Amphetamines and Related Substances

Changes in the use of "amphetamines" (methamphetamine, amphetamine and related substances), 2005 (or latest year available)... 

Burma is second only to Afghanistan as an opium / heroin producer, but production of the illicit drug has been declining substantially, having fallen about 75 percent between 1996 and 2000. Burma remains the principal source of amphetamines and related substances to neighboring areas in Asia. 

Amphetamine and related substances (G) Amphetamine (I) Methamphetamine (I) Barbiturates (G, I) Benzodiazepines (G, I) Cannabinoids (G, I) Methadone/metabolites (G, I) Cocaine/metabolites (G, I) Methaqualone/metabolites (G, I) Opiates (G) Codeine (I) Dihydrocodeine (I) Morphine (I) Phencyclidine/metabolites (G, I) Propoxyphene/metabolites (G, I) Tricyclic antidepressants (G, I)... 

Amphetamine and related substances show symphaticomimetic and CNS stimulant activity. Amphetamines are indirect monoamine agonists and interact with the membrane transporters involved in neurotransmitter reuptake and vesicular storage systems. Therefore, they stimulate the release of norepinephrine, dopamine, and serotonin from presynaptic terminals in the CNS and at the peripheral level (De La Torre et al., 2004). Methamphetamine and the methylenedioxy derivatives (MDA, MDMA, MDEA, MBDB) can inhibit the activity of enzymes of dopamine or serotonin biosynthesis (De La Torre et al., 2004). 

De La Torre, R., M. Farrfe, M. Navarro, R. Pacifici, P. Zuccaro, and S. Pichini. 2004. Clinical pharmacokinetics of amphetamine and related substances. Monitoring in conventional and non-conventional matrices. Clin. Pharmaco. 43 158-185. 

The adverse effects of amphetamine and related sympathomimetic appetite suppressants are well documented. All of these agents are classified by the U.S. Drug Enforcement Administration (DEA) as controlled substances (classes II-IV) according to their potential for causing addiction (see Table 15.4). Class II agents such as amphetamine are highly abused, with prescription restricted to speeial circumstances class TV anorectic drugs such as sibutramine, phentermine, di-ethylpropion, and mazindol have minimal abuse potential. 

Glassification of Substance-Related Disorders. The DSM-IV classification system (1) divides substance-related disorders into two categories (/) substance use disorders, ie, abuse and dependence and (2) substance-induced disorders, intoxication, withdrawal, delirium, persisting dementia, persisting amnestic disorder, psychotic disorder, mood disorder, anxiety disorder, sexual dysfunction, and sleep disorder. The different classes of substances addressed herein are alcohol, amphetamines, caffeine, caimabis, cocaine, hallucinogens, inhalants, nicotine, opioids, phencyclidine, sedatives, hypnotics or anxiolytics, polysubstance, and others. On the basis of their significant socioeconomic impact, alcohol, nicotine, cocaine, and opioids have been selected for discussion herein. 

Comorbid dysthymia and substance disorder. A total of 642 patients were assessed. Thirty-nine had substance-related disorder and dysthymia (SRD-dysthymia) and 308 had SRD only. Data on past use were collected by a research associate using a questionnaire. The patients with SRD-dysthymia and SRD did not differ with regard to use of alcohol, tobacco, and benzodiazepines. The patients with SRD-dysthymia started caffeine use at an earlier age, had shorter use careers of cocaine, amphetamines, and opiates, and had fewer days of cocaine and cannabis use in the last year. They also had a lower rate of cannabis... 

In units terms, more than half of all seizures (59 %) are cannabis, followed by coca related substances (24 %), opiates (12 %) and amphetamine-type stimulants (4%). While cannabis leads the table, irrespective of the measurement used, it may be interesting to note that in terms of drug units seized, cocaine ranks second. In terms of... 

MOTHER NATURE S AMPHETAMINES Amphetamine does not occur naturally, but some substances found in nature are chemically related to amphetamine and have similar effects on the brain. Ephedrine can be found in Ephedra sinica, which has been used in traditional Chinese medicine and is known as ma huang. Its effects on the sympathetic nervous system are similar to amphetamine. However, this extract never achieved complete success as a psychoactive stimulant, primarily because it does not cross the blood—brain barrier as effectively as amphetamine. 

All amphetamines are synthetic, or manufactured, substances derived from alpha-methyl-beta-phenyl-ethyl-amine, a colorless liquid consisting of carbon, hydrogen, and nitrogen. In terms of their chemical structures, amphetamines are related to two natural substances known to boost energy within the human body. Those substances are ephedrine and adrenaline. Ephedrine is a natural stimulant found in plants of the genus Ephedra. It... 

One of the most controversial CNS-acting drugs in contemporary society is methylphenidate (Ritalin ). This drug is structurally related to amphetamine and is a mild stimulant that has abuse potential similar to amphetamine. Methylphenidate is classified as a Schedule II controlled substance. It is effective in the treatment of narcolepsy and attention-deficit hyperactivity disorder (ADHD). Its use in ADHD has caused the greatest controversy. 

Neuromessenger Releasers. Normal CNS functioning could be disrupted by evoking premature or continued release of neuromessengers from presynaptic stores. Although D(+)-amphetamine, a well-known psychostimulant and appetite depressant, does not occur in plants, a closely-related substance, DL-cathinone, does occur. It is found in the leaves of the khat shrub, Catha edulis, which grows in East Africa and in the Arab peninsula. Cathinone evokes the release of norepinephrine from central and peripheral presynaptic stores and has cardiovascular and appetite depressing effects similar to D-amphetamine (23). 

Complications of drug analysis were successfully resolved by the combination of TLC with MALDI-MS. TLC combined with MALDI-MS was used for analysis of psychotropic drugs (3,4-methylenedioxy methamphetamine, 4-hydroxy-3-methoxy methamphetamine, 3,4-methylenedioxy amphetamine, methamphetamine, p-hydroxy methamphetamine, amphetamine, ketamine, caffeine, chlorpromazine, triazolam, and morphine) in biological samples [42]. This technique was able to analyze 3,4-methylenedioxy methamphetamine (MDMA) and its metabolites in urine samples without sample dilution, and the detection limit of the MDMA spot was 0.05 ng/ spot. Crecelius and coworkers described the use of TLC with MALDI-MS/MS for the structural analysis of small drug molecules [43]. This method was successfully applied to analyze two representatives of nonsteroidal antiinflammatory drugs (tenoxi-cam and piroxicam), and pharmaceutically active compound UK-137,457 and one of its related substances UK-124,912. The feasibility of UTLC-atmospheric pressure (AP)-MALDI-MS was described for the analysis of small molecules (triazole, midazolam, verapamil, and metaprolol) [44]. The authors compared the selectivity and sensitivity between UTLC- and HPTLC-AP-MALDI-MS. It was observed that UTLC plates provided 10-100 times better sensitivity in MALDI analysis than the conventional... 

A generic term relating to psychological and/a physical dependence when one or mae psychoactive substances or classes of psychoaaive substances are abused (alcohol sedatives, hypnotics and anxiolytics cannabis opioids cocaine amphetamine and other sympathomimetics hallucinogens caffeine nicotine ... 

Non-Phenethylamine Derivatives - The search for compounds which bear no structural relationship to phenethylamlnes and have anorectic properties continues. Current studies on Wy-5244 (XIV) show it to possess only weak sympathomimetic activity in isolated cat atria and rabbity aortic strips however the compound apparently does alter adrenergic receptor mechanisms since the actions of substances such as norepinephrine, d-amphetamine, phenoxybenzamine, and Imlpramine were profoundly influenced by Wy-5244.31 The synthesis of (XIV) and related compounds has been described.32... 

Substances related to Stimulants such as Amphetamine and its derivatives Sympathomimetic amines... 

Dyn is not yet known, it is likely that such changes reflect variations in the activity of the associated pathways. One possible explanation is that increases in neuropeptide tissue levels are due to decreased release of the transmitter, which dunmishes the extracellular peptide metabolism and results in accumulation of these peptide substances. Another possible contributing factor is a drug-related alteration in neuropeptide synthesis. For example, Bannon et al. (1987) reported that METH administration increased the quantity of striatal messenger RNA for the SP precursor preprotachykinin. Thus, increases in peptide synthesis might contribute to increases in peptide content caused by treatment with METH or the other amphetamine analogs. 

MDMA s history dates to the early years of the 20th century when researchers at the German pharmaceutical company Merck discovered the compound and a number of related amphetamine analogs, including 3,4-methylenedioxyamphetamine (MDA) and 3,4-methyl-enedioxy-N-ethylamphetamine (MDEA). Merck s research began as an attempt to discover a substance that could be used as a vasoconstrictor, a substance that causes a narrowing of blood vessels and can be used to reduce bleeding. 

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