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PROFILES OF PSYCHEDELIC DRUGS
[Text from a January 1977 journal article by Alexander T. Shulgin]
With this issue we are introducing a new column which will present thumbnail
sketches of the known psychedelic drugs. Rather than an attempt to review the
existing literature on each drug (some would have hundreds of references and
some perhaps two), the facts that are known concerning history, human
pharmacology and human psychopharmacology will be amalgamated into a
"profile." The drugs to be presented will be chosen randomly, rather than with
preference given to popularity, unusual potency, or current availability.
Botanical mixtures will not be considered as such, but as their known active
compnents. As there are upwards of a hundred psychedelic drugs currently
known, it is expected that these "profiles" will eventually form an extensive
reference atlas of compactly prsented drug information.
1. DMT
Description and properties:
DMT, N,N-diemethyltryptamine, Nigerine, desoxybufotenine,
3-(2-dimethylaminoethyl)-indole is a white, pungent-smelling, crystalline
solid with a melting point of 49-50 degrees Celsius, hydrochloride salt
hygroscopic, picrate m.p. 171-172 degrees Celsius and methiodide m.p. 215-216
degrees Celsius. It is insoluble in water, but soluble in organic solvents and
aqueous acids.
History:
DMT was first synthesized in 1931, and demonstrated to be hallucinogenic in
1956. It has been shown to be present in many plant genera (Acacia,
Anandenanthera, Mimosa, Piptadenia, Virola) and is a major component of
several hallucinogenic snuffs (cohoba, parica, yopo). It is also present in
the intoxicating beverage "ayahuasca" made from Banisteriopsis caapi, and it
may have oral effectiveness due to the presence of several naturally occuring
inhibitors of catabolic deamination.
Human Biochemistry and Pharmacology:
Both the parent compound tryptamine and the N-methyltransferase system which
is capable of converting it to DMT, occur in humans, but there is as yet no
evidence that DMT is formed "in vivo". DMT has nonetheless been identified in
trace amounts in the blood and urine of both normals and of schizophrenic
patients, but its origins and functions are unknown. Following intramuscular
administration, maximum blood levels of about 100 ng/ml are observed in 10
minutes, coincident with the maximum changes in electroencephalographic
responses. The plasma clearance t-1/2 [half-life] is about 15 minutes.
Elevated blood levels of indoleacetic acid (IAA) are seen during the time of
peak effects, implying its role as a metabolite. Urine levels of IAA are also
elevated and account for about 30% of the administered drug. An increase in
5-hydroxy-IAA excretion suggests the involvement of serotonin in DMT action.
Unchanged DMT is not excreted.
Human Psychopharmacology:
DMT is inactive orally at dosages of over 1000mg. With intramuscular
injection, there is an abrupt threshold of activity shown with 30mg, and a
complete psychedelic experience results from the administration of 50-70mg
(75mg subcutaneously, 30mg by inhalation). An unusual feature of the induced
intoxication is the speed of onset and short duration. Within 5 minutes of
administration there is mydriasis [dilated pupils], tachycardia [rapid heart
beat], a measurable increase in blood pressure, and related vegetative
disturbances which usually persist througout the drug experience. In 10-15
minutes, the full intoxication is realized, generally characterized by
hallucinations with the eyes either open or closed, and extensive movement
within the visual field. There is difficulty in the expression of one's
thoughts, and in concentration on a given subject. There is usually a mood
change to the euphoric with unmotivated laughter, but instances have been
reported in which paranoid ideation has promoted anxieties and feelings of
forboding into a state of panic. The subject is largely symptom-free at 60
minutes, although some residual effects have been seen in the second hour.
With the inhalation route of administration the time scale is contracted, with
onset of effects noted in 10 seconds, a short period of full intoxication at
2-3 minute, and a complete freedom from any residual effects within 10
minutes. At higher drug levels, there are increased vegetative symptoms, and
these effectively overwhelm the psychedelic experience at dosages of 150mg
i.m. Interactions with other drugs are rarely seen; a sensitivity has been
observed with pretreatment with methlysergide, but there is no cross-tolerance
with LSD. Repeated usage does not appear to lead to either physical or
psychological dependency.
Legal Status:
DMT is explicitly named as a Schedule I drug in the Federal Controlled
Substances Act; registry number 7435.
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DMT
[Excerpt from a pharmacology textbook published in 1988]
Chemical structure and source:
This is the prototype member of the tryptamine subclass of indole
derivatives. The structural formula is:
/\ (CH2)2-N(CH3)2
// \ ____/
| || ||
| || ||
\\ /\ /
\/ \N/
H
N,N-dimethyltryptamine
The drug is a constituent of many of the same South American snuffs and drinks
that contain other psychedelic indole deriviatives, it is often found in the
same plants as 5-MeO-DMT, and Indians add a substance containing it to drinks
containing harmala alkaloids. DMT is the major constituent of the bark of
Virola calophylla, mentioned above; it is also found in the seeds of
Anadenanthera peregina; in the seeds of the vine Mimosa hostilis, used in
easter Brazil to make a drink called "ajuca" or "jurema"; in the leaves of
Banisteriopsis rusbyana, which are added to the harmaline drinks derived from
other plants of the Banisteriopsis genus to make "oco-yage"; and in the leaves
of Psychotria viridis, also added to the Banisteriopsis drinks. Like
5-MeO-DMT, DMT must be combined with monoamine oxydase inhibitors to become
active orally.
Dose:
First strong effects are felt at about 50mg, whether it is smoked or
injected. Tolerance develops only after extremely frequent use - injections
every two hours for three weeks in rats; at that dose frequency, but not
otherwise, there is also a cross-tolerance between DMT and LSD (Rosenberg et.
al. 1964; Kovacic and Domino, 1976).
Physiological effects:
Resembles LSD, but sympathomimetic symptoms like dilated pupils, heightened
blood pressure, and increased pulse rate are more common and more intense.
Psychological Effects:
Like LSD but often more intense. Since it is not taken by mouth, the effects
come on suddenly and can be overwhelming. The term "mind blowing" might have
been invented for this drug. The experience was described by Alan Watts as
like "being fired out of the nozzle of an atomic cannon" (Leary 1968a p.215).
Thoughts and visions crowd in at great speed; a sense of leaving or
transcending time and a feeling that objects have lost all form and dissolved
into a play of vibrations are characteristic. The effect can be like instant
transportation to another universe for a timeless sojourn.
Duration of action:
When DMT is smoked or injected, effects begin in seconds, reach a peak in
five to twenty minutes and end after a half hour or so. This has earned it the
name "businessman's trip." The brevity of the experience make its intensity
bearable, and, for some, desirable.
At least two synthetic drugs in which the methyl group of DMT is replaced by
a higher radical are psychedelic:
/\ (CH2)2-N(C2H5)2 /\ (CH2)2-N(CH2CH2CH2)2
// \ ____/ // \ ____/
| || || | || ||
| || || | || ||
\\ /\ / \\ /\ /
\/ \N/ \/ \N/
H H
N,N-diethyltryptamine N,N-dipropyltryptamine
The drug DET is active at the same dose as DMT and the effects last slightly
longer, about one and a half to two hours. DPT is longer-acting still and has
fewer autonomic side effects. In therapeutic experiments its action continues
for one and a half to two hours at the lowest effective dose, 15 to 30mg, and
for four to six hours at doses in the range of 60 to 150mg. Both DET and DPT
are milder than DMT. The drug 6-FDET (6-fluorodiethyltryptamine) resembles DET
in its effects. All these drugs, like DMT, are inactive orally and must be
smoked or injected. Dibutyltryptamine (DBT) and higher substitutions are
inert, but other synthetic drugs related to DMT may be psychoactive.
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