Nitrous Oxide (Dinitrogen Monoxide, Dinitrogen Oxide, Entonox)
Pronunciation: NIGH-truhs OX-eyed
Chemical Abstracts Service Registry Number: 10024-97-2
Formal Names: Dinitrogen Monoxide, Dinitrogen Oxide, Entonox
Informal Names: Fall Down, Gas, Hippie Crack, Hysteria, Laughing Gas, Nitro, Nitrous, Nitrous Acid, Noss, Pan, Shoot the Breeze, Tanks, Thrust, Whippets
Type: Inhalant. Federal Schedule Listing: Unlisted USA Availability: Nonprescription, but sales and usage are controlled in some jurisdictions Read more
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dinitrogen monoxide (135),Dinitrogen oxide (63),nitrous oxide birth defects (41),entonox drug (35),nitrous oxide abuse (30),entonox dose (30),entonox dental (24),long term effects of nitrous oxide abuse (22),entonox in usa (18),nitrous oxide and birth defects (17),Nicotine (Habitrol, Nicoderm, Niconil, Nicorette, Nicotiana rustica, Nicotiana tabacum, Nicotrol, Prostrop, Tobacco)
Pronunciation: NIK-uh-teen (also pronounced NIK-uh-tin)
Chemical Abstracts Service Registry Number: 54-11-5
Formal Names: Habitrol, Nicoderm, Niconil, Nicorette, Nicotiana rustica, Nicotiana tabacum, Nicotrol, Prostrop, Tobacco
Informal Names: Chip (cigarette mixed with PCP), Fry Daddy (cigarette mixed with crack cocaine)
Type: Stimulant (pyridine alkaloids class).
Federal Schedule Listing: Unlisted
USA Availability: Generally available to adults as a component of tobacco products; nonprescription and prescription in pharmaceutical format
Pregnancy Category: C or D (depending on pharmaceutical format) drugsencyclopedia.net/nicotine/nicotine-habitrol-nicoderm-niconil-nicorette-nicotiana-rustica-nicotiana-tabacum-nicotrol-prostrop-tobacco/#more-28″ class=”more-link”>Read more
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Contrary to what its name suggests, opium is not a single chemical compound. Its chemical make-up is more like a salad, consisting of various substances including sugars, proteins, acids, water, and many alkaloids, among others. The people who grow opium for its narcotic value are primarily interested in the alkaloids.
An alkaloid is a complex organic chemical substance found in plants, which characteristically combines nitrogen with other elements, has a bitter taste, and typically has some toxic, stimulant, analgesic effects. There are many different alkaloids, 30 of which are found in the opium plant. While morphine is the most important alkaloid in opium—for its natural narcotic qualities as well as providing the chemical structure for heroin—another alkaloid, codeine, is also sought after for its medicinal attributes. Other alkaloids include papaverine, narcotine, nicotine, atropine, cocaine, and mescaline. While the concentration of morphine in opium varies depending on where and how the plant is cultivated, it typically ranges from 3 percent to 20 percent.
The International Language of Poppy
Bengali Afing-gach, Posto
Burmese Bhainzi
Dutch Papaver
English Poppy
French Pavot somnifere
German Mohnblume
Hindi Post, Khas-khas, Post dana
Hungarian Mak, Kerti mak
Italian Papavero
Japanese Hinageshi
Polish Mak lekarski
Portuguese Popoula
Romanian Mac
Sanskrit Ahiphena
Spanish Adormidera, Amapola
Swedish Vallmo
Thai Ton fin
Turkish Hashhash tohuma
Incoming search terms for the article:
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Pronunciation: fen-MET-rah-zeen
Chemical Abstracts Service Registry Number: 134-49-6
Formal Names: Filon, Preludin
Informal Names: Sweeties
Type: Stimulant (anorectic class).
Federal Schedule Listing: Schedule II (DEA no. 1631)
USA Availability: Prescription
Uses.
Immediately upon announcement of the drug’s discovery in 1954 it was utilized in Germany as an appetite suppressant. A couple years later the same medical use began in the United States with expansive claims about patients obtaining substantial weight loss without having to follow a regimen of dieting, claims that became more modest as experience with the drug spread. One experiment testing the drug’s influence on appetite yielded a result relevant to drug experiments in general: The substance worked better when people knew its intended effect. If people knew they were supposed to feel less hungry, they noticed less desire for food and then ate less. Early reports praised phenmetrazine for producing more appetite loss than amphetamine and with fewer unwanted effects. Since then phenmetrazine has fallen into disfavor due to concern about addictive potential even though the drug is described as resembling caffeine more than amphetamine.
In dogs phenmetrazine has only one sixth to one tenth the strength of amphetamine. One type of canine experiment showed dextroamphetamine to be 250 times stronger than phenmetrazine. In dogs a much higher dose of phenmetrazine is needed for the same weight loss produced by benzphetamine, and an experiment with 75 humans had results consistent with that tendency,
finding phenmetrazine to be less effective than benzphetamine in promoting weight loss. In contrast, another human weight reduction experiment with 81 persons was unable to demonstrate such a difference. That study did show, however, that users obtain fewer amphetamine effects from phenmetrazine than from dextroamphetamine.
Phenmetrazine has worked as an antidepressant, and for some overweight persons that effect may enhance the drug’s appeal (overeating can be a response to depression). The substance shows effectiveness against motion sickness and against symptoms of diabetes insipidus. As a possible cure for bedwetting, the drug produced mixed results. The compound has also been
used to treat asthma and Parkinson’s disease.
Drawbacks.
Intravenous abuse can harm muscles and kidneys. Phenmetrazine can produce standard amphetamine effects such as euphoria, restlessness, jumpiness, insomnia, tics, fatigue reduction, faster breathing, and higher blood pressure. Studies have found phenmetrazine’s actions on patients with heart trouble or hypertension (high blood pressure) to be measurable but negligible.
Taking the high blood pressure medicine propranolol along with phenmetrazine can relieve cardiac effects without diminishing anorectic effects. Studies with diabetic users find phenmetrazine having little influence on blood sugar levels or on insulin needs.
Fluctuating emotions and even psychosis have been attributed to phenmetrazine abuse. Psychosis can include hallucinations and paranoia. That affliction can stop when drug taking stops, or instead the drug may break down barriers releasing full-fledged and long-lasting schizophrenia. Phenmetrazine interferes with dreaming during sleep, which in itself may cause psychological trouble.
Abuse factors.
Tests of drug preference, in which users could choose among several substances, found benzphetamine and phenmetrazine to have about the same amount of appeal even though benzphetamine is a Schedule III substance (a status implying a lower addictive potential than phenmetrazine). In one such test, volunteers found phenmetrazine to be a satisfying substitute
for dextroamphetamine but preferred the latter. Abusers of amphetamine and methamphetamine have routinely switched to phenmetrazine when their favored drug was unavailable.
Drug interactions.
An experiment found that chlorpromazine (Thorazine) interacts with phenmetrazine, hindering phenmetrazine’s normal anorectic benefit.
Cancer.
In pregnant women phenmetrazine may undergo transformations suspected of promoting childhood tumors.
Pregnancy.
Phenmetrazine was formerly prescribed to pregnant women seeking to lose weight. A study of over 10,000 birth and childhood records found the drug having no “severe” impact on fetal development. Other studies have found no birth defects at all, although medical literature from the early 1960s does contain a handful of reports in which the drug is suspected of harming fetuses. Those suspicions were never verified but were strong enough to suspend medical use of the drug in some countries for a while.
Combination products.
Filon combines phenmetrazine theoclate (CAS RN 13931-75-4) and phenbutrazate hydrochloride and is promoted as having phenmetrazine’s weight loss characteristics while lacking hazard of addiction. Initial clinical trials showed Filon to be an effective anorectic with fewer of phenmetrazine’s unwanted qualities, but a later study found the two drugs
to have the same unwanted effects. A case of Filon addiction also surfaced, but that single instance hardly proves Filon to have more addictive potential than any other drug considered to have low or zero potential.
Additional scientific information may be found in:
Gilstrap, L.C. III, and B.B. Little, eds. Drugs and Pregnancy. New York: Elsevier, 1992.
Martin, W.R., et al. “Physiologic, Subjective, and Behavioral Effects of Amphetamine, Methamphetamine, Ephedrine, Phenmetrazine, and Methylphenidate in Man.”
Clinical Pharmacology and Therapeutics 12 (1971): 245–58.
Mellar, J., and L.E. Hollister. “Phenmetrazine: An Obsolete Problem Drug.” Clinical
Pharmacology and Therapeutics 32 (1982): 671–75.
Negulici, E., and D. Christodorescu. “Phenmetrazine Psychosis.” British Medical Journal
3 (1968): 316.
Penick, S.B, and J.R. Hinklele. “The Effect of Expectation on Response to Phenmetrazine.”
Psychosomatic Medicine 26 (1964): 369–73.
Rosen, A., and I.J. Oberman. “Addiction to Phenmetrazine Hydrochloride and Its Psychiatric
Implications.” Journal of the American Osteopathic Association 59 (1960): 722–26.
Spillane, J.P. “The Use of Phenmetrazine.” The Practitioner 185 (1960): 102–6.
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Phendimetrazine (Bontril, Plegine, Prelu-2)
Pronunciation: fen-di-MEH-tra-zeen (also pronounced fen-dye-MEH-trah-zeen)
Chemical Abstracts Service Registry Number: 21784-30-5 (Bontril format); 569-59-5 (Plegine format); 50-58-8 (Prelu-2 format).
Formal Names: Bontril, Plegine, Prelu-2
Informal Names: Pink Hearts
Type: Stimulant (anorectic class).
Federal Schedule Listing: Schedule III (DEA no. 1615)
USA Availability: Prescription
Pregnancy Category: C
Uses.
Phendimetrazine is related to phenmetrazine. Indeed, the body converts part of a phendimetrazine dose into phenmetrazine, a fact to be remembered if employment drug screening unjustly accuses someone of using phenmetrazine. Short-term weight control is the main medical use of phendimetrazine; one experiment found it 20 more times effective than placebo— an astonishing result for any diet pill. Effectiveness declines as administration
continues, and standard practice is then to stop the drug gradually rather than increase the dosage. A derivative of the drug has been found useful for treating pyoderma gangrenosum, a skin affliction involving large sores.
Drawbacks.
If dosage suddenly stops, weariness and depression can occur. A small reduction in blood pressure is observed among some users, but generally the drug raises blood pressure and is considered inappropriate for persons with hypertension (high blood pressure). The compound has been linked with hypertension in blood circulation to lungs, a potentially fatal condition
causing trouble in breathing. Users have experienced edginess, disturbed sleep, headache, dizziness, lightheadedness, accelerated pulse rate, and feelings of heart tremors. Other muscle tremors can occur. Phendimetrazine can interfere with functioning needed to handle a car or dangerous tools. The compound can dry and even inflame the mouth, upset the stomach, loosen or tighten the bowels, and make urination frequent and painful. Persons should avoid the drug if they suffer from restlessness, glaucoma, excessive thyroid activity, heart disease, hardening of the arteries, or drug abuse. The substance may affect diabetics’ insulin needs. Overdose symptoms are similar to those of amphetamine: hyperactivity, fear, aggression, hallucination.
Abuse factors.
Phendimetrazine is a chemical relative of amphetamine and is therefore considered addictive. In an experiment using rhesus monkeys to measure phendimetrazine’s addictive potential, however, the test animals indicated no interest in it. This same study showed the drug having about 10% to 20% of dextroamphetamine’s potency.
Drug interactions.
Drinking milk can counteract phendimetrazine’s anorectic quality. The drug can dangerously increase blood pressure by interacting with monoamine oxidase inhibitors (MAOIs, found in some antidepressants and other medicine). After highly publicized incidents of adverse effects associated with combination therapy of phentermine and fenfluramine, medical practitioners became especially alert to any problems associated with diet drugs. Someone taking phendimetrazine two times a day developed heart and lung difficulty that substantially improved when dosage was halted, and a case of temporary skin rash and kidney inflammation is reported from someone who was taking phendimetrazine and phentermine. The latter drug combination is also suspected of responsibility for temporary trouble with blood circulation in the brain (leading to a stroke in at least one instance). Whether these isolated cases can be extrapolated into general principle is questionable, but such reports raise questions worthy of further scientific investigation.
Cancer.
Not enough scientific information to report.
Pregnancy.
Impact on fetal development is unknown. The drug is not recommended for pregnant women.
Additional scientific information may be found in:
Hadler, A.J. “Sustained-Action Phendimetrazine in Obesity.” Journal of Clinical Pharmacology
8 (1968): 113–17.
Mazansky, H. “A Review of Obesity and Its Management in 263 Cases.” South African
Medical Journal 49 (1975): 1955–62.
Ressler, C., and S.H. Schneider. “Clinical Evaluation of Phendimetrazine Bitartrate.”
Clinical Pharmacology and Therapeutics 2 (1961): 727–32.
Rostagno, C., et al. “Dilated Cardiomyopathy Associated with Chronic Consumption
of Phendimetrazine.” American Heart Journal 131 (1996): 407–409.
Runyan, J.W. “Observations on the Use of Phendimetrazine, a New Anorexigenic
Agent, in Obese Diabetics.” Current Therapeutic Research: Clinical and Experimental
4 (1962): 270–75.
Sash, S.E. “Anorectic Effects of OBEX LA (D-Phendimetrazine Bitartrate) in the Treatment
of Obesity.” Current Therapeutic Research: Clinical and Experimental 31 (1982):
181–84.
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Pronunciation: pay-OH-tih (also pronounced peh-YOH-teh)
Chemical Abstracts Service Registry Number: 11006-96-5
Formal Names: Lophophora williamsii
Informal Names: Bad Seed, Big Chief, Black Button, Britton, Buttons, Cactus, Cactus
Head, Challote, Devil’s Root, Dry Whiskey, Dumpling Cactus, Half Moon, Hikori, Hikuli, Hyatari, Mescal, Mescal Beans, Mescal Buttons, Mescalito, Mescy, Nubs, P, Pellote, Peyotl, Seni, Shaman, Tops
Type: Hallucinogen.
Federal Schedule Listing: Schedule I (DEA no. 7415)
USA Availability: Illegal to possess
Pregnancy Category: None
Uses.
Peyote is part of a cactus plant. Native American folk medicine has used peyote cactus root for doctoring scalp afflictions. In folk medicine peyote has also been used against snake bite, influenza, and arthritis. Scientists have determined that peyote contains substances that might fight infections. Some Native Americans are reported to use light doses of peyote as a stimulant to maintain endurance when engaged in relentless activity permitting little nourishment
or water, a practice sounding much like traditional use of coca. Spaniards observed such peyote usage in the Aztec empire.
Peyote’s main active component is the hallucinogen mescaline. Some other varieties of cactus also contain mescaline, although generally in much smaller amounts. Researchers suspect the peyote cactus may additionally contain chemicals similar to those appearing in the brain upon use of alcohol. In addition to causing hallucinations, peyote can change perception of time.
Psychic effects can include feeling more peaceful and connected with life; craziness of the everyday world can recede. People can use the experience to work through their concerns and may be more open to suggestions. Physical senses may seem enhanced, and barriers between them may melt, such as allowing sounds to be seen.
Normally a Schedule I substance is illegal to possess except under special permission to do research with it, but for many years members of the Native American Church were allowed to possess and use peyote (but not the pure drug mescaline) for religious purposes. During the 1990s their legal situation became confused, and the issue was a matter of controversy when this book was written.
The religion of Peyotism (of which the Native American Church is but one variety) is a topic beyond the scope of this book, but drug-induced visions are only one part of the practitioners’ way of life. Observers have noted that Peyotism can be an effective way of dealing with addiction to alcohol and opiates. Traditional peyote use occurs in a group context, a social gathering
of persons sharing and furthering the same beliefs and goals. A solitary user estranged from such a setting is likely to have a far different peyote experience.
For instance, one element of a peyote session can be nervousness and fear, emotions that may have different impacts depending on whether a user is alone or is with a group of reassuring and supportive persons. A researcher with the Indian Health Service of the U.S. Public Health Service estimated that traditional peyote usage produced bad psychological experiences once in
70,000 doses, a safety record that the researcher attributed to the social context of traditional use. Physical damage has not been noted from traditional use.
Drawbacks.
Chills, muscle tension, nausea, and vomiting are typical unwanted peyote effects.
Abuse factors.
A study published in the 1950s concluded that peyote tolerance, dependence, and craving did not occur from traditional usage—a finding supported by other authorities as well. A canine experiment showed that tolerance to the vomiting effect occurred if dogs received daily peyote for a year.
Drug interactions.
Not enough scientific information to report.
Cancer.
Not enough scientific information to report.
Pregnancy.
Peyote has caused birth defects in hamsters. A study comparing peyote users to nonusers from the same Indian group found no increase in chromosome damage among the users.
Additional information.
Peyote is sometimes called “mescal,” which is also the name of an alcoholic beverage. The two substances are different, and the beverage has no connection with peyote. Likewise “mescal beans” are an alternative peyote name and also the name of a nonhallucinogenic food.
Additional scientific information may be found in:
Bergman, R.L. “Navajo Peyote Use: Its Apparent Safety.” American Journal of Psychiatry
128 (1971): 695–99.
Boyer, L.B., R.M. Boyer, and H.W. Basehart. “Shamanism and Peyote Use among the
Apaches of the Mescalero Indian Reservation.” In Hallucinogens and Shamanism,
ed. M.J. Harner, 53–66. New York: Oxford University Press, 1973.
Bruhn, J.G. “Mescaline Use for 5700 Years.” Lancet 359 (2002): 1866.
Ellis, H. “Mescal: A New Artificial Paradise.” The Contemporary Review 71 (1897). Reprinted
in Smithsonian Institution’s Annual Report 1897. Washington, DC: Author,
1898. 537–48.
Huttlinger, K.W., and D. Tanner. “The Peyote Way: Implications for Culture Care Theory.”
Journal of Transcultural Nursing 5, no. 2 (1994): 5–11.
Kapadia, G.J., and M.B.E. Fayez. “Peyote Constituents: Chemistry, Biogenesis, and Biological
Effects.” Journal of Pharmaceutical Sciences 59 (1970): 1699–1727.
La Barre, W. “Peyotl and Mescaline.” Journal of Psychedelic Drugs 11 (1979): 33–39.
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Pronunciation: pen-toh-BAR-bi-tal
Chemical Abstracts Service Registry Number: 76-74-4
Formal Names: Cafergot, Nembutal, Pentobarbitone, Phenobarbitone
Informal Names: Nebbies, Nembies, Nemmies, Nimbies, Yellow Bullets, Yellow Dolls, Yellow Jackets, Yellows
Type: Depressant (barbiturate class).
Federal Schedule Listing: Schedule II (oral and parentral, DEA no. 2270), Schedule
III for suppositories (DEA no. 2271)
USA Availability: Prescription
Pregnancy Category: D
Uses.
This short-acting substance has sedative qualities but is considered ineffective in treating nervous apprehension. Because of the drug’s sleepinducing characteristics, it is used as a preliminary to administering anesthesia and as a short-term treatment for insomnia. Pentobarbital has been observed to lower blood pressure, body temperature, and muscle tone. The compound can be used as an emergency anticonvulsant when a person has seizures, and
has been used to treat alcohol addicts undergoing withdrawal. Pentobarbital has been found effective in reducing pressure that fluid creates in the brain after severe head injury. Pentobarbital reduces a type of nerve cell death called neuronal apoptosis, and this reduction may help prevent stroke. Animal studies indicate that pentobarbital can help protect brain tissue against radiation, which might have practical application during treatment of brain tumors. Veterinarians use the substance for euthanasia: An unusual demonstration of the drug’s strength occurred when a lion was poisoned by eating meat from a horse that had been killed with pentobarbital.
Drawbacks.
Although the drug is a sedative, it can cause hyperactivity in children. Sudden stoppage of combined pentobarbital and benzodiazepine therapy in an infant caused temporary chorea (involuntary jerking). A feline experiment showed that tremors reminiscent of Parkinson’s disease can occur when pentobarbital is administered with chlorpromazine (also called Thorazine, often used to treat psychotic behavior). Persons with porphyria, a body chemistry affliction that can provoke violence, are supposed to avoid pentobarbital. Examination of epileptic children receiving pentobarbital shows elevated readings for total cholesterol, though levels of high-density lipoprotein (so-called good cholesterol) and triglycerides (associated with heart attack and stroke) seem unaffected.
In a monkey experiment pentobarbital interfered with time perception, ability to learn, short-term memory, attention span, and interest in tasks. The substance impeded task performances in a human experiment, with performance getting worse as the amount of thinking necessary for a chore increased.
Such a drug is unlikely to be welcome in the workplace. Although children using the substance apparently have trouble with language skills, a study found language development to be normal two years after the medication ceased.
Abuse factors.
In a test, alcohol drinkers who were not alcoholics found pentobarbital less appealing than a placebo and experienced no euphoria from pentobarbital, a finding consistent with other studies of persons who do not abuse drugs. When given choices of assorted substances, monkeys chose pentobarbital less often than water, which indicates the compound has low addictive potential. In contrast, drug abusers participating in an experiment found effects of pentobarbital and diazepam to be similar. Those two drugs thus had comparable appeal even though scientists running the experiment found pentobarbital possessing only 10% of diazepam’s strength. A study testing various effects on former drug addicts found pentobarbital to be 15 times
stronger than meprobamate, but morphine acted 6 times stronger than pentobarbital.
Cross-tolerance among chlordiazepoxide, pentobarbital, and alcohol has been observed in rats. A study of sedative drug abusers found alcohol and pentobarbital to deliver similar effects, with pentobarbital possibly having more appeal. A monkey experiment indicates that alcohol increases the attractiveness of pentobarbital. Dependence can develop, and in humans the
pentobarbital withdrawal syndrome can duplicate the delirium tremens of alcohol withdrawal. A mice study found that tolerance to pentobarbital developed more rapidly if assorted drugs of abuse were also being administered (morphine, amphetamine, alcohol, or cocaine).
Drug interactions.
A case report notes that pentobarbital can almost double the speed with which theophylline (commonly used to treat asthma and other breathing difficulties) disappears from the bloodstream, requiring changes in normal theophylline dosage. In a mice experiment alcohol boosted pentobarbital’s potency. A human study found that chronic alcohol ingestion reduces
the effective length of a pentobarbital dose. Grapefruit juice extends the amount of sleep produced by pentobarbital in rats, and in mice the drug inhibits caffeine effects. At one time researchers suspected that taking pentobarbital along with MDMA would reduce organic brain damage caused by MDMA, but rat experiments indicate that any apparent benefit comes simply
from the lower body temperature produced by pentobarbital. Although cocaine is a stimulant, in a rat experiment it increased the sleep-inducing quality of pentobarbital.
Cancer.
In animal experimentation pentobarbital has caused cancer. In humans long-term usage is associated with cancer of the ovaries and bronchi, but that finding is weakened by the patients also smoking cigarettes. Pregnancy. A large survey of pregnancy outcomes found that pentobarbital does not appear to cause birth defects. Nonetheless pregnant women are supposed
to avoid the drug.
Additional information.
Some capsule formats of Nembutal (pentobarbital sodium CAS RN 57-33-0) contain FD&C Yellow No. 5 (tartrazine), which can cause asthma attacks or other allergic responses in sensitive persons, particularly if someone has adverse reactions to aspirin. Cafergot PB is a combination
of bellafoline, caffeine, and ergotamine tartrate. The combination was tested with and without pentobarbital sodium to determine effect on migraine headache. Presence of pentobarbital not only enhanced reduction of pain but also helped treat anxiety, nausea, vomiting, poor appetite, and low tolerance of light.
Additional scientific information may be found in:
Cole-Harding, S., and H. de Wit. “Self-Administration of Pentobarbital in Light and
Moderate Alcohol Drinkers.” Pharmacology, Biochemistry, and Behavior 43 (1992):
563–69.
Hambly, G., C. Frewin, and B. Dodd. “Effect of Anticonvulsant Medication in the Preschool
Years on Later Language Development.” Medical Journal of Australia 148
(1988): 658, 661–62.
Mintzer, M.Z., et al. “Ethanol and Pentobarbital: Comparison of Behavioral and Subjective
Effects in Sedative Drug Abusers.” Experimental and Clinical Psychopharmacology
5 (1997): 203–15.
Pickworth, W.B., M.S. Rohrer, and R.V. Fant. “Effects of Abused Drugs on Psychomotor
Performance.” Experimental and Clinical Psychopharmacology 5 (1997): 235–41.
Pierce, James I. “Drug-Withdrawal Psychoses.” American Journal of Psychiatry 119
(1963): 880–81.
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Pronunciation: PEM-oh-leen
Chemical Abstracts Service Registry Number: 2152-34-3
Formal Names: Cylert
Informal Names: Popcorn Coke
Type: Stimulant.
Federal Schedule Listing: Schedule IV (DEA no. 1530)
USA Availability: Prescription
Pregnancy Category: B
Uses.
In the United States pemoline became available for medical purposes during the 1970s. It is used to treat depression, weariness, and attention deficit hyperactivity disorder (ADHD). The drug’s stimulant effects are described as greater than caffeine but less than amphetamine. Unlike many scheduled stimulants, pemoline is unrelated to amphetamine.
Studies find pemoline useful in reducing symptoms of depression, and experimental usage of pemoline with monoamine oxidase inhibitor (MAOI) antidepressants has helped depressed persons who obtain insufficient relief with other drugs.
Pemoline has eliminated drowsiness felt by persons taking antihistamines. The drug has been proposed for workplace usage to reduce fatigue but has not been tested extensively for that purpose. Tests have found that the drug improves ability to perform arithmetic when users are tired. In a different but more robust experiment, members of the U.S. Navy Special Warfare group stayed awake 64 hours around the clock while using pemoline. Though their performance appeared to decline as the experiment continued, they not only did better than participants who used placebos, but they also did better than persons using methylphenidate. In England, Royal Air Force experimenters concluded that pemoline can help keenness and capabilities during long shifts of duty. A Russian report endorses the drug’s usefulness for “urgent increase” of functioning but notes that persons using pemoline cannot maintain initial ability if body temperature rises and oxygen supply declines, nor does the drug help persons push past emotional strain or fulfill complicated task requirements.
During the 1980s and 1990s sports officials in Belgium found the drug was frequently used by cyclists seeking a competitive edge. Multiple sclerosis patients using pemoline sometimes report less exhaustion than those using a placebo, but investigators who rigorously reviewed studies about multiple sclerosis fatigue found no evidence of pemoline improving weariness.
An instance is known of an elderly man taking pemoline to help him stay awake during lectures, but the regimen seemed to promote prostate trouble. Pemoline has been successfully used against narcolepsy.
Studies find pemoline about as effective as either dextroamphetamine or methylphenidate in helping children with ADHD. Pemoline has been used successfully against ADHD in teenagers and adults as well. Growth rates are below normal in some youngsters with ADHD, and pemoline itself can temporarily hold back such development but without long-term harm—youngsters
develop normal adult weight and height. Those deficient growth rates may be treated with growth hormone. One study found, however, that pemoline seems to make the hormone treatment less effective in some patients. As the age of ADHD patients grows, so can unwanted effects that they experience from pemoline.
Animal experiments in the 1960s indicated that pemoline boosts learning ability. The lure of a “smart pill” had understandable appeal to suffering students and teachers, but when the drug was tested on college students, no improvement in learning ability occurred. The same dismal outcome occurred when elderly persons received the drug; indeed, some performed worse than
elderly persons receiving a placebo. Group results in still another experiment showed either no improvement or worsening of learning scores when people used the drug. In contrast, long-term daily administration of the drug seemed to improve memory in some persons entering senility.
A review covering 10 years of pemoline reports found none attributing euphoria to the drug, a lack that sets it apart from other scheduled stimulants.
Unlike some other stimulants, pemoline also seems to have little effect on pulse rate or blood pressure.
Drawbacks.
The drug can bring on tics and partial muscle movements, in a particularly severe way if an overdose occurs. An instance is known of muscle damage in an adult misusing pemoline. Pemoline is also known to reduce appetite and salivation, increase crankiness, bring on headaches and stomachaches, cause skin rash, and interfere with sleep. Hallucinations from
pemoline have been reported.
In rats and mice pemoline can cause self-harm behavior, and the amount needed to induce such behavior declines when a certain kind of brain damage is present, damage that is often seen in mentally retarded humans. Those findings suggest that such persons receiving pemoline may need monitoring to guard against self-injury. Long-term excessive usage may generate temporary psychotic behavior, but such an outcome appears untypical.
Probably the most serious unwanted results of taking pemoline can be hepatitis and other liver injury, injury so severe as to require a transplant. Damage can continue to worsen after the drug is stopped, and people have died from liver failure induced by pemoline. Victims tend to be children. Such an adverse effect is particularly disquieting because it occurs at therapeutic dosage, rather then being created by reckless abuse. A child can take pemoline for months before harm is apparent, or alarming symptoms can arise after just a week of use.
Methylphenidate is suspected of contributing to liver trouble in persons who are also taking pemoline. Debate exists about how dangerous pemoline is to liver function when no other drugs are being taken, but the debate has limited practical significance because many patients taking pemoline receive other drugs as well. Because of concern about liver damage, parents are supposed to sign a written consent form before their children begin pemoline therapy.
Abuse factors.
Although pemoline is a scheduled substance, a review of reports covering the first 10 years of its medical availability in the United States found little evidence of addiction or abuse. A Norwegian review of pemoline use boldly described it as “a stimulant which cannot be abused.”
1 When given a choice of drugs, animals show no particular interest in pemoline, a sign of low abuse potential. Nonetheless, a case report does exist of a pemoline addict who developed a paranoid psychosis that went away after stopping the drug. A British medical practitioner reported that drug misusers were supplementing their amphetamine habit with pemoline.
An experiment tested pemoline’s ability to help reduce cocaine usage among persons receiving methadone treatment (meaning the persons were addicted to cocaine and heroin both). Results were unencouraging. In contrast, favorable response in an ADHD alcoholic caused researchers to predict that pemoline may be useful for treating alcohol addiction. Mice experimentation
shows that pemoline reduces effects produced by THC, considered the primary drug in marijuana.
Drug interactions.
Pemoline is suspected of interfering with epilepsy medicines.
It can boost mono amine oxidase inhibitor (MAOI) antidepressants and
urinary acidifers (the latter action interfering with pemoline’s psychostimulant
effects).
Cancer.
Rat experiments do not indicate any cancer risk from pemoline.
Pregnancy.
Experiments with rabbits and rats reveal no harm to fetal development, but influence on human fetal development is unknown.
Additional information.
When tested on mentally handicapped workers, magnesium pemoline (CAS RN 18968-99-5) brought on the kinds of temperament modification associated with caffeine but failed to increase either productivity or time worked. Two cocaine addicts who appeared to have mild ADHD were able to reduce their intake of cocaine while receiving magnesium pemoline, a result leading the scientific investigators to wonder if magnesium pemoline might have potential for helping to break cocaine addiction. Animal experiments have shown that both pemoline and magnesium pemoline can provide protection against atomic radiation.
Additional scientific information may be found in:
Bostic, J.Q., et al. “Pemoline Treatment of Adolescents with Attention Deficit Hyperactivity
Disorder: A Short-Term Controlled Trial.” Journal of Child and Adolescent Psychopharmacology 10 (2000): 205–16.
Elizur, A., I. Wintner, and S. Davidson. “The Clinical and Psychological Effects of
Pemoline in Depressed Patients—A Controlled Study.” International Pharmacopsychiatry
14 (1979): 127–34.
Honda, Y., and Y. Hishikawa. “Long Term Treatment of Narcolepsy and Excessive Daytime Sleepiness with Pemoline (Betanamin).” Current Therapeutic Research:
Clinical and Experimental 27 (1980): 429–41.
Langer, D.H., et al. “Evidence of Lack of Abuse or Dependence Following Pemoline
Treatment: Results of a Retrospective Survey.” Drug and Alcohol Dependence 17
(1986): 213–27.
Newlands, W.J. “The Effect of Pemoline on Antihistamine-Induced Drowsiness.” The
Practitioner 224 (1980): 1199–1201.
Shevell, M., and R. Schreiber. “Pemoline-Associated Hepatic Failure: A Critical Analysis
of the Literature.” Pediatric Neurology 16 (1997): 14–16.
Sternbach, H. “Pemoline-Induced Mania.” Biological Psychiatry 16 (1981): 987–89.
Valle-Jones, J.C. “Pemoline in the Treatment of Psychogenic Fatigue in General Practice.”
The Practitioner 221 (1978): 425–27.
Note
1. N. Lie, “Sentralstimuleren Midler ved AD/HD Hos Voksne. Kan De Misbrukes?
[Central Stimulants in Adults with AD/HD. Can They Be Abused?],” Tidsskrift for den
Norske Laegeforening 119 (1999): 82–83. Abstract in English.
