Intro: On earth there are hundreds of thousands of species of plants feeding on the light of the sun. Of these only a few thousand yield food and medicine, only a mere hundred or so contain the compounds that transport the mind to distant realms of ethereal wonder.
A hallucinogen is any chemical substance that distorts the senses and produces hallucinations – perceptions and experiences that depart dramatically from ordinary reality.
The pharmacological activity arises from a small number of chemical compounds. Modern chemistry has, in many cases, been able to duplicate these substances, and to manipulate their chemical structures to produce novel synthetic compounds, nearly all such drugs have their origin in plants.
In the plant kingdom they occur most often in the flowering plants (angiosperms) and the more primitive spore-bearing fungi.
1. Psychoactive drugs affect the central nervous system in various ways by influencing the release of neurotransmitters (chemical messengers within the nervous system, such as acetylcholine, serotonin, dopamine, norepinephrine), or mimicking their actions.
2. Psychoactive drugs are classified as stimulants, hallucinogens, or depressants based on their effects.
a. excite and enhance mental alertness and physical activity
b. reduce fatigue
c. suppress hunger
d. cocaine, caffeine, ephedrine are well-known, plant-derived stimulants
a. produce changes (distortions) in perception , thought, and mood that depart from ordinary reality.
b. often induces a dreamlike state
c. peyote, marijuana (Cannabis), and LSD are examples of hallucinogens
a. dull mental awareness
b. reduce physical performance
c. induce sleep or trance-like state
d. opium and its derivatives, morphine and heroin are classic examples of depressants
6. Narcotic is a drug that induces central nervous system depression, resulting in numbness, lethargy, and sleep. This would include opiates, alcoholic beverages, and kava. In familiar use, narcotic is inferred to include psychoactive compounds that are dangerously addictive. By this definition, nicotine and the stimulant cocaine would also be included as a narcotic.
Chemistry and pharmacology of Psychoactive Drugs
a. The most notable exception is the active compound of marijuana, delta-trans-tetrahydroicannabinol, or THC).
b. Alkaloids are a category of compounds that are considered secondary compounds, or secondary plant products.
c. Secondary because they are not directly related to the plant’s survival.
i. They were formerly believed to be simple wae products of plant metabolism.
ii. They are now believed to provide an important function to the plant.
iii. Some discourage herbivory, others inhibit bacterial or fungal pathogens.
d. Alkaloids share several characteristics:
1. they contain nitrogen.
2. they have a bitter taste.
3. they are usually alkaline (basic)
4. they affect the physiology of animals in several ways but their most pronounced actions are those on the nervous system.
e. Common alkaloids include caffeine, nicotine, cocaine, morphine, quinine, ephedrine (alkaloids mostly end in -ine).
Psychoactive compounds are found primarily in angiosperms and fungi. Angiosperm families especially known for having plants with psychoactive properties include: Solanaceae (nightshade),
Until recently, psychoactive compounds were unknown in the animal kingdom, but now have been discovered in toads. Hallucinogens are known to occur in all parts of the plant, from the roots, leaves, bark, stem, and seeds.
The drugs obtained from plants may be applied in various ways:
a. through the use of powders and snuffs (nasal membranes)
b. to external applications,
c. they may be taken orally (swallowed fresh or drunk in decoctions and infusions) or anally (as enemas), or via vaginal tissue.
According to Richard
Evans Schultes, of
Abbreviated list of plant with known psychoactive properties
1. Atropa belladonna (belladonna), Solanaceae, hallucinogen
2. Cannabis sativa (marijuana), Cannabaceae, hallucinogen
3. Datura spp. (jimsonweed), Solanaceae, hallucinogen
4. Erythroxylon coca (coca), Erythroxylaceae, stimulant
5. Lophophora williamsii (peyote), Cactaceae, hallucinogen
6. Mandragora officinarum (mandrake), Solanaceae, hallucinogen
7. Nicotiana spp. (tobacco), Solanaceae, stimulant/depressant
8. Papaver somniferum (Opium poppy), Papaveraceae, depressant
9. Piper methysticum (kava), Piperaceae, depressant
10. Banisteriopsis sp. (ayahuasca), Malphiginaceae, hallucinogen
Opium poppy (Papaver somniferum) Papaveraceae
1. The poppy, from which opium is derived, is not known from the wild; it has been domesticated for its seeds, which are used for oil and food, and for its dried sap, which produces opium.
2. For centuries, poppies have been bred for increased size of its capsules, wherein the nutritious seeds and opium-rich sap reside. The tender lvs have also been used as an herb.
3. Use of the opium poppy as an analgesic (pain relief) was well-known by early societies.
a. Babylonian, Egyptian, and Greek writings, artifacts, and statuaries attest to the fact that opium was revered for it s analgesic and sleep-inducing properties.
b. the Ebers Papyrus, the Egyptian compendium of medical information from 1500 BCE (3,500 ys ago) mentions opium poppy as a remedy for head pains and as a sedative.
c. Hippocrates, Dioscorides, and Galen leading contributors to Western science, all endorsed the medical use of opium.
d. The statue of Asclepias depicts him holding a bunch of opium capsules in his hand; opium poppies are on the backs of many ancient coins, both Roman and Jewish; Isis (Egyptian goddess of fertility) is sometimes depicted holding poppy heads; Demeter drank opium to relieve her sorrows.
1. Lg annual herb in the Poppy family. Papaver somniferum [somniferous - inducing sleep; soporific; Somnus - Roman god of sleep, analagous to the Greek god, Hypnos].
3. Stem topped with showy, solitary flower of white, pink, red, or purple petals. Often crepe paper-like.
4. Buds are pendulous until they are ready to open (anthesis). As buds open, stems straighten and become erect.
5. Petals are deciduous; they drop early and easily.
6. After pollination the ovary matures into a capsule.
7. Once the petals have fallen, opium is harvested from the whitish-green capsule
horizontal slits are made in the capsule,
usually with a multi-bladed knife. (Professional harvesters in
b. this is done about 2 weeks after petal drop. That’s when the morphine content reaches its maximum concentration.
c. care is taken not to cut thru the capsule entirely, for otherwise the sap will collect inside the capsule and the seeds cannot be harvested (they are spoiled).
d. short incisions can be made every few days, on opposite sides of the capsule, until the capsule on longer exudes latex.
7. The alkaloid, morphine, is produced in the laticifers (latex-secreting structure) in the walls of the seed capsules (pericarp). Laticifers produce latex, which is the “milk” of milkweeds, euphorbias (spurge), dogbane, and poppies.
8. Latex is generally creamy, white, and thick. (Latex comes from the Latin, ‘lac’ for milk). In Hevea tree, from which commercial rubber is extracted, the most important laticifers are in the bark; these are the ones tapped for rubber.
9. Harvesters judge maturity of capsules by their compactness and color. They change from green to whitish-green.
10. The latex is secreted onto the surface of the capsule, after slitting, and dries to a brownish color, and usually harvested the next day before 8 am (sunlight may transform morphine into codeine), with a curved scraper.
11. Crude opium is kneaded into balls, dried to reduce water content form 30%-10%.
12. It can then be smoked or refined further.
How is opium used?
1. Opium has been eaten, drunk, smoked for centuries.
2. In more contemporary times, opium smoking was rediscovered by the Chinese, with the encouragement of the British, who were trying to build up a trade surplus. Opium is smoked in a special pipe that facilitates vaporization of the tarry goo without actually burning it.
3. Opium may be eaten, and the effects are more diffuse.
4. A common method of preparing opium was to dissolve it in alcohol, and this tincture (infusion, extraction, solution), later known as laudanum, became a popular medication for centuries. (medications at that time were not so much administered to heal as they were to simply alleviate pain).
5. Laudanum use reached its peak in the 19th century when it was consumed not only as a medicine but also as a mind-expanding drug by many, including writers, artists, intellectuals of the day: British poets Elizabeth Barrett Browning, Samuel Coleridge, and John Keats were users, Thomas de Quincey (Confessions of an English Opium-Eater), the French poet Baudelaire and composer Berlioz, and the American writer, Edgar Allan Poe.
6. Paregoric was laudanum mixed with some other ingredients, including anise, and was given to children for the treatment of diarrhea.
Associated Press article,
Ancient ceramic pots, most of them
nearly identical in size and shape, found in tombs and settlements throughout
The Mycenaean ceramics were analyzed by gas chromatography and turned up traces of opium. Based on ancient Egyptian medical writings from the third millenium BCE, researchers believe opium and hashish, a smokable drug that comes from the concentrated resin of hemp flowers, were used during surgery and to treat aches and pains and other ailments. Hashish was also used to ease menstrual cramps and was even offered to women during childbirth.
Based on Egyptian writings, archaeologists believe opium was eaten rather than smoked.
Alkaloids - More than 30 alkaloids have been identified in opium, including morphine, codeine, thebaine, papaverine, etc.
1. Morphine was first isolated in 1806 by Frederic Serturner, a german scientist who named the compound after Morpheus, the Greek god of dreams. (It was the first active principle or alkaloid isolated from a plant).
a. It is a very powerful hypnotic and narcotic, with powerful analgesic properties. It is the most abundant component of opium, ranging from 4-21% by weight. Morphine is still unsurpassed in its ability to deaden pain. It is considered the most powerful naturally-occurring analgesic).
b. Originally, it was taken orally, but its full potential wasn’t realized until after the development of the hypodermic syringe in the middle of the 19th century. (Taken orally, morphine is rapidly inactivated and excreted).
c. Morphine depresses the areas of the brain involved in the perception of pain, and reduces the anxiety that accompanies pain.
d. It is a general CNS (central nervous system) depressant and, in overdose, can lead to death by completely suppressing the respiratory center in the brain.
e. Like opium, morphine is highly addictive. This became evident when thousands of injured Civil War soldiers became dependent on the extract after injections of morphine. The addiction became known as Soldier’s Disease.
f. Besides outright control of pain, morphine was frequently prescribed for:
1. diarrhea - it slows peristalsis in the digestive tract.
2. coughing - suppresses the cough reflex in CNS (antitussive)
3. severe burns and visceral pain during post-operative period.
4. used for radiation sickness, allegedly stockpiled for that contingency during the Cold War.
a. 2-3% in opium
b. an analgesic antitussive (suppresses cough reflex), and used in cough syrup.
c. oral analgesic, but only 1/5 as potent as morphine. However, it works well in combination with non-opiate analgesics, such as aspirin.
d. almost all the legal morphine harvested from poppies is converted to codeine.
The study of opium led to the discovery of the first alkaloid, morphine. And the study of morphine has led to the discovery of the brain’s own painkillers, the endorphins, perhaps the most important advance in neurochemistry of the past half century.
Endorphins (endogenous morphines)
1. protein substances formed within the body that relieves pain.
2. similar chemical structure to morphine
3. endorphins are present at the same sites in the brain as morphine (opiate receptors).
4. in addition to analgesic effect, endorphins are thought to be involved in controlling the body’s response to stress, regulating contractions of the intestinal wall, and determining mood.
Heroin (diacetyl morphine)
1. In 1898, the Bayer Co. introduced heroin, which they believed to be a non-addictive opiate with analgesic properties superior to morphine, and cough suppressant properties superior to codeine.
2. The semi-synthetic derivative of morphine was widely dispensed in many over-the-counter medicines for about 2 decades, especially in cough syrups.
3. Heroin was also sold as a cure for morphine addiction .. and it was successful inasmuch as it substituted one addiction for another: heroin is 6 x more addictive than morphine.
4. The number of artists who have used and succumbed to the dangers of heroin are legion (staggering): Jimi Hendrix, Janis Joplin, John Coltrane, Charlie Parker, William Burroughs (Naked Lunch), John Lennon wrote Cold Turkey (refers to goose bumps prominent in a person going thru withdrawal symptoms), Leonard Cohen wrote Dress Rehearsal Rag. In the Wizard of Oz, was it merely coincidental that Dorothy goes to sleep in a field of poppies?
Heroin is no longer used medicinally in the
a. it is, however, used medicinally in other countries to control severe pain
Most illegal opium comes from
Addiction and tolerance to narcotic analgesics, such as morphine, heroin, etc. are thought to be due to suppression of the body’s production of endorphins; withdrawal symptoms are due to the lack of these natural analgesics.
Acupuncture is thought to produce analgesia partly by stimulating the release of endorphins.
Kava (Piper methysticum; Piperaceae)
1. Small shrub in same genus as black pepper.
2. Kava roots (rhizomes) are used to prepare an intoxicating beverage that has been consumed for thousands of years by peoples throughout the islands of the South Pacific.
3. Beverage is a depressant; a small quantity makes people relaxed and friendly and, unlike alcohol, it doesn’t impair alertness. It is, however, a powerful soporific and in large doses can induce deep sleep.
The principal social use of kava throughout the
5. Preparations of kava beverage
a. Traditional - young, unmarried maidens would chew small pieces of the root until the fibers were completely broken down, and then would spit the remaining wad into a ceremonial bowl. After several wads were accumulated, water was added to the bowl, and the mixture stirred. When the desired potency was reached, the pulp was strained and the beverage consumed from a coconut shell.
b. Today - root is finely ground, mixed with water; mixture is coarsely strained. Kava powder is also available that requires no straining.
Components of kava
1. Plants must be allowed to grow for 2-3 years before roots can be harvested. (time is needed both to increase size of root system, and potency of roots). Best roots are those left in the ground for 20 yrs or so.
2. Active ingredients are kava lactones (ester - formed from the reaction between an acid and an alcohol, usually with the elimination of water). Kavain has a modest analgesic effect, about twice that of aspirin, and acts as a mild anaesthetic and tranquilizer.
3. There are a number of different kava clones with differing proportions of the major kava lactones; each produces a slightly different psychoactive effect: a Samoan clone, called “fellowship and brotherhood” makes one feel very friendly. Another, called “white pigeon” imparts a sense of heightened perception, as tho one were flying over the rainforest like a white pigeon.
4. The beverage is ideally served when vexatious matters such as land disputes are to be discussed, or at times of apprehension, as when strangers appear. Both the ceremony and the beverage seem designed to increase friendly feelings and reduce the possibility of hostility.
Kava ceremonies rival the Japanese tea
ceremonies for intricacy of action and sophistication of rhetoric. In
6. Medicinal use
a. used as a tranquilizing elixir that produces relaxation and sleep. Used today as such - health food stores.
b. leaves, stem , and bark have been uses as muscle relaxant to relieve stiffness and muscle fatigue.
Ayahuasca, Vine of the Soul: Banisteriopsis caapi
The Quechua Indians of
A vine native to the Amazon region of
3. By boiling its stem in water, traditional peoples of the Amazon prepare a hallucinogenic beverage used for divination and telepathy. The decoction is bitter, and only a small amount is consumed.
4. Many of the alkaloids responsible for hallucinogenic activity share structural similarities with serotonin, a powerful chemical messenger found in the brain. Serotonin plays an important role in mediating mood and emotion.
5. The carefully controlled use of ayahuasca is embedded in the native religions, but its use outside of its traditional context can be dangerous. Ayahuasca has become a recreational drug in some Amazonian towns: some tourists are attracted by the possibility of a shamanistic experience, while some local people use it to divine the future or to manage their personal lives. There is considerable reason to believe that the use of hallucinogenic plants outside of their traditional religious contexts can produce sorrow rather than transcendence, confusion rather than enlightenment.
1. The Waiki shaman puts a small amount of ebena powder into a reedlike snuff tube and inserts one end of it into in his nostril. His assistant blows a strong blast on the other end of the 1-meter long tube, propelling the bioactive powder into the shaman’s nasopharyngeal airway, where it is absorbed into the bloodstream across the mucous membranes of the respiratory tract.
2. Within 60 seconds, the powerful alkaloids in the powder are distributed throughout the circulatory system by way of the bloodstream.
3. At once the shaman begins to scratch the top of his head with a circular motion and saliva pours uncontrollably from his mouth. Within a few minutes the shaman’s spirit leaves his body and enters the other world, a world controlled by the spirits who act as friend or foe.
a. Ebena snuff is a composite of 3 plants, each of which contributes compounds that enhance the bioactive power of the others.
How do traditional peoples discover that certain plants produce useful pharmacological benefits? How do they discover a means of extracting bioactive fractions that are useful as well as safe?
a. Indigenous people’s science, like our own, proceeds thru a process of trial and error during which it encounters both success and errors, then builds on these successes and failures in an iterative pattern of observation upon observation.
b. Traditional peoples may also employ classification systems for psychoactive plants on the basis of colors or types of visions they produce. One plant may induce red visions, another will include people in the visions; still another will make one fierce and strong.
c. Indians in the Northwest Amazon Valley of Colombia recognize some 14 forms of the stimulant plant Paullinia yoco (Sapindaceae).
Datura spp (Jimson weed) Solanaceae. Nightshsade family
1. Cosmopolitan distribution, used by many indigenous peoples for both medicinal and hallucinogenic purposes..
2. Generic name is based on a Sanskrit word dhatura, meaning poison, reflecting its toxic properties.
3. Datura stramonium is cultivated for its scopolamine content, used today for motion sickness and its sedative effects.
Common name, jimsonweed or
5. Local plant is Datura wrightii. It’s a sprawling perennial with an enormous taproot, that may extend 2’ into the ground.
6. The whole of the plant contains tropane alkaloids: atropine, hyoscyamine, scopolamine
a. they affect the central nervous system
b. they relax smooth muscles
c. dilate the pupils of the eye (atropine: once considered to be a beautiful and mysterious look in Italian women – belladonna means “beautiful lady”, so named because sap from the closely related belladonna plant, Atropa belladonna, was used as eyedrops to dilate pupils.)
c. dilate blood vessels
d. increase heart rate and body temperature
e. induce sleep and lessen pain
f. stimulates and then depresses central nervous system
g. induce hallucinations
h. as a group tropane alkaloids are extremely toxic, capable of inducing coma and death due to respiratory arrest.
i. they can be absorbed thru the skin and mucous membranes (they are fat soluble).
Salves and ointments were applied to various parts of the body.
Witches putatively rubbed their bodies with the hallucinogenic ointments of belladonna, mandrake, and datura.
Much of the behavior associated with witches is as readily attributable to these drugs as to any spiritual communion with demons.
A particularly convenient method of self-administering the drug is thru the moist tissues of the vagina – the witches’ broomstick being the effective applicator.
The common image of a haggard woman on a broomstick comes from the belief that the witches rode their staffs each to the sabbat (orgiastic assembly of demons and sorcerers). It now appears that their journey was not thru space but across the hallucinatory landscape of their own minds.
Probably the best know use of datura among the North American Indian tribes (Algonquin) was the puberty ceremonial dances involving the drinking of a “toloache” (datura) infusion by young boys preparing to enter manhood.
Adolescents were confined to a longhouse for up to 2 weeks sand fed a beverage based in part on datura. During the extended intoxication, and subsequent amnesia (a pharmacological feature of the drug) the young boy forgot what it was to be a child so that he might learn with it meant to be a man.
Ololiuqui (pronounced o-low-lee-oo-key)
Peyote (Lophophora williamsii) Cactaceae
the most famous
2. It is unknown when peyote was first used, but 16th century reports by European explorers describe its use by Aztecs as a divinatory plant.
3. These accounts refer to peyote as the "diabolic root", because the Spanish observed the Aztecs using the plant ritualistically.
a. The Spanish tried to ban the use of peyote by native Indians.
the collapse of the Aztec empire the use of peyote survived among a few Mexican
Indian tribes such as the Huichol and the Tarahumara. In the
5. Indians harvested the plant by cutting off the top of the spineless cactus and leaving the sturdy taproot for regeneration.
6. The stem tips, called buttons, were either eaten fresh or dried for later consumption.
a. Dried, the buttons can keep indefinitely, without losing hallucinogenic properties because the active ingredient isn't volatile.
b. Buttons require a period of softening, either in the mouth or by soaking water, before they can be swallowed.
7. The initial experience of peyote after swallowing is nausea, which gives way to kaleidoscopic visions and hallucinations after a few hours.
8. During this period, which last from 5-12 hours, the faithful report hearing the voices of their ancestors, who help them diagnose and cure their problems.
1. Peyote consists of 30-40 different alkaloids, with mescaline the most active hallucinogen in the group.
is no evidence that either peyote of pure mescaline is addicting, but both the
plant and the compound are illegal to possess or sell in the
2. However, one religious sect, the Native American Church, uses peyote as an integral part of its services.
a. Origins of Native American church goes back to the 1870s, when the Kiowa and Comanche Indians learned of peyote from the tribes of northern Mexico, and brought the plant back with them to Oklahoma (then Indian Territory).
b. The latter half of the 19th century was a time of turmoil and humiliation for the American Indian tribes.
1. Their pristine hunting lands were gradually being taken away from them.
2. They were swindled by Federal authorities.
3. They were forced to move to reservations far from their homes.
4. They were forced to attend schools that denied their heritage.
5. They were corrupted by the white man's alcohol.
6. And they had Christianity forced upon them by missionaries.
c. Quanah parker, son of a Comanche war chief, fashioned a series of ceremonies, with cultural elements from Comanche, Kiowa, Apache, and parts of Christianity, and thereby sowed the seeds of a peyote religion that he hoped would bring dignity, the hope for survival, and spiritual sustenance to the native peoples.
cult grew very rapidly, especially in the southwest, and they formally
incorporated themselves into the
church was initially granted the right to use peyote as a sacramental plant by
the Supreme Court, but later, in 1990, restricted that right by upholding