Chemical Abstracts Service Registry Number: 2152-34-3 Formal Names: Cylert Informal Names: Popcorn Coke Type: Stimulant. See page 11
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) an-tidepressants 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 pemo-line 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 pemo-line, 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.
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.
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