Table 2 - uploaded by Jordi Riba
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Context 1
... the roots and leaves of B. caapi are rarely used in the preparation of the tea. The alkaloid content in the leaves of Psychotria is on average 0.3% (see Table 2), most of it DMT, although in some cases no alkaloids have been found at all, as for instance in a specimen of Psychotria carthaginensis Jacq. analyzed by McKenna et al. (1984). ...
Context 2
... by McKenna et al. (1984). The leaves of Diplopterys cabrerana contain an average of 0.7% of alkaloids (see Table 2). The most complete quantitative analyses of ayahuasca brews and their plant constituents are those undertaken by Rivier and Lindgren (1972) and McKenna and coworkers (1984). ...
Context 3
... the 5-HT 2A and 5-HT 2C are positively coupled to phosphoinositide hydrolysis, the 5-HT 1A subtype is negatively coupled to adenylate cyclase. 5-HT 2A receptors show the highest densities in the neocortex, while 5-HT 2C receptors predominate in the choroid plexus and 5-HT 1A are mainly found in the hyppocampus, amygdala, limbic cortex and notoriously in the raphe nuclei where they act as somatodendritic autoreceptors (for a review see Glennon and Dukat, 1995). ...
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Citations
... The effects of consuming ayahuasca have been variously summarized as "… inducing changes in the perceptual, affective, cognitive, and somatic spheres, with a combination of stimulatory and visual psychoactive effects of longer duration and milder intensity than those previously reported for intravenously administered DMT." (Riba et al. 2001;Riba 2003). Pharmacological studies of acute ayahuasca administration to healthy volunteers and mental health assessments of long-term ayahuasca consumers suggest that this ethnobotanical medicine is relatively safe and effective (Callaway et al. 1999;dos Santos, et al. 2011dos Santos, et al. , 2016ados Santos, et al. , 2016bdos Santos, et al. , 2017. ...
As with all drugs, the route, form, and/or dose of a substance administered or applied can play a defining role in its overall pharmacology and use as a therapeutic. This review will focus on these factors as they relate to the psychedelic N,N-dimethyltryptamine (DMT). It will examine the positive and negative aspects of different formulations and routes of administration of DMT and the observed effects from such administrations in the form of ayahuasca teas; oral “pharmahuasca”; injections by intravenous (IV) and intramuscular (IM) routes; inhalation, insufflation; and other routes; and high-dose, low-dose, and “micro-dose” effects. The review will consider possible oral route of administration alternatives that would not require concomitant use of a monoamine oxidase inhibitor. The review will then address the current research findings for DMT from in vivo and in vitro studies as well as the possibility that these findings may be revealing the role of endogenous DMT in normal brain function.
... His studies on ayahuasca began with his Ph.D. dissertation entitled ''Human pharmacology of ayahuasca,'' concluded in 2003 under the supervision of Professor Manuel José Barbanoj Rodriguez (MD, UAB/HSCSP). 2 At the time of his death, Professor Riba was a researcher at Maastricht University, where he worked in the field of human psychedelic/hallucinogen research. ...
... They contain many β-carbolines and quinazolines, with harmaline being the major alkaloid (Mahmoudian, Jalilpour, & Salehian, 2002). It has been observed that these β-carbolines bind with modest affinity to 5-HT 2A receptors (Riba, 2003), except in the case of harmine, which expresses high affinity with these receptors (Glennon et al., 2000). They also show affinity for 5-HT 2C, 1A , dopamine (Nasehi et al., 2010), gammaaminobutyric acid (GABA; Glennon et al., 2000), imidazoline (I 2 ; Yu, Idle, Krausz, Küpfer, & Gonzalez, 2003), and adrenergic (α 2 ) receptors (Husbands et al., 2001). ...
... These β-carbolines can also interact with opioid receptors (Farouk, Laroubi, Aboufatima, Benharref, & Chait, 2008). However, the most remarkable is their ability to inhibit the enzyme monoamine oxidase (MAO) at concentrations in the micromolar and nanomolar range (Riba, 2003). These substances appear to be more effective at inhibiting MAO-A than at inhibiting MAO-B. ...
... As discussed above, we cannot dismiss the possibility that the active constituents in changa produce a direct analgesic effect. However, those compounds have short half-lives (t ½λz = 260-532 min; Riba, 2003) that are insufficient to explain the pattern that can be clearly observed in the case: an analgesic effect that endured for over 2 weeks. It is well known that a single administration of a psychedelic drug, such as psilocybin, can produce longlasting effects (Griffiths et al., 2011). ...
Background and aims
Pain is the most prevalent symptom of a health condition, and it is inappropriately treated in many cases. Here, we present a case report in which we observe a long-lasting analgesic effect produced by changa, a psychedelic drug that contains the psychoactive N,N-dimethyltryptamine and ground seeds of Peganum harmala, which are rich in β-carbolines.
Methods
We describe the case and offer a brief review of supportive findings.
Results
A long-lasting analgesic effect after the use of changa was reported. Possible analgesic mechanisms are discussed. We suggest that both pharmacological and non-pharmacological factors could be involved.
Conclusion
These findings offer preliminary evidence of the analgesic effect of changa, but due to its complex pharmacological actions, involving many neurotransmitter systems, further research is needed in order to establish the specific mechanisms at work.
... While Aya and EBc were administered orally, EPv was administered i.p. due to expected DMT breakdown by MAO-A in the gastrointestinal tract. Of note, previous studies in humans have suggested that β-carboline-induced MAO inhibition is mainly peripheral and short-lived, and only allows around 15% of the DMT to reach systemic circulation (Riba, 2003;Domínguez-Clavé et al., 2016). Thus, with oral administration of Aya, the proportion of DMT that reaches the brain would be much lower than that of i.p. ...
Ayahuasca is a hallucinogenic beverage produced from the decoction of Banisteriopsis caapi (Bc) and Psychotria viridis (Pv), β-carboline- and N,N-dimethyltryptamine(DMT)-containing plants, respectively. Accumulating evidence suggests that ayahuasca may have therapeutic effects on ethanol abuse. It is not known, however, whether its effects are dependent on the presence of DMT or if non-DMT-containing components would have therapeutic effects. The aim of the present study was to investigate the rewarding properties of ayahuasca (30, 100, and 300 mg/kg, orally), Bc (132, 440, and 1320 mg/kg, orally) and Pv (3.75, 12.5 and 37.5 mg/kg, i.p.) extracts and their effects on ethanol (1.8 g/kg, i.p.) reward using the conditioned place preference (CPP) paradigm in male mice. Animals were conditioned with ayahuasca, Bc or Pv extracts during 8 sessions. An intermediate, but not a high, dose of ayahuasca induced CPP in mice. Bc and Pv did not induce CPP. Subsequently, the effects of those extracts were tested on the development of ethanol-induced CPP. Ayahuasca, Bc or Pv were administered before ethanol injections during conditioning sessions. While Bc and Pv exerted no effects on ethanol-induced CPP, pretreatment with ayahuasca blocked the development of CPP to ethanol. Finally, the effects of a post-ethanol-conditioning treatment with ayahuasca, Bc or Pv on the expression of ethanol-induced CPP were tested. Animals were conditioned with ethanol, and subsequently treated with either ayahuasca, Bc or Pv in the CPP environment previously associated with saline or ethanol for 6 days. Animals were then reexposed to ethanol and ethanol-induced CPP was quantified on the following day. Treatment with all compounds in the ethanol-paired environment blocked the expression of ethanol-induced CPP. Administration of an intermediate, but not a high, dose of ayahuasca and Bc, as well as Pv administration, in the saline-paired compartment blocked the expression of ethanol-induced CPP. The present study sheds light into the components underlying the therapeutic effects of ayahuasca on ethanol abuse, indicating that ayahuasca and its plant components can decrease ethanol reward at doses that do not exert abuse liability. Importantly, the treatment environment seems to influence the therapeutic effects of ayahuasca and Bc, providing important insights into clinical practice.
... Para que los efectos sean perceptibles, se requieren 20mg (0,25 mg/kg) de DMT y 120mg (1,5mg/ kg) de HRM, mientras que para alcanzar el umbral alucinógeno se necesitan 30mg de DMT (0,38 mg/ kg) y 120mg de HRM, aumentando la intensidad de sus efectos de manera dosis-dependiente (15,16). La HRM, por sí misma, puede tener actividad alucinógena cuando se encuentra en cantidades superiores a los 100mg. ...
... Se estima que, tras su ingestión, la DMT alcanza una concentración máxima (C max ) de entre 12,14 a 17,44 ng/ml, en un tiempo (T max ) de 107,50 min, y posee un tiempo de vida media (T 1/2 ) de 259 min. Sus efectos subjetivos se presentan de manera paralela al curso de la concentración plasmática de DMT, de tal manera que son significativos luego de 1 hora, aumentando progresivamente hasta lograr su máxima intensidad entre 1,5 a 2 horas, con un período de meseta de 45 min a 1 hora, seguido de su disminución durante 1 hora más, finalizando luego de 3 a 6 horas, que es el tiempo aproximado que duran las sesiones rituales (15,16). ...
... Aunque varían significativamente dependiendo del individuo, la dosis ingerida y la composición de alcaloides del brebaje (6,15,16), los efectos agudos que puede producir la ayahuasca son: náuseas y vómitos, los más frecuentes (6,16,17), diarrea (11); aumento moderado de la temperatura, frecuencia cardíaca y presión arterial (16,17); alteraciones moderadas de la respiración y el tamaño pupilar; elevación plasmática de prolactina, cortisol y hormona del crecimiento; disminución del porcentaje de linfocitos CD4 y CD3, aumento de las células "natural killer" (17); psíquicos como alucinaciones visuales, alteraciones somatoestésicas y de otras esferas sensoriales, alteraciones del contenido del pensamiento, disforia, Rev Neuropsiquiatr 80 (4), 2017. labilidad emocional, elevación del ánimo y del afecto (6,9,17), desorientación y ansiedad (16), aumento de la introspección, déficits en el procesamiento de la información sensorial y en los procesos atencionales. ...
La ayahuasca es una bebida alucinógena, producto de la decocción de las plantas Banisteriopsis caapi y Psychotria viridis y que cuenta con N,N-dimetiltriptamina y β-carbolinas, como sus compuestos principales. Aunque produce alteraciones somáticas, cognitivas y subjetivas agudas, a menudo intensas, casi no se han reportado efectos adversos luego de un cuadro de intoxicación con este agente. En este artículo se presenta el caso de un varón de 40 años, procedente de la Amazonía peruana, que siguió un curso psicótico tras una sesión ritual de consumo; el episodio psicótico se resolvió favorablemente con tratamiento específico. Aun cuando infrecuentes, estos episodios pueden llegar a ser muy severos y asociarse a conductas violentas. Los usuarios con antecedentes de psicosis, manía o abuso de sustancias psicoactivas parecen estar en mayor riesgo. La literatura en relación al riesgo de reacciones adversas (incluidas conductas psicóticas) debidas al uso de ayahuasca, es escasa y poco concluyente por lo que casos similares al descrito deben evaluarse cuidadosamente y difundirse de manera apropiada.
... De estos estudios se ha demostrado que la DMT y la ayahuasca tienen una farmacodinamia (o acción de un fármaco sobre el organismo) muy diferente. Los efectos agudos de la DMT aparecen de forma casi inmediata e intensa tras su administración endovenosa , mientras que la ayahuasca ejerce su efecto de manera más lenta y progresiva, iniciándose a los 45-60 minutos tras su ingesta, alcanzando su efecto máximo a las 2 horas y desapareciendo entre las 4 y 6 horas (Riba, 2003;dos Santos, 2011). La intensidad máxima de los efectos de la DMT es aproximadamente el doble de la intensidad máxima de los efectos de la ayahuasca a dosis equipotenciales (Grob et al., 1996). ...
... En este sentido, y de acuerdo con la ciencia toxicológica, no debe equipararse dosis psicoactiva mínima con dosis tóxica, si entendemos toxicidad como la capacidad de una sustancia para, al entrar en contacto con el organismo, producir a través de su acción química un efecto perjudicial (Baños y Farré, 2002). Con relación a los efectos de la ayahuasca sobre el organismo, los estudios realizados con voluntarios, tanto en condiciones de laboratorio (Riba, 2003;dos Santos, 2011), como en contextos naturales (McKenna, 2004), muestran que la ayahuasca es, fisiológicamente, bastante segura. El impacto de la ayahuasca sobre el sistema cardiovascular es mínimo, produciendo ligeros incrementos sin implicaciones clínicas de la presión arterial y de la frecuencia cardíaca (Riba et al., 2001dos Santos et al., 2012). ...
... El principal efecto secundario que induce la ayahuasca es náusea y vómito (Callaway, et al., 1999;Riba et al., 2001;Riba, 2003;Riba & Barbanoj, 2005;dos Santos, 2011;dos Santos et al., 2012). ...
... At some point in the remote past, the indigenous people of the Amazon Basin discovered that adding the leaves of Psychotria viridis (which, as previously mentioned, contain DMT) to a decoction of Banisteriopsis caapi (which contains harmala alkaloids), makes the DMT bioactive. This is due to the harmala alkaloids, which, acting as MAO inhibitors (MAOIs), block the MAO present in the gastrointestinal tract and in this way the DMT present in the leaves of P. viridis can reach the brain (Mckenna et al., 1984;Riba et al., 2003). Pure DMT on its own is inactive when consumed orally . ...
... In these studies, it has been demonstrated that DMT and ayahuasca have very different pharmaco-dynamics. The acute effects of DMT appear in an intense and almost immediate way after its intravenous administration , while ayahuasca produces effects in a slower and more progressive way, beginning from 45 to 60 minutes after administration, reaching maximum effects after 2 hours, which disappear after 4 to 6 hours (Riba, 2003;dos Santos, 2011). The maximum intensity of the effects of DMT is approximately two times that of ayahuasca at equivalent doses (Grob et al., 1996), which makes the global effects of ayahuasca much more controllable than pure DMT. ...
... The curve of effects that ayahuasca produces corresponds with the curve of the presence of DMT and harmalines (MAOIs) in plasma, which disappears from the organism after eight hours (Riba et al., 2003;Schenberg et al., 2015). ...
... At some point in the remote past, the indigenous people of the Amazon Basin discovered that adding the leaves of Psychotria viridis (which, as previously mentioned, contain DMT) to a decoction of Banisteriopsis caapi (which contains harmala alkaloids), makes the DMT bioactive. This is due to the harmala alkaloids, which, acting as MAO inhibitors (MAOIs), block the MAO present in the gastrointestinal tract and in this way the DMT present in the leaves of P. viridis can reach the brain (Mckenna et al., 1984;Riba et al., 2003). Pure DMT on its own is inactive when consumed orally . ...
... In these studies, it has been demonstrated that DMT and ayahuasca have very different pharmaco-dynamics. The acute effects of DMT appear in an intense and almost immediate way after its intravenous administration , while ayahuasca produces effects in a slower and more progressive way, beginning from 45 to 60 minutes after administration, reaching maximum effects after 2 hours, which disappear after 4 to 6 hours (Riba, 2003;dos Santos, 2011). The maximum intensity of the effects of DMT is approximately two times that of ayahuasca at equivalent doses (Grob et al., 1996), which makes the global effects of ayahuasca much more controllable than pure DMT. ...
... The curve of effects that ayahuasca produces corresponds with the curve of the presence of DMT and harmalines (MAOIs) in plasma, which disappears from the organism after eight hours (Riba et al., 2003;Schenberg et al., 2015). ...
... To our knowledge, the effects of harmaline and THH on neurogenesis have not been studied before. While harmaline is only present in small amounts in B. caapi, THH is the second most abundant β-carboline in the plant 4,29 . Additionally, THH shows more consistent plasma levels between individuals and studies than harmine, which is rapidly degraded to harmol when taken orally 29,34 . ...
Banisteriopsis caapi is the basic ingredient of ayahuasca, a psychotropic plant tea used in the Amazon for ritual and medicinal purposes, and by interested individuals worldwide. Animal studies and recent clinical research suggests that B. caapi preparations show antidepressant activity, a therapeutic effect that has been linked to hippocampal neurogenesis. Here we report that harmine, tetrahydroharmine and harmaline, the three main alkaloids present in B. caapi, and the harmine metabolite harmol, stimulate adult neurogenesis in vitro. In neurospheres prepared from progenitor cells obtained from the subventricular and the subgranular zones of adult mice brains, all compounds stimulated neural stem cell proliferation, migration, and differentiation into adult neurons. These findings suggest that modulation of brain plasticity could be a major contribution to the antidepressant effects of ayahuasca. They also expand the potential application of B. caapi alkaloids to other brain disorders that may benefit from stimulation of endogenous neural precursor niches.
... To our knowledge, the effects of harmaline and THH on neurogenesis have not been studied before. While harmaline is only present in small amounts in B. caapi, THH is the second most abundant β-carboline in the plant 4,29 . Additionally, THH shows more consistent plasma levels between individuals and studies than harmine, which is rapidly degraded to harmol when taken orally 29,34 . ...
Banisteriopsis caapi is the basic ingredient of ayahuasca, a psychotropic plant tea used in the Amazon for ritual and medicinal purposes, and by interested individuals worldwide. Animal studies and recent clinical research suggests that B. caapi preparations show antidepressant activity, a therapeutic effect that has been linked to hippocampal neurogenesis. Here we report that harmine, tetrahydroharmine and harmaline, the three main alkaloids present in B. caapi, and the harmine metabolite harmol, stimulate adult neurogenesis in vitro. In neurospheres prepared from progenitor cells obtained from the subventricular and the subgranular zones of adult mice brains, all compounds stimulated neural stem cell proliferation, migration, and differentiation into adult neurons. These findings suggest that modulation of brain plasticity could be a major contribution to the antidepressant effects of ayahuasca. They also expand the potential application of B. caapi alkaloids to other brain disorders that may benefit from stimulation of endogenous neural precursor niches.
