First Posted 12/30/2013
Paul Dessauer, Outreach Coordinator at WASUA, the Western Australian Substance Users’ Association, often adds insight to issues that come up on my blog. He shared a few comments in response to my post about ibogaine, and at my request gave permission to post his remarks here. His comments include a summary of the receptor actions of ibogaine known to date, a description of the legal status of ibogaine ‘down under’, and several links to further information.
The information provides a good example of how knowledge is gained about psychoactive substances through combining research data from different areas of study. Psychologists assess the effects of the drug on different aspects of behavior. Neurochemists identify the actions of the substance at different receptor systems, with an understanding of the anatomy and interconnections of those receptor systems. Neurophysiologists identify the effects of the substance on firing patterns in different brain regions. All of this knowledge is added to the things we already know about brain function, to push our understanding a bit further. Neuroscience is inefficient, as single studies rarely provide significant gains, and some studies yield results counter to the findings of other studies. But little by little, over years, we gain an understanding of how a substance affects brain function.
I thought it appropriate to share some information about WASUA:
To improve the health and social circumstances of substance users, utilising a framework underpinned by harm reduction and peer education.
To provide support, education and advocacy and to reduce transmission of Blood Borne Viruses and the harms and hazards associated with substance use amongst people in Western Australia.
We should always be skeptical in the extreme of any treatment modality that is presented as a universal “cure” or “magic bullet”, but at the same time we must be careful that the blind zeal of enthusiasts doesn’t cause us to dismiss potentially useful tools out of hand.
Pharmacologically, Ibogaine is a very interesting substance, as it’s a psychedelic tryptamine that is an agonist at 5-HT2A (serotonin receptors) but also acts as an antagonist at NMDA receptors, is an agonist for kappa-opioid receptors and also non-competitively inhibits nAChR (nicotinic acetylcholine receptors).
Serotonin agonists include LSD and a great many other hallucinogenic drugs.
Like dopamine and glutamate, NMDA (N-methyl-D-aspartate) is heavily implicated in the development and maintenance of dependence to many drugs.
Nicotine binds to nAChR (nicotinic acetylcholine receptors), and the drug Zyban (bupropion), which is used as a smoking cessation treatment, blocks acetylcholine receptors.
Just to complicate this pharmacological profile further, Ibogaine is metabolized in the liver (via CYP450 2D6) to produce a psychoactive metabolite noribogaine (12-hydroxyibogamine).
Noribogaine is most potent as a serotonin reuptake inhibitor, reinforcing the serotonergic effects of the parent molecule. It also acts as a moderate κ-opioid receptor antagonist and a weak µ-opioid receptor full agonist, (mu-opioid receptors mediate the euphoric effect of opioids).
(Opioid receptors come in three classes- kappa, mu, and delta. Ibogaine binds most strongly to κ- opioid receptors, shows less affinity for μ receptors, and no affinity for δ receptors. Noribogaine binds to all three classes more strongly than Ibogaine does).
It is possible that this action of noribogaine at the κ-opioid receptor may contribute to the psychoactive effects; the hallucinogenic plant Salvia divinorum contains the chemical salvinorin A which is a highly selective kappa opioid agonist.
As an opioid receptor agonist, Ibogaine actually potentiates opioids. It’s been demonstrated in a couple of small studies that co-administering Ibogaine with morphine stops the development of tolerance and decreases the chance of dependence- but no-one has used this effect clinically, apparently because the dangers of overdose due to potentiation.
Animal studies show that Ibogaine appears to reduce or repress the urge to self-administer morphine in some, but not all, rats who are morphine-dependent.
It also inhibits cocaine self-administration.
Both of those rodent studies show a dose-response relationship, with more of the rats ceasing or reducing self-admin if they were given three doses over a three week period, than from a single dose.
Although Ibogaine treatment is apparently not illegal in Australia, Ibogaine is a very strictly controlled substance.
The import of ibogaine is specifically prohibited under Schedule 4 (import regulations) of the Customs Act. Under the definition of the law ANY material containing the listed substance is deemed to be that substance. Hence, all ibogaine containing material is a drug prohibited import. However, there are no restrictions on possessing ibogaine containing material, seed or live plants in Australia, except that pure ibogaine may not be sold or possessed as a therapeutic product without prescription.
NOTE: Under customs law the importation of 1g of ibogaine is equivalent to importing 1g of heroin. The importation of 100g of iboga bark is equivalent to importing 100g of heroin. The importation of 1g of ibogaine dissolved in 100ml of water/alcohol (eg a tincture) is equivalent to importing 100g of heroin.
New Zealand’s regulators decided to classify Ibogaine and its primary metabolite as a prescription medicine, but this actually makes it more difficult to legally source, as previously it was unregulated. Interestingly, in their review they mention that Ibogaine in NZ as an un-regulated drug was associated with about the same number of deaths per annum as the most strictly regulated prescription drug, methadone.
There is a native Australian Ibogaine Shrub, containing extractable quantities of the drug, although there appears to be no surviving tradition of Aboriginal people ever using it. (Although just because there is no surviving evidence of current or pre-European-settlement Aboriginal cultures using it, doesn’t mean none have ever done so during the 60,000 years or more that they’ve populated Australia. Other psychoactive plants, like Pitjuri (contains nicotine and scopolamine) and Psilocybin mushrooms were exploited ritually and recreationally by traditional Aboriginal peoples, and Pitjuri was traded all over the continent).
I’ve met a handful of people who have used Ibogaine to treat drug dependency, but not a large or broad enough sample to have a strong opinion about its effectiveness. (In a similar fashion, I’ve met a couple of Americans and one Mexican guy who, every six to nine months, go out in the desert with Huicol people and eat peyote, and all three swear this is what has allowed them to overcome serious drug addictions). Because of the ambiguous legal status in Australia, only 1 or two places advertise Ibogaine treatment, I don’t know how many customers they get, and I don’t know how professional these outfits are.
Ibogaine treatment centres in Australia and New Zealand.
Hope this is a useful info.