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Ayahuasca

Various alkaloid profiles in decoctions of Banisteriopsis caapi

September 7, 2011 / Ayahuasca, Biology & Ethnobotany, Papers, Pharmacology & Chemistry, Publications / By /

Abstract

Twenty nine decoctions of Banisteriopsis caapi from four different sources and one specimen of B. caapi paste were analyzed for N,N-dimethyltryptamine (DMT), tetrahydroharmine (THH), harmaline and harmine. Other plants were also used in the preparation of these products, typically Psychotria viridis, which provides DMT. There were considerable variations in alkaloid profiles, both within and between sample sources. DMT was not detected in all samples. Additional THH may be formed from both harmine and harmaline during the preparation of these products. The alkaloid composition of one decoction sample did not change significantly after standing at room temperature for 80 days, but the initial acidic pH was neutralized by natural fermentation after 50 days.

Callaway, J. C. (2005). Various alkaloid profiles in decoctions of Banisteriopsis caapi. Journal of Psychoactive Drugs, 37(2), 151-155. 10.1080/02791072.2005.10399796
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Snuff synergy: preparation, use and pharmacology of yopo and Banisteriopsis caapi among the Piaroa of southern Venezuela

September 6, 2011 / Ayahuasca, Biology & Ethnobotany, Papers, Pharmacology & Chemistry, Publications / By /

Abstract

Current understanding of the preparation and use of yopo, a hallucinogenic snuff made from the ground seeds of the Anadenanthera peregrina tree, has departed little from the accounts of scientists and travelers made over a century ago. Schultes and others have made refinements to these early accounts. While several scholars have drawn attention to the fact that little ethnographic work has been conducted to assess the ethnobotanical diversity and cultural framework of the snuff hallucinogen complex, few subsequent studies deal with botanical variations in preparation and use. This article contrasts historical accounts of yopo preparation with ethnographic data I have recently collected among the Piaroa of southern Venezuela to demonstrate one way in which yopo preparation and use deviates from the basic model established by Humboldt, Spruce and Safford. Piaroa shamans include B. caapi cuttings in the preparation of yopo and consume doses of B. caapi prior to snuff inhalation concomitant with the strength of visions desired for particular tasks. I argue that the combined use of yopo and B. caapi by Piaroa shamans is pharmacologically and ethnobotanically significant, and substantiates claims of the use of admixtures in snuff; further ethnographic investigation of the snuff hallucinogen complex is necessary.

Rodd, R. (2002). Snuff synergy: preparation, use and pharmacology of yopo and Banisteriopsis caapi among the Piaroa of southern Venezuela. Journal of psychoactive drugs, 34(3), 273-279. 10.1080/02791072.2002.10399963
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In Vivo Imaging of Cerebral Serotonin Transporter and Serotonin 2A Receptor Binding in MDMA and Hallucinogen Users

June 6, 2011 / Ayahuasca, DMT, LSD, MDMA, Mescaline / Cacti, Mushrooms / Psilocybin, Neuroscience, Papers, Psychology, Publications, Salvia / Salvinorin A / By / , , , , , ,

Abstract

Context:
Both hallucinogens and 3,4-methylenedioxy-methamphetamine (MDMA or “ecstasy”) have direct agonistic effects on postsynaptic serotonin 2A receptors, the key site for hallucinogenic actions. In addition, MDMA is a potent releaser and reuptake inhibitor of presynaptic serotonin.

Objective:
To assess the differential effects of MDMA and hallucinogen use on cerebral serotonin transporter (SERT) and serotonin2Areceptor binding.

Design:
A positron emission tomography study of 24 young adult drug users and 21 nonusing control partici-pants performed with carbon 11 (11C)–labeled 3-amino-4-[2-[(di(methyl)amino)methyl]phenyl]sulfanylbenzo-nitrile (DASB) and fluorine 18 (18F)–labeled altanserin, respectively. Scans were performed in the user group after a minimum drug abstinence period of 11 days, and the group was subdivided into hallucinogen-preferring users (n = 10) and MDMA-preferring users (n = 14).

Participants:
Twenty-four young adult users of MDMA and/or hallucinogenic drugs and 21 nonusing controls.

Main Outcome Measures:
In vivo cerebral SERT and serotonin 2A receptor binding.

Results:
Compared with nonusers, MDMA-preferring users showed significant decreases in SERT nondisplaceable binding potential (neocortex, −56%; pallidostriatum, −19%; and amygdala, −32%); no significant changes were seen in hallucinogen-preferring users. Both cortical and pallidostriatal SERT nondisplaceable binding potential was negatively correlated with the number of life-time MDMA exposures, and the time of abstinence from MDMA was positively correlated with subcortical, but not cortical, SERT binding. A small decrease in neocortical serotonin 2A receptor binding in the serotonin 2A receptor agonist users (both user groups) was also detected.

Conclusions
We found evidence that MDMA but not hallucinogen use is associated with changes in the cerebral presynaptic serotonergic transmitter system. Because hallucinogenic drugs primarily have serotonin 2A receptor agonistic actions, we conclude that the negative association between MDMA use and cerebral SERT binding is mediated through a direct presynaptic MDMA effect rather than by the serotonin 2A agonistic effects of MDMA. Our cross-sectional data suggest that subcortical, but not cortical, recovery of SERT binding might take place after several months of MDMA abstinence.

Erritzoe, D., Frokjaer, V. G., Holst, K. K., Christoffersen, M., Johansen, S. S., Svarer, C., … Knudsen, G. M. (2011). In Vivo Imaging of Cerebral Serotonin Transporter and Serotonin 2A Receptor Binding in 3,4-Methylenedioxymethamphetamine (MDMA or “Ecstasy”) and Hallucinogen Users. Archives of General Psychiatry, 68(6), 562-576. http://dx.doi.org/10.1001/archgenpsychiatry.2011.56
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β-Carboline Compounds, Including Harmine, Inhibit DYRK1A and Tau Phosphorylation at Multiple Alzheimer's Disease-Related Sites

May 6, 2011 / Ayahuasca, Papers, Psychiatry & Medicine, Publications / By / , , , , , ,

Abstract

Harmine, a β-carboline alkaloid, is a high affinity inhibitor of the dual specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) protein. The DYRK1A gene is located within the Down Syndrome Critical Region (DSCR) on chromosome 21. We and others have implicated DYRK1A in the phosphorylation of tau protein on multiple sites associated with tau pathology in Down Syndrome and in Alzheimer’s disease (AD). Pharmacological inhibition of this kinase may provide an opportunity to intervene therapeutically to alter the onset or progression of tau pathology in AD. Here we test the ability of harmine, and numerous additional β-carboline compounds, to inhibit the DYRK1A dependent phosphorylation of tau protein on serine 396, serine 262/serine 356 (12E8 epitope), and threonine 231 in cell culture assays and in vitro phosphorylation assays. Results demonstrate that the β-carboline compounds (1) potently reduce the expression of all three phosphorylated forms of tau protein, and (2) inhibit the DYRK1A catalyzed direct phosphorylation of tau protein on serine 396. By assaying several β-carboline compounds, we define certain chemical groups that modulate the affinity of this class of compounds for inhibition of tau phosphorylation.

Frost, D., Meechoovet, B., Wang, T., Gately, S., Giorgetti, M., Shcherbakova, I., & Dunckley, T. (2011). β-carboline compounds, including harmine, inhibit DYRK1A and tau phosphorylation at multiple Alzheimer’s disease-related sites. PLoS One, 6(5). https://dx.doi.org/10.1371/journal.pone.0019264

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Ayahuasca, Entheogenic Education & Public Policy

April 18, 2011 / Anthropology & Sociology, Ayahuasca, Papers, Publications / By /

Abstract

Ayahuasca is an entheogenic decoction prepared from two Amazonian plants containing controlled substances, including dimethyltryptamine. Traditionally drunk ritually (and revered as a healing “plant teacher”) by Amazonian indigenous and mestizo peoples, in the 20th century ayahuasca became a sacrament for several new Brazilian religions. One of these, the Santo Daime, has expanded into Canada, where in 2001 a Montreal-based chapter applied for a federal legal exemption to allow drinking of the brew in its rituals. This dissertation undertakes a critical policy analysis of Health Canada’s decision on the Santo Daime request, using government documents obtained through an Access to Information request as data. My goals are to illustrate how modern stereotypes about “drugs” and “drug abuse” in dominant public and political discourses may hinder well-informed policy decision making about ayahuasca, and to consider how entheogenic practices such as ayahuasca drinking are traditional indigenous ways of knowing that should be valued, rather than reflexively demonized and criminalized. My research method is a critical discourse analysis approach to policy analysis, an eclectic means of demonstrating how language contributes to conceptual frames and political responses to public policy issues. I combine insights from recent research on language, discourse and public policy to show how ayahuasca has become an unexpected policy conundrum for liberal democratic states attempting to balance competing interests of criminal justice, public health, and human rights such as religious freedom. I trace ayahuasca’s trajectory as a contemporary policy concern by sketching histories of psychoactive substance use, today’s international drug control regime, and the discursive foundations of its underlying drug war paradigm. Regarding Health Canada’s 2006 decision “in principle” to recommend exemption for the Daime brew, I critique how the government defined ayahuasca as a policy problem, what policy stakeholders it considered in its decision making, and what knowledge about ayahuasca it used. To conclude, I explore modern schooling’s systemic antipathy to wonder and awe, and propose that policy reforms allowing circumspect use of entheogens such as ayahuasca as cognitive tools may help stimulate re-enchantment and appreciation of the need to address human and planetary ecological predicaments of the 21st century.

Tupper, K. W. (2011). Ayahuasca, entheogenic education & public policy (Doctoral dissertation, University of British Columbia). 10.14288/1.0064622
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Consumption of Ayahuasca by Children and Pregnant Women: Medical Controversies and Religious Perspectives

April 8, 2011 / Anthropology & Sociology, Ayahuasca, Papers, Psychology, Publications / By /

Abstract

In 2010, the Brazilian Government agency responsible for drug-related issues formulated official Resolutions that categorized the consumption of ayahuasca by pregnant women and children in the Santo Daime and Uniatildeo do Vegetal ayahuasca-based religions as an “exercise of parental rights.” Although ayahuasca groups do enjoy a relative degree of social legitimacy and formal legal recognition in Brazil, the participation of pregnant women and children nevertheless continues to provoke heated discussion. This article raises the main issues involved in the public debate over this subject. In the first part, a diverse group of biomedical and health specialists was consulted, and their opinions were briefly analyzed. In the second, a full interview with a follower of one branch of Santo Daime, mother of four children who took ayahuasca during all her pregnancies, and whose children all drink ayahuasca, is presented. Her interview reveals important cultural parameters of ayahuasca consumption. The article explores common themes and contradictions found between the biomedical, anthropological, and ayahuasca-users’ discourses. It raises central issues regarding the limits of freedom of religion and the state’s right to interfere in family matters. The following analysis also has implications regarding the role of science in influencing policy decisions on drug use.

Labate, B. C. (2011). Consumption of Ayahuasca by Children and Pregnant Women: Medical Controversies and Religious Perspectives. Journal of Psychoactive Drugs, 43(1), 27-35. http://dx.doi.org/10.1080/02791072.2011.566498
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Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens

January 20, 2011 / Ayahuasca, DMT, LSD, Mescaline / Cacti, Mushrooms / Psilocybin, Neuroscience, Papers, Psychology, Publications / By / ,

Abstract

Serotonergic hallucinogens produce profound changes in perception, mood, and cognition. These drugs include phenylalkylamines such as mescaline and 2,5-dimethoxy-4-methylamphetamine (DOM), and indoleamines such as (+)-lysergic acid diethylamide (LSD) and psilocybin. Despite their differences in chemical structure, the two classes of hallucinogens produce remarkably similar subjective effects in humans, and induce cross-tolerance. The phenylalkylamine hallucinogens are selective 5-HT(2) receptor agonists, whereas the indoleamines are relatively non-selective for serotonin (5-HT) receptors. There is extensive evidence, from both animal and human studies, that the characteristic effects of hallucinogens are mediated by interactions with the 5-HT(2A) receptor. Nevertheless, there is also evidence that interactions with other receptor sites contribute to the psychopharmacological and behavioral effects of the indoleamine hallucinogens. This article reviews the evidence demonstrating that the effects of indoleamine hallucinogens in a variety of animal behavioral paradigms are mediated by both 5-HT(2) and non-5-HT(2) receptors.

Halberstadt, A. L., & Geyer, M.A. (2011). Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens. Neuropharmacology, 61(3), 364-381. http://dx.doi.org/10.1016/j.neuropharm.2011.01.017
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Ayahuasca, Salutogenesis and the Need for „Ecological“ Approaches

November 14, 2010 / Ayahuasca, Papers, Publications / By /

Abstract

In Western science, extraordinary or visionary states of consciousness are traditionally discussed mainly in terms of psychopathology, that is, in the sense of mental disease. This applies even more when they are associated with psychoactive substances such as the herbal decoction Ayahuasca, which are generally called “hallucinogens” with the connotation “not objective, unreal”. However, responsible work with psychoactive herbal decoctions like Ayahuasca – similar to many forms of meditation – has salutogenic potential, i.e. it can enhance physical, mental and spiritual health by calling into play what is referred to as “participating consciousness”. Rigid feeling, thought, and behavioural patterns can unclench, the self can rearrange itself and develop its inner and outer resources more deeply.

The thesis of this article is that for an adequate understanding of these processes, the familiar “linear” thinking no longer suffices, rather, an “ecology of mind” is needed (Bateson 1972), i.e. less divisive, less objectifying explanations which also do not exclude the fundamental paradoxes of human existence. Of course, such approaches occasionally need some getting used to.

In the following, a few basic elements of the ecological approach will be explained (chapter 2). Chapter 3 will then analyze whether or not and to what extent this approach can explain extraordinary states of consciousness better than traditional, linear thinking.

Friczewski, F. (2010). Ayahuasca, Salutogenesis and the Need for „Ecological“ Approaches.

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Psychobiology of Drug-Induced Religious Experience: From the Brain 'Locus of Religion' to Cognitive Unbinding

November 13, 2010 / Ayahuasca, LSD, Mushrooms / Psilocybin, Neuroscience, Papers, Psychology, Publications / By / ,

Abstract

The recent interest in the psychopharmacological underpinnings of religious experiences has led to both the laboratory characterizations of drug-induced mystical events and psychobiological models of religious experiences rooted in evolution and fitness. Our examination of this literature suggests that these theories may be congruent only within more modern religious and cultural settings and are not generalizable to all historical beliefs, as would be expected from an evolutionarily conserved biological mechanism. The strong influence of culture on the subjective effects of drugs as well as religious thoughts argues against the concept of a common pathway in the brain uniquely responsible for these experiences. Rather, the role of personal beliefs, expectations and experiences may interject bias into the interpretation of psychoactive drug action as a reflection of biologically based religious thought. Thus, psychobiological research proposing specific brain mechanisms should consider anthropological and historical data to address alternative explanations to the “fitness” of religious thought. A psychobiological model of the religious experience based on the concept of cognitive unbinding seems to accommodate these data better than that of a specific brain locus of religion.

Nencini, P., & Grant, G. A. (2010). Psychobiology of Drug-Induced Religious Experience: From the Brain ‘Locus of Religion’ to Cognitive Unbinding. Substance Use & Misuse, 45(13), 2130–2151. http://dx.doi.org/10.3109/10826081003713803
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Methodology for and the determination of the major constituents and metabolites of the Amazonian botanical medicine ayahuasca in human urine

October 26, 2021 / Ayahuasca, Papers, Publications / By / , , , ,

Abstract

Ayahuasca, also known as caapi or yage among various South American groups, holds a highly esteemed and millennia-old position in these cultures’ medical and religious pharmacopeia. There is now an increasing interest in the potential for modern medical applications of ayahuasca, as well as concerns regarding its increasing potential for abuse. Toxicological and clinical research to address these issues will require information regarding its metabolism and clearance. Thus, a rapid, sensitive and specific method for characterization and quantitation of the major constituents and of the metabolites of ayahuasca in urine is needed. The present research provides a protocol for conducting such analyses. The characteristics of the method, conducted by sample dilution and using HPLC–electrospray ionization (ESI)–selected reaction monitoring (SRM)–tandem mass spectrometry, are presented. The application of the analytical protocol to urine samples collected from three individuals that were administered ayahuasca has also been demonstrated. The data show that the major metabolite of the hallucinogenic component of ayahuasca, N,N-dimethyltryptamine (DMT), is the corresponding N-oxide, the first time this metabolite has been described in in vivo studies in humans. Further, very little DMT was detected in urine, despite the inhibition of monoamine oxidase afforded by the presence of the harmala alkaloids in ayahuasca. The major harmala alkaloid excreted was tetrahydroharmine. Other excretion products and metabolites were also identified and quantified. The method described would be suitable for use in further toxicological and clinical research on ayahuasca.

McIlhenny, E. H., Riba, J., Barbanoj, M. J., Strassman, R., & Barker, S. A. (2011). Methodology for and the determination of the major constituents and metabolites of the Amazonian botanical medicine ayahuasca in human urine. Biomedical Chromatography, 25(9), 970-984. 10.1002/bmc.1551
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