to treat heroin addicts in Christiania
, Denmark, a squatter village where heroin addiction was widespread in 1982. Indra extract was offered for sale over the Internet until 2006, when the Indra web presence disappeared. It is unclear whether the extracts currently sold as "Indra extract" are actually from Waltenburg's original stock, or whether any of that stock is even viable or in existence. Ibogaine and related indole
compounds are susceptible to oxidation when exposed to oxygen
, as opposed to their salt form, which is stable. The exact methods and quality of the original Indra extraction was never documented, so the real composition of the product remains uncertain.
An ibogaine research project was funded by the US National Institute on Drug Abuse
in the early 1990s. The National Institute on Drug Abuse (NIDA) abandoned efforts to continue this project into clinical studies in 1995, citing other reports that suggested a risk of brain damage with extremely high doses and fatal heart arrhythmia in patients having a history of health problems, as well as inadequate funding for ibogaine development within their budget. However, NIDA funding for ibogaine research continued in indirect grants often cited in peer-reviewed ibogaine publications.
Data demonstrating ibogaine's efficacy in attenuating opioid withdrawal in drug-dependent human subjects was published by Alper et al. (1999) and Mash et al. (2000).
In addition, after years of work and a number of significant changes to the original protocol, on August 17, 2006, a MAPS
-sponsored research team received "unconditional approval" from a Canadian Institutional Review Board (IRB) to proceed with a long-term observational case study that will examine changes in substance use in 20 consecutive people seeking ibogaine-based therapy for opiate dependence at the Iboga Therapy House in British Columbia, Canada.
Currently, pure crystalline ibogaine hydrochloride is the most standardized formulation. It is typically produced by the semi-synthesis from voacangine
in commercial laboratories. Ibogaine has two separate chiral
centers which means that there are four different stereoisomers of ibogaine. These four isomers are difficult to resolve
.
A synthetic derivative of ibogaine, 18-methoxycoronaridine
(18-MC), is a selective α3β4 antagonist that was developed collaboratively by the neurologist Stanley D. Glick (Albany) and the chemist Martin E. Kuehne (Vermont). This discovery was stimulated by earlier studies on other naturally occurring analogues of ibogaine such as coronaridine
and voacangine
that showed these compounds also have anti-addictive properties.
systems simultaneously.
Because of its fairly low potency at any of its target sites, ibogaine is used in doses anywhere from 5 mg/kg of body weight for a minor effect to 30 mg/kg in the cases of strong polysubstance addiction. It is unknown whether doses greater than 30 mg/kg in humans produce effects that are therapeutically beneficial, medically risky, or simply prolonged in duration. In animal neurotoxicity studies, there was no observable neurotoxicity of ibogaine at 25 mg/kg, but at 50 mg/kg, one-third of the rats had developed patches of neurodegeneration, and at doses of 75 mg/kg or above, all rats showed a characteristic pattern of degeneration of Purkinje neurons, mainly in the cerebellum
. While caution should be exercised when extrapolating animal studies to humans, these results suggest that neurotoxicity of ibogaine is likely to be minimal when ibogaine is used in the 10–20 mg/kg range typical of drug addiction interruption treatment regimes, and indeed death from the other pharmacological actions of the alkaloids is likely to occur by the time the dose is high enough to produce consistent neurotoxic changes.
in the human body by cytochrome P450 2D6, and the major metabolite is noribogaine
(12-hydroxyibogamine). Noribogaine is most potent as a serotonin reuptake inhibitor and acts as a moderate κ- and weak µ-opioid receptor
full agonist and therefore, also has an aspect of an opiate replacement
similar to compounds like methadone
. It is possible that this action of noribogaine at the kappa opioid receptor may indeed contribute significantly to the psychoactive effects attributed to ibogaine ingestion; salvia divinorum
, another plant recognized for its strong hallucinogenic properties, contains the chemical salvinorin-A which is a highly selective kappa opioid agonist. Both ibogaine and noribogaine have a plasma half-life of around two hours in the rat, although the half-life of noribogaine is slightly longer than the parent compound. It is proposed that ibogaine is deposited in fat and metabolized into noribogaine as it is released. Noribogaine shows higher plasma levels than ibogaine and may therefore be detected for longer periods of time than ibogaine. Noribogaine is also more potent than ibogaine in rat drug discrimination assays when tested for the subjective effects of ibogaine. Noribogaine differs from ibogaine in that it contains a hydroxy
instead of a methoxy
group
at the 12 position.
Ibogaine and its salts
were regulated by the U.S. Food and Drug Administration
in 1967 pursuant to its enhanced authority to regulate stimulants, depressants, and hallucinogens granted by the 1965 Drug Abuse Control Amendments (DACA) to the Federal Food, Drug, and Cosmetic Act
. In 1970, with the passage of the Controlled Substances Act
, it was classified as a Schedule I-controlled substance in the United States, along with other psychedelics such as DMT
and mescaline
. Since that time, several other countries, including Sweden, Denmark, Belgium, and Switzerland, have also banned the sale and possession of Ibogaine. Although illegal in these countries, Ibogaine has been used by hundreds of drug dependents in the United States and abroad. Howard Lotsof
, a pioneer in bringing awareness to Ibogaine's success in helping long-time drug dependents to quit their addiction, and others have been offering willing persons the treatment. In the Czech Republic and Slovenia, taking advantage of less prohibitive legal systems, ibogaine has been applied to people coming from the U.S. and other countries seeking a safe haven.
Ibogaine is not the subject of any regulation in Canada. In Sweden, a non-profit foundation was formed in early 2006 to address the issue of providing ibogaine for addiction interruption within established drug treatment care.
accused Democratic candidate Edmund Muskie
of being addicted to ibogaine in a satirical piece while covering the Wisconsin primaries of the 1972 U.S. Presidential primaries
for Rolling Stone
magazine. Many readers, and even other journalists, did not realize that Thompson was being facetious. The claim was completely unfounded, and Thompson himself is documented in the movie Gonzo: The Life and Work of Dr. Hunter S. Thompson
discussing the self-fabricated joke of Muskie's alleged ibogaine use and his surprise that anyone actually believed the claim.
Ibogaine has been the subject of several full-length documentary films including Detox or Die in 2004, by director David Graham Scott a feature film aired by the BBC, documenting Scott's own drug addiction and ibogaine treatment. Ibogaine Rite of Passage, directed by Ben Deloenen in 2005, with Howard Lotsof
and Patrick K. Kroupa
which focused on both native Bwiti ritualistic use of ibogaine as well as modern science and treatment clinics. In 2007 filmmaker Magnolia Martin directed Facing the Habit documenting a one-time millionaire and former stockbroker whose life spiraled out of control due to heroin addiction traveling to Mexico to receive ibogaine treatment. In 2009 a feature documentary I'm Dangerous with Love by filmmaker Michel Negroponte, covered the work of Dimitri Mugianis and his long-running underground ibogaine treatment for heroin addiction.
In addition to documentaries, ibogaine has played a central role in the plot-lines of several episodes of television programs, including:
The X-Files: Via Negativa, Season 8, Episode 7 (2000)
C.S.I.: Getting Off, Season 4, Episode 16 (2004)
Law & Order Special Victims Unit: Users, Season 11, Episode 7 (2009)
Nikita: Echoes, Season 1, Episode 16 (2011)
Psychoactive drug
A psychoactive drug, psychopharmaceutical, or psychotropic is a chemical substance that crosses the blood–brain barrier and acts primarily upon the central nervous system where it affects brain function, resulting in changes in perception, mood, consciousness, cognition, and behavior...
substance found in a number of plants, principally in a member of the Apocynaceae
Apocynaceae
The Apocynaceae or dogbane family is a family of flowering plants that includes trees, shrubs, herbs, and lianas.Many species are tall trees found in tropical rainforests, and most are from the tropics and subtropics, but some grow in tropical dry, xeric environments. There are also perennial herbs...
family known as Iboga (Tabernanthe iboga). A hallucinogen with both psychedelic
Psychedelic
The term psychedelic is derived from the Greek words ψυχή and δηλοῦν , translating to "soul-manifesting". A psychedelic experience is characterized by the striking perception of aspects of one's mind previously unknown, or by the creative exuberance of the mind liberated from its ostensibly...
and dissociative properties, the substance is banned in some countries; in other countries it is being used to treat addiction
Addiction
Historically, addiction has been defined as physical and psychological dependence on psychoactive substances which cross the blood-brain barrier once ingested, temporarily altering the chemical milieu of the brain.Addiction can also be viewed as a continued involvement with a substance or activity...
to opiate
Opiate
In medicine, the term opiate describes any of the narcotic opioid alkaloids found as natural products in the opium poppy plant.-Overview:Opiates are so named because they are constituents or derivatives of constituents found in opium, which is processed from the latex sap of the opium poppy,...
s, methamphetamine
Methamphetamine
Methamphetamine is a psychostimulant of the phenethylamine and amphetamine class of psychoactive drugs...
and other drugs. Derivatives of ibogaine that lack the substance's hallucinogen properties are under development.
Ibogaine-containing preparations are used in medicinal and ritual purposes within Africa
Africa
Africa is the world's second largest and second most populous continent, after Asia. At about 30.2 million km² including adjacent islands, it covers 6% of the Earth's total surface area and 20.4% of the total land area...
n spiritual traditions of the Bwiti
Bwiti
Bwiti is a West Central African spiritual practice by the forest-dwelling Babongo and Mitsogo people of Gabon, where it is counted as one of the three official religions, and the Fang people of Gabon and Cameroon...
, who claim to have learned it from the Pygmy
Pygmy
Pygmy is a term used for various ethnic groups worldwide whose average height is unusually short; anthropologists define pygmy as any group whose adult men grow to less than 150 cm in average height. A member of a slightly taller group is termed "pygmoid." The best known pygmies are the Aka,...
. Although it was first commonly advertised as having anti-addictive properties in 1962 by Howard Lotsof
Howard Lotsof
Howard Lotsof was an American scientific researcher and patent holder.When he was 19 years old and addicted to heroin, he accidentally discovered the anti-addictive effects of ibogaine in 1962. He later attended Fairleigh Dickinson University and then New York University, graduating with a degree...
, its western use predates that by at least a century. In France it was marketed as Lambarene, a medical drug used for dieting. Additionally, Freedom of Information Act documents released in the 1980s show that the U.S. Central Intelligence Agency
Central Intelligence Agency
The Central Intelligence Agency is a civilian intelligence agency of the United States government. It is an executive agency and reports directly to the Director of National Intelligence, responsible for providing national security intelligence assessment to senior United States policymakers...
(CIA) studied the effects of ibogaine in the 1950s.
Ibogaine is an indole alkaloid that is obtained either by extraction from the iboga plant or by semi-synthesis from the precursor compound voacangine
Voacangine
Voacangine is an alkaloid found predominantly in the rootbark of the Voacanga africana tree, as well as in other plants such as Tabernanthe iboga, Tabernaemontana africana, Trachelospermum jasminoides and Ervatamia yunnanensis...
, another plant alkaloid. A full organic synthesis of ibogaine has been achieved. The synthesis process is too expensive and challenging to be used to produce a commercially significant yield, primarily due to the need to conduct the synthesis in an anoxic environment.
While ibogaine's prohibition
Prohibition (drugs)
The prohibition of drugs through sumptuary legislation or religious law is a common means of attempting to prevent drug use. Prohibition of drugs has existed at various levels of government or other authority from the Middle Ages to the present....
in the U.S. has slowed scientific research into its anti-addictive properties, the use of ibogaine for drug treatment has grown in the form of a large worldwide medical subculture
Subculture
In sociology, anthropology and cultural studies, a subculture is a group of people with a culture which differentiates them from the larger culture to which they belong.- Definition :...
. Ibogaine is now used by treatment clinics in 12 countries on six continents to facilitate detoxification and relief of chemical dependence to substances such as methadone, heroin, alcohol, powder cocaine, crack cocaine, and methamphetamine
Methamphetamine
Methamphetamine is a psychostimulant of the phenethylamine and amphetamine class of psychoactive drugs...
, and to facilitate psychological introspection
Transpersonal psychology
Transpersonal psychology is a form of psychology that studies the transpersonal, self-transcendent or spiritual aspects of the human experience....
and spiritual exploration.
Pharmacodynamics
Ibogaine is considered a 'complex tryptamineTryptamine
Tryptamine is a monoamine alkaloid found in plants, fungi, and animals. It is based around the indole ring structure, and is chemically related to the amino acid tryptophan, from which its name is derived...
'. Because of the ibogaine molecule's tryptamine core, ibogaine acts as an agonist for the 5-HT2A receptor
5-HT2A receptor
The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor . This is the main excitatory receptor subtype among the GPCRs for serotonin , although 5-HT2A may also have an inhibitory effect on certain areas such...
set like other psychedelic
Psychedelic drug
A psychedelic substance is a psychoactive drug whose primary action is to alter cognition and perception. Psychedelics are part of a wider class of psychoactive drugs known as hallucinogens, a class that also includes related substances such as dissociatives and deliriants...
tryptamine
Tryptamine
Tryptamine is a monoamine alkaloid found in plants, fungi, and animals. It is based around the indole ring structure, and is chemically related to the amino acid tryptophan, from which its name is derived...
s (such as DMT
Dimethyltryptamine
N,N-Dimethyltryptamine is a naturally occurring psychedelic compound of the tryptamine family. DMT is found in several plants, and also in trace amounts in humans and other mammals, where it is originally derived from the essential amino acid tryptophan, and ultimately produced by the enzyme INMT...
and psilocybin
Psilocybin
Psilocybin is a naturally occurring psychedelic prodrug, with mind-altering effects similar to those of LSD and mescaline, after it is converted to psilocin. The effects can include altered thinking processes, perceptual distortions, an altered sense of time, and spiritual experiences, as well as...
) and other serotonergic psychedelic
Serotonergic psychedelic
Serotonergic psychedelics are a class of hallucinogenic drugs with a method of action strongly tied to the serotonin neurotransmitter...
s like LSD and mescaline
Mescaline
Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally occurring psychedelic alkaloid of the phenethylamine class used mainly as an entheogen....
. However what makes ibogaine's pharmacodynamic
Pharmacodynamics
Pharmacodynamics is the study of the biochemical and physiological effects of drugs on the body or on microorganisms or parasites within or on the body and the mechanisms of drug action and the relationship between drug concentration and effect...
properties and subjective experience unique from that of other psychedelic tryptamines and serotonergic psychedelics is that it also acts as a dissociative through antagonism of the NMDA receptor
NMDA receptor
The NMDA receptor , a glutamate receptor, is the predominant molecular device for controlling synaptic plasticity and memory function....
set (like ketamine
Ketamine
Ketamine is a drug used in human and veterinary medicine. Its hydrochloride salt is sold as Ketanest, Ketaset, and Ketalar. Pharmacologically, ketamine is classified as an NMDA receptor antagonist...
) as well as acting as an agonist for the κ-opioid receptor
Kappa Opioid receptor
The κ-opioid receptor is a protein that in humans is encoded by the OPRK1 gene. The κ-opioid receptor is one of five related receptors that bind opium-like compounds in the brain and are responsible for mediating the effects of these compounds...
set, like the diterpenoid
Terpenoid
The terpenoids , sometimes called isoprenoids, are a large and diverse class of naturally occurring organic chemicals similar to terpenes, derived from five-carbon isoprene units assembled and modified in thousands of ways. Most are multicyclic structures that differ from one another not only in...
compound salvinorin A
Salvinorin A
Salvinorin A is the main active psychotropic molecule in Salvia divinorum, a Mexican plant which has a long history of use as an entheogen by indigenous Mazatec shamans...
(found in Salvia divinorum
Salvia divinorum
Salvia divinorum is a psychoactive plant which can induce dissociative effects and is a potent producer of "visions" and other hallucinatory experiences...
). Ibogaine's agonism to the κ-opioid receptors is thought to be what is responsible for ibogaine's well-documented anti-addictive properties, as salvinorin A exhibits a similar alleviation of withdrawal symptoms in individuals addicted to opiate
Opiate
In medicine, the term opiate describes any of the narcotic opioid alkaloids found as natural products in the opium poppy plant.-Overview:Opiates are so named because they are constituents or derivatives of constituents found in opium, which is processed from the latex sap of the opium poppy,...
s and methamphetamine
Methamphetamine
Methamphetamine is a psychostimulant of the phenethylamine and amphetamine class of psychoactive drugs...
.
Psychoactive effects
The subjective experience of ibogaine is often divided into two phases: a vivid dreamlike hallucinogenic visual phase (akin to the subjective effects of other hallucinogens like the psychedelicPsychedelic drug
A psychedelic substance is a psychoactive drug whose primary action is to alter cognition and perception. Psychedelics are part of a wider class of psychoactive drugs known as hallucinogens, a class that also includes related substances such as dissociatives and deliriants...
DMT
Dimethyltryptamine
N,N-Dimethyltryptamine is a naturally occurring psychedelic compound of the tryptamine family. DMT is found in several plants, and also in trace amounts in humans and other mammals, where it is originally derived from the essential amino acid tryptophan, and ultimately produced by the enzyme INMT...
and the dissociative ketamine
Ketamine
Ketamine is a drug used in human and veterinary medicine. Its hydrochloride salt is sold as Ketanest, Ketaset, and Ketalar. Pharmacologically, ketamine is classified as an NMDA receptor antagonist...
; see above) and an introspective phase (ostensibly the comedown).
The visual phase is characterized by open-eye visuals, closed-eye visuals, and dreamlike sequences. Objects may be seen as distorted, projecting tracers, or having moving colors or textures. When the eyes are closed, extremely detailed and vivid geometric and fractal visions may be seen. Subjective reports often include a movie-like recollection of earlier life experiences as well as dreamlike sequences with symbolism of one's present or anticipated future. Other effects in the visual phase may include laughing, sensations of euphoria or fear, and temporary short-term memory impairment. The visual phase usually ends after one to four hours, after which the introspective phase begins.
Ibogaine has been referred to as an oneirophrenic
Oneirophrenia
Oneirophrenia is a hallucinatory, dream-like state caused by several conditions such as prolonged sleep deprivation, sensory deprivation, or drugs . From the Greek words "ὄνειρο" and "φρενός"...
(especially during the initial wave of psychedelic research following the discovery of LSD that occurred in late 1950s
1950s
The 1950s or The Fifties was the decade that began on January 1, 1950 and ended on December 31, 1959. The decade was the sixth decade of the 20th century...
and early 1960s
1960s
The 1960s was the decade that started on January 1, 1960, and ended on December 31, 1969. It was the seventh decade of the 20th century.The 1960s term also refers to an era more often called The Sixties, denoting the complex of inter-related cultural and political trends across the globe...
), referring to the dreamlike nature of its hallucinogenic effects. Ibogaine catalyzes an altered state of consciousness
Altered state of consciousness
An altered state of consciousness , also named altered state of mind, is any condition which is significantly different from a normal waking beta wave state. The expression was used as early as 1966 by Arnold M. Ludwig and brought into common usage from 1969 by Charles Tart: it describes induced...
reminiscent of dreaming while fully conscious and aware so that memories; life experiences; and issues of trauma can be processed in a subjective manner.
The introspective phase is typically reported to bring elevated mood, a sense of calm and euphoria, and a distinct intellectual and emotional clarity. Subjects often report being able to accomplish deep emotional and intellectual introspection into psychological and emotional concerns. It is also during this period that opioid addicts first notice the absence of withdrawal symptoms or cravings. The duration of the introspective phase is highly variable, usually lasting hours but sometimes lasting days.
Side effects and safety
One of the first noticeable effects of large-dose ibogaine ingestion is ataxiaAtaxia
Ataxia is a neurological sign and symptom that consists of gross lack of coordination of muscle movements. Ataxia is a non-specific clinical manifestation implying dysfunction of the parts of the nervous system that coordinate movement, such as the cerebellum...
, a difficulty in coordinating muscle motion which makes standing and walking difficult without assistance. Xerostomia
Xerostomia
Xerostomia is the medical term for the subjective complaint of dry mouth due to a lack of saliva. Xerostomia is sometimes colloquially called pasties, cottonmouth, drooth, or doughmouth. Several diseases, treatments, and medications can cause xerostomia. It can also be exacerbated by smoking or...
(dry mouth), nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
, and vomiting may follow. These symptoms may be long in duration, ranging from 4 to 24 hours in some cases. Ibogaine is sometimes administered by enema
Enema
An enema is the procedure of introducing liquids into the rectum and colon via the anus. The increasing volume of the liquid causes rapid expansion of the lower intestinal tract, often resulting in very uncomfortable bloating, cramping, powerful peristalsis, a feeling of extreme urgency and...
to help the subject avoid vomiting up the dose. Psychiatric medications are strongly contraindicated in ibogaine therapy due to adverse interactions. Some studies also suggest the possibility of adverse interaction with heart conditions. In one study of canine subjects, ibogaine was observed to increase sinus arrhythmia (the normal change in heart rate during respiration). Ventricular ectopy has been observed in a minority of patients during ibogaine therapy. It has been proposed that there is a risk of QT-interval prolongation following ibogaine administration. This risk was further demonstrated by a case reported in the New England Journal of Medicine
New England Journal of Medicine
The New England Journal of Medicine is an English-language peer-reviewed medical journal published by the Massachusetts Medical Society. It describes itself as the oldest continuously published medical journal in the world.-History:...
documenting prolonged QT interval and ventricular tachycardia
Ventricular tachycardia
Ventricular tachycardia is a tachycardia, or fast heart rhythm, that originates in one of the ventricles of the heart...
after initial use.
There are 12 documented fatalities that have been loosely associated with ibogaine ingestion. Exact determinations of the cause of death have proven elusive due to the quasi-legal status of ibogaine and the unfamiliarity of medical professionals with this relatively rare substance. No autopsy to date has implicated ibogaine as the sole cause of death. Causes given range from significant pre-existing medical problems to the co-consumption of drugs such as opiates which are potentiated by ibogaine. Also, because ibogaine is one of the many drugs that are partly metabolized by the cytochrome P450 complex, caution must be exercised to avoid foods or drugs that inhibit CP450, in particular foodstuffs containing bergamottin
Bergamottin
Bergamottin is a natural furanocoumarin found principally in grapefruit juice. It is also found in the oil of bergamot, from which it was first isolated and from which its name is derived. To a lesser extent, bergamottin is also present in the essential oils of other citrus fruits...
or bergamot oil, common ones being grapefruit juice and Earl Grey tea
Earl Grey tea
Earl Grey tea is a tea blend with a distinctive flavour and aroma derived from the addition of oil extracted from the rind of the bergamot orange, a fragrant citrus fruit....
.
Treatment for opioid addiction
The most-studied therapeutic effect of ibogaine is the reduction or elimination of addictionSubstance dependence
The section about substance dependence in the Diagnostic and Statistical Manual of Mental Disorders does not use the word addiction at all. It explains:...
to opioid
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
s. An integral effect is the alleviation of symptoms of opioid withdrawal
Withdrawal
Withdrawal can refer to any sort of separation, but is most commonly used to describe the group of symptoms that occurs upon the abrupt discontinuation/separation or a decrease in dosage of the intake of medications, recreational drugs, and alcohol...
. Research also suggests that ibogaine may be useful in treating dependence on other substances such as alcohol
Alcohol
In chemistry, an alcohol is an organic compound in which the hydroxy functional group is bound to a carbon atom. In particular, this carbon center should be saturated, having single bonds to three other atoms....
, methamphetamine
Methamphetamine
Methamphetamine is a psychostimulant of the phenethylamine and amphetamine class of psychoactive drugs...
, and nicotine
Nicotine
Nicotine is an alkaloid found in the nightshade family of plants that constitutes approximately 0.6–3.0% of the dry weight of tobacco, with biosynthesis taking place in the roots and accumulation occurring in the leaves...
and may affect compulsive behavioral patterns not involving substance abuse or chemical dependence. However, researchers note that there remains a "need for systematic investigation in a conventional clinical research setting."
Proponents of ibogaine treatment for drug addiction have established formal and informal clinics or self-help groups in Canada
Canada
Canada is a North American country consisting of ten provinces and three territories. Located in the northern part of the continent, it extends from the Atlantic Ocean in the east to the Pacific Ocean in the west, and northward into the Arctic Ocean...
, Mexico
Mexico
The United Mexican States , commonly known as Mexico , is a federal constitutional republic in North America. It is bordered on the north by the United States; on the south and west by the Pacific Ocean; on the southeast by Guatemala, Belize, and the Caribbean Sea; and on the east by the Gulf of...
, the Caribbean
Caribbean
The Caribbean is a crescent-shaped group of islands more than 2,000 miles long separating the Gulf of Mexico and the Caribbean Sea, to the west and south, from the Atlantic Ocean, to the east and north...
, Costa Rica
Costa Rica
Costa Rica , officially the Republic of Costa Rica is a multilingual, multiethnic and multicultural country in Central America, bordered by Nicaragua to the north, Panama to the southeast, the Pacific Ocean to the west and the Caribbean Sea to the east....
, the Czech Republic
Czech Republic
The Czech Republic is a landlocked country in Central Europe. The country is bordered by Poland to the northeast, Slovakia to the east, Austria to the south, and Germany to the west and northwest....
, France
France
The French Republic , The French Republic , The French Republic , (commonly known as France , is a unitary semi-presidential republic in Western Europe with several overseas territories and islands located on other continents and in the Indian, Pacific, and Atlantic oceans. Metropolitan France...
, Slovenia
Slovenia
Slovenia , officially the Republic of Slovenia , is a country in Central and Southeastern Europe touching the Alps and bordering the Mediterranean. Slovenia borders Italy to the west, Croatia to the south and east, Hungary to the northeast, and Austria to the north, and also has a small portion of...
, the Netherlands
Netherlands
The Netherlands is a constituent country of the Kingdom of the Netherlands, located mainly in North-West Europe and with several islands in the Caribbean. Mainland Netherlands borders the North Sea to the north and west, Belgium to the south, and Germany to the east, and shares maritime borders...
, Brazil
Brazil
Brazil , officially the Federative Republic of Brazil , is the largest country in South America. It is the world's fifth largest country, both by geographical area and by population with over 192 million people...
, South Africa
South Africa
The Republic of South Africa is a country in southern Africa. Located at the southern tip of Africa, it is divided into nine provinces, with of coastline on the Atlantic and Indian oceans...
, the United Kingdom
United Kingdom
The United Kingdom of Great Britain and Northern IrelandIn the United Kingdom and Dependencies, other languages have been officially recognised as legitimate autochthonous languages under the European Charter for Regional or Minority Languages...
and New Zealand
New Zealand
New Zealand is an island country in the south-western Pacific Ocean comprising two main landmasses and numerous smaller islands. The country is situated some east of Australia across the Tasman Sea, and roughly south of the Pacific island nations of New Caledonia, Fiji, and Tonga...
, where ibogaine is administered as an experimental compound . Many users of ibogaine report experiencing visual phenomena during a waking dream state, such as instructive replays of life events that led to their addiction, while others report therapeutic shamanic visions that help them conquer the fears and negative emotions that might drive their addiction. It is proposed that intensive counseling, therapy and aftercare during the interruption period following treatment is of significant value. Some individuals require a second or third treatment session with ibogaine over the course of the next 12 to 18 months. A minority of individuals relapse completely into opiate addiction within days or weeks. A comprehensive article (Lotsof 1995) on the subject of ibogaine therapy detailing the procedure, effects and aftereffects is found in "Ibogaine in the Treatment of Chemical Dependence Disorders: Clinical Perspectives". Ibogaine has also been reported in multiple small-study cohorts to reduce cravings for methamphetamine.
There is also evidence that this type of treatment works with LSD
LSD
Lysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide and colloquially as acid, is a semisynthetic psychedelic drug of the ergoline family, well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synaesthesia, an...
which has been shown to have therapeutic effect on alcoholism as far back as the 1960s. Both ibogaine and LSD appear to be effective at encouraging introspection and giving the user occasion to reflect on where their addiction came from while also occasioning an intense, transformative experience that can put established patterns of behaviour into perspective; ibogaine has the added benefit of preventing withdrawal effects.
Chronic pain management
In 1957, Jurg Schneider, a pharmacologist at CIBA, found that ibogaine potentiates morphineMorphine
Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...
analgesia. Further research was abandoned, and no additional data was ever published by Ciba researchers on ibogaine–opioid interactions. Almost 50 years later, Patrick Kroupa and Hattie Wells released the first treatment protocol for concomitant administration of ibogaine with opioids in human subjects, indicating ibogaine reduced tolerance to opioid drugs. Kroupa et al. published their research in the Multidisciplinary Association for Psychedelic Studies
Multidisciplinary Association for Psychedelic Studies
The Multidisciplinary Association for Psychedelic Studies is a membership-based 501 non-profit research and educational organization working to develop psychedelics and marijuana into legal prescription drugs...
Journal demonstrating that administration of low-"maintenance" doses of ibogaine HCl with opioids decreases tolerance. It should be noted however, that the potentiation action of ibogaine may make this a very risky procedure.
Psychotherapy
Ibogaine has been used as an adjunct to psychotherapyPsychotherapy
Psychotherapy is a general term referring to any form of therapeutic interaction or treatment contracted between a trained professional and a client or patient; family, couple or group...
by Claudio Naranjo
Claudio Naranjo
Claudio Naranjo is a Chilean psychiatrist who is considered a pioneer in integrating psychotherapy and the spiritual traditions. He is one of the three successors named by Fritz Perls , and a developer of the Enneagram of Personality and founder of the Seekers After Truth Institute...
, documented in his book The Healing Journey.
History
It is uncertain exactly how long iboga has been used in African spiritual practice, but its activity was first observed by French and Belgian explorers in the 19th century. The first botanical description of the Tabernanthe iboga plant was made in 1889. Ibogaine was first isolated from T. ibogaIboga
Tabernanthe iboga or Iboga is a perennial rainforest shrub and hallucinogen, native to western Central Africa. Iboga stimulates the central nervous system when taken in small doses and induces visions in larger doses. In parts of Africa where the plant grows the bark of the root is chewed for...
in 1901 by Dybowski and Landrin and independently by Haller and Heckel in the same year using T. iboga samples from Gabon
Gabon
Gabon , officially the Gabonese Republic is a state in west central Africa sharing borders with Equatorial Guinea to the northwest, Cameroon to the north, and with the Republic of the Congo curving around the east and south. The Gulf of Guinea, an arm of the Atlantic Ocean is to the west...
. In the 1930s, ibogaine was sold in France in 8 mg tablets under the name "Lambarene". The total synthesis of ibogaine was accomplished by G. Büchi in 1966. Since then, several further totally synthetic routes have been developed.
In the early 1960s, anecdotal reports appeared concerning ibogaine's effects. The use of ibogaine in treating substance use disorders in human subjects was first observed by Howard Lotsof
Howard Lotsof
Howard Lotsof was an American scientific researcher and patent holder.When he was 19 years old and addicted to heroin, he accidentally discovered the anti-addictive effects of ibogaine in 1962. He later attended Fairleigh Dickinson University and then New York University, graduating with a degree...
in 1962, for which he was later awarded in 1985. In 1969, Claudio Naranjo was granted a French patent for the use of ibogaine in psychotherapy.
Ibogaine was placed in US Schedule 1 in 1967 as part of the US government's strong response to the upswing in popularity of psychedelic substances, though iboga itself was scarcely known at the time. Ibogaine's ability to attenuate opioid withdrawal
Withdrawal
Withdrawal can refer to any sort of separation, but is most commonly used to describe the group of symptoms that occurs upon the abrupt discontinuation/separation or a decrease in dosage of the intake of medications, recreational drugs, and alcohol...
confirmed in the rat was first published by Dzoljic et al. (1988). Ibogaine's use in diminishing morphine
Morphine
Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...
self-administration in preclinical studies was shown by Glick et al. (1991) and ibogaine's capacity to reduce cocaine
Cocaine
Cocaine is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. The name comes from "coca" in addition to the alkaloid suffix -ine, forming cocaine. It is a stimulant of the central nervous system, an appetite suppressant, and a topical anesthetic...
self-administration in the rat was shown by Cappendijk et al. (1993). Animal model support for ibogaine claims to treat alcohol dependence
Alcohol dependence
Alcohol dependence, as described in the DSM-IV, is a psychiatric diagnosis describing an entity in which an individual uses alcohol despite significant areas of dysfunction, evidence of physical dependence, and/or related hardship.-Definition and diagnosis:According to the DSM-IV criteria for...
were established by Rezvani (1995).
The name "Indra extract", in strict terms, refers to 44 kg of an iboga extract manufactured by an unnamed European industrial manufacturer in 1981. This stock was later purchased by Carl Waltenburg, who distributed it under the name "Indra extract". Waltenburg used this extract to treat heroin addicts in Christiania
Freetown Christiania
Not to be confused with Christiania, Norway, another name for Oslo.Christiania, also known as Freetown Christiania is a self-proclaimed autonomous neighbourhood of about 850 residents, covering 34 hectares in the borough of Christianshavn in the Danish capital Copenhagen...
, Denmark, a squatter village where heroin addiction was widespread in 1982. Indra extract was offered for sale over the Internet until 2006, when the Indra web presence disappeared. It is unclear whether the extracts currently sold as "Indra extract" are actually from Waltenburg's original stock, or whether any of that stock is even viable or in existence. Ibogaine and related indole
Indole
Indole is an aromatic heterocyclic organic compound. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered nitrogen-containing pyrrole ring. Indole is a popular component of fragrances and the precursor to many pharmaceuticals. Compounds that contain an...
compounds are susceptible to oxidation when exposed to oxygen
, as opposed to their salt form, which is stable. The exact methods and quality of the original Indra extraction was never documented, so the real composition of the product remains uncertain.
An ibogaine research project was funded by the US National Institute on Drug Abuse
National Institute on Drug Abuse
The National Institute on Drug Abuse is a United States federal-government research institute whose mission is to "lead the Nation in bringing the power of science to bear on drug abuse and addiction."-History:...
in the early 1990s. The National Institute on Drug Abuse (NIDA) abandoned efforts to continue this project into clinical studies in 1995, citing other reports that suggested a risk of brain damage with extremely high doses and fatal heart arrhythmia in patients having a history of health problems, as well as inadequate funding for ibogaine development within their budget. However, NIDA funding for ibogaine research continued in indirect grants often cited in peer-reviewed ibogaine publications.
Data demonstrating ibogaine's efficacy in attenuating opioid withdrawal in drug-dependent human subjects was published by Alper et al. (1999) and Mash et al. (2000).
In addition, after years of work and a number of significant changes to the original protocol, on August 17, 2006, a MAPS
Multidisciplinary Association for Psychedelic Studies
The Multidisciplinary Association for Psychedelic Studies is a membership-based 501 non-profit research and educational organization working to develop psychedelics and marijuana into legal prescription drugs...
-sponsored research team received "unconditional approval" from a Canadian Institutional Review Board (IRB) to proceed with a long-term observational case study that will examine changes in substance use in 20 consecutive people seeking ibogaine-based therapy for opiate dependence at the Iboga Therapy House in British Columbia, Canada.
Formulations
In Bwiti religious ceremonies, the rootbark is pulverized and swallowed in large amounts to produce intense psychoactive effects. In Africa, iboga rootbark is sometimes chewed, which releases small amounts of ibogaine to produce a stimulant effect. Ibogaine is also available in a total alkaloid extract of the Tabernanthe iboga plant, which also contains all the other iboga alkaloids and thus has only about one-fifth the potency by weight as standardized ibogaine hydrochloride.Currently, pure crystalline ibogaine hydrochloride is the most standardized formulation. It is typically produced by the semi-synthesis from voacangine
Voacangine
Voacangine is an alkaloid found predominantly in the rootbark of the Voacanga africana tree, as well as in other plants such as Tabernanthe iboga, Tabernaemontana africana, Trachelospermum jasminoides and Ervatamia yunnanensis...
in commercial laboratories. Ibogaine has two separate chiral
Chirality (chemistry)
A chiral molecule is a type of molecule that lacks an internal plane of symmetry and thus has a non-superimposable mirror image. The feature that is most often the cause of chirality in molecules is the presence of an asymmetric carbon atom....
centers which means that there are four different stereoisomers of ibogaine. These four isomers are difficult to resolve
Chiral resolution
Chiral resolution in stereochemistry is a process for the separation of racemic compounds into their enantiomers. It is an important tool in the production of optically active drugs...
.
A synthetic derivative of ibogaine, 18-methoxycoronaridine
18-Methoxycoronaridine
-18-Methoxycoronaridine is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont...
(18-MC), is a selective α3β4 antagonist that was developed collaboratively by the neurologist Stanley D. Glick (Albany) and the chemist Martin E. Kuehne (Vermont). This discovery was stimulated by earlier studies on other naturally occurring analogues of ibogaine such as coronaridine
Coronaridine
Coronaridine is an alkaloid found in Tabernanthe iboga and related species....
and voacangine
Voacangine
Voacangine is an alkaloid found predominantly in the rootbark of the Voacanga africana tree, as well as in other plants such as Tabernanthe iboga, Tabernaemontana africana, Trachelospermum jasminoides and Ervatamia yunnanensis...
that showed these compounds also have anti-addictive properties.
Pharmacology
The pharmacology of ibogaine is quite complex, affecting many different neurotransmitterNeurotransmitter
Neurotransmitters are endogenous chemicals that transmit signals from a neuron to a target cell across a synapse. Neurotransmitters are packaged into synaptic vesicles clustered beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to...
systems simultaneously.
Because of its fairly low potency at any of its target sites, ibogaine is used in doses anywhere from 5 mg/kg of body weight for a minor effect to 30 mg/kg in the cases of strong polysubstance addiction. It is unknown whether doses greater than 30 mg/kg in humans produce effects that are therapeutically beneficial, medically risky, or simply prolonged in duration. In animal neurotoxicity studies, there was no observable neurotoxicity of ibogaine at 25 mg/kg, but at 50 mg/kg, one-third of the rats had developed patches of neurodegeneration, and at doses of 75 mg/kg or above, all rats showed a characteristic pattern of degeneration of Purkinje neurons, mainly in the cerebellum
Cerebellum
The cerebellum is a region of the brain that plays an important role in motor control. It may also be involved in some cognitive functions such as attention and language, and in regulating fear and pleasure responses, but its movement-related functions are the most solidly established...
. While caution should be exercised when extrapolating animal studies to humans, these results suggest that neurotoxicity of ibogaine is likely to be minimal when ibogaine is used in the 10–20 mg/kg range typical of drug addiction interruption treatment regimes, and indeed death from the other pharmacological actions of the alkaloids is likely to occur by the time the dose is high enough to produce consistent neurotoxic changes.
Metabolites
Ibogaine is metabolizedMetabolite
Metabolites are the intermediates and products of metabolism. The term metabolite is usually restricted to small molecules. A primary metabolite is directly involved in normal growth, development, and reproduction. Alcohol is an example of a primary metabolite produced in large-scale by industrial...
in the human body by cytochrome P450 2D6, and the major metabolite is noribogaine
Noribogaine
Noribogaine, or 12-hydroxyibogamine, is a major active metabolite of ibogaine, and is thought to be involved in the anti-addictive effects of ibogaine-containing plant extracts.-See also:* Dissociative* Ibogaine* 18-Methoxycoronaridine* Voacangine...
(12-hydroxyibogamine). Noribogaine is most potent as a serotonin reuptake inhibitor and acts as a moderate κ- and weak µ-opioid receptor
Opioid receptor
Opioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin receptors...
full agonist and therefore, also has an aspect of an opiate replacement
Opiate replacement therapy
Opioid replacement therapy is the medical procedure of replacing an illegal opioid drug such as heroin with a longer acting but less euphoric opioid, usually methadone or buprenorphine, that is taken under medical supervision. In some countries patients may be treated with slow-release morphine...
similar to compounds like methadone
Methadone
Methadone is a synthetic opioid, used medically as an analgesic and a maintenance anti-addictive for use in patients with opioid dependency. It was developed in Germany in 1937...
. It is possible that this action of noribogaine at the kappa opioid receptor may indeed contribute significantly to the psychoactive effects attributed to ibogaine ingestion; salvia divinorum
Salvia divinorum
Salvia divinorum is a psychoactive plant which can induce dissociative effects and is a potent producer of "visions" and other hallucinatory experiences...
, another plant recognized for its strong hallucinogenic properties, contains the chemical salvinorin-A which is a highly selective kappa opioid agonist. Both ibogaine and noribogaine have a plasma half-life of around two hours in the rat, although the half-life of noribogaine is slightly longer than the parent compound. It is proposed that ibogaine is deposited in fat and metabolized into noribogaine as it is released. Noribogaine shows higher plasma levels than ibogaine and may therefore be detected for longer periods of time than ibogaine. Noribogaine is also more potent than ibogaine in rat drug discrimination assays when tested for the subjective effects of ibogaine. Noribogaine differs from ibogaine in that it contains a hydroxy
Hydroxyl
A hydroxyl is a chemical group containing an oxygen atom covalently bonded with a hydrogen atom. In inorganic chemistry, the hydroxyl group is known as the hydroxide ion, and scientists and reference works generally use these different terms though they refer to the same chemical structure in...
instead of a methoxy
Methoxy
In chemistry , methoxy refers to the functional group consisting of a methyl group bound to oxygen. This alkoxy group has the formula O–CH3.The word is used in organic nomenclature usually to describe an ether...
group
Functional group
In organic chemistry, functional groups are specific groups of atoms within molecules that are responsible for the characteristic chemical reactions of those molecules. The same functional group will undergo the same or similar chemical reaction regardless of the size of the molecule it is a part of...
at the 12 position.
Legal status
Ibogaine has been placed in the strictest drug prohibition schedules in the United States and a handful of other countries. Canada and Mexico both allow ibogaine therapy facilities to operate and contribute to further understanding of the detoxification and therapeutic process that ibogaine has the potential to facilitate.Ibogaine and its salts
Hydrochloride
In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base . This is also known as muriate, derived from hydrochloric acid's other name: muriatic acid....
were regulated by the U.S. Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
in 1967 pursuant to its enhanced authority to regulate stimulants, depressants, and hallucinogens granted by the 1965 Drug Abuse Control Amendments (DACA) to the Federal Food, Drug, and Cosmetic Act
Federal Food, Drug, and Cosmetic Act
The United States Federal Food, Drug, and Cosmetic Act , is a set of laws passed by Congress in 1938 giving authority to the U.S. Food and Drug Administration to oversee the safety of food, drugs, and cosmetics. A principal author of this law was Royal S. Copeland, a three-term U.S. Senator from...
. In 1970, with the passage of the Controlled Substances Act
Controlled Substances Act
The Controlled Substances Act was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970. The CSA is the federal U.S. drug policy under which the manufacture, importation, possession, use and distribution of certain...
, it was classified as a Schedule I-controlled substance in the United States, along with other psychedelics such as DMT
DMT
DMT may refer to:In chemical substances:* Dimethyltryptamine, a psychedelic tryptamine* Dimethyl terephthalate, a polyester precursor* Desoxymethyltestosterone, a designer anabolic steroid...
and mescaline
Mescaline
Mescaline or 3,4,5-trimethoxyphenethylamine is a naturally occurring psychedelic alkaloid of the phenethylamine class used mainly as an entheogen....
. Since that time, several other countries, including Sweden, Denmark, Belgium, and Switzerland, have also banned the sale and possession of Ibogaine. Although illegal in these countries, Ibogaine has been used by hundreds of drug dependents in the United States and abroad. Howard Lotsof
Howard Lotsof
Howard Lotsof was an American scientific researcher and patent holder.When he was 19 years old and addicted to heroin, he accidentally discovered the anti-addictive effects of ibogaine in 1962. He later attended Fairleigh Dickinson University and then New York University, graduating with a degree...
, a pioneer in bringing awareness to Ibogaine's success in helping long-time drug dependents to quit their addiction, and others have been offering willing persons the treatment. In the Czech Republic and Slovenia, taking advantage of less prohibitive legal systems, ibogaine has been applied to people coming from the U.S. and other countries seeking a safe haven.
Ibogaine is not the subject of any regulation in Canada. In Sweden, a non-profit foundation was formed in early 2006 to address the issue of providing ibogaine for addiction interruption within established drug treatment care.
Popular culture
In 1972, journalist Hunter S. ThompsonHunter S. Thompson
Hunter Stockton Thompson was an American journalist and author who wrote The Rum Diary , Fear and Loathing in Las Vegas and Fear and Loathing on the Campaign Trail '72 .He is credited as the creator of Gonzo journalism, a style of reporting where reporters involve themselves in the action to...
accused Democratic candidate Edmund Muskie
Edmund Muskie
Edmund Sixtus "Ed" Muskie was an American politician from Rumford, Maine. He served as Governor of Maine from 1955 to 1959, as a member of the United States Senate from 1959 to 1980, and as Secretary of State under Jimmy Carter from 1980 to 1981...
of being addicted to ibogaine in a satirical piece while covering the Wisconsin primaries of the 1972 U.S. Presidential primaries
United States presidential election, 1972
The United States presidential election of 1972 was the 47th quadrennial United States presidential election. It was held on November 7, 1972. The Democratic Party's nomination was eventually won by Senator George McGovern, who ran an anti-war campaign against incumbent Republican President Richard...
for Rolling Stone
Rolling Stone
Rolling Stone is a US-based magazine devoted to music, liberal politics, and popular culture that is published every two weeks. Rolling Stone was founded in San Francisco in 1967 by Jann Wenner and music critic Ralph J...
magazine. Many readers, and even other journalists, did not realize that Thompson was being facetious. The claim was completely unfounded, and Thompson himself is documented in the movie Gonzo: The Life and Work of Dr. Hunter S. Thompson
Gonzo: The Life and Work of Dr. Hunter S. Thompson
Gonzo: The Life and Work of Dr. Hunter S. Thompson is a 2008 documentary film directed by Alex Gibney. It details Hunter S. Thompson's landmark writings on music and politics...
discussing the self-fabricated joke of Muskie's alleged ibogaine use and his surprise that anyone actually believed the claim.
Ibogaine has been the subject of several full-length documentary films including Detox or Die in 2004, by director David Graham Scott a feature film aired by the BBC, documenting Scott's own drug addiction and ibogaine treatment. Ibogaine Rite of Passage, directed by Ben Deloenen in 2005, with Howard Lotsof
Howard Lotsof
Howard Lotsof was an American scientific researcher and patent holder.When he was 19 years old and addicted to heroin, he accidentally discovered the anti-addictive effects of ibogaine in 1962. He later attended Fairleigh Dickinson University and then New York University, graduating with a degree...
and Patrick K. Kroupa
Patrick K. Kroupa
Patrick Karel Kroupa is an American writer, hacker and activist. Kroupa was a member of the legendary Legion of Doom hacker group and co-founded MindVox in 1991, with Bruce Fancher...
which focused on both native Bwiti ritualistic use of ibogaine as well as modern science and treatment clinics. In 2007 filmmaker Magnolia Martin directed Facing the Habit documenting a one-time millionaire and former stockbroker whose life spiraled out of control due to heroin addiction traveling to Mexico to receive ibogaine treatment. In 2009 a feature documentary I'm Dangerous with Love by filmmaker Michel Negroponte, covered the work of Dimitri Mugianis and his long-running underground ibogaine treatment for heroin addiction.
In addition to documentaries, ibogaine has played a central role in the plot-lines of several episodes of television programs, including:
The X-Files: Via Negativa, Season 8, Episode 7 (2000)
C.S.I.: Getting Off, Season 4, Episode 16 (2004)
Law & Order Special Victims Unit: Users, Season 11, Episode 7 (2009)
Nikita: Echoes, Season 1, Episode 16 (2011)
Further reading
- Daniel PinchbeckDaniel PinchbeckDaniel Pinchbeck is an author living in New York’s East Village, where he is editorial director of Reality Sandwich, a blog website centered around New Age philosophy and activism. He is the author of Breaking Open the Head: A Psychedelic Journey into the Heart of Contemporary Shamanism and 2012:...
writes of his own experience with ibogaine (among other psychoactives) in Breaking Open the HeadBreaking Open the HeadBreaking Open the Head: A Psychedelic Journey into the Heart of Contemporary Shamanism is a book written by author and journalist Daniel Pinchbeck, founding editor of the literary journal Open City...
.