The use of stimulant compounds has a long history. Chinese native physicians have been using the drug Ma-huang for more than 5000 years. In 1887, Nagai found the active agent in Ma-huang to be ephedrine.
Showing posts with label Stimulant. Show all posts
Showing posts with label Stimulant. Show all posts
29 July 2014
23 May 2014
Pemoline (Cylert)
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.
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.
09 March 2009
Phenmetrazine (Filon, Preludin)
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.
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.
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.
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.
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)
Uses.
Tobacco’s history is mentioned on page 18. Nicotine is the addictive drug component of tobacco and is found in other plants as well. Nicotine is one of the more hazardous drugs, and dosage via tobacco smoke adds still more peril. Although nicotine has medical uses, characteristics of the natural product tobacco fall within the criteria of a Schedule I controlled substance. Nonetheless, federal law explicitly excludes tobacco from such control, making the tobacco industry legal. At the time this book was written debate was under way about limiting adult access to nicotine products, a restrictive effort requiring changes in law.
Traditional medical uses of the drug include treatment of insect bites, skin and intestinal parasites, vomiting, earache, toothache, runny nose, hernia, and heart pain. Although tobacco smoking worsens a gastrointestinal inflammation called Crohn’s disease, medical practice uses nicotine skin patches, oral capsules, or suppositories to treat inflammation of the colon and rectum caused by ulcerative colitis. Nicotine chewing gum has been used successfully to treat finger or toe sores deriving from Buerger’s disease, an affliction in which blood vessels get blocked off (and which, despite the usefulness of pharmaceutical nicotine, seems to be worsened by smoking). Pharmaceutical nicotine helps some persons suffering from the tics of Tourette’s syndrome.
Researchers have found cigarette smoking to reduce the likelihood of getting preeclampsia, a potentially serious disease of late pregnancy in which women suffer fluid retention, high blood pressure, and too-high urine protein levels.
Cigarette smoking is also associated with a lower probability of getting Parkinson’s or Alzheimer’s disease. Even though “association” does not demonstrate cause and effect, some experiments using pharmaceutical nicotine to treat those afflictions show positive results. Such results, however, have not yet given nicotine a generally accepted role in treating those diseases. Nicotine reduces hunger pains and raises blood sugar, effects that help users eat less (Native Americans have traditionally chewed tobacco to better endure circumstances involving little food, water, or rest). Nicotine initially raises blood pressure, but continued dosage will lower it.
Drawbacks.
Tobacco smoking can lead to lung cancer and heart disease. Many other afflictions are attributed to tobacco smoking: bronchitis, emphysema, cataracts, mouth cancer, pancreas cancer, bone density loss (making broken bones more likely), abdominal aortic aneurysm (a sac ballooning out from the blood vessel wall), brain aneurysm, and gastroesophageal reflux (recurrent backward flow of acid and partially digested food from the stomach to the esophagus, making esophageal cancer more likely). One study noted that smoking tends to produce changes causing women to go through menopause at a younger age than nonsmokers. Laboratory tests imply that smokeless tobacco promotes tooth decay. Still more unwanted actions are known, partly because tobacco has simply been studied so intensively that more is known about it than is known about many other substances. Whether nicotine itself causes afflictions produced by tobacco is uncertain. For example, some investigators suspect that heart disease in smokers comes from carbon monoxide and tar constituents of smoke rather than the nicotine.
In adults 40 mg to 100 mg of pharmaceutical nicotine can produce fatal poisoning; an equivalent dose through cigarettes would require a person to quickly smoke several packs. Smaller dosages can be dangerous for children who play with nicotine patches or gum or who consume tobacco.
Abuse factors.
As with many drugs, persons often find nicotine unpleasant at first but learn to ignore bad sensations and focus upon effects that are enjoyed. Experiments examining differences that users perceive in various drugs find that some sensations from nicotine, amphetamine, and cocaine are similar, so similar that in one experiment persons receiving injections of nicotine typically identified it as cocaine. A user can establish a physical dependence
with nicotine, causing withdrawal symptoms if dosage stops:
nervousness, tenseness, crankiness, lightheadedness, broken sleep, weariness, distractedness, tremors. These symptoms often last a few days, sometimes longer, and can relate to a person’s expectations (a psychosomatic component).
Debate exists about how addictive nicotine is. A study published in 1994 noted that about 33% of tobacco smokers become addicted. A study published in 2000 found that 20% to 60% of adolescent smokers are addicted. Many smokers with no interest in quitting can nonetheless substantially reduce their cigarette consumption with little difficulty. In contrast, many smokers wanting to stop find themselves unable to cease, and for them even pharmaceutical
nicotine can be an insufficient replacement for tobacco. Among such persons the persistence of a smoking habit suggests that something more than the drug nicotine is involved. Tobacco smoke contains thousands of chemical ingredients besides nicotine; perhaps some of the less-studied ones are important. In addition, the paraphernalia and mechanics of cigarette smoking provide a psychological buffer to users, allowing continual brief respites in interactions with other persons (such as breaking eye contact during a puff). Nicotine itself is a mild stimulant able to release adrenaline and increase pulse rate and blood pressure, with the physiological arousal produced by the drug masking physical arousal provoked by life’s tensions, thereby making smokers feel less nervous despite the stimulant effects. Smokers tend to have lower levels of body chemicals that are supplemented by antianxiety and antidepressant drugs.
Such pharmaceuticals, unfortunately, seemingly have little ability to help smokers quit their tobacco addiction.
As with any addiction, the power of nicotine and tobacco depends upon needs met by those substances. People do not smoke simply to avoid temporary withdrawal symptoms. If a person’s life is filled with situations that smoking eases like nothing else can, breaking the addiction is hard. If a person finds other ways of dealing adequately with those situations, desire for cigarettes can go away and never be bothersome again. Contrary to expectations of researchers, a laboratory test found nicotine to be no more appealing to exsmokers than to persons who have never smoked—a finding implying that life circumstances, and not just chemistry, determine this drug’s appeal.
Alcohol and illicit drug abusers reliably tend to be tobacco cigarette smokers, so reliably that the amount of tobacco use can be used to estimate the amount of cocaine and opiate usage by persons in drug abuse treatment programs.
An experiment found that persons smoked less tobacco when they had access to marijuana, suggesting that those persons used the two substances for similar purposes. Nonsmokers tend to avoid drug abuse, implying that smokers and nonsmokers use different strategies to cope with life’s challenges.
Cigarette smoking is more prevalent among schizophrenics, seriously depressed persons, and persons with low-grade psychiatric disturbance that may lack outward symptoms. Almost two thirds of smokers in one research project turned out to have a history of present or past psychiatric abnormality.
Among such individuals smoking may be a strategy of self-medication. One study found that withdrawal symptoms can depend on the extent to which the drug is used for self-medication.
Improvement has been measured in alertness, energy, and happiness as cigarette smokers start their day’s consumption in the morning. Conversely, cutting off a smoker’s supply of cigarettes produces measurable increases in fatigue, irritation, sadness, stress, and disorientation. New users do not get favorable effects sought by experienced users but instead have measurable nausea and general uneasiness. Among new users nicotine reduces job performance skills such as physical coordination and accuracy in memory tasks the opposite of what happens with experienced users.
Although pharmaceutical nicotine has various medical applications, its main use is for treatment of addiction to tobacco smoking. One authority aptly described nicotine chewing gum as the methadone of cigarettes, meaning that such a treatment strategy is intended to switch addicts from tobacco to pharmaceutical nicotine, just as treatment personnel seek to switch heroin addicts to methadone. Although such programs may have an official goal of eliminating a person’s addiction, in practice simply switching a person from a more harmful drug to a less harmful drug is often considered a success.Drug interactions. Nicotine interacts with commonly used medical drugs.
Antipsychotic drugs and the anti–blood clot medicine heparin flush from the body faster if a person uses nicotine. Nicotine also reduces the sedative effect of benzodiazepines and reduces pain relief from various opioids. Cigarette smoke acts as a monoamine oxidase inhibitor (MAOI), a type of chemical found in some antidepressants and that can have serious adverse effects when
used simultaneously with some medicines (though acute danger from cigarette interactions may be small). Caffeine seems to make nicotine more pleasurable.
Rat studies show that nicotine increases alcohol’s appeal and worsens pancreas inflammation caused by both drugs. Birth control pills increase the boost that nicotine gives to pulse rate, and some researchers speculate that such increase is related to the elevated risk of heart disease found among smokers who use birth control pills.
Cancer.
Tests indicate that pure nicotine (as opposed to smoke containing nicotine) does not cause cancer.
Pregnancy.
Smoking reduces female fertility according to most studies of the topic, and studies of Canadian farm couples and of men in the Netherlands found an apparent reduction in male fertility as well. Pregnant women who smoke tobacco increase the chance of miscarriage, premature birth, smaller full-term infants, and sudden infant death syndrome (SIDS or “crib death”).
The children are more likely to have muscle tone abnormalities. Smoking harms male and female gametes, damages chromosomes, and can change DNA in ways linked with childhood cancer. Nicotine usage by a pregnant woman changes movements and heart action of a fetus. One researcher warns that nicotine patches or chewing gum may deliver even more nicotine to a
fetus than smoking would. Nicotine enters the milk of nursing mothers. Rat experiments indicate that fetal exposure to nicotine combined with newborn exposure to nicotine in milk increases the risk of offspring developing lung trouble similar to emphysema. Human birth defects have been attributed to tobacco smoking. Although a study of teenage tobacco smokers did not see
any increased incidence of birth defects in their infants, research based on animal experimentation and published in 1998 declared that nicotine causes defects in fetal brain development leading to problems in thinking and learning that may not become apparent until years after birth. The children tend to have lower scores on psychological measurements, somewhat reminiscent of “cocaine babies,” deficits that continue for years. Some investigators see a link between pregnant smokers and offspring with psychological problems.
Investigators tracking mothers and daughters for three decades found that daughters were more likely to take up smoking if their mothers smoked during pregnancy.
Additional information.
Scientific studies find that “passive smoking” threatens health of bystanders who inhale smoke from tobacco products and exhalations of smokers. A study of spontaneous abortions found them more likely in pregnant nonsmoking women who inhale environmental smoke and use a lot of caffeine or a moderate amount of alcohol. Infants from nonsmoker women who were exposed to tobacco smoke during pregnancy are more likely to have lower birth weight and persistent pulmonary hypertension. Offspring also exhibit the same kinds of lower psychological test scores that are seen in children of active smokers. Inhalation of smoke by infants is suspected of
contributing to SIDS. For sure, compared to children in nonsmoking households, infants of smokers are hospitalized more often for pneumonia and bronchitis. The level of environmental smoke necessary for ill effects is often unclear in scientific studies; a person working in a poorly ventilated smokey bar for eight hours a day will have a considerably different exposure than
someone in a nonsmoking household who sits outside once a week with a friend who smokes a couple of cigarettes.
Additional scientific information may be found in:
Brown, C. “The Association between Depressive Symptoms and Cigarette Smoking in an Urban Primary Care Sample.” International Journal of Psychiatry in Medicine 30 (2000): 15–26.
Brown, K.G. “Lung Cancer and Environmental Tobacco Smoke: Occupational Risk to Nonsmokers.” Environmental Health Perspectives 107 (1999, Suppl. 6): 885–90.
Colby, S.M., et al. “Are Adolescent Smokers Dependent on Nicotine? A Review of the
Evidence.” Drug and Alcohol Dependence 59 (2000, Suppl. 1): S83–S95.
Dursun, S.M., and S. Kutcher. “Smoking, Nicotine and Psychiatric Disorders: Evidence
for Therapeutic Role, Controversies and Implications for Future Research.” Medical
Hypotheses 52 (1999): 101–9.
Haustein, K.O. “Cigarette Smoking, Nicotine and Pregnancy.” International Journal of
Clinical Pharmacology and Therapeutics 37 (1999): 417–27.
Parrott, A.C., and F.J. Kaye. “Daily Uplifts, Hassles, Stresses and Cognitive Failures:
In Cigarette Smokers, Abstaining Smokers, and Non-smokers.” Behavioural Pharmacology
10 (1999): 639–46.
Robinson, J.H., and W.S. Pritchard. “The Role of Nicotine in Tobacco Use.” Psychopharmacology
108 (1992): 397–407.
Stolerman, I.P., and M.J. Jarvis. “The Scientific Case That Nicotine Is Addictive.” Psychopharmacology 117 (1995): 2–10.
Van Gilder, T.J., P.L. Remington, and M.C. Fiore. “The Direct Effects of Nicotine Use
on Human Health.” Wisconsin Medical Journal 96 (1997): 43–48.
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)
Uses.
Tobacco’s history is mentioned on page 18. Nicotine is the addictive drug component of tobacco and is found in other plants as well. Nicotine is one of the more hazardous drugs, and dosage via tobacco smoke adds still more peril. Although nicotine has medical uses, characteristics of the natural product tobacco fall within the criteria of a Schedule I controlled substance. Nonetheless, federal law explicitly excludes tobacco from such control, making the tobacco industry legal. At the time this book was written debate was under way about limiting adult access to nicotine products, a restrictive effort requiring changes in law.
Traditional medical uses of the drug include treatment of insect bites, skin and intestinal parasites, vomiting, earache, toothache, runny nose, hernia, and heart pain. Although tobacco smoking worsens a gastrointestinal inflammation called Crohn’s disease, medical practice uses nicotine skin patches, oral capsules, or suppositories to treat inflammation of the colon and rectum caused by ulcerative colitis. Nicotine chewing gum has been used successfully to treat finger or toe sores deriving from Buerger’s disease, an affliction in which blood vessels get blocked off (and which, despite the usefulness of pharmaceutical nicotine, seems to be worsened by smoking). Pharmaceutical nicotine helps some persons suffering from the tics of Tourette’s syndrome.
Researchers have found cigarette smoking to reduce the likelihood of getting preeclampsia, a potentially serious disease of late pregnancy in which women suffer fluid retention, high blood pressure, and too-high urine protein levels.
Cigarette smoking is also associated with a lower probability of getting Parkinson’s or Alzheimer’s disease. Even though “association” does not demonstrate cause and effect, some experiments using pharmaceutical nicotine to treat those afflictions show positive results. Such results, however, have not yet given nicotine a generally accepted role in treating those diseases. Nicotine reduces hunger pains and raises blood sugar, effects that help users eat less (Native Americans have traditionally chewed tobacco to better endure circumstances involving little food, water, or rest). Nicotine initially raises blood pressure, but continued dosage will lower it.
Drawbacks.
Tobacco smoking can lead to lung cancer and heart disease. Many other afflictions are attributed to tobacco smoking: bronchitis, emphysema, cataracts, mouth cancer, pancreas cancer, bone density loss (making broken bones more likely), abdominal aortic aneurysm (a sac ballooning out from the blood vessel wall), brain aneurysm, and gastroesophageal reflux (recurrent backward flow of acid and partially digested food from the stomach to the esophagus, making esophageal cancer more likely). One study noted that smoking tends to produce changes causing women to go through menopause at a younger age than nonsmokers. Laboratory tests imply that smokeless tobacco promotes tooth decay. Still more unwanted actions are known, partly because tobacco has simply been studied so intensively that more is known about it than is known about many other substances. Whether nicotine itself causes afflictions produced by tobacco is uncertain. For example, some investigators suspect that heart disease in smokers comes from carbon monoxide and tar constituents of smoke rather than the nicotine.
In adults 40 mg to 100 mg of pharmaceutical nicotine can produce fatal poisoning; an equivalent dose through cigarettes would require a person to quickly smoke several packs. Smaller dosages can be dangerous for children who play with nicotine patches or gum or who consume tobacco.
Abuse factors.
As with many drugs, persons often find nicotine unpleasant at first but learn to ignore bad sensations and focus upon effects that are enjoyed. Experiments examining differences that users perceive in various drugs find that some sensations from nicotine, amphetamine, and cocaine are similar, so similar that in one experiment persons receiving injections of nicotine typically identified it as cocaine. A user can establish a physical dependence
with nicotine, causing withdrawal symptoms if dosage stops:
nervousness, tenseness, crankiness, lightheadedness, broken sleep, weariness, distractedness, tremors. These symptoms often last a few days, sometimes longer, and can relate to a person’s expectations (a psychosomatic component).
Debate exists about how addictive nicotine is. A study published in 1994 noted that about 33% of tobacco smokers become addicted. A study published in 2000 found that 20% to 60% of adolescent smokers are addicted. Many smokers with no interest in quitting can nonetheless substantially reduce their cigarette consumption with little difficulty. In contrast, many smokers wanting to stop find themselves unable to cease, and for them even pharmaceutical
nicotine can be an insufficient replacement for tobacco. Among such persons the persistence of a smoking habit suggests that something more than the drug nicotine is involved. Tobacco smoke contains thousands of chemical ingredients besides nicotine; perhaps some of the less-studied ones are important. In addition, the paraphernalia and mechanics of cigarette smoking provide a psychological buffer to users, allowing continual brief respites in interactions with other persons (such as breaking eye contact during a puff). Nicotine itself is a mild stimulant able to release adrenaline and increase pulse rate and blood pressure, with the physiological arousal produced by the drug masking physical arousal provoked by life’s tensions, thereby making smokers feel less nervous despite the stimulant effects. Smokers tend to have lower levels of body chemicals that are supplemented by antianxiety and antidepressant drugs.
Such pharmaceuticals, unfortunately, seemingly have little ability to help smokers quit their tobacco addiction.
As with any addiction, the power of nicotine and tobacco depends upon needs met by those substances. People do not smoke simply to avoid temporary withdrawal symptoms. If a person’s life is filled with situations that smoking eases like nothing else can, breaking the addiction is hard. If a person finds other ways of dealing adequately with those situations, desire for cigarettes can go away and never be bothersome again. Contrary to expectations of researchers, a laboratory test found nicotine to be no more appealing to exsmokers than to persons who have never smoked—a finding implying that life circumstances, and not just chemistry, determine this drug’s appeal.
Alcohol and illicit drug abusers reliably tend to be tobacco cigarette smokers, so reliably that the amount of tobacco use can be used to estimate the amount of cocaine and opiate usage by persons in drug abuse treatment programs.
An experiment found that persons smoked less tobacco when they had access to marijuana, suggesting that those persons used the two substances for similar purposes. Nonsmokers tend to avoid drug abuse, implying that smokers and nonsmokers use different strategies to cope with life’s challenges.
Cigarette smoking is more prevalent among schizophrenics, seriously depressed persons, and persons with low-grade psychiatric disturbance that may lack outward symptoms. Almost two thirds of smokers in one research project turned out to have a history of present or past psychiatric abnormality.
Among such individuals smoking may be a strategy of self-medication. One study found that withdrawal symptoms can depend on the extent to which the drug is used for self-medication.
Improvement has been measured in alertness, energy, and happiness as cigarette smokers start their day’s consumption in the morning. Conversely, cutting off a smoker’s supply of cigarettes produces measurable increases in fatigue, irritation, sadness, stress, and disorientation. New users do not get favorable effects sought by experienced users but instead have measurable nausea and general uneasiness. Among new users nicotine reduces job performance skills such as physical coordination and accuracy in memory tasks the opposite of what happens with experienced users.
Although pharmaceutical nicotine has various medical applications, its main use is for treatment of addiction to tobacco smoking. One authority aptly described nicotine chewing gum as the methadone of cigarettes, meaning that such a treatment strategy is intended to switch addicts from tobacco to pharmaceutical nicotine, just as treatment personnel seek to switch heroin addicts to methadone. Although such programs may have an official goal of eliminating a person’s addiction, in practice simply switching a person from a more harmful drug to a less harmful drug is often considered a success.Drug interactions. Nicotine interacts with commonly used medical drugs.
Antipsychotic drugs and the anti–blood clot medicine heparin flush from the body faster if a person uses nicotine. Nicotine also reduces the sedative effect of benzodiazepines and reduces pain relief from various opioids. Cigarette smoke acts as a monoamine oxidase inhibitor (MAOI), a type of chemical found in some antidepressants and that can have serious adverse effects when
used simultaneously with some medicines (though acute danger from cigarette interactions may be small). Caffeine seems to make nicotine more pleasurable.
Rat studies show that nicotine increases alcohol’s appeal and worsens pancreas inflammation caused by both drugs. Birth control pills increase the boost that nicotine gives to pulse rate, and some researchers speculate that such increase is related to the elevated risk of heart disease found among smokers who use birth control pills.
Cancer.
Tests indicate that pure nicotine (as opposed to smoke containing nicotine) does not cause cancer.
Pregnancy.
Smoking reduces female fertility according to most studies of the topic, and studies of Canadian farm couples and of men in the Netherlands found an apparent reduction in male fertility as well. Pregnant women who smoke tobacco increase the chance of miscarriage, premature birth, smaller full-term infants, and sudden infant death syndrome (SIDS or “crib death”).
The children are more likely to have muscle tone abnormalities. Smoking harms male and female gametes, damages chromosomes, and can change DNA in ways linked with childhood cancer. Nicotine usage by a pregnant woman changes movements and heart action of a fetus. One researcher warns that nicotine patches or chewing gum may deliver even more nicotine to a
fetus than smoking would. Nicotine enters the milk of nursing mothers. Rat experiments indicate that fetal exposure to nicotine combined with newborn exposure to nicotine in milk increases the risk of offspring developing lung trouble similar to emphysema. Human birth defects have been attributed to tobacco smoking. Although a study of teenage tobacco smokers did not see
any increased incidence of birth defects in their infants, research based on animal experimentation and published in 1998 declared that nicotine causes defects in fetal brain development leading to problems in thinking and learning that may not become apparent until years after birth. The children tend to have lower scores on psychological measurements, somewhat reminiscent of “cocaine babies,” deficits that continue for years. Some investigators see a link between pregnant smokers and offspring with psychological problems.
Investigators tracking mothers and daughters for three decades found that daughters were more likely to take up smoking if their mothers smoked during pregnancy.
Additional information.
Scientific studies find that “passive smoking” threatens health of bystanders who inhale smoke from tobacco products and exhalations of smokers. A study of spontaneous abortions found them more likely in pregnant nonsmoking women who inhale environmental smoke and use a lot of caffeine or a moderate amount of alcohol. Infants from nonsmoker women who were exposed to tobacco smoke during pregnancy are more likely to have lower birth weight and persistent pulmonary hypertension. Offspring also exhibit the same kinds of lower psychological test scores that are seen in children of active smokers. Inhalation of smoke by infants is suspected of
contributing to SIDS. For sure, compared to children in nonsmoking households, infants of smokers are hospitalized more often for pneumonia and bronchitis. The level of environmental smoke necessary for ill effects is often unclear in scientific studies; a person working in a poorly ventilated smokey bar for eight hours a day will have a considerably different exposure than
someone in a nonsmoking household who sits outside once a week with a friend who smokes a couple of cigarettes.
Additional scientific information may be found in:
Brown, C. “The Association between Depressive Symptoms and Cigarette Smoking in an Urban Primary Care Sample.” International Journal of Psychiatry in Medicine 30 (2000): 15–26.
Brown, K.G. “Lung Cancer and Environmental Tobacco Smoke: Occupational Risk to Nonsmokers.” Environmental Health Perspectives 107 (1999, Suppl. 6): 885–90.
Colby, S.M., et al. “Are Adolescent Smokers Dependent on Nicotine? A Review of the
Evidence.” Drug and Alcohol Dependence 59 (2000, Suppl. 1): S83–S95.
Dursun, S.M., and S. Kutcher. “Smoking, Nicotine and Psychiatric Disorders: Evidence
for Therapeutic Role, Controversies and Implications for Future Research.” Medical
Hypotheses 52 (1999): 101–9.
Haustein, K.O. “Cigarette Smoking, Nicotine and Pregnancy.” International Journal of
Clinical Pharmacology and Therapeutics 37 (1999): 417–27.
Parrott, A.C., and F.J. Kaye. “Daily Uplifts, Hassles, Stresses and Cognitive Failures:
In Cigarette Smokers, Abstaining Smokers, and Non-smokers.” Behavioural Pharmacology
10 (1999): 639–46.
Robinson, J.H., and W.S. Pritchard. “The Role of Nicotine in Tobacco Use.” Psychopharmacology
108 (1992): 397–407.
Stolerman, I.P., and M.J. Jarvis. “The Scientific Case That Nicotine Is Addictive.” Psychopharmacology 117 (1995): 2–10.
Van Gilder, T.J., P.L. Remington, and M.C. Fiore. “The Direct Effects of Nicotine Use
on Human Health.” Wisconsin Medical Journal 96 (1997): 43–48.