Ibogaine Therapy

By Samuel B. Obembe M.B;B.S., C.A.D.C., in Practical Skills and Clinical Management of Alcoholism & Drug Addiction, 2012 

Ibogaine is a naturally occurring psychoactive substance extracted from the roots of a plant (shrub) called Iboga. Iboga (Tabernanthe iboga) is classified as a member of the Apocynaceae family. This is the richest source for Ibogaine, an indole alkaloid.

Iboga plants are common vegetation that extends from Cameroon to the Congo in the tropical heat and humidity of Africa. But Gabon, one of the countries along the coast of Africa, is where Iboga grows best. The Tabernanthe manii root also contains Ibogaine as one of several alkaloids. In West Africa, Voacanga agricana is a widespread shrub containing Ibogaine in its bark. In Australia, Ervatamia orientalis produces Ibogaine in its leaves. And in South America, a shrub called Anartia meyer, found in Trinidad and Tobago, Venezuela, Colombia, Surinam, and French Guyana, has been discovered to contain Ibogaine.

Ibogaine’s unique psychoactive effect defies predictable clinical manifestations. For centuries, the sacred root of the Iboga has been used in medicinal and ritual preparations according to African spiritual traditions of the Bwiti of Gabon in a personal quest for knowledge and inner power, a shamanic aspiration. The Nganga African tribe traditionally uses Iboga to treat mental illnesses including depression, anxiety, and even schizophrenia.

When Ibogaine is administered, the visionary phase comes first. This is described as a lucid or active dream that extends from 4 to 6 h. This visual phenomenon is an awakening dream state without loss of consciousness. This state produces brain waves characteristic of REM sleep and has been characterized as a recreation of fetal sleep. It is documented that this produces instructive replays of life events that led to addiction.

During the introspection phase, Ibogaine promotes psychotherapeutic effect that empowers the client to conquer fear and negative emotions that may drive their addictions. This phase allows clients to explore psychological issues and behavior patterns that support addictions and other psychological problems. Hallucinogenic and euphoric actions of psychoactive drugs normally graduate into a state of “dependency” when addiction is established. This would be the case with LSD “trips” and flashbacks. But Ibogaine’s unique psychoactivities, which are the hallucinogenic and introspective phases, are utilized as individual “therapy” that is focused, devoid of euphoria and dependency. This hallucinogenic experience or vision was characterized by “Narranjo, a psychiatrist who studied ibogaine and harmaine as oneirophrenics or dream makers from the Greek oneiros, ‘dream’ and phren ‘think’ as opposed to hallucinogens. French researchers (Goutarel, Gollnhofer and Sillans) have suggested that iboga (Ibogaine) allows people to disconnect the ‘self’ from the external reality in order to reconnect themselves to an inner reality, while still being able at any time to return to what is happening around them” (Ravalec, Mallendi, & Paicheler, 2007).

Studies indicate that Ibogaine interrupts addiction and diminishes or eradicates cravings and withdrawal symptoms. All research conducted arrived at clinical affirmations that Ibogaine therapy can put an end to physical and psychological dependence, as well as terminate withdrawal symptoms of addictions to psychoactive drugs and alcoholism.

Pharmacology and Pharmacokinetics of Ibogaine

Ibogaine has unique and complex pharmacological properties, including a broad spectrum of binding on receptors sites as an agonist (hallucinogenic) and antagonist (antiaddictives). This reflects its peculiar clinical characteristics. The primary target sites are the NMDA, nicotinic, σ-, κ-opioid, and μ-receptors. NMDA are receptors of the messengers of glutamate, calcium, aspartate, amino acid, and glycine. Glutamate is noted to be the most important neurotransmitter booster of the CNS. The glutamate neurons are the major neuronal transmitting network of the cortex, modulating cognition, hippocampus (memory), and amygdalas (emotion). These are essential for mental functions that preserve our daily existence.

Ibogaine acts on these multiple transmitter sites in an antagonist function as a “reducing agent,” mitigating “excitotoxic damage in the brain.” This is the apparent mechanism of action in effecting the antiaddictive process. Its application for “neuropathic pain” or treatment of Parkinson disease and Alzheimer disease is a possible future use.

The proposal for therapeutic use is worthy of clinical trials. Women are much more sensitive to Ibogaine than men, thus care must be taken in dose measurement to avoid overdose or fatality. Ibogaine could be a future “wonder drug” if patented as an antineurotoxic medication.

Molecular Level of Activities

The drug is a noncompetitive antagonist for α3β4 nicotinic receptors. Other α3β4 antagonists such as bupropion (Welbutrin or Zyban) and mecamylamine have been used in treatment of nicotine addiction. A combination of Ibogaine and other α3β4 antagonists such as 18-MC, dextromethorphan, or mecamylamine have a stronger antiaddictive effect than Ibogaine administered alone. Ibogaine’s antagonist actions on opioid and glutamatergic systems can be effective as antiaddictive functions within an hour of administration. Ibogaine is also a serotonin 5-HT2A, 5-HT2C, and σ2 receptor agonists. This is most probably responsible for its hallucinogenic effects.

Noribogaine (12-hyrdoxyibogamine) is a major metabolic product of Ibogaine. Ibogaine is metabolized in the human body by cytochrome P450 2D6. Noribogaine is very potent as a serotonin reuptake inhibitor and also acts as a full agonist of moderate κ- and weak μ-opioid receptors. This substance can displace opiates in a similar fashion as methadone. The agonist action of Noribogaine, especially at the κ-opioid receptor, contributes to the psychoactive effect of Ibogaine intake.

Ibogaine exhibits relatively low potency at its target sites. It is used at a dosage of 5 mg/kg body weight in minor treatment, and up to 30 mg/kg in intense poly-substance addiction management. Based on rat studies, it is probable that high doses may cause adverse side effects. When animals were subjected to 50 mg/kg, one-third developed neurodegeneration. A dosage of 75 mg/kg caused all of the rats to show a characteristic pattern of Purkinje neuron degeneration, primarily in the cerebellum. A dosage of 10–20 mg/kg is recommended as a safe dosage (with minimal neurotoxicity) in the treatment of addiction.

A single treatment has a healing effect that lasts 2–3 years. But some individuals require a second or third treatment session over a period of 12–18 months. Intensive counseling therapy and aftercare is critical during the interruption periods for effective treatment.

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.

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.

Global Use

At present, Ibogaine use for the treatment of addiction is prohibited in the United States. Ibogaine is classified like heroin as a schedule I substance. In 1994, Deborah Mash, PhD, received FDA authorization to conduct experimental treatments. Ibogaine is legally recognized in the United Kingdom, France, and Germany.

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 centre 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.”