Drugs Education and Vice Control By: Prof. Nino M. Kabiling
Leader: Jim Kenneth Abregunda Members: Kit Kevin Dizon Albert Noel Gonzales Mark Justin Palo Joey Elbert Baltazar Jon Rudy Reyes
HISTORY of LSD Lysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide and colloquially as acid, is a semisyntheticpsychedelic drug of the ergoline family. LSD is non-addictive and well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synaesthesia, an altered sense of time and spiritual experiences, as well as for its key role in 1960s counterculture. It is used mainly as an entheogen, recreational drug and as an agent in psychedelic therapy. LSD was first synthesized by Albert Hofmann in 1938 from ergotamine, a chemical derived by Arthur Stoll from ergot, a grain fungus that typically grows on rye. The short form "LSD" comes from its early code name LSD-25, which is an abbreviation for the German "Lysergsure-diethylamid" followed by a sequential number. [3][4] LSD is sensitive to oxygen, ultraviolet light, and chlorine, especially insolution, though its potency may last for years if it is stored away from light and moisture at low temperature. In pure form it is a colorless, odorless, and mildly bitter solid. [5] LSD is typically delivered orally, usually on a substrate such as absorbent blotter paper, asugar cube, or gelatin. In its liquid form, it can also be administered by intramuscular or intravenous injection. LSD is very potent, with 2030 g (micrograms) being the threshold dose. [6]
Introduced by Sandoz Laboratories, with trade-name Delysid, as a drug with various psychiatric uses in 1947, LSD quickly became atherapeutic agent that appeared to show great promise. [7] In the 1950s the CIA thought it might be applicable to mind control andchemical warfare; the agency's MKULTRA research program propagated the drug among young servicemen and students. The subsequent recreational use of the drug by youth culture in the Western world during the 1960s led to a political firestorm that resulted in its prohibition. [8] A number of organizationsincluding the Beckley Foundation, MAPS, Heffter Research Institute and the Albert Hofmann Foundationexist to fund, encourage and coordinate research into its medicinal and spiritual uses. Lysergic Acid Diethylamide - : A crystalline solid, C 20 H 25 N 3 O, the diethyl amide of lysergic acid, a powerful psychedelic drug that produces temporary hallucinations and a psychotic state. LSD (lysergic acid) is best known as Acid on the streets. It belongs to a class of drugs known as hallucinogens that distort perceptions of reality. It is odorless, colorless and has a slightly bitter taste. LSD is the most potent mood and perception altering drug known to man. It is a commonly abused drug among teens and young adults as a club drug making its way to parties and raves. The manufacturing, sale and use of LSD is illegal throughout the United States.
STREET NAME back breaker, battery-acid, Elvis, loony toons, Lucy in the sky with diamonds, window pane, acid, superman, Zen, pane, dose, dot -
EFFECTS The effects of LSD are unpredictable. Usually, the first effects of the drug are felt 30 to 90 minutes after taking it. The user may experience extreme changes in mood, feel several different emotions at once, or swing rapidly from one emotion to another. If taken in large enough doses, the drug produces delusions and visual hallucinations. The physical effects include dilated pupils; higher body temperature and sweating; nausea and loss of appetite; increased blood sugar, heart rate and blood pressure; sleeplessness; dry mouth and tremors. The user may also suffer impaired depth and time perception, with distorted perception of the size and shape of objects, movements, color, sound, touch and own body image. Sensations may seem to "cross over," giving the feeling of hearing colors and seeing sounds. These changes can be frightening and can cause panic. Some LSD users also experience severe, terrifying thoughts and feelings, fear of losing control, fear of insanity and death. An experience with LSD is referred to as a "trip" and acute adverse reactions as a "bad trip". These experiences are long, with the effects of higher doses lasting for 10 to 12 hours.
Symptoms of LSD Withdrawal LSD is no considered to be physically addictive, however this does not mean that users do no develop a dependency. Many are psychologically dependent on LSD, typically experiencing; strong cravings agitation Aggression Paranoia Depression
LSD (lysergic acid) Use addiction, autism, alcoholism, and terminally ill cancer patients. It was also used to study the LSD was initially used as an experimental medication in the treatment of neuroses, narcotic mechanisms of psychotic diseases like schizophrenia. The effects of LSD were too great and the drug was made illegal under the Drug Abuse Control Amendment of 1965. Today is production, sale and use is illegal throughout the United States and is no longer used in medical treatment. HOW IT WORKS LSD happens to be even better at activating serotonin receptors than serotonin itself, so it essentially increases the normal levels of signaling by serotonin (it does this through a variety of mechanisms, not just limited to better binding - it actually releases extra serotonin, changes the lock to accept keys more readily, etc.). In a lot of ways its like turning up the volume on quiet music. Not only are the already audible pieces more audible, but things you previously could not hear are now audible (whispers you might have missed, or background noise might now become audible). Because it increases the signal, it also increases the signal noise (if you turn the volume up on a microphone very high, you sometimes get feedback loops, or that annoying high pitched noise). In addition, if you have the volume extremely high, you may not be able to differentiate between the louder sounds very well. On LSD, this often results in hallucinations - hearing, seeing, touching, tasting, etc. things that are not actually there. In addition, through a relatively unknown mechanism, LSD increases 'cross-talk' between areas of the brain. That is to say, it helps stimulate areas of the brain that don't normally talk to each other, to start talking to each other. Over the long term, it can even help create connections that previously didn't exist - much like putting up extra telephone or internet lines. This increased cross-talk while under the influence of LSD (combined with the increased sensory input) often results in something known as synesthesia, or a mixing of the senses. What this means is that people might experience a sense across multiple senses - they might see sound, taste colors, or feel smells. Since the mechanism of cognition (what causes us to think the way we do) is not known, I cannot explain why it changes a person's mindset, only that it does. People often describe it as 'thinking outside the box'. Having done LSD myself many times, I agree that it shifts the paradigm of thought. It likely is associated with this 'cross-talk' mechanism, at least to some extent, but the increase in serotonin and dopamine likely has an effect as well. Other serotonergic drugs, such as ecstasy (which is very similar to hallucinogens), shift how you think as well because increased serotonin results in a sort of euphoria (happiness). It also seems to increase one's ability to empathize with someone else - that is to say, you more easily relate with someone else's emotional state. This increased empathy also changes how you think about things. It's important to note that no hallucinogens have any proven addictive mechanisms (they are the only recreational drugs that have no addictive qualities). In addition, casual use is not associated with any permanent brain damage. Any use, casual or not, will reduce the relative abundance of serotonin (and other catecholamine receptors, such as dopamine) receptors. However, anecdotal evidence suggests that a single use of a moderate dose can be recovered from within about 1-2 weeks of abstinence.
MANUFACTURING PROCESS Synthesis of Lysergic Acid By reacting N-benzoyl-3-(B-carboxyethyl)-dihydroindole (see JCS, 3158 (1931) for the preparation of this compound) with thionyl chloride, followed by aluminum chloride gives 1-benzoyl-5-keto-1,2,2a,3,4,5-hexahydrobenzindole. This is then brominated to give the 4-bromo-derivative, which is converted to the ketol-ketone by reacting with methylamine acetone ethylene ketol. This is then hydrolized by acid to yield the diketone and treated with sodium methoxide to convert it to the tetracyclic ketone. Acetylate and reduce this ketone with sodium borohydride to get the alcohol, which is converted to the hydrochloride form, as usual. The above hydrochloride is treated with thionyl chloride in liquid sulfur dioxide, to produce an amorphous chloride hydro chloride, which is converted to the nitrile with sodium cyanide in liquid hydrogen cyanide. Methanolysis then gives the ester of the nitrile. Alkaline hydrolysis of this last compound, followed by catalytic dehydrogenation in water using a deactivated Raney Nickle catalyst (see JOC. 13, 455 1948) gives dl-lysergic acid. TOTAL SYNTHESIS OF LYSERGIC ACID This is the easiest way to totally synthesize lysergic acid. There are other ways, but after reviewing other methods, I found this to be superior. It is quite complicated and it takes good modern equipment. JACS, 78, 3087 (1956). 3-Indolepropionic acid, 94.5 g (0.5 mole) is dissolved in 600 ml of water containing 20 g of NaOH. The solution is mixed with 100 g of Raney Nickle catalyst and hydrogenated at room temp in a steel bomb at about 3,500 psi until the uptake of hydrogen stops (about 20-30 hours). Filter off the catalyst and wash it with a little water to remove the product that is clinging to it. Add 85 ml of concd HCl acid to the filtrate, and cool. If your reduction is incomplete, you will now have unreacted starting material separate, and this must be removed by filtration. Benzoylate the filtrate (the Schotten and Baumann method is preferable), using 210 ml of 12 N NaOH 180 ml of benzoyl chloride. Keep the solution alkaline throughout the benzoylation, and keep the temp below 40C by cooling. When the benzoyl chloride is fully reacted, the reaction mixture is cooled and acidified with 300 ml of HCl acid. Filter the crude product by filtration, wash with water, and extract with four 1 liter portions of hot water. Separate, and crystallize the resulting syrupy product from a few volumes of methanol. Filter and wash with a little cold methanol to get a little over 100 g that melts at 151-153. This is l-Benzoyl-3-beta-carboxyethyl-2,3-dihydroindole. This can be purchased to eliminate this step. 1-Benzoyl-5-keto-1,2,2a,3,4,5,-hexahydrobenzindole. 118 g of the above product (1-benzoyl-3-B-carboxyethyl-2,3-dihydroindole) is mixed with 200 ml of pure thionyl chloride. This solution is allowed to stand for 30 min, then it is warmed gently for 15-21 min on a steam bath. Excess thionyl chloride is completely evaporated with the temp maintained between 22-26C in vacuo. The crude acid chloride is dissolved in dry carbon disulfate. This solution is added, in a thin stream, to a well stirred suspension of 240 g of aluminum chloride in 1750 ml of carbon disulfate in a 5,000 cc flask. Note: this must be done under a fume hood. A complex will separate and bog down the stirring device. Heat this mixture under reflux with stirring for 1 hour. Decompose this mixture by adding 500 g of ice, 250 ml of concd HCl acid, and 500 ml of water, all while good stirring is continued. Cooling of this operation is affected by periodic distillation of the carbon disulfate in vacuo. After the decomposition is complete, any remaining carbon disulfate is removed completely in vacuo, and the product is extracted with 2 liters of benzene. The extract is washed well with 500 ml of 2 N NaOH in three portions, and then with water. Dry (with the usual magnesium sulfate), and evaporate to a small volume in vacuo. Add this small volume to several portions of ether to get the ketone to crystallize (add slowly), and filter, then wash with ether to get 85 g of pure title product, mp: 146-147C. 1-Benzoyl-4-bromo-5-keto-1,2,2a,3,4,5-hexahydrobenzindole. A solution of the above indole (305 g) in 2,200 ml of glacial acetic acid is warmed to 40C. While the reaction is illuminated with a 250 watt bulb, 352 g of pyridine hydrobromide perbromide is added in portions, over 5 min with shaking. The solution is then heated to 60 and is held between there and 55C for 30 min. Treat the mixture with carbon, and evaporate to a small volume in vacuo. The residue is taken up with 2,200 ml of chloroform, and wash this solution with several portions of water, dry as above, and concentrate in vacuo. Crystallize the residue from 2,200 ml of 50% acetic acid and 50% ether to get 270 g of title product that melts at 180.5- 181.5C. Another crop can be obtained from concentrating the fltrates. Yield: 30 g of less pure product. 1-Benzoyl-2,2a,3,4-tetrahydro-4-methyl-2-methyl-1,3-dioxolan-2-yl-methyl- aminobenzindol-5-(1H)one. A solution of the last indole product above (270 g) and 307 g of methylaminoacetone ethylene ketol in 4,500 ml of dry benzene is refluxed for 21 hours under a slow stream of nitrogen. The mixture is cooled and 151 g of methylaminoacetone ethylene ketol hydrobromide is filtered off. The filtrate is washed with ice water, then extracted with 2.5 liters of cold dilute HCl acid containing 150 ml of the concd acid. The acid extracts are immediately added to an excess of ice cold dilute NaOH. Extract with 1 1iter of chloroform, dry over magnesium sulfate, treat with carbon and concentrate by evaporation in vacuo. The residual ketol-ketone is crystallized from acetone to yield 220 g, mp: 135-136C. 5-Keto-4-N-methyl-N-acetonylamino-1,2,2a,3,4,5-hexahydrobenzindole. 20 g of the above product is dissolved in a mixture of 250 ml of concd HCl acid and 250 ml of water, and the solution is kept under nitrogen for 5 days at 37. Cool the mixture, treat with carbon, filter, and concentrate the filtrate in vacuo to a small volume. Treat the residue with an excess of sodium bicarbonate, extract with cold chloroform, and remove the chloroform by evaporation in vacuo at room temp. The crude diketone is powdered, slurried with 75 ml of benzene-ether, and filtered. Yield: 9.8 g, mp: 105-107C. 9-keto-7-methyl-4,5,5a,6,6a,7,8,9-octahydroindolo-(4,3)isoquinoline. 25 g of the above product is mixed with 550 ml of absolute ethanol. Stir this mixture under nitrogen and cool to -15 with an external freezing mixture. Sodium methoxide is added (17 g) and the mixture is stirred for 10 min at -10 to -12. Cool to -25, and the product is filtered and washed (while still in the funnel) with cold ethanol and ether. Without exposure to air the crude ketone is immediately slurried with a little ice water and filtered. Wash with ice water, ethanol, then ether (all cold) to yield 16 g of product melting at 145-147. 4-Acetyl-9-keto-7-methyl-4,5,5a,6,6a,7,8,9-octahydroindolo-4,3-quinoline. 24 g of the last product is added to 80 ml of cold acetic anhydride. The mixture is held at 25 for about 5 min, then thoroughly cooled, filtered, and the product (a solid) washed with ether to yield 20.5 g, mp: 169-170. A second crop is obtained by concentrating the mother liquor by evaporation. A mixture of the last product (1.0 g) and 10 g of palladium carbon (5%), in 35 ml of xylene, is heated under reflux for 4 hours. The catalyst is filtered and extracted with hot methanol and chloroform. The combined extract filtrates and the initial filtrate are combined and evaporated in vacuo. The residue is recrystallized from water to give 0.6 g of a monohydrate product that melts at 255-256. This product is called 4-acetyl-4,5,5a,6-tetrahydro-9-hydroxy-7-methylindolo-(4,3fg)- quinolinium hydroxide betaine. 4-Acetyl-9-hydroxy-7-methyl-4,5,5a,6,7,8,9,10-octahydroindolo-(4,3fg)-quinoline. 1 g of the above betaine in a mixture of 20 ml of ethanol and 5 ml of water, is treated with 0.08 g of sodium borohydride, and this solution is refluxed for 10 min and kept at 25 for 1 hour after the reflux is finished. The solvent is distilled off, and the residue is taken up in a mixture of chloroform and water. The chloroform solution is separated, dried as above, and then the solvent is distilled off. The residue is recrystallized from a nitromethane-ethyl acetate mixture to yield 0.2 g (21%), mp 193-196. Not only is this a small scale, but it is a poor yield, requiring you to perform it several times to get enough product to perform the next step. When you have more than enough, convert the product into its hydrochloride form by dissolving in dry methanol and precipitating with dry hydrogen chloride. 4-acetyl-9-chloro-7-methyl-4,5,5a,6,6a,7,8,9-octahydroindolo-(4,3fg)-quinoline hydrochloride. 3.1 g of the above product in its hydrochloride form is dissolved in 75 ml of liquid sulfur dioxide contained in a glass lined, high pressure bomb, or autoclave. Thionyl chloride (1.2 ml) is added and the vessel is sealed and kept at 25 for 6 hours. Vent the vessel carefully and remove the mixture. Evaporate the sulfur dioxide while keeping the volume of the solution constant by the slow addition of dry ether. The amorphous chloro hydrochloride is filtered, washed with ether (dry) and dried by evaporating in vacuo to give 3.5 g of product, mp:130-135. 4-Acetyl-9-cyano-7-methyl-4,5,5a,6,6a,7,8,9-octahydroindolo-(4,3fg)-quinoline. 40 g of dry, powdered sodium cyanide, is added to ice cold liquid hydrogen cyanide and stirred gently with ice bath cooling. Speed up the stirring, continue the cooling, and add 7.5 g of the amorphous product directly above. Continue stirring for 30 min, then the hydrogen cyanide is distilled under enough reduced pressure to keep it coming over the condenser at a temp below 10-12. The residue is mixed with chloroform and ice water, and the resulting mixture is filtered. The organic layer of the filtrate is separated and the aqueous layer is extracted with two separate portions of chloroform. The combined extracts (this would include the separated chloroform, as usual) are dried over magnesium sulfate, decolorized, and the solvent removed by distillation in vacuo. Crystallize the product in ethyl acetate. Yield: 3.3 g, mp: 173-174. Recrystallize again for extra purity. 9-Carbomethoxy-7-methyl-4,5,5a,6,6a,7,8,9-octahydroindolo-(4,3fg)-quinoline. 1 g of the last product is mixed with 15 ml of methanol and 0.25 ml of water. With external (ice bath) cooling add 2 ml of concd sulfuric acid slowly. Seal this solution in a high pressure bomb with a glass liner (or in a glass tube taking safety precautions in case of explosion) with a nitrogen atmosphere, and heat at 100 for 23-24 hours. Note: I have seen a big pressure cooker (like gramma cans peas with) work for some of these bomb procedures. I do not recommend it, but here is how to do it right, if you feel you must. Use only the great big heavy duty models, in excellent condition, set the pop off (relief valve) for near maximum position; never, ever tamper or modify this valve to get more pressure. Put the product in a glass beaker, put it in the cooker, flush with nitrogen, heat and stay in a different house during the reaction. Carefully turn off heat, notice or record pressure gauge after time has elapsed. Wait until pressure drops noticeably, bleed off remaining pressure and get product. Treat the mixture with decolorizing carbon and then evaporate in vacuo to 10 ml. Pour onto a mixture of 30 ml of chloroform, ice, and 10 g of sodium bicarbonate. Separate the chloroform layer, and extract the aqueous phase with three 10 ml portions of chloroform. The combined chloroforms are dried, evaporated to dryness in vacuo, and the product is crystallized from benzene to give 1/2 g of product that melts at 159-160. You may purify more by recrystallizing from ethyl acetate. This is not very much product. As with the procedure 4 steps back, you will have to perform this step over and over. If you try to double or triple the amounts given, you may get more product, but you will hurt the yield. dl-Lysergic acid. 3.9 g of the last product is mixed with 78 ml of 1.5% potassium hydroxide solution. Reflux for 30 min under nitrogen. 8.5 g of hydrogen sodium arsonate, and Raney Nickle (16 g wet), that has previously been deactivated by boiling in xylene suspension (see JOC, 455 (1948) to deactivate), is added and the mixture is refluxed and stirred under a nitrogen atmosphere for 20 hours. The solution is treated with carbon, and the crude lysergic acid is precipitated by neutralization to pH 5.6, and then filter it off and wash with water. Yield: 1.04 g. A second crop is obtained in the usual manner (0.15 g). Purify by dissolving in dilute ammonium hydroxide, treat with decolorizing carbon, and reprecipitate with carbon dioxide to get a mp of 242-243. You may be able to get an analytical or laboratory consultant to make one of these products near the final step, thereby eliminating the need to go through all of the steps as described. This will save you much time, but as these people are highly trained, their time will be costly. Lysergic acid can be made from many ergot derivatives by hydrolysis of these compounds. These compounds include ergonovine, ergotamine, ergokryptine, ergosine, methysergide, ergine, and a few others. Total synthesis of these compounds is impractical, as lysergic acid is made before the alkaloid. You could stop the operation as soon as you reach lysergic acid, otherwise you will have to hydrolyze as described below. There are many analogs of these alkaloids that end with the ine suffix. These are not as suspicious as the former because they lead to an inactive iso-LSD. They will look like this: the ergotamine isomer = ergotaminine, the ergonovine isomer = ergonovinine, etc. These analogs are easily converted to the active forms or they may be used exactly as the non-iso versions to give the iso-LSD, which is converted very easily to LSD as also described below.
History of Mescaline In the beginning of the 16 th century, peyote was first forbidden in Europe as the users went through frightening experiences. By the end of the 19 th century, the native tribes in other regions of the United States used this drug. During the year 1922, an estimate of about 13000-22000 people started to use peyote for religious purposes in the United States. In the year 1919, Mescaline, the active element in peyote was originally produced. More than twelve states declared mescaline as illegal by the year 1930. During the 20 th century, a number of researches were carried out on mescaline or peyote. It was found that this drug did not have any valuable medical use. In the year 1967, mescaline was prohibited in the United States and in 1970; it was place on schedule 1.Buttons or the head of the peyote can be soaked in water and then ingested, grounded and chewed. The powder (from the grounded buttons) is sold in the form of gelatin capsules to the users. Peyote is a small, spineless cactus. Mescaline is a hallucinogenic substance found within the Peyote cactus. Mescaline can be taken from the Peyote cactus or created synthetically. Throughout history, Peyote and Mescaline have been used by natives in northern Mexico and the southwestern United States as a part of traditional religious rites.
Mescaline Derived From Mescaline is a hallucinogen obtained from the small, spineless cactus Peyote (Lophophora williamsi). A spineless cactus with small protrusions called buttons that are used for psychoactive hallucinogenic purposes. Mescaline, an amphetamine, is the principal active psychedelic compound in peyote. It is a hallucinogen derived from several different cacti the Peyote cactus that grows in the southwestern United States and Mexico, the San Pedro cactus (Trichocereus pachanoi) found in Peru, or the Peruvian Torch cactus (Trichocereus peruvianus). The limited growing area of this cactus restricts drug supply severely, so it is a common practice to sell other drugs such as PCP or LSD as mescaline. Mescaline can also be produced in a laboratory by chemical synthesis. A white crystalline material, mescaline sulfate, is the pure form of mescaline and can be put in capsule form. Peyote and mescaline are listed as Schedule I hallucinogens under the Controlled Substances Act in the United States. In a rare exception, the nondrug use of peyote in bona fide religious ceremonies of the Native American Church, and by members of the Native American Church is legal.
Who discovered Mescaline?
Dr. Arthur Heffler (1897)
Terminology (street names) Slang Terms for Peyote: Bad seed, britton, hikori, hikuli, half moon, hyatari, P, nubs, seni, tops Slang Terms for Mescaline: Cactus, cactus buttons, cactus joint, mesc, mescal, mese, mezc, moon, topi Use and Users Cactus head peyote user Love trip mescaline and MDMA or MDA
Effects Mescaline produces perceptual, cognitive, and emotional experiences that vary widely among users based on size, setting, expectations, personality, and drug history. The only documented long-term effect of mescaline is a possible prolonged psychotic state similar to that of paranoid schizophrenia. It is suggested that this may only affect those who were previously diagnosed as mentally ill.
Physical Effects
Numbness, tension, anxiety, rapid reflexes, muscle twitches and weakness, impaired motor coordination, dizziness, trembling, dilation of the pupils Increased blood pressure and heart rate Intense nausea and violence Appetite suppression Elevated body temperature and sweating Chills and sweating
Psychological Effects
Vivid mental images and distorted vision Synesthesia: perception of seeing music or hearing colors Altered space and time perception Joy, exhilaration, panic, extreme anxiety, or terror Distorted sense of body (users can feel either weighed down or weightless) Heightened sensory experience (i.e. brighter colors, sharper visual definition, increased hearing acuity, more distinguished taste) Difficulty focusing, maintaining attention, concentrating, and thinking Loss of sense of reality; melding past experiences with present Preoccupation with trivial thoughts, experiences, or objects Highly adverse reactions (bad trip), including frightening hallucinations, confusion, disorientation, paranoia, agitation, depression, panic, and/or terror
SYMTHOMPS These include: Nausea Vomiting Shaking hands and feet Colorful hallucinations that may last for hours Distortions in physical senses A sensation of floating through space Panic attacks Attacks of terror Sweating Dizziness High blood pressure Speeded up heart rate No appetite Exaggerated emotions Rapid mood swings False feelings of power or safety Confusion
Methods of Use Peyote The peyote cactus contains buttons that can be cut from the root and dried. The buttons can either be chewed or soaked in water to produce an ingestible liquid.12 Peyote buttons may also be ground into a powder and then smoked with a leaf material, such as cannabis or tobacco.13
Mescaline Mescaline is administered orally in the form of powder, a tablet, a capsule, or liquid. In its pure liquid form, mescaline can be ingested; however, this method is unpopular. Users typically consume between 300-500 mg (which is approximately the amount contained in 3-6 peyote buttons.) Effects generally appear within 1-2 hours, and gradually disappear 10-12 hours after administration.14
Essential Features The structure of this drug resembles dopamine and norepinephrine, the catecholamine neurotransmitters.
Medical Purposes Mescaline and peyote are used by Mexican natives for their therapeutic benefits. From the 1950s to the 1960s, psychedelic drugs like mescaline and LSD were used for experimental psychiatry. For a time, these drugs were used for the treatment of a variety of diseases, including alcoholism, neurotic disorders, and childhood autism. However, due to increased illicit use, it became difficult to access the drugs and obtain funds for additional professional research. The abusive use of mescaline led to various mescaline addiction treatment options and therapies.
Manufacturing Process SAFETY GOGGLES AND RUBBER GLOVES MUST BE WORN AT ALL TIME WHEN HANDLING CAUSTIC SODA AND HYDROCHLORIC ACID 1. Add 500 ml deionised water to a preserving jar or bottle. Then add 25 g of caustic soda while wearing protective goggles and gloves. Allow enough space for shaking. The caustic soda will need shaking to dissolve, or the bottle base will become very hot. Once dissolved add 50 g powdered San Pedro - a large bore funnel is useful if using a bottle. Shake the bottle - initially the powder will form into a solid lump. Leave the basified cacti for a few days to thin out.
2. Add at least 10% xylene to the volume, recap the jar or bottle and warm to hand hot in a water bath (around 50 C). Remember that xylene fumes are flammable. (Storing xylene in a freezer will reduce the fumes or wear a mask with a charcoal filter.) Loosen and retighten the lid to release any pressure. (If necessary, wrap PTFE plumbing tape around a plastic wine cork to get a tight fit, but ensure that it is held firmly during agitation.) Care is required if using plastic screw cap bottles as they can deform and leak when heated excessively. The bottle must now be shaken vigorously for at least a minute while wearing protective goggles and gloves - the mescaline shuffle! Vigorous agitation will create an emulsion but gives a much greater yield than gentle agitation. Heat will not clear the emulsion but it should resolve gradually by repeatedly freezing and thawing. Once frozen there should be a clear partition between the solid caustic soda solution and the (now green) xylene floating on top, which can be poured in another sealed container. A number of freezing and thawing cycles are required to remove all the xylene - avoid hot water with frozen glass bottles as they may crack. The lid should be tight, although it may need hot water to unfreeze it, as xylene vapour will taint any food in the freezer. If the lid is left loose then secure Clingfilm over the opening with an elastic band or use plumbing tape to prevent fumes. 3. Pour the collected xylene into a rectangular Pyrex dish. Cover the dish with a cloth to keep out dust and insects and leave in a well ventilated area until all the xylene has evaporated (preferably outdoors in a garage or shed). Remember that xylene fumes are flammable. You should be left with waxy deposits with tiny crystals which can be scraped up with a single edged razor blade. The extract can be scraped off the razor with a scalpel into a Rizla paper - keep the scalpel blade in a wine cork when not in use. The process should be repeated at least once. The most active extract is dark in colour, while later extractions will consist of green waxy material.
If hydrochloric acid is available a hydrochloride salt can be produced which makes measurement of dosage more accurate and enables the xylene to be reused. To create pure white crystals hydrogen chloride gas is bubbled through the non-polar solvent. Aqueous extractions will produce a brown powder which although less attractive is perfectly adequate and far less hazardous to produce. Ten drops of 10% HCl solution by volume (v/v) are added to deionised water and shaken in a sealed container with the collected xylene, after warming to hand hot in a water bath. The phases are separated by freezing. Pour the xylene back into the basified cactus container and thaw the aqueous phase - avoid hot water with frozen glass bottles as they may crack. The liquid is then evaporated in a rectangular Pyrex dish on a hotplate outdoors or in a well ventilated area, away from people or animals. The resulting extract can be rinsed in acetone (ideally anhydrous) to remove the sticky green material, making handling easier. Scrape all the extract into one corner of the rectangular Pyrex dish, tilt and add acetone with a pipette (as it is difficult to pour). Mix the extract thoroughly in the acetone, allow to settle, then slowly tip the acetone out of the opposite corner of the dish, removing any residue with a tissue. Repeat if necessary. Dry the dish on a hotplate, then powder the extract by chopping with a single edged razor blade. The (now yellow) xylene should be reused to extract the remaining mescaline from the basified cactus powder.
For health and safety reasons the amount of HCl used should be minimal and safety goggles and rubber gloves must be worn at all times. Mescaline freebase is C11H17NO3, molar mass 211 g/mol. HCl has molar mass 36.5 g/mol. (H=1, C=12, N=14, O=16, Cl=35.5) 50 g of dried San Pedro might contain at most 1% mescaline = 0.5 g. This would be neutralised with a solution of deionised water containing 86.5 mg HCl (36.5/211 x 500 mg). A 10% solution by volume (v/v) of HCl contains 105 g/litre, so this would require 0.824 g of solution (1000/105 x 86.5 mg). A drop weighs around 50 mg so around 16 drops of 10% HCl solution would be required in total. The freebase content of mescaline hydrochloride is 85% (211/247.5).
Magnetic Stirrer Before shaking After shaking After freezing
Hotplate Dried Extract Shavings Extract rinsed in acetone These pictures show a bulk extraction using a gallon demijohn with a magnetic stirrer. The previous demijohn cracked under heat and the caustic soda removed the paint from the top of the hotplate - so this one is not being heated! Use a cork bung in preference to a rubber one which will swell from xylene exposure. It is left on slow stir for several hours which is preferable to shaking as it doesn't create any emulsion. Getting the stir bar centred is quite tricky - it can be held with a strong magnet on the outside and lifted to the top centre of the demijohn and dropped back in. Once it falls into the right position avoid turning the speed up too quickly or you will have to start again! It can take 24 hours to freeze the basified cactus in the demijohn. It's best to pour the xylene off into the bottle first before adding dilute acid, in case the aqueous phase in the demijohn hasn't frozen completely, so you can pour it back and freeze it for a bit longer if necessary. Once the dilute acid in the bottle has frozen, the xylene is poured back into the demijohn for a second extraction. Repeat the process until no more extract is produced. (Almost all of the mescaline should be removed from the xylene in a single extraction if the bottle is warmed and shaken vigorously - wear safety goggles and rubber gloves.) A small quantity of yellow xylene will remain on top of the dilute acid after separation by freezing. The bulk of the dilute acid can be removed with a glass poultry baster and a pipette will separate the last portion (impossible with toluene as it forms an emulsion). The dilute acid is thawed and evaporated on the hotplate outdoors. To remove some of the impurity before extracting with dilute acid, the xylene can be washed with deionised water with a little caustic soda added (to ensure that the mescaline remains in freebase form). Again the phases are separated by freezing. The extract shown above in the Rizla was produced by this method. The shavings shown above were produced without washing the xylene first. Acetone will remove the sticky material but not the dark colour. It can take several xylene extractions to remove all the mescaline from the basified cactus, although the process could be expedited using a 5 litre borosilicate Erlenmeyer flask, which can be heated while slowly being magnetically stirred, to avoid emulsion. 5 mm aluminium sheet should be placed under the flask as its base area considerably exceeds the dimensions of most hotplates. Phase separator paper can be used as an alternative to freezing or using a separatory funnel. The paper is impregnated with silicone which retains the aqueous phase while passing the solvent phase through. Available from Camlab - at a price!
HISTORY of Psilocybin. Magic Mushrooms, Shrooms, Mushies, and Magics are present commercial names for mycelium fungi containing a compound called psilocybin. According to Dr. Paul Kroeger, a leading Canadian mycologist, Magic Mushrooms are of great importance through history for thousands of years, particularly in the area now known as Mexico and in lost civilizations such as the Aztecs and the Mayans. But evidence that these mushrooms have also been used in other parts of the world are known through murals in the Sahara, Algeria, and through folk traditions in Europe. These early people are the pioneering discoverers as well as users of Psilocybin containing mushrooms. These people used mushrooms significantly during religious practice, rituals, and in divinatory or spiritual contexts. To them, magic mushrooms are sacred. Magic mushrooms are known to be Ethenogenic (from the root word meaning God Within) which means that it can induce states of consciousness that have lasting personal meaning and spiritual significance in individuals who are religious or spiritually inclined This effect derived from ingesting psilocybin containing mushrooms means that it can also be easily abused by people who are seeking easy ways of reaching High The introduction of Psilocybin containing mushrooms to the modern world cannot be attributed to one individual only. An American banker and amateur mycologist named R. Gordon Wasson published an article in Life magazine describing his experiences in ingesting magic mushrooms. A French mycologist called Roger Heim, who accompanied Wasson on a follow up expedition, identified the so-called magic mushrooms as members of the Psilocybe species. Shortly afterward, Dr. Heim sent samples of the mushroom to French chemist, Albert Hoffman, who isolated the compound psilocybin from the mushroom Psilocybe mexicana. Hofmans employer sold pure psilocybin to physicians and clinicians worldwide for use in psychedelic therapy. Since the 1990s, there has been a renewal of scientific research into the potential medical and psychological therapeutic benefits of psilocybin for treating conditions including Obsessive- Compulsive Disorder, cluster headaches, and anxiety related to terminal cancer. However, psilocybin containing mushrooms has been outlawed in most countries, and it has been classified as a scheduled drug in the united states.
Psilocybin is a naturally occurring psychedelic compound produced by more than 200 species of mushrooms, collectively known as psilocybin mushrooms.
STREET TERMS FOR PSILOCYBIN Boomers Flower flipping (MDMA used with psilocybin) God's flesh Hippieflip (MDMA used with psilocybin) Hombrecitos Las mujercitas Little smoke Mexican mushrooms Musk Sacred mushroom Silly putty Simple simo
EFFECTS The effects of magic mushrooms vary a great deal. The exact amount of active ingredient in each mushroom is impossible to determine, except in a laboratory, and so the dosage is difficult to get right. A typical dose is 2030 small mushrooms. The effects begin some 20 minutes or so after consumption and last for between six and eight hours. Younger users seem to feel the onset of effects more quickly than older users. Most users will experience feelings of euphoria and happiness. Excessive yawning can also be observed. Many begin to giggle, often uncontrollably, become excitable and animated, and may be unable to keep still. Users also experience a mild level of visual and auditory hallucination. They may range from mild distortion of the shape and colour of objects and people, to the appearance of strange shapes, objects and creatures. The user may also experience some tactile hallucinations, during which they may feel that insects are crawling all over them or that they are dissolving or changing shape.
ADVERSE EFFECTS Magic mushrooms sometimes cause bouts of nausea and dizziness, particularly in first-time users. Many cases have occurred in which regular users of magic mushrooms have become depressed or suffered delusions and required inpatient treatment in a psychiatric hospital. The main danger with the use of magic mushrooms lies in using the wrong variety, which can be poisonous. This cannot be stressed too strongly. It is difficult enough to be sure of what you are getting when the mushrooms are fresh, let alone when a user is buying them in dried form. It is not uncommon for bags of so-called magic mushrooms offered for sale to contain many other varieties than those that the user expects. These will have been added either by mistake on the part of the collector or purposefully by the dealer in order to bulk out shortages of the correct fungus. There are many varieties of mushroom that are superficially similar to the hallucinogenic types but that contain very powerful poisons.
WITHDRAWAL SYMPTOMS & TREATMENT HELP Psilocybin is a hallucinogen substance found in many species of mushrooms in South America, Mexico and the United States. Natural occurring psilocybin and psilocin can be manufactured synthetically. Mushrooms can be fresh with white/gray stems and dark brown edges around the cap. Dried mushrooms are rusty brown with white speckles. Psilocybin mushrooms are typically taken orally when fresh or dried, but they can also be brewed into a tea or added to other foods. Some people coat the mushrooms with chocolate to mask the bitter taste. Psilocybin is considered a Schedule I substance by the Drug Enforcement Administration. These mushrooms should not be confused with Amanita muscaria (known as fly agaric), which can produce a different type of hallucinogenic trip. There are closely regulated studies occurring now using psilocybin to treat certain types of cancer, obsessive-compulsive disorders, end of life anxiety, post-traumatic stress disorder and addiction. HOW IT WORKS It has been commonly assumed that psychedelics work by increasing neural activity, but it turns out psilocybin actually reduced blood flow and neural activity in several brain regions, such as the thalamus and anterior and posterior cingulate cortex. And subjects in which these regions were most inhibited tended to report the most intense hallucinatory experiences in the experiment.
TOLERANCE POTENTIAL Tolerance develops very rapidly with continued use of magic mushrooms. The dosage required to achieve the desired effects rises quickly to such a point that it becomes very difficult to achieve anything at all. Users are aware of this and will rest for a week or so following a bout of mushroom use. This restores their tolerance level to normal and they can then make effective use of the drug again. HABITUATION POTENTIAL Because of the rapid development of a high tolerance to mushrooms, to the point where no effects are achieved, it is rare for anyone to keep on taking the drug over an extended period of time. There seems to be little danger of the user developing marked physical or psychological dependence on the drug.
WITHDRAWAL EFFECTS Once a user stops using magic mushrooms, they will experience little in the way of withdrawal effects. Some may find their lives a little flat and will have to devise other ways of getting enjoyment and pleasure.
OVERDOSE POTENTIAL The potential for overdose of genuine magic mushrooms is low due to the very large quantities of the fungi that the user would need to obtain and consume. The overdose potential from other varieties of more dangerous fungi is very high. Some of the poisonous varieties require minute amounts to be consumed in order to cause very real problems.
PHARMACOLOGY When the compound psilocybin goes inside the body, it is rapidly changed to a substance called psilocin which hinders several seretonergic receptors (pain hormone). This psilocin mimics the effects of serotonin (happy hormone). As is known, it is this chemical which regulates a persons mood and motivation. The effects begin some 20 minutes or so after consumption and last for between six and eight hours. Younger users seem to feel the onset of effects more quickly than older users. Most users will experience feelings of euphoria and happiness. Excessive yawning can also be observed. Many begin to giggle, often uncontrollably, become excitable and animated, and may be unable to keep still. Users also experience a mild level of visual and auditory hallucination. They may range from mild distortion of the shape and colour of objects and people, to the appearance of strange shapes, objects and creatures.
METHODS OF USE Magic mushrooms are commonly taken orally. The fresh or dried forms can be eaten raw or cooked in some way. It is known that both fresh and dried mushrooms are added to omelettes, stews and pancakes and even to be eaten on toast. They may also be infused in boiling water to make a sort of soupy tea, which is then drunk. The tablet forms are also taken orally. Occasionally, the dried form of the mushroom is mixed with tobacco or cannabis and smoked in hand-rolled cigarettes or pipes. A small number of users have tried liquidising mushrooms in a domestic food processor, straining the resultant liquid and then injecting it.
METHOD OF MANUFACTURING When prepared for use, it is usually cut up into pieces measuring about 3cm across before drying. After being dried, the original colour is lost and the fungi is seen as rather hard brown irregular lumps that are indistinguishable from many other varieties of large fungi.
History of Phencyclidine First synthesized in 1926, PCP was developed by Parke, Davis and Company under the trade name Sernyl for use as a general anesthetic for humans in the 1950s, and subsequently was used in veterinary medicine as a tranquilizer. By 1965, use with humans was discontinued as clinical studies revealed that patients experienced delusions, severe anxiety and agitation when emerging from the drugs effects. Today, use even in the veterinary community is rare, though small amounts continue to be manufactured for research purposes. Manufactured in clandestine laboratories, PCP emerged as a substance of abuse in the mid- 1960s. It often appeared in pill form and was known as The PeaCe Pill, a term that contributed to the acronym PCP. Its use spread in the 1970s and peaked around 1978 as snorting or smoking (giving users a more immediate high) the powder form of PCP became more popular. PCP in Disguise in the time it has been on the illicit drug scene, PCP has been sold under the guise of a number of other drugs, including THC, methamphetamine, mescaline, and LSD. Today we can add MDMA and formaldehyde to that list. According to the DEA, in 2000 law enforcement agencies reported that some pills sold as MDMA or ecstasy actually contain PCP or a combination of PCP and other substances. The website EcstasyData.org, which provides results of laboratory tests done on pills sold as ecstasy, confirms that PCP has been found with other drugs in pills that had been sold as ecstasy across the country. Pills with such names as green kryptonite, orange pokemon, and purple tear drops contained ketamine, pseudo/ephedrine, caffeine, or methamphetamine in addition to PCP, but contain little or no MDMA. Some drug users claim they dip marijuana or tobacco cigarettes in embalming fluid (known as loveboat or dippers) to enhance the high. While these users believe that what they are smoking has been treated with formaldehyde, researchers speculate that this fluid is actually PCP, sometimes referred to as embalming fluid, or formaldehyde cut with PCP. Some who use loveboat experience effects very similar to the effects of PCP, including delusions, difficulty concentrating, and agitation. It is difficult to substantiate these suspicions, and researchers have called for further analysis.
PHENCYCLIDINE (PCP) Phencyclidine (PCP) is a synthetic dissociative drug originally developed as a general anesthetic. The effects of dissociative drugs like PCP include feelings of detachment from the environment and self. In its pure form, PCP is a white crystalline powder that dissolves easily in water or alcohol. As a liquid, it is clear, yellow, or tan and often is sold in vanilla extract bottles. PCP is also mixed with dyes to produce colored powder, tablets or capsules. It is currently a Schedule II controlled substance.
Slang Terms for PCP (street names) Straight PCP: Angel Dust Amoeba Amp Belladonna Animal Tank Zoom Peace Pills Boat Sherm Sticks Super Grass STP Embalming Fluid Marijuana/PCP combination: Wet Dust Blunt Happy Stick Fry Sticks Love Boat Illy Dippers PCP and MDMA: Elephant Flipping Pikachu
EFFECTS Short Term Effects The effects of PCP are influenced by the size of the dose, the setting in which it is taken, the users expectations of and past experience with the drug, and the users personality. The following psychological effects may occur and vary in intensity, depending on the dosage. Doses of less than 5 mg may produce milder effects, while doses of 10 mg or more may lead to more intense and erratic behavior. Mild to intense euphoria Relaxation or drowsiness Feelings of unreality and dissociation with the environment Distorted sense of ones body, including a feeling of weightlessness Distorted sense of time and space Visual and auditory hallucinations and other sensory distortions Difficulty concentrating and thinking Anxiety o Agitation Paranoid thoughts Confusion and disorientation Intense feelings of alienation Depression Bizarre or hostile behavior Obsession with trivial matters Grandiose delusions Panic, terror, and the overwhelming fear of imminent death The physical effects may also vary in intensity with the dose: Impaired motor skills Blurred vision and constricted pupils Dizziness Painful reaction to sound Blank staring Speech disturbances, ranging from difficulty articulating to incoherent speech or inability to speak Muscular rigidity Decreased sensitivity and awareness of pain, touch, and position Stupor or coma Irregular heartbeat Alternately abnormally low and abnormally high blood pressure Slow, shallow, and irregular breathing Nausea Vomiting Salivation Increased body temperature and sweating alternating with chills and shivering Very high doses may result in an overdose and lead to coma, convulsions, or death
Effects of Long Term Use Runs- Chronic users may binge use PCP, taking it repeatedly for 2 or 3 days at a time without eating or sleeping, followed by a period of sleep. These runs may occur as many as four times in a month. Impaired memory Flashbacks similar to those experienced by chronic LSD users Persistent speech problems, such as stuttering, inability to articulate, or the inability to speak at all Chronic and severe anxiety and depression, possibly leading to suicide attempts Social withdrawal and isolation Toxic psychosis may appear in chronic users who do not have a prior history of psychiatric disturbances. The symptoms of toxic psychosis are aggressive or hostile behavior, paranoia, delusional thinking and auditory hallucinations. PCP and Violence Despite its reputation in the media as a drug that causes bizarrely violent behavior and gives users superhuman strength, research does not support the idea that PCP itself is the cause of such behavior and strength. Instead, those who experience violent outbursts while under the influence of PCP often have a history of psychosis or antisocial behavior that may or may not be related to their drug abuse. Additionally , someone under the influence of PCP is often unaware of the dangers and limitations they face, and may react to physical confrontations in a way that makes it seem as though they have extraordinary muscular strength.
SYMPTOMS Stuttering Impaired memory Inability to think clearly Inability to speak Suicidal thoughts Anxiety Depression Isolation and withdrawal How PCP is Abused
ADDICTION AND TOLERANCE There is little research on addiction to PCP in humans, and reports of physical dependence are rare.17 A 1981 study reported that PCP users who sought treatment for PCP withdrawal experienced depression, drug craving, increased appetite, and increased need for sleep.18 Some evidence suggests that psychological dependence may develop in those who use high doses (10 mg or more) of PCP. Tolerance to PCP has not been directly studied in humans. Users report that they increase the amount of PCP they take over time to achieve the same effects, which suggests a possible tolerance to the drug. METHODS OF USE PCP is ingested orally, snorted, smoked, or injected. When the powder form is snorted or sprinkled on marijuana, parsley, or mint, and smoked, the effects are felt within 2 to 5 minutes and last 4 to 6 hours.13 Users dip tobacco or marijuana cigarettes in liquid PCP and smoke it as well.14 PCP can be pressed into pills or put in capsules and swallowed; when ingested orally, effects are felt in 30 to 60 minutes and last 6 to 24 hours. Injection of PCP appears to be uncommon. HOW IT WORKS ON THE BRAIN PCP disrupts the functioning of receptors for the neurotransmitter glutamate, which plays a major role in the perception of pain as well as in learning, memory, and emotion. It also influences the actions of the neurotransmitter dopamine, which causes the euphoria associated with drug use.