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Ayahuasca: alkaloids, plants & analogs
assembled by Keeper of the Trout
Section 1 :
Dosages & activity

120 mg of harmine base (1.5 mg per kilogram is a better view) is usually recommended as the absolute lower limit for full oral activation of DMT. Some Ayahuasca brews have been found to contain slightly in excess of 400 mg per dose.

Increasing the dosage of the b-carboline only increases the somatic effects (including nausea) as the psychoactive effects which are said to occur do so only at much higher levels than a person is likely to consume (or want to consume). The best idea is to use the least amount of harmine that will work and regulate the effect by varying the amount of active entheogen that is used.

Bioassays by Ott and others have helped delineate the lowest threshold. Ott determined that 141 mg of harmine hydrochloride [equivalent to 47 mg of harmine hydrochloride] was sufficient to enable full oral activation of DMT but 40 mg of the free base [equivalent to 120 mg of harmine base; in Ott's case 1.5 mg./ kg.] was not [1].

Harmaline is said to be about 1.5 times as active as harmine but 100 mg of it has been determined to be the amount required to orally activate DMT [2]. Others have claimed it twice as potent as harmine in activity. It might be noted that activity and the ability to orally potentiate or activate tryptamines can not automatically be assumed to be synonymous.

It has been stated by Naranjo 1967 that 300 mg of racemic tetrahydroharmine is equal to 100 mg of harmaline. This is based on a single experiment involving one person. So far as can be determined, no attempts have been made to determine whether it is effective in the oral activation of tryptamines but the oral activity of UdV hoasca determined to contain only subthreshold amounts of harmine as well as tetrahydroharmine suggests that it may be effective for this purpose. Its presence as the lone alkaloid in an ayahuasca additive that was reported active, as noted by Shulgin stresses the need for evaluation, as does the aforementioned analysis of UdV prepared ayahuasca which contained a substantial but subthreshhold dose of harmine co-occurring with a similar amount of tetrahydroharmine.

Despite its decent MAOI (and stronger sedative) properties, 250 mg of Harman [3]did not activate several more-than-adequate dosages of DMT. Attempts to determine whether a larger amount would work have not been performed.

Despite assorted armchair assumptions online to the contrary, it seems unlikely that Tetrahydroharman would be any more effective than harman and apparently this known weak MAOI has not been specifically evaluated for this purpose.

Tetrahydroharmine is suggested to be effective for this purpose based on its sometimes high presence in effective UdV hoasca brews containing what are thought to be subthreshold levels of harmine, but Callaway has pointed out that there are several potential routes for it to affect the activity of DMT (see comments elsewhere here) and it may show psychoactivity of its own (which is another subject in serious need of real study).

In experiments designed to ascertain relative MAO inhibiting abilities, Udenfriend and associates (1958) determined harmine and harmaline to be about equal in activity with harman and tetrahydroharmine less potent, McKenna and coworkers (1984a) obtained similar results, as did Buckholtz & Boggan 1977, but found harmaline to be slightly more active than harmine. In contrast to this is McIsaac & Estévez 1966 who reported harman as having the greatest activity (and norharman having yet greater activity). McIsaac & Estévez used calf liver mitochondrial homogenates, while Udenfriend and McKenna had both used rat liver homogenates and Buckholtz & Boggan: rat liver and brain homogenate. [Comments adapted from Ott 1994]

It is this author's recommendation that if planning on using an MAOI to orally activate DMT, that harmine and harmaline be used as the substances of choice. They are proven to be reliable and short-acting; their MAO inhibition is totally and readily reversible once the dosage wears off.

Both are reasonably safe when used as directed, are fairly readily available, relatively inexpensive and have both well known dosage levels and parameters of effects. Tetrahydroharmine may be useful as well but its activity needs to be much better defined.

The pharmaceutical product moclobemide [4] has also been determined to be effective for this purpose and is preferred by some due to the ability of the user to precisely regulate the dosage and also its lack of any sedative side-effects. It similarly is a reversible MAOI but its potential for adverse drug interactions is unclear.

Cultivation of B. caapi as a plant grown outdoors but overwintered indoors and used for leaf production (and young stem trimmings) is a relatively unexplored area that the literature suggests would be quite fruitful. While the alkaloid content is much lower than P. harmala, the growth of B. caapi under good conditions is phenomenal.

The leaf is said by at least one ayahuascero not to be used for making ayahuasca due to it not tasting right. In what data points we have the alkaloid levels of the bark seem to be less than those of the leaves (or the roots or the seeds in increasing order) but more analytical investigations are needed. Even with greenhouses, northern climate cultivation of B. caapi for stem bark is realistically viable only for relatively small amounts; adequate for an individual but not feasible for commercial scale production. The standard recommendation among growers is that harvest of stem-bark should not begin until the material reaches 7 years of age but the reasons for this are unclear.

While reliably within a useful range, the actual levels of total alkaloid found within P. harmala seeds varies from 2-7% according to Ott 1993. To account for the variability, Ott recommended 3 to 4 grams of the seeds be used for oral activation. (approx. 1 tsp.)

Marion reported quantitative assay yields of 2.09% harmaline and 1.60% harmine. Hasenfratz recovered 1.5% harmaline and 1% harmine.

Even if present at levels as low as 1%; this will still yield 4.5 grams of harmine for each pound of P. harmala. (A pound of green seeds testing as well as Degtyarev's would yield over 19 grams of harmine)

Purchased in bulk from seed suppliers, pound prices range from $20 on up. [Seeds for dye purposes generally command lower prices than do viable seeds intended for sowing.] If obtained as incense from Middle Eastern groceries under the name Esphand it will cost between $6 and $12 a lb. retail.

A pound of seeds will average out to around two dozen mao inhibiting doses capable of orally activating tryptamines even if the material was the weakest available (over a hundred average dosages if the green seeds mentioned above were used).

There are vast differences in alkaloids depending on source of material and also on time of harvest. [See elsewhere here for a few examples.]

Extracting and using pure alkaloids has the advantage of enabling one to always being able to take a known dose. This is something which is not always possible when dealing with either commercial or wild plant material.

It cannot be stressed enough that just because a particular plant species has been reported in the literature to yield a given percentage, this does not mean that a given sample of the same species will contain an identical concentration or even the identical alkaloids! Either or both of these points are true for virtually any plant and plant alkaloid.

Contrary to popular belief, by themselves, MAO inhibitors like harmine are not hallucinogenic [5], Ott best described them when he said that they produced a "Valium like sedation." [6] This effect persists for a couple hours after the tryptamines wear off [7].

Notes #
  1. Ott 1994 also evaluated 63 mg of harmine hydrochloride (54 mg base: 0.67 mg/ kg for him), 70 mg of the hydrochloride and 94 mg of harmine hydrochloride (80 mg base: 1.0 mg per kg. for him). These dosages enabled him to sense or feel the DMT somewhat but all were clearly below the entheogenic threshold he had crossed with 4 grams of P. harmala seeds.
  2. Ott 1994 describes experiments where 150 mg of harmaline hydrochloride (130 mg of the base or 2.0 mg/kg) was sufficient to orally activate DMT but 50 mg of the HCl (43 mg of the base or 0.66 mg/ kg) was not.
  3. It should be mentioned that Gracie & Zarkov reported persistent and pronounced unpleasant side-effects when using Passiflora incarnata extract as an oral activator, which they did not experience from Banisteriopsis or Peganum. Whether this is due to the aforementioned β-carbolines in Passiflora or to other extracted components was never determined. As a general statement, Harman is usually by far the major alkaloid in the Passiflora species. Harmine and harmaline, when present, are most often present only in relatively small amounts.
  4. This substance, p-chloro-N-(2-morpholinoethyl)benzamide is marketed by Roche under the brand name Aurorix. 75-150 mg is the dosage range reported to have been successfully evaluated in humans as a potentiator for 2C-B and/or MDMA or as on oral activator for DMT. The low end is suggested as it is every bit as effective for this purpose.] We would suggest using some caution if combining this compound with phenethylamines. [In contrast to the harmala alkaloids David Aardvark reported that the synthetic MAOI moclobemide produces no sedation.
  5. Harmaline MAY BE hallucinogenic if given intravenously. This is a poorly explored area. Anecdotal accounts indicate psychoactivity but whether it is a true hallucinogen remains to be clarified. Pennes & Hoch 1957 reported that even a 960 mg dose of harmine was not hallucinogenic.
  6. Gracie & Zarkov had similar results reporting calmness and "at best" hypnogogic imagery. While regarding 50 milligrams of smoked P. harmala alkaloid as the minimum necessary amount to enable full effects without overt somatic symptoms, they also considered 5 grams of P. harmala seeds to be a threshold oral dosage. While it shows no interaction with foods in general, and has "mininal potential for interaction with tyramine", the manufacturer recommends that people with high blood pressure avoid excessive consumption of tyramine rich foods.
  7. Closed eye imagery does exist as does an enhancement of mental perception, but no one with experience with hallucinogens would consider them hallucinogenic in the true sense of the words anymore than they would consider them, or DMT, `narcotics' in any truly meaningful sense of the word although as meditation enhancement aids they are quite useful. While it is true that these alkaloids will augment closed eye imagery, in my mind, this is not a good indicator of a true hallucinogen. Good sex will also substantially enhance closed eye imagery yet it is not generally thought of as a hallucinogenic, or even hallucinatory, experience.

    The word `narcotic' is also often applied to these substances in the literature but this most unfortunate choice of words has largely been perpetuated by an author who uses it in a very broad and classical sense which unfortunately is not understood by many of those who encounter it in today's pharmacophobic context and directly leads to a gross misrepresentation of their action and effects, especially to the uninitiated.

    Curiously, this same author never describes chicha or alcohol as narcotics although they clearly fall even more squarely within his definition of the word.

    In our society, `narcotic' is a word which has extremely pejorative connotations that these alkaloids clearly do not deserve. No one who has a clue what true narcotics feel like would refer to these substances as narcotics.

    They are blessed substances as they enable to the effects of DMT to be felt, it's onset mellowed and effects prolonged, via oral ingestion. Whether it takes you through heaven or hell, DMT is one of the true wonders of the world.