Authors

Olga Maria Duarte
Mario Simoes

Ayahuasca is a South American traditional herbal preparation typically produced by decoction of a mixture of Banisteriopsis caapi stem and Psychotria viridis leaf. Among others, it contains as marker compounds the psychedelic 5-HT2A and sigma-1 agonist N,Ndimethyltryptamine (DMT) from P. viridis plus β-carboline alkaloids with monoamine-oxidase (MAO)-inhibiting properties like harmine, harmaline and tetrahydroharmine from Banisteriopsis caapi. These marker compounds, when administered to humans, produce transitory modifications in emotion, thought content, perception and somatic sensations, while the capacity of the individual to interact with its surroundings is significantly preserved. Studies of medium- and longterm ayahuasca’s use suggest that brain alterations manifested as increased spiritual tendencies, can be produced. Ayahuasca therapeutic potential of “decentering” is considered important in clinical psychology and psychiatry. It can produce psychological changes in patients like selftranscendence, personal development, the search for psychological wellbeing, better environment adaptation and treatment for some neuropsychiatric disorders, as some research is supporting. Ayahuasca is used as antidepressant, in the treatment of alcohol and drug dependence, in posttraumatic stress disorder (PTSD), Parkinson Disease, Alzheimer and antisocial behavior. This traditional herbal preparation has been object of a wide series of scientific studies, and the results have been proven on its therapeutic potential. However, the variability inherent to the use of biological material from different sources together with different dosages and forms of preparation means that in most cases it is not possible to
compare the results obtained by different teams. In this context there is still a way to go, to allow the profit of the integral therapeutic potential of this herbal medicine.
Ayahuasca is a therapeutic potential herbal
medicine, mind enhancer, psychiatric disorders
Introduction
Ayahuasca is a traditional herbal preparation made by decoction according to different traditional recipes, based on Psychotria viridis (Ruciaceae) leaf and Banisteriopsis caapi stem (Malphigiaceae), used fresh or sometimes dried. Other species like Diplopterys cabreraba or other Psychotria spp. and Nicotiana sp., Brugmansia sp. and Brunfelsia sp. are also referred as possible constituents of this herbal preparation. The traditional use of this interesting and complex hallucinogen South American traditional herbal preparation was already referred since the preColombian on the neo-Inca cultural historical complex. It is commonly known as ayahuasca, caapi or yage and in hoasca (Portuguese language). The first West writing report of ayahuasca indigenous use for “divination, mystification and bewitchment” was made by the Jesuit missionaries Pablo Maroni in 1737 and Franz Xaver Veigl in 1768. However, it is estimated that this preparation will be used for these purposes from about 8000 years. Currently the use of this preparation in religious and ritualistic context is recognized, among others, in different European countries, United States of America, Australia, Peru, Ecuador, Colombia, Bolivia and Brazil and by at least 72 different indigenous tribes of the Amazon. This paper aims at a brief review of the knowledge obtained through the studies carried out by many authors on this interesting traditional herbal preparation as an entheogen agent.

Ritual

Generally, what is sought when attending an ayahuasca session is an inner and transformative experience. Almost always this type of experiences assumes psychological and biographical contents such as
traumatic events in the person’s past. Under the influence of the brew, those events are revived, and it is hoped that an answer, or another meaning, emerges in order to change or influence the present situation of life. These situations can be or not traumatic but, anyway, they can be experienced in a new perspective, often pointing to an imagined and wished positive future, remaining a “future memory”. It is also possible that significate “encounters” happen with people already deceased for a releasement of a misunderstood relationship or for bringing advice. This does not necessarily have to occur in a ritualistic environment and some groups organize events as a form of expanding consciousness. This administration can occur in a single intake and, in this case, it would be the sum of two or three doses normally drank in a ritual. In the course of a ritual, normally, one drinks ayahuasca in three to four times, separated by a two hours interval, in a session of 4 to 8 hours duration. On the other hand, these sessions in ritualistic context are accompanied by songs, oriented by the shaman. These chants have a religious connotation, almost always Christian, and in Brazil they are called “Hinários” and in the rest of South America they are called “Ícaros” and their content connotation has much to do with the fauna and Gods of the jungle and even old relatives (grandfather, grandmother) of people who take part in the ceremony.
Phenomenology
It is known that Ayahuasca has a rich phenomenology, normally appearing in a natural context of a ritual. Visions and other phenomena depend also on the personality, the quantity of compounds present in the brew and intention of the experiencer. In summary one can say that set and setting have a prominent role. It is known today that the amount of DMT present frankly increases the phenomenology of visionary type. Just before the visions one feels a light tremor in the eyelids and “everything” starts with geometric patterns and lights in a fantastic sight! These visions appear with closed eyes and are of various types, including mammals, reptiles, insect like forms and humans. Animals are in the majority snakes and jaguars, but, curiously, also another type of insect like, for example, mantis. Sometimes visions of deceased ancestors
or living persons also make their appearance. These visions have a special feature, in the sense that it is possible to interact with the characters observed. In addition to the aforementioned animals, insects or people it often arises scenes according to the motivation to drink the brew, in a vision that corresponds to a response or a searched solution of a problem or question. Other times it feels like a flight of the own conscience to another time and space, in the past or in the future, as it were a “soul flight”. Then, experiences of clairvoyance or precognition arise, respectively, concerning situations taking place, in another space, at the same moment of the intake or a situation in the future. Other times still appear visions linked to the transcendent, the ominous, visions that are inscribed in a mystical experience or evoking a near- death experience. The kind of transformative experiences are of the emotional kind. They range from an inner pacification, through a “cleaning” of the mind, to a self-knowledge of the best and the worst of oneself. Ethical issues are taking in account and there is an inner promise that it does not happen again. Sometimes it arises a state of ecstasy, a feeling of integration and belonging in a Divine and Universal project. Still in these high emotional experiences, it often arises a direct confrontation with the own emotions of the past and of the present and even eventually with respect to the future, normally connected with personal relations. Frequently, in relation to this aspect, there is an increased empathy, compassion or a benevolence that translates in a better relational capacity. It can even touch the “contact “with the Divine, which is often called as the “tremendum et fascinans misterium”. Very often, after these experiences, the subjects change their attitudes to their previous lives, becoming more ethical, spiritual and less materialistic.

Marker compounds

Traditional herbal preparations produced by decoction of the mixture of Banisteriopsis caapi stem and Psychotria viridis leaf contains alkaloids as main marker compounds, namely N,N-dimethyltryptamine (DMT) from P. viridis and β-carboline alkaloids like harmine, harmaline and tetrahydroharmine from Banisteriopsis caapi.
DMT is an indole alkaloid endogenous in animals and in species from different botanical genus like Phalaris, Delosperma, Acacia, Desmodium, Mimosa, Virola, and Psychotria. This compound when ingested causes brief and episodic visual hallucinations at high concentration and may have a role in normal animals’ physiological and/or psychopathology. DMT interacts with ionotropic and metabotropic receptors. In special, it is an agonist of serotonin (5-HT) receptors, namely of 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT5A, 5-HT6 and 5-HT7 receptors (affinities ranging from 39 nM to 2.1 μM) an of TAAR and sigma-1 receptors. DMT is substrate for both cell-surface serotonin uptake transporters (SERTS) and neuronal vesicle monoamine transporters (VMAT2). In humans, DMT

(dimethyltryptamine fumarate salt form) doses of 0.1 and 0.05 mg/kg iv are not hallucinogenic: at 0.05 mg/Kg iv dose a somaesthetic effect was verified and at 1 mg/Kg iv changes in perception were also observed. Doses between 0.1-0.2 mg/kg were described as enhancing the intensity of feeling and affection, cognition and volition and 0.2 mg/kg iv was the threshold dose for hallucinogenic effects. The β-carboline alkaloids type harman are well known reversible and competitive monoamine oxidase inhibitors. EC50 values of 8×10-8 M for harmine, 6×10-8 M for harmaline and 1.4×10-5 M for tetrahydroharmine (THH) were obtained concerning the monoamine-oxidase A inhibition (MAO-A) but higher concentrations were required for both harmine and harmaline to inhibit MAO-B. Although THH is a poor MAOI can acting as a 5-HT reuptake inhibitor.
Pharmacological and Clinical Evidence.

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