Ibogaine in substance abuse treatment… have you heard of this compound yet? When most think of psychedelics, what comes to mind is psilocybin, LSD, DMT, and maybe MDMA. But there are a variety of up and coming stars in the psychedelic scene. Ibogaine is a compound you may not have heard of yet, but I’m sure you’ll be hearing more about it soon enough.
If you’d like to follow more and learn about psychedelics from the viewpoints of pharmacists as well as what they mean for the pharmacy profession, please check out the Psychedelic Pharmacists Association.
Thanks to P4 student Darren J Barrow Jr. who offered to give an overview after deep-diving into ibogaine during one of his rotations. Now, on to Darren’s post!
I am a 4th year Student Pharmacist at the University of Tennessee College of Pharmacy. I recently had a mental health rotation and wanted to know more about psychedelics’ use for mental health. I came across ibogaine while researching treatment options for substance use disorder. Natural medicine is not taught in-depth during pharmacy school, so I have taken it upon myself to learn more about the treasures nature has to offer.
The Discovery and Beginnings of Ibogaine
Ibogaine is a compound that can be found in plants in the family Apocynaceae such as Tabernanthe iboga, Voacanga africana, and Tabernaemontana undulata. The compound does have effects on the body and mind. Much like psilocybin, DMT, or LSD, ibogaine is classified as a psychedelic.
The Tabernanthe iboga plant is native to the following countries in Africa:
- Central African Republic
Within indigenous tribes, the natural compound was historically used by hunters as a stimulant and it was used ceremonially for rituals centered on entering adulthood.
A Frenchman, Henri Ernest Baillon, “formally” published the plant; making it known to the Western world.
Modern Explorations of Ibogaine
In 1962, Howard Lotsof was traveling and partook of ibogaine and noticed something interesting. He said “afterwards, I was walking and I looked at this tree, and as I looked at it I realized I no longer had any fear of death. Also that I was no longer addicted to narcotics.” Before his psychedelic trip, he was a 19-year-old addicted to heroin. This set him on a course for introducing ibogaine as particularly useful for treating substance use disorders.
Despite his lack of medical training, Lotsof was granted five (yes, five) patents internationally on the treatments of various substance use disorders between the years of (1985-1990). The following are his patents and what they were granted for:
•Rapid method for interrupting the narcotic addiction syndrome (1985): 4499096A
•Rapid method for interrupting the cocaine and amphetamine abuse syndrome (1986): 4587243A
•Rapid method for attenuating the alcohol dependency syndrome (1989): 4857523
•Rapid method for interrupting or attenuating the nicotine dependency syndrome (1991): 5026697A
•Rapid method for interrupting or attenuating poly-drug dependency syndromes (1992): 5152994A
Lotsof is credited with creating both the Global Ibogaine Therapy Alliance (GITA) and the Ibogaine Dossier. Lotsof conducted all of his research without a medical background, and he was able to shed light on an alternative treatment option. In the United States (US), psychedelics are classified as Schedule I drugs which have both high potential for abuse and no medical use. At this time, ibogaine is only available outside of the US in places such as Mexico, Canada, Netherlands, New Zealand, and South Africa.
If you are still interested in ibogaine, I am sure you are wondering if it works, but let’s first talk about what someone may experience when ingesting the substance.
The Ibogaine Experience
Once ibogaine is ingested, the psychoactive effects or “trip” can last 24+ hours. According to The Third Wave, this experience can be separated into three different phases.
Ibogaine Phase 1: Acute Phase
This phase starts within 1-3 hours and can last from 4-8 hours. Ibogaine does not cause visual and auditory hallucinations in everyone (that depends on the dosage and individual variations). It is often described as a dream-like state that can feel like space-walking or being weightless. During this phase, people report many memories being brought to the forefront of their minds. This can have implications for the treatment of trauma or forgotten memories.
Ibogaine 2: Evaluative or Reflective Phase
This phase starts within 4-8 hours and can last from 8-20 hours. It is described as more reflective with a neutral mood. It also allows for one to be introspective of the acute phase. Phase 2 does not have as many repressed memories resurfacing as phase 1 does. An environment free from stimuli is said to be most important during the first 2 phases.
Ibogaine Phase 3: Residual Stimulation Phase
This phase starts within 12-24 hours and can last from 24-72 hours or more. As the psychoactive effects of ibogaine and introspection decrease, then the focus shifts to the external world. It is called the residual stimulation phase because of reduced fatigue and hypervigilance. People report being transformed due to their experience with resurfacing of memories and reflection. They can take this experience with them weeks to months after applying what they learn to everyday life. There is evidence that it works, but it does come with risks.
“Ibogaine comes from nature and therefore it is completely safe to use”. This statement is far from the truth. Moderation is key with all things that are consumed. Too much of a good thing can be a bad thing and ibogaine is no different.
The “typical” dosage of ibogaine varies depending upon what resources are used. Lotsof wrote about 33 subjects who on average were ingesting a range from 6-24 mg/kg to treat withdrawal symptoms and addiction. For example, a patient who weighs 180 lbs or 81.8 kg is seeking addiction treatment. The patient would receive 81.8 kg times 6 mg of ibogaine to ingest a total of 490.8 mg/day. High doses are required to decrease opioid withdrawals, but one should tread lightly on new substances. “Start low and go slow” is the best advice for almost all psychedelics.
Dose-Dependent Effects of Ibogaine (What Happens When Someone Takes “Too Much”)?
The common side effects of ibogaine are headache, nausea, vomiting, and visual disturbances (bothersome ones that are NOT associated with any hallucinations). Ingesting ibogaine with food is likely to reduce stomach irritation (this is not medical advice).
Can an ibogaine overdose cause death?
When taken in absurdly large amounts, yes. Overdosing on ibogaine can result in cardiac arrest, seizures, and yes, death. Ibogaine has activity on the Human Ether-a-go-go Related Gene (hERG) potassium channel. The study highlighted ibogaine’s effect on myocardioctyes’ QTc. Ibogaine and its metabolite block the hERG potassium channel, preventing the hyperpolarization of the action potential. This activity is dose-dependent and one of the known mechanisms behind its cardiotoxicity. The risks come when too much is taken and not enough precaution.
Research shows ibogaine is safe to use in controlled environments; where someone can monitor the subject after ingestion.
Ibogaine Mechanism of Action and Pharmacokinetics
Ibogaine has activity on various receptors within the body. Studies show that ibogaine acts as a serotonin (5-HT) reuptake inhibitor, Mu opioid receptor agonist, Kappa 1 and Kappa 2 opioid receptor partial agonist, and an NMDA channel blocker. Its activity on the Mu opioid receptor explains its potential with addiction treatment. It also has implications for the treatment of depression due to its inhibition of serotonin reuptake within the brain.
Opiates have depressant effects and ibogaine can counteract that through both Mu receptor and serotonin reuptake inhibitor activity. Ibogaine is metabolized into noribogaine by CYP2D6 (major), CYP2C9 (minor), and CYP3A4 (minor). The half-life of ibogaine is around 7.45 hours, while noribogaine has a half-life of around 24 to 30 hours. The drug interactions to consider are major CYP2D6 inhibitors (fluoxetine, paroxetine, bupropion, etc.).
Clinical Utility of Ibogaine
Why do people use ibogaine? There are several reasons. In the African tribes, it had various uses such as stimulation and ceremonies. In the US, it could be used with therapy for treating addiction (psychedelic-assisted therapy). The only treatments currently available are Suboxone (Buprenorphine/Naltrexone) and methadone. This is known as Opioid Substitution Therapy (OST) or Methadone Maintenance Therapy (MMT).
There is evidence that ibogaine can be used for various addictions (opioids, amphetamines, alcohol, and cocaine). There is a case report of a 37-year-old female who was able to stay sober from opioids after a 4-day ibogaine treatment in Vancouver for 18-months. Previously, the longest the patient could abstain from opioids was two months consecutively. To go from 2-months to 18-months with one ibogaine treatment sounds wonderful, right? It should sound good.
Lotsof’s 33-subject paper illustrated similar results. It was more observation and subjective information than a purely scientific paper. The authors were able to recognize symptoms of opioid withdrawal and noticed that ibogaine reduced these physical responses. The psychoactive portion of ibogaine’s effect within the brain may contribute to its success in treating addiction. The role of psychedelics, such as ibogaine on the brain’s neuroplasticity is a key feature in the theory of how psychedelics can help treat a variety of mental health-related illnesses.
Psychedelics and Neuroplasticity
The final aspect of ibogaine’s potential is the theory behind psychedelic use in mental health by way of increasing neuroplasticity.
Neuroplasticity is a fancy way of saying how well our brains can adapt and re-learn concepts and information.
The brain on the psychedelic compound psilocybin, found in many species of mushrooms, has been shown to have increased connections compared to a brain at baseline. If your brain can rewire its connections to trauma, maybe it can potentially rewire itself to curb addiction. Rewiring supports how people experience ibogaine’s psychoactive effects.
The psychedelic space has been getting a lot more attention due to potential applications in clinical medicine. Ibogaine has medicinal properties but until psychedelics are legal in the US, its access is limited. This post is to inform others of a psychedelic that is not well known. Hopefully, this post sheds light, starts a conversation, and prompts a search for more knowledge. Thank you for reading, and always remember to stay safe.