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Amphetamine

Amphetamine (Alpha-Methyl-PHenEThylAMINE), also known as speed, is a synthetic stimulant used to suppress the appetite, control weight, and treat disorders including narcolepsy and Attention-deficit hyperactivity disorder. It is also used recreationally and for performance enhancement (these uses are illegal in most countries). more...

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Due to the widespread use of amphetamines as a treatment for ADD/ADHD in the USA, they frequently find their way onto the street and are one of the most frequently-abused drugs in high schools and colleges.

Patients with acute toxicity from amphetamines may have symptoms of lock-jaw, diarrhea, palpitations, arrhythmia, syncope, hyperpyrexia, and hyperreflexia progressing to convulsions and coma. Patients with chronic use of amphetamines develop a rapid tolerance to the drug and may have to increase the number of pills to reach a desired affect and eventually develop addiction. Patients that develop addiction show symptoms of restlessness, anxiety, depression, insomnia, and suicidal behavior. A urine drug screen can be performed to determine the presence of amphetamines. Patients may need to be hospitalized. Supportive therapy is important. Cooling blankets may be used for hyperthermia. Sedation may be obtained with lorazepam or diazepam. Haloperidol may be given for agitation and delusions. Hypertension and arrhythmias should be treated.

Pharmacology

Amphetamine is a synthetic drug with strong stimulant effects. In the United States, it is most commonly used for treatment of attention-deficit disorders and narcolepsy, but is also approved as a weight-loss medication in certain cases of obesity. Within the armed forces only, it is also frequently prescribed as an anti-fatigue pill for pilots and other individuals in situations requiring vigilance and alertness. Amphetamine is also used illegally to take advantage of these effects.

The term amphetamine causes a certain amount of confusion because it is often used incorrectly. In the general sense, amphetamine can describe other drugs with similar, stimulant effects, namely methamphetamine and methylphenidate. Chemists often use the term "amphetamine class" to describe chemicals that are structurally similar (and often similar in effect as well) to amphetamine - namely, chemicals with an ethyl backbone, terminal phenyl and amine groups, and a methyl group adjacent to the amine. A large number of chemicals fall into this category, including the club drug MDMA (Ecstasy) and methamphetamine. It is important to note that such an "amphetamine class" does not technically exist. In the pharmacodynamic sense, these drugs all fall under the umbrella of central nervous system stimulants; in the chemical sense, they are phenylethylamines. Amphetamine, for example, is methylated phenylethylamine, and methamphetamine is double-methylated phenylethylamine.

Amphetamine traditionally comes in the salt-form amphetamine sulphate and is comprised of 50% l-amphetamine and 50% d-amphetamine (where l- and d- refer to levo and dextro, the two optical orientations the amphetamine structure can have). In the United States, pharmaceutical products containing solely amphetamine (for example, Biphetamine) are no longer manufactured. Today, dextroamphetamine (d-amphetamine) sulphate is the predominant form of the drug used; it consists entirely of d-isomer amphetamine, which acts in a slightly different way on the brain than does l-amphetamine. Attention disorders are often treated using Adderall or generic-equivalent formulations of mixed amphetamine salts that contain both d/l-amphetamine and d-amphetamine in the sulfate and saccharate forms mixed to a final ratio of 3 parts d-amphetamine to 1 part l-amphetamine.

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They're synthetic. They're clandestine. They can heal. They can kill - amphetamine-type stimulants
From UN Chronicle, 6/22/98 by Sandeep Chawla

The ancient Greek word pharmakon meant both medicine and poison. It was the quantity, dose and pattern of use which determined the difference between one and the other, between use and abuse, recalls Sandeep Chawla, Senior Research Coordinator, UNDCP, in this contribution to the Chronicle.

Today, astonishing changes, many of them largely unnoticed, are taking place in the grey world of drag trafficking and abuse. The most significant of these is probably the emergence of clandestine synthetic drugs as a global problem. Recognition of this problem has long been delayed by control systems, national and international, which are mesmerized by the three "classical", botanical drugs: cocaine, heroin and cannabis. Present debates about the validity of controlling cannabis under the same strict regime as cocaine and heroin continue to divert attention from tackling the problem of clandestine synthetic drugs.

Another source of difficulty is the sheer complexity of the synthetic drug problem. Psychoactive drugs - drugs whose pharmacological effect is on the central nervous system (CNS) of the body - have been around for millennia: opium, coca leaf, betel nuts, even tea. They have always had a dual nature and switchback quality. They could be used medicinally, or they could be poisonous or toxic. The development of science and technology gradually perpetuated this duality. The effects of the drug, which were sought by the abuser, were precisely those which were treated as unwanted side-effects in medicine. Pharmaceutical research on CNS-active drugs was thus set on the path of finding ever greater benefit-to-risk ratios - effort to separate the desirable (therapeutic) effects from the undesirable (addictive) side-effects.

Starting from the nineteenth century, when the active ingredients of many plants were chemically isolated or extracted - for example morphine, caffeine, ephedrine and cocaine - a more complex category of semi-synthetic drags was created. These were still, however, based on the chemical and pharmacological models of the old natural drugs, which were the essential raw material. Only at the end of the nineteenth and the early twentieth centuries did a class of fully synthetic drugs emerge. These are substances which have no counterpart in nature and can be produced in unlimited amounts from readily available chemicals. Many of these drugs were designed as structural modifications of naturally occurring drugs, with similar though more specific or enhanced therapeutic effects.

Technological progress, allowing for the use of refined natural products or purely synthetic substances, was clearly a milestone in modern medicine. Yet the duality of the drug problem was still in evidence. A new era in the abuse of psychoactive drugs began. This implies the use of potent and pure substances instead of the plant material which contains the active ingredient together with other compounds - the distinctions, for example, between heroin and opium, or cocaine and the coca leaf. Or, as examples of fully synthetic drugs, amphetamine and methamphetamine, which have no botanical raw material, yet substitute the CNS-stimulant effect of cocaine. Another characteristic of the new era of drug abuse is the shift from instrumental use to recreational use. The former means the use of pharmaceutical products as a means to an end, such as medication or improving occupational performance. Recreational use means use as an end in itself, aimed exclusively at experiencing the pharmacological effects of the drags. As recreational use grows, the next stage is obviously the appearance on illicit markets of new drugs with no therapeutic use, designed exclusively for psychoactive mind-altering purposes.

Among the bewildering array of synthetic drugs available in illicit markets, the most common are probably a group of CNS-stimulants which share the basic chemical structure of amphetamine. They are consequently known as amphetamine-type stimulants (ATS) and provide a test case to illustrate the problem of synthetic drugs, of how to control them and how the shift from licit manufacture and use to illicit synthesis and abuse takes place.

ATS include two subgroups with slightly different pharmacological properties: the amphetamine group and the ecstasy group. The former includes amphetamine, methamphetamine and methcathinone. Most of them were developed as therapeutic drugs: amphetamine in 1887; methamphetamine in 1919. They began to appear in pharmaceutical markets in the 1930s. Their therapeutic utility was over-rated, primarily because they not only enhanced performance and endurance, but also had an anorectic (weight-losing) effect. They were widely used among combatants in both sides during the Second World War. Oversupply from licit sources created the first amphetamine epidemics after the war. The risks and addictive potential gradually became evident, and the amphetamine group now has few legitimate medical uses: for narcolepsy, obesity and attention deficit disorder. Illicit manufacture has meanwhile swollen to fulfil expanding demand.

The substance known commonly as "ecstasy" (MDMA) has given its name to a whole range of related substances. They are sometimes called the hallucinogenic amphetamines because, in addition to the CNS-stimulant effect, they produce effects of empathy, loquacity and serenity. MDMA was synthesized in 1914, but not used until the 1970s when its capacity to foster inter-personal communication gave it some uses in psychotherapy. Its dangerous potential was only recognized in the mid- 1980s, by when its abuse had spread widely, closely tied to the dance and "rave" subculture. It was then put under stringent international control.

Growth rates through the 1990s in the manufacture, trafficking and abuse of ATS have even surpassed those of heroin and cocaine. The challenges posed by ATS can be seen in at least four areas. First, the expanding demand for them. The need for stimulants in a modern performance-oriented society is self-evident. Their recreational use, particularly of the ecstasy group, is expanding among younger sections of the population. Patterns of use, and even the drugs themselves, are quite different from the "classical" drugs, and their image is simultaneously benign and modern in comparison.

Secondly, the information age exacerbates the problem. Modern information technology has expanded public access to information on recipes and techniques for clandestine manufacture: what precursor chemicals to use; where they are available; what techniques can be used to evade control; and how one might set up a simple "kitchen lab" in one's backyard.

Thirdly; ATS have a double supply system: diversions from licit pharmaceutical trade or licit trade in chemicals, as well as illicit manufacture. Controlling the supply of synthetic drugs is difficult, because there are neither any easily identifiable botanical raw materials to target nor any long trafficking mutes linking production and consumption areas to interdict. Clandestine ATS are usually made from precursor chemicals, in or close to the area of final consumption. The precursor control regime is still young, since it only began with the 1988 Convention against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. In any case, it is not feasible to put all possible precursors for ATS under international control because they have a vast amount of licit industrial uses.

Finally, the present control system - the 1971 Convention on Psychotropic Substances - is simply inadequate for controlling illicit markets. It was developed to resolve the dilemma of duality discussed above: to distinguish between the therapeutic potential and public health risk of particular drugs, which were put into a sliding scale of four schedules, with those in Schedule I having the highest public health risk, and those in Schedule IV having the greatest therapeutic potential. But the scheduling process is slow and cumbersome; individual substances, rather than chemically or pharmacologically-related classes of drugs, are put under control. New individual substances with no therapeutic potential, structurally different though pharmacologically similar (the ATS "analogues"), perpetually appear on illicit markets. They cannot be scheduled fast enough. The control regime is thus bound to lag behind illicit innovation.

These four challenges - demand, information, supply and control system - are now at the heart of an international Action Plan against the Manufacture, Trafficking and Abuse of ATS. Representing the culmination of an applied research process which began at the United Nations International Drug Control Programme (UNDCP) in 1996 and went through scientific study and investigation, expert consultations and political negotiation in the Commission on Narcotic Drugs, the Action Plan will go before the Special Session of the General Assembly in June 1998. If adopted, it will provide the nuts and bolts of a strategy to tackle the most serious drug problem of the next century.

Fact: In recent years, the amount of stimulants, sedatives and hypnotics diverted into illicit channels has totalled several tonnes, representing hundreds of millions of tablets - or street doses.

COPYRIGHT 1998 United Nations Publications
COPYRIGHT 2004 Gale Group

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