Thursday, September 17, 2015

30. Stimulants

Cocaine


Cocaine is a crystalline alkaloid that is obtained from the leaves of the coca plant. It is both a stimulant of the central nervous system and an appetite suppressant. Specifically, it is a dopamine reuptake inhibitor. It gives a feeling to what has been described as a euphoric sense of happiness and increased energy. It is most often used recreationally for this effect. For a thousand years, South American indigenous peoples have chewed the coca leaf that contains vital nutrients as well as numerous alkaloids, including cocaine. Cocaine in its purest form is a white, pearly product. Cocaine appearing in powder form is a salt. Its possession, cultivation, and distribution are illegal for non-medicinal and non-government sanctioned purposes in virtually all parts of the world.  
Like a lizard.


Cocaine, also known as benzoylmethylecgonine or coke, is a strong stimulant mostly used as a recreational drug.[9] It is commonly snorted, inhaled, or injected into the veins. Mental effects may include loss of contact with reality, an intense feeling of happiness, or agitation. Physical symptoms may include a fast heart rate, sweating, and large pupils.[8] High doses can result in very high blood pressure or body temperature.[10] Effects begin within seconds to minutes of use and last between five and ninety minutes.[8] Cocaine has a small number of accepted medical uses such as numbing and decreasing bleeding during nasal surgery.[11]
Cocaine is addictive due to its effect on the reward pathway in the brain. After a short period of use, there is a high risk that dependence will occur.[9] Its use also increases the risk of stroke, myocardial infarction, lung problems in those who smoke it, blood infections, and sudden cardiac death.[9][12] Cocaine sold on the street is commonly mixed with local anesthetics, cornstarch, quinine, or sugar which can result in additional toxicity.[13] Following repeated doses a person may have decreased ability to feel pleasure and be very physicially tired.[9]
Cocaine acts by inhibiting the reuptake of serotonin, norephinephrine, and dopamine. This results in greater concentrations of these three neurotransmitters in the brain.[9] It can easily cross the blood–brain barrier and may lead to the breakdown of the barrier.[14][15] Cocaine is made from the leaves of the coca plant which are mostly grown in South America.[8] In 2013, 419 kilograms were produced legally.[16] It is estimated that the illegal market for cocaine is 100 to 500 billion USD each year. With further processing crack cocaine can be produced from cocaine.[9]
After cannabis, cocaine is the most frequently used illegal drug globally.[17] Between 14 and 21 million people use the drug each year. Use is highest in North America followed by Europe and South America. Between one and three percent of people in the developed world use cocaine at some point in their life.[9] In 2013 cocaine use directly resulted in 4,300 deaths, up from 2,400 in 1990.[18] The leaves of the coca plant have been used by Peruvians since ancient times.[13] Cocaine was first isolated from the leaves in 1860.[9] Since 1961 the international Single Convention on Narcotic Drugs has required countries to make recreational use of cocaine a criminal offence.[19]

Kokain (auch Cocain) ist ein starkes Stimulans und Arzneimittel.[9] Es findet weltweit Anwendung als Rauschdroge mit hohem psychischen, aber keinem physischen[1] Abhängigkeitspotenzial. Chemisch-strukturell gehört es zu den Tropan-Alkaloiden und ist ein Derivat von Ecgonin. Verwendet wird oft das – im Gegensatz zur wenig wasserlöslichen freien Base[2] – besser lösliche Hydrochlorid.[3]

La cocaïne est un alcaloïde tropanique extrait de la feuille de coca. Psychotrope, elle est un puissant stimulant du système nerveux central, et sa consommation est addictive. Elle constitue également un vasoconstricteur périphérique. Elle est classifiée comme stupéfiant par la convention unique sur les stupéfiants de 1961 de l'ONU. Illégale dans tous les pays, elle est cependant dépénalisée dans quelques pays comme la République tchèque4 et le Portugal5. Un vaccin anti-cocaïne a été testé avec succès chez l'animal et chez l'homme, sans effets indésirables graves ; il semble être un traitement porteur d'espoir contre l'addiction à ce produit, sous réserve que des études faites à plus grande échelle confirment son innocuité.

La cocaína (benzoilmetilecgonina) (DCI) es un alcaloide tropano cristalino que se obtiene de las hojas de la planta de coca.5 El nombre viene de la Coca además del sufijo alcaloide -ina, formando cocaína.
Es un estimulante del sistema nervioso central, un supresor del apetito, y un anestésico tópico. Específicamente, es un inhibidor de la recaptación de serotonina-norepinefrina-dopamina (también conocido como un inhibidor de la recaptación triple (TRI)), que media en la funcionalidad de estos neurotransmisores como un ligando de transportador de catecolamina exógeno.
Es altamente adictiva debido a la forma en que afecta el sistema de recompensa mesolímbico. Entre otros efectos al consumirla provoca la agudización del estado de alerta y manía persecutoria. Además, incrementa la agresividad. 6
A diferencia de la mayoría de las moléculas, la cocaína posee bolsillos con alta eficiencia hidrófila y lipófila, vulnerando la regla de equilibrio hidrófilo-lipófilo. Esto provoca que cruce la barrera hematoencefálica con un refuerzo muy superior que otras sustancias químicas psicoactivas.
Su posesión, producción, y distribución son ilegales para fines sancionados no médicos y no gubernamentales en prácticamente todas las partes del mundo. A pesar de que su libre comercialización es ilegal y se ha visto severamente penalizada en casi todos los países, su uso en todo el mundo sigue siendo muy extenso en muchos ámbitos sociales, culturales y personales.
La hoja de coca es la única parte que contiene cocaína.

Methamphetamin


Methamphetamine (C10H15N) causes euphoria and excitement and thus it is prone to abuse and addiction. Users may become obsessed or perform repetitive tasks such as cleaning, hand-washing, or assembling and disassembling objects. Withdrawal is characterized by excessive sleeping, eating and depression-like symptoms, often accompanied by anxiety and drug-craving.


Methamphetamine[note 1] (contracted from N-methyl-alpha-methylphenethylamine) is a strong central nervous system (CNS) stimulant that is mainly used as a recreational drug. Methamphetamine hydrochloride is approved by the United States Food and Drug Administration (USFDA) under the trade name Desoxyn for attention deficit hyperactivity disorder and obesity in adults and children, and is sometimes prescribed off label for narcolepsy and idiopathic hypersomnia. It is rarely prescribed due to concerns involving human neurotoxicity, the availability of safer substitute drugs with comparable treatment efficacy, and the high potential for recreational use, among other concerns. Methamphetamine exists as two dextrorotary and levorotary enantiomers: dextromethamphetamine and levomethamphetamine.[note 2] Methamphetamine properly refers to a specific chemical, the racemic free base, which is an equal parts mixture of levomethamphetamine and dextromethamphetamine in their pure amine forms. Dextromethamphetamine is a stronger CNS stimulant than levomethamphetamine; however, both enantiomers are neurotoxic and addictive.
Both methamphetamine and enantiopure dextromethamphetamine are illicitly trafficked and sold due to their potential for recreational use as an aphrodisiac and euphoriant; the highest prevalence of illegal methamphetamine use occurs in parts of Asia, Oceania, and in the United States, where both racemic methamphetamine, levomethamphetamine, and dextromethamphetamine are classified as schedule II controlled substances; however, enantiopure levomethamphetamine is available as an over-the-counter drug for use as an inhaled nasal decongestant in the United States.[note 3] Internationally, the production, distribution, sale, and possession of methamphetamine is restricted or banned in many other countries due to its placement in schedule II of the United Nations Convention on Psychotropic Substances treaty. While enantiopure dextromethamphetamine is a more potent drug than racemic methamphetamine, the racemic form is sometimes produced and sold instead of dextromethamphetamine due to the relative ease of its synthesis by certain methods and the limited availability of associated chemical precursors.
In low doses, methamphetamine can elevate mood, increase alertness, concentration, and energy in fatigued individuals, reduce appetite and promote (initial) weight loss. At higher doses, it can induce psychosis, rhabdomyolysis and cerebral hemorrhage. Chronic high dose use can precipitate unpredictable and rapid mood swings, prominent delusions and violent behavior. Recreationally, methamphetamine's ability to increase energy has been reported to lift mood and increase sexual desire to an extent of users ability to engage in sexual activity continuously for several days.[16] Methamphetamine is known to have a high addiction liability (i.e., compulsive methamphetamine use) and dependence liability (i.e., withdrawal symptoms occur when methamphetamine use ceases). Heavy recreational use of methamphetamine may lead to a post-acute-withdrawal syndrome, which can persist for months beyond the typical withdrawal period.[i] Unlike amphetamine, methamphetamine is neurotoxic to humans, damaging both dopamine and serotonin neurons in the CNS.[i] Contrary to the long-term use of amphetamine,[iii] there is evidence that methamphetamine causes brain damage from long-term use in humans;[ii] this damage includes adverse changes in brain structure and function, such as reductions in grey matter volume in several brain regions and adverse changes in markers of metabolic integrity.[ii]
Methamphetamine belongs to the substituted phenethylamine and substituted amphetamine chemical classes. It is related to the other dimethylphenethylamines as a positional isomer of these compounds, which share the common chemical formula: C10H15N1.

Methamphetamin (N-methyl-alpha-Methylphenethylamin), auch Metamfetamin oder N-Methylamphetamin (früher auch Pervitin) genannt, ist eine synthetisch hergestellte Substanz aus der Stoffgruppe der Phenylethylamine. Sie wird in der Pharmazie als Arzneistoff verwendet und ist Bestandteil nicht-halluzinogener euphorisierender Drogen (umgangssprachlich Crystal Meth, Meth oder Crystal).
Methamphetamin gehört zur Substanzklasse der Amphetamine, der etliche weitere psychotrope Substanzen angehören, unter anderem Amphetamin und das in der Natur vorkommende Ephedrin. Es ist ein Stimulans und indirektes Sympathomimetikum, d. h. es regt die sympathischen Teile des vegetativen Nervensystems an.
Der Handel und Besitz von Methamphetamin ohne Erlaubnis ist in Deutschland und den meisten europäischen Ländern strafbar.

La méthamphétamine est une drogue de synthèse psycho-stimulante hautement addictive. Elle provoque une euphorie et une forte stimulation mentale.
Pure, la méthamphétamine se présente sous une forme solide cristalline (d'où sa dénomination de « crystal »), incolore et inodore, qui peut rappeler du verre pilé ou de la glace (d'où sa dénomination de « ice »)4. Elle se consomme généralement fumée dans une pipe.
Aux États-Unis, elle est aussi appelée meth, crystal meth, crystal, ice ou encore Tina. En Thaïlande, c’est yaa baa, le « médicament qui rend fou », où elle est présentée sous forme de cachets colorés et sucrés. La méthamphétamine et son chlorhydrate (sel de l'amine avec le chlorure d'hydrogène, HCl) ont par ailleurs de très nombreuses dénominations5. Au Japon, à Hong Kong, aux Philippines, en Malaisie et en Indonésie elle est connue sous l'appellation shabu. La méthamphétamine a été commercialisée sous diverses formes dont le Desoxyn, qui se présente sous forme de comprimés colorés et sucrés.
La méthamphétamine est également désignée au Canada sous les noms de : 222, beurre d'arachides, chalk, crank, glass, hawaiian salt, high speed, chicken feed, jib, koolaid, kryptonite, peach, pinotte, rock candy, sketch, soiks, speed, spooch, stove top, tweak, zip6.

La metanfetamina (desoxiefedrina) es un potente psicoestimulante. Es un agente agonista adrenérgico sintético, estructuralmente relacionado con el alcaloide efedrina y con la hormona adrenalina.
El compuesto es un líquido aceitoso a temperatura ambiente, insoluble en agua. El hidrocloruro de metanfetamina se presenta como cristales blancos, muy solubles en agua o etanol.

 Caffeine


Caffeine is a stimulant drug. Caffeine is found in varying quantities in the beans, leaves, and fruit of over 60 plants, where it acts as a natural pesticide that paralyzes and kills certain insects feeding on the plants. It is most commonly consumed by humans in infusions extracted from the beans of the coffee plant and the leaves of the tea bush. Caffeine is a central nervous system stimulant, having the effect of temporarily warding off drowsiness and restoring alertness. Beverages containing caffeine, such as coffee, tea, soft drinks and energy drinks enjoy great popularity; caffeine is the world's most widely consumed psychoactive substance, but unlike most other psychoactive substances, it is legal and unregulated in nearly all jurisdictions. In North America, 90% of adults consume caffeine daily.


Caffeine is a central nervous system (CNS) stimulant of the methylxanthine class of psychoactive drugs.[9] It is the world's most widely consumed psychoactive drug, but unlike many other psychoactive substances, it is legal and unregulated in nearly all parts of the world. It is a bitter, white crystalline purine, a methylxanthine alkaloid, and thus closely related chemically to the adenine and guanine contained in deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). It is found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia. The most well known source of caffeine is the seed (commonly incorrectly referred to as the "bean") of Coffea plants. Beverages containing caffeine are ingested to relieve or prevent drowsiness and to increase one's energy level. Caffeine is extracted from the plant part containing it for making beverages by steeping it in water, a process called infusion. These beverages are very popular; in North America, 90% of adults consume caffeine daily.[10]
Caffeine is classified by the Food and Drug Administration as "generally recognized as safe" (GRAS). Toxic doses, over 10 grams per day for an adult, are much higher than typical dose of under 500 milligrams per day. A cup of coffee contains 80–175 mg of caffeine, depending on what "bean" (seed) is used and how it is prepared (e.g. drip, percolation, or espresso). Thus it requires roughly 50–100 ordinary cups of coffee to reach a lethal dose. However pure powdered caffeine, which is available as a dietary supplement, can be lethal in tablespoon-sized amounts. There are several known mechanisms of action to explain the effects of caffeine. The most prominent is to reversibly block the action of adenosine on its receptor, which blocks the onset of drowsiness induced by adenosine. Caffeine also stimulates certain portions of the autonomic nervous system.
Caffeine can have both positive and negative health effects. It can be used to treat bronchopulmonary dysplasia of prematurity, and to prevent apnea of prematurity: caffeine citrate was placed on the WHO Model List of Essential Medicines in 2007.[11] It may confer a modest protective effect against some diseases,[12] including Parkinson's disease[13] and certain types of cancer. One meta-analysis concluded that cardiovascular disease such as coronary artery disease and stroke is less likely with 3–5 cups of non-decaffeinated coffee per day but more likely with over 5 cups per day.[14] Some people experience insomnia or sleep disruption if they consume caffeine, especially during the evening hours, but others show little disturbance. Evidence of a risk during pregnancy is equivocal; some authorities recommend that pregnant women limit consumption to the equivalent of two cups of coffee per day or less.[15][16] Whether or not caffeine is an addictive drug depends on how an addiction is defined. It can produce a mild form of drug dependence – associated with withdrawal symptoms such as sleepiness, headache, and irritability – when an individual stops using caffeine after repeated daily intake.[2][4][17] Tolerance to the autonomic effects of increased blood pressure and heart rate, and increased urine output, develops with chronic use (i.e., these symptoms become less pronounced or do not occur following consistent use).[citation needed]
Caffeine confers a survival advantage on the plant containing it in three ways. First, if it is ingested by an insect feeding on and potentially damaging or killing the plant, caffeine functions as a natural pesticide which can paralyze and kill the insect. Second, droppings from the plant infuse the surrounding soil with caffeine, which can inhibit the growth of and kill competing seedlings (and potentially its own progeny and itself). Third, caffeine can enhance the reward memory of pollinators such as honey bees, thus increasing the numbers of its progeny.



Coffein (auch Koffein, Tein oder Thein) ist ein Alkaloid aus der Stoffgruppe der Xanthine und gehört zu den psychotropen Substanzen aus der Gruppe der Stimulantien. Coffein ist der anregend wirkende Bestandteil von Genussmitteln wie Kaffee, Tee, Cola, Mate, Guaraná, Energy-Drinks und (in geringeren Mengen) von Kakao. In reiner Form tritt es als weißes, geruchloses, kristallines Pulver mit bitterem Geschmack auf.
Coffein ist weltweit die am häufigsten konsumierte pharmakologisch aktive Substanz.[3]

La caféine, aussi désignée sous les noms de théine, guaranine, 1,3,7-triméthylxanthine ou méthylthéobromine est un alcaloïde de la famille des méthylxanthines, présent dans de nombreux aliments, qui agit comme stimulant psychotrope et comme léger diurétique. La caféine a été découverte en 1819 par le chimiste allemand Friedlieb Ferdinand Runge. Il la nomma « kaffein » en tant que composé chimique du café, qui en français devint « caféine ».
La caféine est présente dans les graines, les feuilles et les fruits de différentes plantes où elle agit comme insecticide naturel14, paralysant15 ou tuant les insectes qui s'en nourrissent. La caféine, extraite des graines du caféier, est chimiquement identique à :
la guaranine, extraite de graines de guarana,
la matéine, contenu dans les infusions de feuilles de yerba maté,
et la théine, contenu dans les infusions de feuilles et bourgeons de théier.
C'est donc une même molécule, de formule brute C8H10N4O2, avec les mêmes effets - mais elle n'est consommée ni seule, ni de la même manière, ni à la même concentration. Ces noms sont donc synonymes et seule change la provenance.
Chez l'homme, la caféine agit comme stimulant du système nerveux central et du système cardio-vasculaire, diminuant la somnolence et augmentant l'attention temporairement. Des boissons très populaires contiennent de la caféine : café ou thé, certains sodas et boissons énergisantes à base de dérivés de la noix de kola qui en contient de grandes quantités. Le cacao consommé de diverses manières en contient aussi un peu.
De fait, la caféine est la substance psychoactive la plus consommée au monde ; elle est légale dans tous les pays à la différence d'autres substances psychoactives. En Amérique du Nord, 90 % des adultes consomment de la caféine quotidiennement. La Food and Drug Administration liste la caféine parmi les « substances alimentaires à buts multiples généralement reconnues comme sans danger » aux doses habituelles, mais toxique au-delà d'une certaine dose.

La cafeína es un alcaloide del grupo de las xantinas, sólido cristalino, blanco y de sabor amargo, que actúa como una droga psicoactiva, levemente disociativa y estimulante por su acción antagonista no selectiva de los receptores de adenosina.3 La cafeína fue descubierta en 1819 por el químico alemán Friedrich Ferdinand Runge: fue él quien acuñó el término Kaffein, un compuesto químico presente en el café, término que pasaría posteriormente al español como cafeína. La cafeína recibe también otros nombres (guaranina, teína, mateína) relativos a las plantas de dónde se puede extraer y porque contiene otras sustancias que aparecen en esos casos. La denominada guaranina del guaraná, y la teína del , son en realidad la misma molécula de cafeína, hecho que se ha confirmado en análisis de laboratorio. Estas plantas contienen algunos alcaloides adicionales como los estimulantes cardíacos teofilina y teobromina y a menudo otros compuestos químicos como polifenoles, que pueden formar complejos insolubles con la cafeína.
Es consumida por los humanos principalmente en infusiones extraídas del fruto de la planta del café y de las hojas del arbusto del , así como también en varias bebidas y alimentos que contienen productos derivados de la nuez de cola. Otras fuentes incluyen la yerba mate, el fruto de la Guaraná y el acebo de Yaupón.
En los humanos, la cafeína es un estimulante del sistema nervioso central que produce un efecto temporal de restauración del nivel de alerta y eliminación de la somnolencia. Las bebidas que contiene cafeína, tales como el café, el té, algunas bebidas no alcohólicas (especialmente los refrescos de cola) y las bebidas energéticas gozan una gran popularidad. La cafeína es la sustancia psicoactiva más ampliamente consumida en el mundo. En Norteamérica, el 90 % de los adultos consumen cafeína todos los días.[cita requerida] En los Estados Unidos, la Food and Drug Administration (Administración de Drogas y Alimentos) se refiere a la cafeína como una "sustancia alimentaria Generalmente Reconocida Como Segura (Generally Recognized As Safe) utilizada para múltiples propósitos".
La cafeína tiene propiedades diuréticas, si se administra en dosis suficientes a individuos que no tienen tolerancia a ella. Los consumidores regulares, sin embargo, desarrollan una fuerte tolerancia a este efecto, y los estudios generalmente no han podido demostrar la creencia general de que el consumo regular de bebidas cafeinadas contribuye significativamente a la deshidratación.

Nicotine


Nicotine is an alkaloid found in the nightshade family of plants, predominantly in tobacco and coca, and in lower quantities in tomato, potato, eggplant (aubergine), and green pepper. It functions as an antiherbivore chemical, being a potent neurotoxin with particular specificity to insects; therefore nicotine was widely used as an insecticide in the past, and currently nicotine derivatives such as imidacloprid continue to be widely used. In low concentrations, it acts as a stimulant in mammals and is one of the main factors responsible for the dependence-forming properties of tobacco smoking. According to the American Heart Association, "Nicotine addiction has historically been one of the hardest addictions to break." 


Nicotine is a potent parasympathomimetic alkaloid found in the nightshade family of plants (Solanaceae) and is a stimulant drug. Nicotine is a nicotinic acetylcholine receptor (nAChR) agonist,[3][4] (a Na/K ionophore through neural postsynaptic membranes in mammals and insects) except at nAChRα9 and nAChRα10 where it acts as an antagonist.[3] It is made in the roots of and accumulates in the leaves of the nightshade family of plants. Nicotine is found in the leaves of Nicotiana tabacum, the tobacco plant, and Nicotiana rustica in amounts of 2–14 %, as well as in Duboisia hopwoodii and Asclepias syriaca.[5]
It constitutes approximately 0.6–3.0% of the dry weight of tobacco[6] and is present in the range of 2–7 µg/kg of various edible plants.[7] It functions as an antiherbivore chemical; consequently, nicotine was widely used as an insecticide in the past[8][9] and neonicotinoids such as imidacloprid are currently widely used.
In lesser doses (an average cigarette yields about 2 mg of absorbed nicotine), the substance acts as a stimulant in mammals, while high amounts (50–100 mg) can be harmful.[10][11][12] This stimulant effect is the major contributing factor to the addictive properties of tobacco smoking. Nicotine is associated with cardiovascular disease, potential birth defects, and poisoning.[13] Laboratory studies have associated it with cancer, but nicotine outside tobacco has not been shown to be associated with cancer in the real world.[13]

Nicotin, auch Nikotin, ist ein natürlich in der Tabakpflanze sowie in geringerer Konzentration auch in anderen Nachtschattengewächsen vorkommendes Alkaloid. In der ganzen Tabakpflanze ist es mit einem Massenanteil von bis zu fünf Prozent enthalten. Selten werden Nicotinderivate als Nicotinoide[9] bezeichnet; meist sind damit die synthetischen, als Insektizide eingesetzten Neonicotinoide[10] gemeint.

La nicotine (qui doit son nom au fait que le tabac a été introduit en France par Jean Nicot7) est un alcaloïde présent dans les plantes de la famille des solanacées, notamment dans les feuilles de tabac. La nicotine confère aux plantes des propriétés acaricides, insecticides et fongicides.

La nicotina es un compuesto orgánico, un alcaloide encontrado principalmente en la planta del tabaco (Nicotiana tabacum), con alta concentración en sus hojas (constituye cerca del 5% del peso de la planta y del 3% del peso del tabaco seco)1 estando también presente en otras plantas de la familia Solanacea aunque de forma marginal (en el rango de 2–7 µg/kg), como en el caso del tomate, la berenjena, el pimiento y la patata.2 En cantidades aún más marginales, ha sido encontrado en otras plantas como la coliflor, la pimienta verde o el té negro.3 La nicotina debe su nombre a Jean Nicot, quien introdujo el tabaco en Francia en 1560. Se sintetiza en las zonas de mayor actividad de las raíces de las plantas del tabaco y es trasportada por la savia a las hojas verdes. El depósito se realiza en forma de sales de ácidos orgánicos.
Es un potente veneno e incluso se ha usado históricamente como insecticida.4 En bajas concentraciones, la sustancia es un estimulante y es uno de los principales factores de adicción al tabaco. Es polar y soluble en agua.
Methylphenidate 


Methylphenidate (MPH) is most commonly known by the trademark name Ritalin. It is a prescription stimulant commonly used to treat Attention-deficit hyperactivity disorder, or ADHD. It is also one of the primary drugs used to treat the daytime drowsiness symptoms of narcolepsy and chronic fatigue syndrome. The drug is seeing early use to treat cancer-related fatigue.
Like Nicotine with a tail.


Methylphenidate (trade names Concerta, Methylin, Medikinet, Ritalin, Equasym XL, Quillivant XR, Metadate) is a central nervous system (CNS) stimulant of the phenethylamine[3] and piperidine classes that is used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. Methylphenidate has been studied and researched for over 50 years and has a very good efficacy and safety record for the treatment of ADHD.[4] The original patent was owned by CIBA, now Novartis Corporation. It was first licensed by the U.S. Food and Drug Administration (FDA) in 1955 for treating what was then known as hyperactivity.
Prescribed to patients beginning in 1960, the drug has become increasingly prescribed since the 1990s, when the diagnosis of ADHD itself became more widely accepted.[5][6] Between 2007 and 2012 methylphenidate prescriptions increased by 50% in Britain and in 2013 global methylphenidate consumption increased to 2.4 billion doses, a 66% increase compared to the year before. The US continues to account for more than 80% of global consumption.[7][8]
ADHD and other similar conditions are believed to be linked to sub-performance of the dopamine and norepinephrine functions in the brain, primarily in the prefrontal cortex, responsible for self-regulatory function (e.g., inhibition, motivation, and memory) and executive function (e.g., reasoning, organizing, problem solving, and planning).[9][10] Methylphenidate's mechanism of action involves the inhibition of catecholamine reuptake, primarily as a dopamine reuptake inhibitor. Methylphenidate acts by blocking the dopamine transporter and norepinephrine transporter, leading to increased concentrations of dopamine and norepinephrine within the synaptic cleft. This effect in turn leads to increased neurotransmission of dopamine and norepinephrine. Methylphenidate is also a 5HT1A receptor agonist.[11]

Methylphenidat (kurz: MPH; Handelsname u. a. Ritalin) ist ein Arzneistoff mit stimulierender Wirkung. Er gehört zu den Derivaten des Amphetamins. Methylphenidat findet bei der medikamentösen Therapie der Aufmerksamkeitsdefizit-/Hyperaktivitätsstörung (ADHS) sowie der Narkolepsie Anwendung.

Le méthylphénidate ou MPH, est un stimulant du système nerveux central dérivé des pipéridines2et proche, d'un point de vue pharmacologique, des amphétamines. Il est utilisé en pharmacie pour la fabrication de psychostimulants. Sa principale indication est le trouble du déficit de l'attention avec ou sans hyperactivité (TDAH), et secondairement pour traiter la narcolepsie ou l'hypersomnie. On le retrouve dans différents médicaments sous les noms commerciaux de Ritalin(e) (Rilatine en Suisse romande et en Belgique, Ritalin en Suisse alémanique et au Québec), Concerta, Quasym ou Equasim, Focalin (forme dextrogyre), Biphentin (Québec) et Medikinet.

El metilfenidato, también abreviado como MFD, es un medicamento psicoestimulante aprobado para el tratamiento de trastorno por déficit de atención con hiperactividad, síndrome de taquicardia ortostática postural y narcolepsia. También podría ser prescrito para casos resistentes a tratamientos de fatiga y depresión. El MFD pertenece a la clase de compuestos piperidina e incrementa los niveles de dopamina y norepinefrina en el cerebro a través de la inhibición de recaptación de los respectivos transportadores de monoaminas. El metilfenidato posee similitudes estructurales a la anfetamina, pero su efecto no es el mismo.1 2 3
El MFD existe desde hace ya más de 60 años. Sin embargo, cobró especial notoriedad a partir de los años noventa. Esto se debió a la difusión del diagnóstico de trastorno por déficit de atención con hiperactividad (TDAH4 ) en niños y adultos, fenómeno unido a la prescripción del MFD, fármaco de elección para este tratamiento. A modo de ejemplo, Concerta (una de las tantas marcas de MFD) alcanzó en EE.UU. volúmenes de venta superiores a los 839 millones de dólares durante el año 2005.5
Tanto el diagnóstico como el fármaco han sido objetados desde diferentes perspectivas; la amplia documentación sobre sus efectos negativos, tanto a nivel físico como psicológico, tales como el desarrollo de comportamientos obsesivo-compulsivo, depresión, perdida de sociabilidad, han sido estudiados por científicos críticos de la medicalización con estimulantes.
Sin embargo, quienes aprueban el uso terapéutico del MFD atribuyen tal rechazo a un pánico moral6 del público no especializado ante el concepto de tratamiento medicamentoso en niños, o bien a creencias (muchas veces, infundadas) respecto de sus consecuencias.7 La temática ocupó a los medios de comunicación masiva, interviniendo figuras del psicoanálisis y de la antipsiquiatría.8
Las críticas al TDAH y al metilfenidato devienen, a menudo, de un rechazo al concepto general de disfunción neurobiológica y a los supuestos neuroquímicos que subyacen a las prácticas de la psiquiatría contemporánea. En 1998, un panel de expertos designado por los National Institutes of Health (NIH) de los Estados Unidos redactó un consenso procurando legitimar la entidad clínica de este trastorno y la necesidad de tratar el mismo.9 Hallazgos recientes en neurociencias, por ejemplo, los provistos por neuroimágenes, parecen ratificar el arraigo orgánico del síndrome, habiéndose identificado patrones específicos de expresión fisiológica. Por último, estudios en materia de herencia biológica han revelado una fuerte asociación de éste con determinados genes.10
Amphetamine 


Amphetamine is a prescription stimulant commonly used to treat attention-deficit hyperactivity disorder (ADHD) in adults and children. It is also used to treat chronic fatigue syndrome. Initially it was more popularly used to diminish the appetite and to control weight. Brand names of the drugs that contain amphetamine include Adderall and Dexedrine. The drug is also used illegally as a recreational club drug and as a performance enhancer.
Like an ant.


Amphetamine[note 1] (contracted from alphamethylphenethylamine) is a potent central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. Amphetamine was discovered in 1887 and exists as two enantiomers:[note 2] levoamphetamine and dextroamphetamine. Amphetamine properly refers to a specific chemical, the racemic free base, which is equal parts of the two enantiomers, levoamphetamine and dextroamphetamine, in their pure amine forms. However, the term is frequently used informally to refer to any combination of the enantiomers, or to either of them alone. Historically, it has been used to treat nasal congestion, depression, and obesity. Amphetamine is also used as a performance and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant. It is a prescription medication in many countries, and unauthorized possession and distribution of amphetamine are often tightly controlled due to the significant health risks associated with recreational use.[sources 1]
The first pharmaceutical amphetamine was Benzedrine, a brand of inhalers used to treat a variety of conditions. Currently, pharmaceutical amphetamine is prescribed as racemic amphetamine, Adderall,[note 3] dextroamphetamine, or the inactive prodrug lisdexamfetamine. Amphetamine, through activation of a trace amine receptor, increases biogenic amine and excitatory neurotransmitter activity in the brain, with its most pronounced effects targeting the catecholamine neurotransmitters norepinephrine and dopamine. At therapeutic doses, this causes emotional and cognitive effects such as euphoria, change in libido, increased wakefulness, and improved cognitive control. It induces physical effects such as decreased reaction time, fatigue resistance, and increased muscle strength.[sources 2]
Much larger doses of amphetamine may impair cognitive function and induce rapid muscle breakdown. Drug addiction is a serious risk with large recreational doses, but rarely arises from medical use. Very high doses can result in psychosis (e.g., delusions and paranoia) which rarely occurs at therapeutic doses even during long-term use. Recreational doses are generally much larger than prescribed therapeutic doses and carry a far greater risk of serious side effects.[sources 3]
Amphetamine belongs to the phenethylamine class. It is also the parent compound of its own structural class, the substituted amphetamines,[note 4] which includes prominent substances such as bupropion, cathinone, MDMA (ecstasy), and methamphetamine. As a member of the phenethylamine class, amphetamine is also chemically related to the naturally occurring trace amine neuromodulators, specifically phenethylamine[note 5] and N-methylphenethylamine, both of which are produced within the human body. Phenethylamine is the parent compound of amphetamine, while N-methylphenethylamine is a constitutional isomer that differs only in the placement of the methyl group.[sources 4]

Amphetamin (alpha-Methylphenethylamin), auch Phenylisopropylamin oder Amfetamin genannt, ist eine vollsynthetisch hergestellte Substanz aus der Stoffgruppe der Amphetamine. Sie findet derzeit in der Pharmazie als Arzneistoff zur Behandlung der Aufmerksamkeitsdefizit-/Hyperaktivitätsstörung (ADHS) sowie Narkolepsie Verwendung. Amphetamin wirkt stark stimulierend bzw. aufputschend, wie alle Amphetamine und die meisten Stimulanzien appetitzügelnd und euphorisierend und ist insbesondere in der Drogenszene unter Bezeichnungen wie Speed oder Pep(p) weit verbreitet.
Amphetamin ist die Stammverbindung der Substanzklasse Amphetamine, der etliche weitere psychotrope Substanzen angehören, unter anderem Methamphetamin und das in der Natur vorkommende Ephedrin. Es ist ein Stimulans und indirektes Sympathomimetikum, d. h., es regt die sympathischen Teile des vegetativen Nervensystems an.
Da Amphetamin in der Bundesrepublik Deutschland aufgrund seiner Aufführung in der Anlage III im Betäubungsmittelgesetz ein verkehrsfähiges und verschreibungsfähiges Betäubungsmittel darstellt, wird der Handel und Besitz ohne Erlaubnis strafrechtlich verfolgt.

L'amphétamine (DCI) est une substance sympathicomimétique aux effets anorexigènes et psychoanaleptiques. Dans la plupart des pays du monde, l'amphétamine est considérée comme un stupéfiant.
Le nom « amphétamine » trouve son origine de ses noms chimiques et est une abréviation dont l'étymologie est facile à comprendre : l'amphétamine, c'est une phénéthylamine à laquelle a été rajouté un groupement méthyle (-CH3) en position α (alpha) de sa chaîne, ce qui donne Alpha-Méthyl-Phénéthylamine ; c'est la version développée. Du nom "Alpha-Méthyl-PHÉnéThylAMINE" ne seront retenues par simplification que les lettres capitales, ce qui donne finalement : AMPHÉTAMINE. Par extension, un grand nombre de molécules similaires, ayant pour point commun un groupement méthyle (-CH3) en position α, sont appelées amphétamines.

La anfetamina es un agente adrenérgico sintético, potente estimulante del sistema nervioso central. La dexanfetamina (dextro-anfetamina), surge de la separación del compuesto racémico (d, l-anfetamina) en sus dos configuraciones ópticas posibles, y la extracción de aquella que corresponda isómero óptico dextrógiro.
La expresión anfetamininas (forma plural de la anterior) tiene al menos dos acepciones posibles. La más restringida, se usa para referir la tríada formada por las sustancias: anfetamina, dexanfetamina y metanfetamina. En tanto que la más general alude también a los estimulantes de tipo anfetamínico (ATS: acrónimo inglés de Amphetamine-Type Stimulants). Los ATS son la familia farmacológica integrada por compuestos con estructura química análoga o derivada de la molécula de anfetamina, con propiedades clínicas similares, y con grado de actividad farmacológica (potencia) comparable. Esta acepción es más frecuente, y es la que utilizaremos en este artículo (salvo indicación en contrario). Habilita para incluir también en el grupo de las sustancias anfetamínicas a estimulantes como el metilfenidato (análogo estructural) y el dexmetilfenidato; y a derivados químicos con propiedades entactógenas, como el MDMA; y anorexígenas, como el fenproporex, el dietilpropión (anfepramona), la fentermina, la benzfetamina, la fendimetrazina, siendo estas últimas las de menor potencia relativa.
La anfetamina es utilizada con fines terapéuticos, así como droga recreativa o para mejorar el rendimiento deportivo.
 

No comments:

Post a Comment