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Amphetamine
Systematic (IUPAC) name
1-phenylpropan-2-amine
Identifiers
CAS number 300-62-9
405-41-4 (hydrochloride), 60-13-9 (sulfate)
ATC code N06BA01
PubChem 3007
DrugBank APRD00480
Chemical data
Formula C9H13N 
Mol. mass 135. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System containing Psychoanaleptics. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 2084
SMILES eMolecules & PubChem
Synonyms (±)-alpha-methylbenzeneethanamine, alpha-methylphenethylamine, beta-phenyl-isopropylamine
Physical data
Melt. point 280–281 °C (536–538 °F)
Solubility in water 50–100 mg/mL (16C°) mg/mL (20 °C)
Pharmacokinetic data
Bioavailability Oral "good"[1]; nasal 75%; rectal 95–99%; intravenous 100%
Protein binding 15–40%
Metabolism Hepatic (CYP2D6[2])
Half life 10 hours for d-isomer, 13 hours for l-isomer
Excretion Renal; significant portion unaltered
Therapeutic considerations
Pregnancy cat.

C(US)
Legal status

Controlled (S8)(AU) Schedule III(CA) Class B(UK) Schedule II(US) Prescription-Only Medicine
Routes Oral, intravenous, vaporization, insufflation, suppository, sublingual

Amphetamine is a prescription CNS stimulant commonly used to treat attention-deficit disorder (ADD) and attention-deficit hyperactivity disorder (ADHD) in adults and children. This article deals with the general meaning of the term "synonym" The melting point of a solid is the temperature range at which it changes state from solid to Liquid. Solubility is the characteristic Physical property referring to the ability of a given substance the Solute, to dissolve in a Solvent. Water ( H2[[oxygen O]] H OH) is the most abundant Molecule on Earth 's surface composing of about 70% of the Earth's surface as In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. 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For a topic outline on this subject see List of basic Australia topics. The Controlled Drugs and Substances Act is Canada 's federal drug control statute Country to "Dominion of Canada" or "Canadian Federation" or anything else please read the Talk Page The Misuse of Drugs Act 1971 (c38 is an Act of Parliament, by which the United Kingdom aims to control the possession and supply of numerous drugs The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located The Controlled Substances Act ( CSA) was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control The United States of America —commonly referred to as the In Pharmacology and Toxicology, a route In Pharmacology and Toxicology, a route Evaporation is the process by which Molecules in a Liquid state (e Insufflation (Latin insufflatio "blowing on or into" is the practice of inhaling substances into a Body cavity. A suppository is a drug delivery system that is inserted either into the Rectum (rectal suppository Vagina (vaginal suppository or Urethra (urethral In Vertebrates the central nervous system ( CNS) is the part of the Nervous system which is enclosed in the Meninges. ADHD predominantly inattentive (ADHD-I is one of the three subtypes of Attention-deficit hyperactivity disorder (ADHD Attention-Deficit Hyperactivity Disorder (ADHD is a neurobehavioral developmental disorder affecting about 3-5% of the world's population It is also used to treat symptoms of traumatic brain injury and the daytime drowsiness symptoms of narcolepsy and chronic fatigue syndrome. Traumatic brain injury (TBI also called intracranial injury, occurs when Physical trauma injures the Brain. Narcolepsy is a Neurological condition most characterized by Excessive Daytime Sleepiness (EDS in which a person falls asleep during the day at inappropriate Chronic fatigue syndrome ( CFS) is the most common name given to a poorly understood variably debilitating disorder or disorders of uncertain causation Initially it was more popularly used to diminish the appetite and to control weight. Note "Anorectic" is also a term for an anorexic person a person suffering from Anorexia nervosa Anorectics, anorexigenics Brand names of the drugs that contain amphetamine include Adderall and Dexedrine. Adderall is a brand-name pharmaceutical Psychostimulant composed of mixed Amphetamine salts, the actions of which are Sympathomimetic Dextroamphetamine is a Psychostimulant which produces increased wakefulness energy and self-confidence in association with decreased fatigue and appetite The drug is also used illegally as a recreational club drug and as a performance enhancer. Club drugs are a loosely-defined category of Recreational drugs which are associated with discothèques in the 1970s and Dance clubs parties and Raves in The name amphetamine is derived from its chemical name: alpha-methylphenethylamine. The name is also used to refer to the class of compounds derived from amphetamine, often referred to as the substituted amphetamines. The substituted Amphetamines are a family of amphetamine-based Stimulants, Hallucinogens, and other Recreational drugs.

Contents

History

Amphetamine was first synthesized in 1887 by Lazăr Edeleanu in Berlin, Germany. Lazăr Edeleanu (1861-1941 was a Romanian Chemist of Jewish origin Berlin is the capital city and one of sixteen states of Germany. [3] He named the compound phenylisopropylamine. It was one of a series of compounds related to the plant derivative ephedrine, which had been isolated from Ma-Huang that same year by Nagayoshi Nagai. Ephedrine (EPH is a Sympathomimetic Amine commonly used as a Stimulant, appetite suppressant concentration aid Decongestant, and to treat ( 8 August 1844 - 10 February 1929) was a notable Japanese Organic chemist and Pharmacologist, best known for [4] No pharmacological use was found for amphetamine until 1929, when pioneer psychopharmacologist Gordon Alles resynthesized and tested it on himself, in search of an artificial replacement for ephedrine. Psychopharmacology (from Greek grc ψῡχή psȳkhē, "breath life soul" grc φάρμακον pharmakon, "drug" and grc -λογία From 1933 or 1934 Smith, Kline and French began selling the volatile base form of the drug under the name Benzedrine Inhaler, useful as a decongestant (and readily usable for non-medical purposes too). GlaxoSmithKline plc () is a United Kingdom -based pharmaceutical, biological and Healthcare Company. Benzedrine is the trade name of the Racemic mixture of Amphetamine (dl-amphetamine [5] During World War II amphetamine was extensively used to combat fatigue and increase alertness in soldiers. After decades of reported abuse, the FDA banned Benzedrine inhalers, and limited amphetamines to prescription use in 1965, but non-medical use remained common. Benzedrine is the trade name of the Racemic mixture of Amphetamine (dl-amphetamine Amphetamine became a schedule II drug under the Controlled Substances Act in 1971. The Controlled Substances Act ( CSA) was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control

The related compound methamphetamine was first synthesized from ephedrine in Japan in 1918 by chemist Akira Ogata via reduction of ephedrine using red phosphorus and iodine. Akira Ogata (Ogata Akira 緒方 章 1887-1978 was a Japanese Chemist and the first to synthesize Methamphetamine in crystalline form in 1919 Elemental Phosphorus can exist in several allotropes; the most common of which are white and red Iodine (ˈaɪədaɪn ˈaɪədɪn or /ˈaɪədiːn/ from ιώδης iodes "violet" is a Chemical element that has the symbol I and Atomic The German military was notorious for their use of methamphetamine in World War II. World War II, or the Second World War, (often abbreviated WWII) was a global military conflict which involved a majority of the world's nations, including It is also rumored that Adolf Hitler was receiving daily shots of a medicine that contained certain essential vitamins and amphetamines. The pharmaceutical Pervitin was a tablet of 3 mg methamphetamine which was available in Germany from 1938 and widely used in the Wehrmacht, but by mid-1941 it became a controlled substance, partly because of the amount of time needed for a soldier to rest and recover after use and partly because of abuse. For the rest of the war military doctors continued to issue the drug, but ever less frequently, and with increasing discrimination as the war progressed onwards towards Nazi Germany's and the Axis' eventual defeat in 1945. [6]

In 1997[7] and 1998,[8] researchers at Texas A&M University reported finding amphetamine and methamphetamine in the foliage of two Acacia species native to Texas, A. berlandieri and A. rigidula. Texas A&M University, often called A&M or TAMU, is a Coeducational public Research University located in College Station Acacia is a Genus of Shrubs and Trees belonging to the Subfamily Mimosoideae of the family Fabaceae, first Texas ( is a state geographically located in the South Central United States and is also known as the Lone Star State. Acacia berlandieri ( Berlandier Acacia, Guajillo Acacia, guajillo, huajillo) is a Shrub native to the Southwestern Acacia rigidula is native to Mexico and the southern US ( Texas) and is closely related to Acacia berlandieri. Previously, both of these compounds had been thought to be human inventions. [9]

Indications

Indicated for:
Contraindications:
  • CNS Stimulants
  • Agitated states
  • Patients with a history of drug abuse
  • Glaucoma
  • MAOI use
Adverse effects:
Other information:

Neuropharmacology:

Along with methylphenidate (Ritalin, Concerta, etc. Note "Anorectic" is also a term for an anorexic person a person suffering from Anorexia nervosa Anorectics, anorexigenics ADHD predominantly inattentive (ADHD-I is one of the three subtypes of Attention-deficit hyperactivity disorder (ADHD Attention-Deficit Hyperactivity Disorder (ADHD is a neurobehavioral developmental disorder affecting about 3-5% of the world's population Narcolepsy is a Neurological condition most characterized by Excessive Daytime Sleepiness (EDS in which a person falls asleep during the day at inappropriate Major depressive disorder, also known as major depression, unipolar depression, unipolar disorder, clinical depression, or simply depression In Medicine, a contraindication (pronounced as contra-indication is a condition or factor that increases the Risks involved in using a particular drug, Monoamine oxidase inhibitors ( MAOIs) are a class of powerful antidepressant drugs prescribed for the treatment of depression. An adverse drug reaction (abbreviated ADR) or adverse drug event (abbreviated ADE) is an expression that describes the unwanted negative consequences This is an article about the rock music band "Circulatory System" Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels particularly the large Arteries, Arterioles A palpitation (medical term ectopic heart beat) is an abnormal awareness of the beating of the Heart, whether it is too slow too fast irregular The ear is the sense organ that detects Sounds The Vertebrate ear shows a common biology from Fish to Humans with variations Anatomically a nose is a protuberance in Vertebrates that houses the Nostrils or nares which admit and expel air for respiration in conjunction with the In Anatomy, the throat is the anterior part of the Neck, in front of the vertebral column. A decongestant is a broad class of Medications used to relieve Nasal congestion. Xerostomia is the medical term for a dry mouth due to a lack of Saliva. Eyes are organs that detect Light, and send signals along the Optic nerve to the visual areas of the brain "Dilated pupil" redirects here An Eye examination sometimes requires the dilation of the pupil In the Esophagus After food is chewed into a bolus it is swallowed to move it into the esophagus Muscle (from Latin musculus, diminutive of mus "mouse" is contractile tissue of the body and is derived from the In Biology, the skeleton is a strong and often a rigid framework that supports the body of an animal holding it upright and giving it shape and strength (Also skeletal In Animal physiology, respiration is the transport of Oxygen from the outside air to the cells within tissues and the transport of Carbon dioxide A bronchodilator is a substance that dilates the bronchi and Bronchioles decreasing airway resistance and thereby facilitating airflow In Anatomy, the genitourinary system is the Organ system of all the Reproductive organs and the Urinary system. Urinary retention also known as ischuria is a lack of ability to Urinate. Many different terms are often used to describe what is collectively known as dizziness. Euphoria is a medically recognized emotional state related to Pleasure and Happiness. Insomnia is a symptom of a sleeping disorder characterized by persistent difficulty falling asleep or staying asleep despite the opportunity Neuropharmacology is concerned with drug-induced changes in the functioning of cells in the nervous system Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates An agonist is a term used to describe a type of ligand or drug that binds and alters the activity of a receptor. Norepinephrine ( INN) (abbreviated norepi or NE) or noradrenaline ( BAN) (abbreviated NA or NAd) is a An agonist is a term used to describe a type of ligand or drug that binds and alters the activity of a receptor. Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons An agonist is a term used to describe a type of ligand or drug that binds and alters the activity of a receptor. Monoamine oxidase inhibitors ( MAOIs) are a class of powerful antidepressant drugs prescribed for the treatment of depression. ), amphetamine is one of the standard treatments for ADHD. Attention-Deficit Hyperactivity Disorder (ADHD is a neurobehavioral developmental disorder affecting about 3-5% of the world's population Beneficial effects for ADHD can include improved impulse control, improved concentration, decreased sensory overstimulation, decreased irritability and decreased anxiety. These effects can be dramatic in both young children and adults. The ADHD medication Adderall is composed of four different amphetamine salts, and Adderall XR is a timed-release formulation of these same salt forms. A salt, in Chemistry, is defined as the product formed from the neutralisation reaction of Acids and bases. Adderall is a brand-name pharmaceutical Psychostimulant composed of mixed Amphetamine salts, the actions of which are Sympathomimetic

When used within the recommended doses, side-effects like loss of appetite tend to decrease over time. However, amphetamines last longer in the body than methylphenidate (Ritalin, Concerta, etc. ), and tend to have stronger side-effects on appetite and sleep.

Amphetamines are also a standard treatment for narcolepsy, as well as other sleeping disorders. Narcolepsy is a Neurological condition most characterized by Excessive Daytime Sleepiness (EDS in which a person falls asleep during the day at inappropriate If used within therapeutic limits, amphetamines are generally effective over long periods of time without producing addiction or physical dependence.

Amphetamines are sometimes used to augment anti-depressant therapy in treatment-resistant depression.

Medical use for weight loss is still approved in some countries, but is regarded as obsolete and dangerous in others.

Contraindications

Stimulants such as amphetamines elevate cardiac output and blood pressure making them dangerous for use by patients with a history of heart disease or hypertension. Heart disease is an Umbrella term for a variety for different diseases affecting the Heart. Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated Also, patients with a history of drug dependence or anorexia should not be treated with amphetamines due to their addictive and appetite suppressing properties. Amphetamines can cause a life-threatening complication in patients taking MAOI antidepressants. Monoamine oxidase inhibitors ( MAOIs) are a class of powerful antidepressant drugs prescribed for the treatment of depression. Amphetamine is not suitable for patients with a history of glaucoma.

Amphetamines have also been shown to pass through into breast milk. Because of this, mothers taking medications containing amphetamines are advised to avoid breastfeeding during their course of treatment. [10]

Major Neurobiological Mechanisms

Primary Sites of Action

Amphetamine exerts its behavioral effects by modulating the behavior of several key neurotransmitters in the brain, including dopamine, serotonin, and norepinephrine. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons Norepinephrine ( INN) (abbreviated norepi or NE) or noradrenaline ( BAN) (abbreviated NA or NAd) is a However, the activity of amphetamine throughout the brain does not appear to be non-specific;[11] certain receptors that respond to amphetamine in some regions of the brain tend not to do so in other regions. For instance, dopamine D2 receptors in the hippocampus, a region of the brain associated with forming new memories, appear to be unaffected by the presence of amphetamine. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Dopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the Vertebrate Central nervous system (CNS The hippocampus is a part of the Forebrain, located in the medial Temporal lobe. [12]

The major neural systems affected by amphetamine are largely implicated in the brain’s reward circuitry. Moreover, neurotransmitters involved various reward pathways of the brain appear to be the primary targets of amphetamine. [13] One such neurotransmitter is dopamine, a chemical messenger heavily active in the mesolimbic and mesocortical reward pathways. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates The mesolimbic pathway is one of the Neural pathways in the Brain that links the Ventral tegmentum in the Midbrain to the Nucleus accumbens The mesocortical pathway is a Neural pathway that connects the Ventral tegmentum to the Cerebral cortex, particularly the Frontal lobes It is Not surprisingly, the anatomical components of these pathways—including the caudate putamen, the nucleus accumbens, and the ventral striatum—have been found to be primary sites of amphetamine action. "Putamen" is also a botanical term for the stone in a Fruit, such as a Peach. The nucleus accumbens (NAcc also known as the accumbens nucleus or as the nucleus accumbens septi (Latin for nucleus leaning against the Septum The striatum is a subcortical (ie inside rather than on the outside part of the Telencephalon. [14][15]

That amphetamines influence neurotransmitter activity specifically in regions implicated in reward provides insight into the behavioral consequences of the drug, such as the stereotyped onset of euphoria. [16] A better understanding of the specific mechanisms by which amphetamines operate may increase our ability to treat amphetamine addiction, as the brain’s reward circuitry has been widely implicated in addictions of many types. The term " addiction " is used in many contexts to describe an obsession compulsion or excessive Physical dependence or psychological dependence such as [17]

Endogenous Amphetamines

Amphetamine has been found to have several endogenous analogues; that is, molecules of a similar structure found naturally in the brain. [18] Phenylalanine and β-Phenethylamine are two examples, which are formed in the peripheral nervous system as well as in the brain itself. Phe redirects here For the BitTorrent feature see PHE. For the constellation see Phoenix (constellation. These molecules are thought to modulate levels of excitement and alertness, among other related affective states.

Dopamine

Perhaps the most widely studied neurotransmitter with regard to amphetamine action is dopamine, the “reward neurotransmitter” that is highly active in numerous reward pathways of the brain. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Various studies have shown that in select regions, amphetamine increases the concentrations of dopamine in the synaptic cleft, thereby heightening the response of the post-synaptic neuron. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Chemical synapses are specialized junctions through which Neurons signal to each other and to non-neuronal cells such as those in Muscles or Glands [19] This specific action hints at the hedonic response to the drug as well as to the drug’s addictive quality.

The specific mechanisms by which amphetamines affect dopamine concentrations have been studied extensively. Currently, two major hypotheses have been proposed, which are not mutually exclusive. One theory emphasizes amphetamine’s actions on the vesicular level, increasing concentrations of dopamine in the cytosol of the pre-synaptic neuron. In a Neuron, synaptic vesicles, also called neurotransmitter vesicles, store the various Neurotransmitters that are released during Calcium -regulated Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates [20][21] The other focuses on the role of the dopamine transporter DAT, and proposes that amphetamine may interact with DAT to induce reverse transport of dopamine from the presynaptic neuron into the synaptic cleft. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Chemical synapses are specialized junctions through which Neurons signal to each other and to non-neuronal cells such as those in Muscles or Glands [22][23][24][25]

The former hypothesis is backed by data demonstrating that injections of amphetamines result in rapid increases of cytosolic dopamine concentrations. [26] Amphetamine is believed to interact with dopamine-containing vesicles in the axon terminal, called VMATs, in a way that releases dopamine molecules into the cytosol. Chemical synapses are specialized junctions through which Neurons signal to each other and to non-neuronal cells such as those in Muscles or Glands The redistributed dopamine is then believed to interact with DAT to promote reverse transport. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine [27] Calcium may be a key molecule involved in the interactions between amphetamine and VMATs. [28]

The latter hypothesis postulates a direct interaction between amphetamine and the DAT transporter. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine The activity of DAT is believed to depend on specific phosphorylating kinases, such as PCK-β. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine Protein kinase C ('PKC') is a family of protein kinases consisting of ~10 Isozymes. [29] Upon phosphorylation, DAT undergoes a conformational change that results in the transportation of DAT-bound dopamine from the extracellular to the intracellular environment. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates [30] In the presence of amphetamine, however, DAT has been observed to function in reverse, spitting dopamine out of the presynaptic neuron and into the synaptic cleft. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine Chemical synapses are specialized junctions through which Neurons signal to each other and to non-neuronal cells such as those in Muscles or Glands [31] Thus, beyond inhibiting reuptake of dopamine, amphetamine also stimulates the release of dopamine molecules into the synapse. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates [32]

In support of the above hypothesis, it has been found that PKC-β inhibitors eliminate the effects of amphetamine on extracellular dopamine concentrations in the striatum of rats. Protein kinase C ('PKC') is a family of protein kinases consisting of ~10 Isozymes. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates [33] This data suggests that the PKC-β kinase may represent a key point of interaction between amphetamine and the DAT transporter. Protein kinase C ('PKC') is a family of protein kinases consisting of ~10 Isozymes. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine

Serotonin

Amphetamine has been found to exert similar effects on serotonin as on dopamine. Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates [34] Like DAT, the serotonin transporter SERT can be induced to operate in reverse upon stimulation by amphetamine. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine The Serotonin transporter (SERT is a Monoamine transporter Protein. [35] This mechanism is thought to rely on the actions of calcium molecules, as well as on the proximity of certain transporter proteins. [36]

The interaction between amphetamine and serotonin is only apparent in particular regions of the brain, such as the mesocorticalimbic projection. Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons The mesocortical pathway is a Neural pathway that connects the Ventral tegmentum to the Cerebral cortex, particularly the Frontal lobes It is Recent studies additionally postulate that amphetamine may indirectly alter the behavior of glutamatergic pathways extending from the ventral tegmental area to the prefrontal cortex. The glutamatergic Neurotransmitter system plays a crucial role in memory formation and information processing The ventral tegmentum or the ventral tegmental area (VTA ( tegmentum, Latin for covering) is part of the Midbrain, lying close to the Substantia [37] Glutamatergic pathways are strongly correlated with increased excitability at the level of the synapse. The glutamatergic Neurotransmitter system plays a crucial role in memory formation and information processing Increased extracellular concentrations of serotonin may thus modulate the excitatory activity of glutamatergic neurons. Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons [38]

The proposed ability of amphetamine to increase excitability of glutamatergic pathways may be of significance when considering serotonin-mediated addiction. The glutamatergic Neurotransmitter system plays a crucial role in memory formation and information processing The term " addiction " is used in many contexts to describe an obsession compulsion or excessive Physical dependence or psychological dependence such as [39] An additional behavioral consequence may be the stereotyped locomotor stimulation that occurs in response to amphetamine exposure. [40]

Other Relevant Neurotransmitters

Several other neurotransmitters have been linked to amphetamine activity. For instance, extracellular levels of glutamate, the primary excitatory neurotransmitter in the brain, have been shown to increase upon exposure to amphetamine. Glutamic acid (abbreviated as Glu or E) is one of the 20 Alpha Amino acids It is not among the human Essential amino acids Its Consistent with other findings, this effect was found in the areas of the brain implicated in reward; namely, the nucleus accumbens, striatum, and prefrontal cortex. The nucleus accumbens (NAcc also known as the accumbens nucleus or as the nucleus accumbens septi (Latin for nucleus leaning against the Septum The striatum is a subcortical (ie inside rather than on the outside part of the Telencephalon. [41]

Additionally, several studies demonstrate increased levels of norepinephrine, a neurotransmitter related to adrenaline, in response to amphetamine. Norepinephrine ( INN) (abbreviated norepi or NE) or noradrenaline ( BAN) (abbreviated NA or NAd) is a This is believed to occur via reuptake blockage as well as via interactions with the norepinephrine neuronal transport carrier. [42]

Long-term Neurological Effects

The long-term effects of amphetamine remain unknown to a large extent, though some literature on the topic does exist. Several of the postulated effects include reductions in dopamine content, DAT density, and tyrosine hydroxylase (the dopamine synthesizing enzyme) in the striatum and nearby areas. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine Tyrosine hydroxylase or tyrosine 3-monooxygenase is the Enzyme responsible for catalyzing the conversion of the Amino acid L-tyrosine to The striatum is a subcortical (ie inside rather than on the outside part of the Telencephalon. [43]

Pharmacology

Chemical Properties

Amphetamine is a chiral compound. The term chiral (pronounced /ˈkaɪɹ(əl̩/ is used to describe an object that is non- superimposable on its mirror image The racemic mixture can be divided into its optical isomers: levo- and dextro-amphetamine. In Chemistry, a racemic mixture, or racemate, is one that has equal amounts of left- and right-handed enantiomers of a chiral Dextroamphetamine is a Psychostimulant which produces increased wakefulness energy and self-confidence in association with decreased fatigue and appetite Amphetamine is the parent compound of its own structural class, comprising a broad range of psychoactive derivatives, e. In Chemistry, a derivative is a compound that is formed from a similar compound or a compound that can be imagined to arise from another compound if one g. , MDMA (Ecstasy) and the N-methylated form, methamphetamine. MDMA ( 34-methylenedioxy- N -methylamphetamine) most commonly known today by the street name Ecstasy (often abbreviated E, X, Amphetamine is a homologue of phenethylamine. In Chemistry, a homologous series is a series of Organic compounds with a similar General formula, possessing similar chemical properties due to the presence Phenethylamine, or β -phenylethylamine or 2-phenylethylamine is an Alkaloid and Monoamine.

At first, the medical drug came as the salt racemic-amphetamine sulfate (racemic-amphetamine contains both isomers in equal amounts). Attention disorders are often treated using Adderall or a generic equivalent, a formulation of mixed amphetamine and dextroamphetamine salts that contain

Pharmacodynamics

Amphetamine has been shown to both diffuse through the cell membrane and travel via the dopamine transporter (DAT) to increase concentrations of dopamine in the neuronal terminal. Adderall is a brand-name pharmaceutical Psychostimulant composed of mixed Amphetamine salts, the actions of which are Sympathomimetic The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates

Amphetamine, both as d-amphetamine (dextroamphetamine) and l-amphetamine (or a racemic mixture of the two isomers), is believed to exert its effects by binding to the monoamine transporters and increasing extracellular levels of the biogenic amines dopamine, norepinephrine (noradrenaline) and serotonin. Dextroamphetamine is a Psychostimulant which produces increased wakefulness energy and self-confidence in association with decreased fatigue and appetite Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Norepinephrine ( INN) (abbreviated norepi or NE) or noradrenaline ( BAN) (abbreviated NA or NAd) is a Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons It is hypothesized that d-amphetamine acts primarily on the dopaminergic systems, while l-amphetamine is comparatively norepinephrinergic (noradrenergic). The primary reinforcing and behavioral-stimulant effects of amphetamine, however, are linked to enhanced dopaminergic activity, primarily in the mesolimbic dopamine system. In neuroscience neuromodulation is the process in which several classes of Neurotransmitters in the nervous system regulate diverse populations of Neurons (one

Amphetamine and other amphetamine-type stimulants principally act to release dopamine into the synaptic cleft. Chemical synapses are specialized junctions through which Neurons signal to each other and to non-neuronal cells such as those in Muscles or Glands The increased amphetamine concentration releases endogenous stores of dopamine from vesicular monoamine transporters (VMATs), thereby increasing intra-neuronal concentrations of transmitter. The vesicular monoamine transporter is a Transport protein located within the presynaptic cell. This increase in concentration effectively reverses transport of dopamine via the dopamine transporter (DAT) into the synapse. The Dopamine transporter (also dopamine active transporter DAT SLC6A3 is a membrane-spanning protein that binds the Neurotransmitter Dopamine [44] In addition, amphetamine binds reversibly to the DATs and blocks the transporter's ability to clear DA from the synaptic space. Amphetamine also acts in this way with norepinephrine (noradrenaline) and to a lesser extent serotonin.

In addition, amphetamine binds to a group of receptors called TrAce Amine Receptors (TAAR). Trace amine-associated receptors, abbreviated TAAR and previously abbreviated TAR and TA, are a class of G protein-coupled receptors identified [45] TAAR are a newly discovered receptor system which seems to be affected by a range of amphetamine-like substances called trace amines. Trace amines are Endogenous compounds structurally related to classical Biogenic amines, such as Catecholamines, Serotonin and Histamine

Effects

Physical effects

Physical effects of amphetamine could include reduced appetite, dilated pupils, flushing, loss of coordination, restlessness, dry mouth, headache, tachycardia, increased breathing rate, increased blood pressure, fever, sweating, diarrhea, constipation, blurred vision, impaired speech, dizziness,uncontrollable movements, insomnia, numbness, palpitations, arrhythmia. "Dilated pupil" redirects here An Eye examination sometimes requires the dilation of the pupil Xerostomia is the medical term for a dry mouth due to a lack of Saliva. A headache ( cephalalgia in medical terminology is a condition of pain in the Head; sometimes Neck or upper back pain may also be interpreted Blood pressure is also the title of a short story by Damon Runyan in Guys and Dolls and Other Stories Fever (also known as pyrexia, from the Greek pyretos meaning fire or a febrile response, from the Latin word Febris In Medicine, diarrhea, also spelled diarrhoea (see spelling differences) is frequent loose or liquid Bowel movements Acute diarrhea Constipation, costiveness, or irregularity, is a condition of the Digestive system in which a person (or animal experiences hard Feces that Blurred vision is an Ocular Symptom. Causes There are many causes of blurred vision including use of Atropine. Many different terms are often used to describe what is collectively known as dizziness. Insomnia is a symptom of a sleeping disorder characterized by persistent difficulty falling asleep or staying asleep despite the opportunity Paresthesia (pron /ˌpɛɹɪsˈθiʒə/ paraesthesia in British English, pron A palpitation (medical term ectopic heart beat) is an abnormal awareness of the beating of the Heart, whether it is too slow too fast irregular Dysrhythmia redirects here For the American band see Dysrhythmia (band. In high doses or chronic use convulsions, dry or itchy skin, acne, pallor can occur. An epileptic seizure is caused by excessive and/or hypersynchronous electrical Neuronal activity and is usually self-limiting Acne vulgaris (commonly called acne) is a Skin disease caused by changes in the Pilosebaceous units (skin structures consisting of a Hair follicle Pallor (also called pastiness or wanness) is a reduced amount of oxy Hemoglobin in Skin or Mucous membrane, a pale color which can [46][47][48][49]

Young adults who abuse amphetamines may be at greater risk of suffering a heart attack. Myocardial infarction ( MI or AMI for acute myocardial infarction) also known as a heart attack, occurs when the blood supply In a study published in the journal Drug and Alcohol Dependence,[50] researchers examined data from more than 3 million people between 18 and 44 years old hospitalized from 2000 through 2003 in Texas and found a relationship between a diagnosis of amphetamine abuse and heart attack. 2000 ( MM) was a Leap year that started on Saturday of the Common Era, in accordance with the Gregorian calendar. Year 2003 ( MMIII) was a Common year starting on Wednesday of the Gregorian calendar. [51]

Psychological effects

Psychological effects of amphetamine could include euphoria, a sense of well being, increased alertness, increased concentration, increased talkativeness, increased energy, excitability, feeling of power or superiority, repetitive behaviors, increased aggression, and in rare cases paranoia. In Chemistry, concentration is the measure of how much of a given substance there is mixed with another substance In Psychology and other social and Behavioral sciences aggression refers to behavior that is intended to cause harm Paranoia is a disturbed thought process characterized by excessive Anxiety or Fear, often to the point of Irrationality and Delusion. Effects are similar, to cocaine, especially when insufflated or injected. Cocaine ( benzoylmethyl ecgonine) is a Crystalline Tropane Alkaloid that is obtained from the leaves of the Coca plant Insufflation (Latin insufflatio "blowing on or into" is the practice of inhaling substances into a Body cavity. [47][52]

Withdrawal effects

Withdrawal from use of amphetamines can include the following: anxiety, depression, agitation, fatigue, excessive sleeping, increased appetite, psychosis, suicidal thoughts. Anxiety is a physiological and psychological state characterized by Cognitive, Somatic, Emotional and Behavioral components In the fields of Psychology and Psychiatry, the terms depression or depressed refer to both expected and pathologically chronic or severe Sleep is a Natural state of bodily rest observed throughout the animal kingdom Psychosis (from the Greek ψυχή "psyche" for mind or soul and -οσις "-osis" for abnormal condition with adjective psychotic [53]

Dependence & Addiction

Tolerance is developed rapidly in amphetamine abuse, therefore increasing the amount of the drug that is needed to satisfy the addiction. Drug tolerance occurs when a subject's reaction to a Psychoactive drug (such as a painkiller or intoxicant decreases so that larger doses are required to achieve the same effect [54] Repeated amphetamine use can produce "reverse tolerance", or sensitization to some psychological effects. [55][56][57][58][59] Many users will repeat the amphetamine cycle by taking more of the drug during the withdrawal. Withdrawal, also known as withdrawal/abstinence syndrome, refers to the characteristic signs and symptoms that appear when a drug that causes Physical dependence is This leads to a very dangerous cycle and may involve the use of other drugs to get over the withdrawal process. Users will commonly stay up for 2 or 3 days avoiding the withdrawals then dose themselves with benzodiazepines or barbiturates to help them stay calm while they recuperate. Chronic users of amphetamines typically snort or resort to drug injection to experience the full effects of the drug in a faster and more intense way, with the added risks of infection, vein damage, and higher risk of overdose. Because of the abuse of amphetamines in the U. S. , most brands were discontinued by the 1990s, including the highly abused brand names Biphetamine (known as "black beauties") and Preludin, known on the street as "slams", whose coating was peeled and then injected. Adderall is a brand-name pharmaceutical Psychostimulant composed of mixed Amphetamine salts, the actions of which are Sympathomimetic Phenmetrazine is a Stimulant of the central nervous system It was previously sold under the trade name Preludin as an Anorectic. Only a few brands of amphetamines are still produced in the United States: those prescribed for narcolepsy, attention-deficit hyperactivity disorder, treatment-resistant depression, and extreme obesity.

Performance-enhancing use

Amphetamine is used by college and high-school students as a study and test-taking aid. [60] Amphetamine increases energy levels, concentration, and motivation, allowing students to study for an extended period of time. These drugs are often acquired through ADHD prescriptions to students and peers, rather than illicitly produced drugs. [61]

Amphetamines have been, and are still used, by militaries around the world. British troops used 72 million amphetamine tablets in the second world war[62] and the RAF got through so many that "Methedrine won the Battle of Britain" according to one report[63]. American bomber pilots use amphetamines ("go pills") to stay awake during long missions. The Tarnak Farm incident in 2002 is an example of when an American F16-pilot accidentally killed several friendly soldiers on the ground, partly due to the use of amphetamine. The Tarnak Farm incident refers to the accidental killing of four Canadian soldiers and the injury of eight others from the Third Battalion of Princess Patricia's Canadian See also 2002 (disambiguation Year 2002 ( MMII) was a Common year starting on Tuesday of the Gregorian calendar.

Amphetamine is also used by professional,[64] collegiate[65] and high school[66] athletes for its strong stimulant effect. Energy levels are perceived to be dramatically increased and sustained, believed to allow for more vigorous and longer play, though at least one study has found that this effect is not measurable. [67] This practice can be extremely dangerous, and athletes have died as a result, for example, British cyclist Tom Simpson. Tom Simpson ( 30 November 1937 &ndash 13 July 1967) was an English Road racing cyclist who died of exhaustion on the

Amphetamine use has historically been especially common among Major League Baseball (MLB) athletes and is usually known by the slang term "greenies". [68] In 2006, MLB banned the use of amphetamines and the ban is enforced by periodic drug-testing. Consequences if a player tests positive are significant, but MLB has received some criticism because these consequences are dramatically less severe than for steroids, with the first offense bringing only a warning and further testing[69]. [70][71]

Truck drivers, especially long-haul drivers, take amphetamine[72] to combat symptoms of somnolence and to increase their concentration on driving.

Legal issues

Internationally, amphetamine is a Schedule II drug under the Convention on Psychotropic Substances. The Convention on Psychotropic Substances is a United Nations Treaty designed to control Psychoactive drugs such as Amphetamines Barbiturates [75]

A chart comparing the chemical structures of different amphetamine derivatives
A chart comparing the chemical structures of different amphetamine derivatives

See also

References and notes

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  2. ^ Determination of amphetamine, methamphetamine, and ...
  3. ^ Edeleanu L. Adderall is a brand-name pharmaceutical Psychostimulant composed of mixed Amphetamine salts, the actions of which are Sympathomimetic Attention-Deficit Hyperactivity Disorder (ADHD is a neurobehavioral developmental disorder affecting about 3-5% of the world's population Benzylpiperazine (with trade names such as "A2" "Frenzy" and "Nemesis" commonly referred to as BZP) is a Recreational drug with Clandestine chemistry generally refers to Chemistry carried out in illegal drug Laboratories (known colloquially as labs) but can include any N-ethylamphetamine (Etilamfetamine Apetinil is a Stimulant drug derived from Amphetamine which was invented in the early 1900s Dextroamphetamine is a Psychostimulant which produces increased wakefulness energy and self-confidence in association with decreased fatigue and appetite Lisdexamfetamine (L-lysine-d-amphetamine is an inactive molecule Prodrug (brand name Vyvanse) consisting of the Psychostimulant d-amphetamine Desoxyn is a brand of Methamphetamine hydrochloride (also known as desoxyephedrine hence the name "Desoxyn" indicated for treatment of Attention Deficit/Hyperactivity Phenethylamine, or β -phenylethylamine or 2-phenylethylamine is an Alkaloid and Monoamine. N-propylamphetamine is a Stimulant drug derived from Amphetamine which was invented in the 1970s A psychostimulant is a substance that enhances locomotor behavior "Uber einige Derivate der Phenylmethacrylsaure und der Phenylisobuttersaure". Ber Deutsch Chem Ges. 1887;Vol 20:616.
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  68. ^ Frias, Carlos (2006-04-02). Year 2006 ( MMVI) was a Common year starting on Sunday of the Gregorian calendar. Events 68 - Galba, Governor of Hispania, names himself legatus senatus populique Romani, breaking the line of Baseball and amphetamines. Palm Beach Post. Retrieved on 2007-12-02. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 1409 - The University of Leipzig opens 1755 - The second Eddystone Lighthouse is destroyed by fire
  69. ^ Kreidler, Mark (2005-11-15). Year 2005 ( MMV) was a Common year starting on Saturday (link displays full calendar of the Gregorian calendar. Events 655 - Battle of Winwaed: Penda of Mercia is defeated by Oswiu of Northumbria. Baseball finally brings amphetamines into light of day. ESPN. com. Retrieved on 2007-12-02. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 1409 - The University of Leipzig opens 1755 - The second Eddystone Lighthouse is destroyed by fire
  70. ^ Klobuchar, Jim (2006-03-31). Year 2006 ( MMVI) was a Common year starting on Sunday of the Gregorian calendar. Events 307 - After divorcing his wife Minervina, Constantine marries Fausta, the daughter of the retired Roman Emperor Can baseball make a clean sweep?. Christian Science Monitor. Retrieved on 2007-12-02. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 1409 - The University of Leipzig opens 1755 - The second Eddystone Lighthouse is destroyed by fire
  71. ^ Associated Press (2007-01-18). Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 350 - Generallus Magnentius deposes Roman Emperor Constans and proclaims himself Emperor MLB owners won't crack down on 'greenies'. MSNBC. com. Retrieved on 2007-12-02. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 1409 - The University of Leipzig opens 1755 - The second Eddystone Lighthouse is destroyed by fire
  72. ^ Lund, Adrian K; David F. Preusser, Richard D. Blomberg, Allan F. Williams, J. Michael Walsh (1989). "Drug Use by Tractor-Trailer Drivers", Drugs in the Workplace: Research and Evaluation Data, National Institute on Drug Abuse Research. Rockville, MD: National Institute on Drug Abuse, 47-67. Retrieved on 2007-12-02. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 1409 - The University of Leipzig opens 1755 - The second Eddystone Lighthouse is destroyed by fire  “This study has provided the first objective data regarding the use of potentially abusive drugs by tractor-trailer drivers. . . Prescription stimulants, such as amphetamine, methamphetamine, and phentermine were found in 5 percent of the [317] drivers [who participated in the study], often in combination with similar but less potent stimulants, such as phenylpropanolamine. Nonprescription stimulants were detected in 12 percent of the drivers, about half of whom gave no medical explanation for their presence. . . One limitation of these findings is that 12 percent of the randomly selected drivers refused to participate in the study or provided insufficient urine and blood for testing; the distribution of drugs among these 42 drivers is unknown. . . Finally, the results apply to tractor-trailer drivers operating on a major east-west interstate route in Tennessee. Drug incidence among other truck-driver populations are unknown and may be higher or lower than reported here. (64)” 
  73. ^ Template:Cite web title=homeoffice url=http://www. homeoffice. gov. uk/drugs/drugs-law/Class-a-b-c/ accessdate=2007-07-23
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  75. ^ List of psychotropic substances under international control (PDF). International Narcotics Control Board. Retrieved on November 19, 2005.

External links

PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The term chiral (pronounced /ˈkaɪɹ(əl̩/ is used to describe an object that is non- superimposable on its mirror image PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The term chiral (pronounced /ˈkaɪɹ(əl̩/ is used to describe an object that is non- superimposable on its mirror image

Dictionary

amphetamine

-noun

  1. (organic chemistry) 1-phenyl-2-propylamine; a colourless volatile liquid; any of its derivatives.
  2. A class of drugs used as a stimulant of the central nervous system in the treatment of ADHD, depression, and narcolepsy, and abused illegally as a stimulant.
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