Stimulant
Encyclopedia
Stimulants are psychoactive drug
s which induce temporary improvements in either mental or physical function or both. Examples of these kinds of effects may include enhanced alertness, wakefulness, and locomotion, among others. Due to their effects typically having an "up" quality to them, stimulants are also occasionally referred to as "uppers". Depressant
s or "downers", which decrease mental and/or physical function, are in stark contrast to stimulants and are considered to be their functional opposites. Stimulants are widely used throughout the world as prescription medicines and as illicit substances
of recreational use
or abuse
.
and peripheral nervous system
s. Common effects, which vary depending on the substance in question, may include enhanced alertness
, awareness
, wakefulness, endurance
, productivity
, and motivation
, increased arousal
, locomotion
, heart rate
, and blood pressure
, and the perception of a diminished requirement for food
and sleep
. Many stimulants are also capable of improving mood and relieving anxiety, and some can even induce feelings of euphoria
. It should be noted, however, that many of these drugs are also capable of causing anxiety and heart failure, even the ones that may paradoxically reduce it to a degree at the same time. Stimulants exert their effects through a number of different pharmacological mechanisms, the most prominent of which include facilitation of norepinephrine
(noradrenaline) and/or dopamine
activity (e.g., via monoamine transporter
inhibition or reversal), adenosine receptor
antagonism
, and nicotinic acetylcholine receptor
agonism
.
Caffeine is a mild stimulant compound that is found naturally in coffee
, tea
, and to a lesser degree, in cocoa
or chocolate
. It is included in many soft drink
s, as well as a larger amount in energy drink
s. Caffeine is the world's most widely used psychoactive drug and by far the most common stimulant. The vast majority (over 85%) of people in the United States consume caffeine on a daily basis. Few jurisdictions restrict its sale and use. Caffeine is also included in some medications, usually for the purpose of enhancing the effect of the primary ingredient, or reducing one of its side effects (especially drowsiness). Tablets containing standardized doses of caffeine are also widely available.
is the active chemical constituent in tobacco
, which is available in many forms, including cigarette
s, cigar
s, chewing tobacco
, and smoking cessation
aids such as nicotine patch
es and nicotine gum
. Nicotine is used widely throughout the world for its stimulating effects.
Amphetamines are a group of phenylethylamine stimulants such as amphetamine and methamphetamine. Like NDRIs
, amphetamine increases the levels of norepinephrine and dopamine in the brain via reuptake inhibition; however, the more important mechanism by which amphetamines cause stimulation is through the direct release of these catecholamine
s from storage vesicles
in cells. Amphetamines are known to cause elevated mood and euphoria
as well as rebound depression
and anxiety
.
Amphetamine
s are often used for their therapeutic effects; physicians occasionally prescribe amphetamine
s to treat major depression, where subjects do not respond well to traditional SSRI
medications, and numerous studies have demonstrated the effectiveness of drugs such as Adderall
in controlling symptoms associated with ADD
/ADHD
. In rare cases, ADD
/ADHD
patients who are not responding sufficiently to traditional amphetamine
s are prescribed dextrorotary methamphetamine
. Due to their availability and fast-acting effects, amphetamine
s are prime candidates for abuse.
Methylenedioxymethamphetamine (MDMA), known by its common street name "Ecstasy", is an illicit substance that typically comes in either tablet, capsule, or powder/crystal form. It had a medical application as a treatment for depression until 1985 when the DEA placed MDMA into schedule 1, prohibiting most medical studies and applications. Notably, MDMA is also unique and very popular for its entactogenic properties. The stimulant effects of MDMA include hypertension
, anorexia
(appetite loss), euphoria
, social disinhibition, insomnia
(or enhanced wakefulness), improved energy, increased arousal, and increased perspiration, among others.
shrub, which grows in the mountain regions of South American countries such as Bolivia
, Colombia
, and Peru
. In Europe, North America, and in some parts of Asia, the most common form of cocaine is a white crystalline powder. Cocaine is a stimulant but is not normally prescribed therapeutically for its stimulant properties, although it sees clinical use as a local anesthetic, particularly in ophthalmology
. Most cocaine use is recreational and its abuse potential is high, and so its sale and possession are strictly controlled in most jurisdictions. Other tropane
derivative drugs related to cocaine are also known such as troparil and lometopane but have not been widely sold or used recreationally.
(Wellbutrin, Zyban), and the two best-known NRIs are atomoxetine (Strattera) and reboxetine
(Edronax). Many of these drugs have a considerably lower abuse potential in comparison to other stimulants like the amphetamines and cocaine.
(MPH; Ritalin, Concerta, Metadate, or Methylin) is a drug
approved for treatment
of attention-deficit hyperactivity disorder
, postural orthostatic tachycardia syndrome
, and narcolepsy
. It belongs to the piperidine
class of compounds and increases the levels of dopamine
and norepinephrine
in the brain through reuptake inhibition
of the monoamine transporter
s. It also increases the release of dopamine and norepinephrine. MPH possesses structural similarities to amphetamine
, and, though it is less potent, its pharmacological effects are even more closely related to those of cocaine
.
Modafinil, like other stimulants, increases the release of monoamines but also elevates hypothalamic histamine levels, leading some researchers to consider Modafinil a "wakefulness promoting agent" rather than a classic amphetamine-like stimulant.
Modafinil has been shown to be effective in the treatment of Attention-Deficit Hyperactivity Disorder (ADHD), depression, cocaine addiction, Parkinson's Disease, schizophrenia, shift workers' sleep disorder and disease-related fatigue.
Adrafinil
is the prodrug of Modafinil, and is metabolized into it in about one hour, when taken on an empty stomach.
Armodafinil
is a new version of Modafinil.
s, or eugeroic
s, (good arousal). These stimulants tend to increase alertness without the peripheral (body) effects or addiction/tolerance/abuse potential of the traditional stimulants. They have minimal effect on sleep structure, and do not cause rebound hypersomnolence or "come down" effects. Ampakines such as ampalex and CX717
have been developed but are still in clinical trials and have not yet been sold commercially. Another compound with similar effects to these drugs is carphedon
, which is sold as a general stimulant in Russia under the brand name Phenotropil.
chemical class with stimulant and aphrodisiac effects. Yohimbine is sometimes used to remedy Type-2 Diabetes
in animals and humans that carry the polymorphisms of the α2A-adrenergic receptor gene.
of central nervous system
stimulants is common. Addiction
to CNS stimulants can quickly lead to medical, psychiatric and psychosocial
deterioration. Drug tolerance, dependence, sensitisation as well as a withdrawal
syndrome can occur.
Psychoactive drug
A psychoactive drug, psychopharmaceutical, or psychotropic is a chemical substance that crosses the blood–brain barrier and acts primarily upon the central nervous system where it affects brain function, resulting in changes in perception, mood, consciousness, cognition, and behavior...
s which induce temporary improvements in either mental or physical function or both. Examples of these kinds of effects may include enhanced alertness, wakefulness, and locomotion, among others. Due to their effects typically having an "up" quality to them, stimulants are also occasionally referred to as "uppers". Depressant
Depressant
A depressant, or central depressant, is a drug or endogenous compound that depresses the function or activity of a specific part of the brain...
s or "downers", which decrease mental and/or physical function, are in stark contrast to stimulants and are considered to be their functional opposites. Stimulants are widely used throughout the world as prescription medicines and as illicit substances
Prohibition (drugs)
The prohibition of drugs through sumptuary legislation or religious law is a common means of attempting to prevent drug use. Prohibition of drugs has existed at various levels of government or other authority from the Middle Ages to the present....
of recreational use
Recreational drug use
Recreational drug use is the use of a drug, usually psychoactive, with the intention of creating or enhancing recreational experience. Such use is controversial, however, often being considered to be also drug abuse, and it is often illegal...
or abuse
Drug abuse
Substance abuse, also known as drug abuse, refers to a maladaptive pattern of use of a substance that is not considered dependent. The term "drug abuse" does not exclude dependency, but is otherwise used in a similar manner in nonmedical contexts...
.
Effects
Stimulants (analeptics) produce a variety of different kinds of effects by enhancing the activity of the centralCentral nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
and peripheral nervous system
Peripheral nervous system
The peripheral nervous system consists of the nerves and ganglia outside of the brain and spinal cord. The main function of the PNS is to connect the central nervous system to the limbs and organs. Unlike the CNS, the PNS is not protected by the bone of spine and skull, or by the blood–brain...
s. Common effects, which vary depending on the substance in question, may include enhanced alertness
Alertness
Alertness is the state of paying close and continuous attention, being watchful and prompt to meet danger or emergency, or being quick to perceive and act. It is related to psychology as well as to physiology...
, awareness
Awareness
Awareness is the state or ability to perceive, to feel, or to be conscious of events, objects or sensory patterns. In this level of consciousness, sense data can be confirmed by an observer without necessarily implying understanding. More broadly, it is the state or quality of being aware of...
, wakefulness, endurance
Endurance
Endurance is the ability for a human or animal to exert itself and remain active for a long period of time, as well as its ability to resist, withstand, recover from, and have immunity to trauma, wounds, or fatigue. In humans, it is usually used in aerobic or anaerobic exercise...
, productivity
Productivity
Productivity is a measure of the efficiency of production. Productivity is a ratio of what is produced to what is required to produce it. Usually this ratio is in the form of an average, expressing the total output divided by the total input...
, and motivation
Motivation
Motivation is the driving force by which humans achieve their goals. Motivation is said to be intrinsic or extrinsic. The term is generally used for humans but it can also be used to describe the causes for animal behavior as well. This article refers to human motivation...
, increased arousal
Arousal
Arousal is a physiological and psychological state of being awake or reactive to stimuli. It involves the activation of the reticular activating system in the brain stem, the autonomic nervous system and the endocrine system, leading to increased heart rate and blood pressure and a condition of...
, locomotion
Animal locomotion
Animal locomotion, which is the act of self-propulsion by an animal, has many manifestations, including running, swimming, jumping and flying. Animals move for a variety of reasons, such as to find food, a mate, or a suitable microhabitat, and to escape predators...
, heart rate
Heart rate
Heart rate is the number of heartbeats per unit of time, typically expressed as beats per minute . Heart rate can vary as the body's need to absorb oxygen and excrete carbon dioxide changes, such as during exercise or sleep....
, and blood pressure
Blood pressure
Blood pressure is the pressure exerted by circulating blood upon the walls of blood vessels, and is one of the principal vital signs. When used without further specification, "blood pressure" usually refers to the arterial pressure of the systemic circulation. During each heartbeat, BP varies...
, and the perception of a diminished requirement for food
Food
Food is any substance consumed to provide nutritional support for the body. It is usually of plant or animal origin, and contains essential nutrients, such as carbohydrates, fats, proteins, vitamins, or minerals...
and sleep
Sleep
Sleep is a naturally recurring state characterized by reduced or absent consciousness, relatively suspended sensory activity, and inactivity of nearly all voluntary muscles. It is distinguished from quiet wakefulness by a decreased ability to react to stimuli, and is more easily reversible than...
. Many stimulants are also capable of improving mood and relieving anxiety, and some can even induce feelings of euphoria
Euphoria
Euphoria is an emotional and mental state defined as a sense of great elation and well being.Euphoria may also refer to:* Euphoria , a genus of scarab beetles* Euphoria, a genus name previously used for the longan and other trees...
. It should be noted, however, that many of these drugs are also capable of causing anxiety and heart failure, even the ones that may paradoxically reduce it to a degree at the same time. Stimulants exert their effects through a number of different pharmacological mechanisms, the most prominent of which include facilitation of norepinephrine
Norepinephrine
Norepinephrine is the US name for noradrenaline , a catecholamine with multiple roles including as a hormone and a neurotransmitter...
(noradrenaline) and/or dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
activity (e.g., via monoamine transporter
Monoamine transporter
Monoamine transporters are protein structures that function as integral plasma membrane transporters to regulate concentrations of extracellular monoamine neurotransmitters. Three major classes of MATs are responsible for the reuptake of their associated amine neurotransmitters...
inhibition or reversal), adenosine receptor
Adenosine receptor
The adenosine receptors are a class of purinergic receptors, G protein-coupled receptors with adenosine as endogenous ligand.-Pharmacology:...
antagonism
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
, and nicotinic acetylcholine receptor
Nicotinic acetylcholine receptor
Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction...
agonism
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
.
Indications
Stimulants are used both individually and clinically for therapeutic purposes in the treatment of a number of indications, including the following:- To counteract lethargy and fatigue throughout the day while at work or while doing other activities.
- To reduce sleepiness and to keep the person awake when necessary, as well as to treat narcolepsyNarcolepsyNarcolepsy is a chronic sleep disorder, or dyssomnia, characterized by excessive sleepiness and sleep attacks at inappropriate times, such as while at work. People with narcolepsy often experience disturbed nocturnal sleep and an abnormal daytime sleep pattern, which often is confused with insomnia...
. - To decrease appetite and promote weight loss, as well as to treat obesityObesityObesity is a medical condition in which excess body fat has accumulated to the extent that it may have an adverse effect on health, leading to reduced life expectancy and/or increased health problems...
. - To improve concentration and focus while at work or school, especially for those with attentional disorders such as ADHD.
- Occasionally, they are also used off label to treat clinical depressionClinical depressionMajor depressive disorder is a mental disorder characterized by an all-encompassing low mood accompanied by low self-esteem, and by loss of interest or pleasure in normally enjoyable activities...
, more particularly, non-typical depression and treatment-resistant depression.
Caffeine
Caffeine is a mild stimulant compound that is found naturally in coffee
Coffee
Coffee is a brewed beverage with a dark,init brooo acidic flavor prepared from the roasted seeds of the coffee plant, colloquially called coffee beans. The beans are found in coffee cherries, which grow on trees cultivated in over 70 countries, primarily in equatorial Latin America, Southeast Asia,...
, tea
Tea
Tea is an aromatic beverage prepared by adding cured leaves of the Camellia sinensis plant to hot water. The term also refers to the plant itself. After water, tea is the most widely consumed beverage in the world...
, and to a lesser degree, in cocoa
Cocoa solids
Cocoa solids are the low-fat component of chocolate. When sold as an end product, it may also be called cocoa powder, cocoa, and cacao....
or chocolate
Chocolate
Chocolate is a raw or processed food produced from the seed of the tropical Theobroma cacao tree. Cacao has been cultivated for at least three millennia in Mexico, Central and South America. Its earliest documented use is around 1100 BC...
. It is included in many soft drink
Soft drink
A soft drink is a non-alcoholic beverage that typically contains water , a sweetener, and a flavoring agent...
s, as well as a larger amount in energy drink
Energy drink
Energy drinks are beverages whose producers advertise that they "boost energy." These advertisements usually do not emphasize energy derived from the sugar and caffeine they contain but rather increased energy release due to a variety of stimulants and vitamins....
s. Caffeine is the world's most widely used psychoactive drug and by far the most common stimulant. The vast majority (over 85%) of people in the United States consume caffeine on a daily basis. Few jurisdictions restrict its sale and use. Caffeine is also included in some medications, usually for the purpose of enhancing the effect of the primary ingredient, or reducing one of its side effects (especially drowsiness). Tablets containing standardized doses of caffeine are also widely available.
Nicotine
NicotineNicotine
Nicotine is an alkaloid found in the nightshade family of plants that constitutes approximately 0.6–3.0% of the dry weight of tobacco, with biosynthesis taking place in the roots and accumulation occurring in the leaves...
is the active chemical constituent in tobacco
Tobacco
Tobacco is an agricultural product processed from the leaves of plants in the genus Nicotiana. It can be consumed, used as a pesticide and, in the form of nicotine tartrate, used in some medicines...
, which is available in many forms, including cigarette
Cigarette
A cigarette is a small roll of finely cut tobacco leaves wrapped in a cylinder of thin paper for smoking. The cigarette is ignited at one end and allowed to smoulder; its smoke is inhaled from the other end, which is held in or to the mouth and in some cases a cigarette holder may be used as well...
s, cigar
Cigar
A cigar is a tightly-rolled bundle of dried and fermented tobacco that is ignited so that its smoke may be drawn into the mouth. Cigar tobacco is grown in significant quantities in Brazil, Cameroon, Cuba, the Dominican Republic, Honduras, Indonesia, Mexico, Nicaragua, Philippines, and the Eastern...
s, chewing tobacco
Chewing tobacco
Chewing tobacco Chewing tobacco Chewing tobacco (also known colloquially as hoobastank, backy, tobac, doogooos,Hogleg, chewpoos, chits, chewsky, chawsky, dip, flab, chowers, guy, or a wad, as well as referred to as dipsky, snuff, a pinch, a yopper, a Packing a bomb, a tobbackey or packing a...
, and smoking cessation
Smoking cessation
Smoking cessation is the process of discontinuing the practice of inhaling a smoked substance. This article focuses exclusively on cessation of tobacco smoking; however, the methods described may apply to cessation of smoking other substances that can be difficult to stop using due to the...
aids such as nicotine patch
Nicotine patch
A nicotine patch is a transdermal patch that releases nicotine into the body through the skin. It is used as an aid in nicotine replacement therapy , a process for smoking cessation. The first published study of the pharmacokinetics of a transdermal nicotine patch in humans was authored by Jed E....
es and nicotine gum
Nicotine gum
Nicotine gum is a type of chewing gum that delivers nicotine to the body. It is used as an aid in nicotine replacement therapy , a process for smoking cessation and quitting smokeless tobacco. The nicotine is delivered to the bloodstream via absorption by the tissues of the mouth.It is currently...
. Nicotine is used widely throughout the world for its stimulating effects.
Amphetamines
Norepinephrine-dopamine reuptake inhibitor
A norepinephrine-dopamine reuptake inhibitor is a drug which acts as a reuptake inhibitor for the neurotransmitters norepinephrine and dopamine by blocking the action of the norepinephrine transporter and the dopamine transporter , respectively...
, amphetamine increases the levels of norepinephrine and dopamine in the brain via reuptake inhibition; however, the more important mechanism by which amphetamines cause stimulation is through the direct release of these catecholamine
Catecholamine
Catecholamines are molecules that have a catechol nucleus consisting of benzene with two hydroxyl side groups and a side-chain amine. They include dopamine, as well as the "fight-or-flight" hormones adrenaline and noradrenaline released by the adrenal medulla of the adrenal glands in response to...
s from storage vesicles
Vesicle (biology)
A vesicle is a bubble of liquid within another liquid, a supramolecular assembly made up of many different molecules. More technically, a vesicle is a small membrane-enclosed sack that can store or transport substances. Vesicles can form naturally because of the properties of lipid membranes , or...
in cells. Amphetamines are known to cause elevated mood and euphoria
Euphoria
Euphoria is an emotional and mental state defined as a sense of great elation and well being.Euphoria may also refer to:* Euphoria , a genus of scarab beetles* Euphoria, a genus name previously used for the longan and other trees...
as well as rebound depression
Clinical depression
Major depressive disorder is a mental disorder characterized by an all-encompassing low mood accompanied by low self-esteem, and by loss of interest or pleasure in normally enjoyable activities...
and anxiety
Anxiety
Anxiety is a psychological and physiological state characterized by somatic, emotional, cognitive, and behavioral components. The root meaning of the word anxiety is 'to vex or trouble'; in either presence or absence of psychological stress, anxiety can create feelings of fear, worry, uneasiness,...
.
Amphetamine
Amphetamine
Amphetamine or amfetamine is a psychostimulant drug of the phenethylamine class which produces increased wakefulness and focus in association with decreased fatigue and appetite.Brand names of medications that contain, or metabolize into, amphetamine include Adderall, Dexedrine, Dextrostat,...
s are often used for their therapeutic effects; physicians occasionally prescribe amphetamine
Amphetamine
Amphetamine or amfetamine is a psychostimulant drug of the phenethylamine class which produces increased wakefulness and focus in association with decreased fatigue and appetite.Brand names of medications that contain, or metabolize into, amphetamine include Adderall, Dexedrine, Dextrostat,...
s to treat major depression, where subjects do not respond well to traditional SSRI
Selective serotonin reuptake inhibitor
Selective serotonin re-uptake inhibitors or serotonin-specific reuptake inhibitor are a class of compounds typically used as antidepressants in the treatment of depression, anxiety disorders, and some personality disorders. The efficacy of SSRIs is disputed...
medications, and numerous studies have demonstrated the effectiveness of drugs such as Adderall
Adderall
Adderall is a brand name of amphetamine salts–based medication used for attention-deficit hyperactivity disorder and narcolepsy. It is a brand-name psychostimulant medication composed of racemic amphetamine aspartate monohydrate, racemic amphetamine sulfate, dextroamphetamine saccharide, and...
in controlling symptoms associated with ADD
ADHD predominantly inattentive
ADHD predominantly inattentive is one of the three subtypes of Attention-deficit hyperactivity disorder . While ADHD-PI is sometimes still called "attention deficit disorder" by the general public, these older terms were formally changed in 1994 in the new Diagnostic and Statistical Manual of...
/ADHD
Attention-deficit hyperactivity disorder
Attention deficit hyperactivity disorder is a developmental disorder. It is primarily characterized by "the co-existence of attentional problems and hyperactivity, with each behavior occurring infrequently alone" and symptoms starting before seven years of age.ADHD is the most commonly studied and...
. In rare cases, ADD
ADHD predominantly inattentive
ADHD predominantly inattentive is one of the three subtypes of Attention-deficit hyperactivity disorder . While ADHD-PI is sometimes still called "attention deficit disorder" by the general public, these older terms were formally changed in 1994 in the new Diagnostic and Statistical Manual of...
/ADHD
Attention-deficit hyperactivity disorder
Attention deficit hyperactivity disorder is a developmental disorder. It is primarily characterized by "the co-existence of attentional problems and hyperactivity, with each behavior occurring infrequently alone" and symptoms starting before seven years of age.ADHD is the most commonly studied and...
patients who are not responding sufficiently to traditional amphetamine
Amphetamine
Amphetamine or amfetamine is a psychostimulant drug of the phenethylamine class which produces increased wakefulness and focus in association with decreased fatigue and appetite.Brand names of medications that contain, or metabolize into, amphetamine include Adderall, Dexedrine, Dextrostat,...
s are prescribed dextrorotary methamphetamine
Methamphetamine
Methamphetamine is a psychostimulant of the phenethylamine and amphetamine class of psychoactive drugs...
. Due to their availability and fast-acting effects, amphetamine
Amphetamine
Amphetamine or amfetamine is a psychostimulant drug of the phenethylamine class which produces increased wakefulness and focus in association with decreased fatigue and appetite.Brand names of medications that contain, or metabolize into, amphetamine include Adderall, Dexedrine, Dextrostat,...
s are prime candidates for abuse.
MDMA ("Ecstasy")
Methylenedioxymethamphetamine (MDMA), known by its common street name "Ecstasy", is an illicit substance that typically comes in either tablet, capsule, or powder/crystal form. It had a medical application as a treatment for depression until 1985 when the DEA placed MDMA into schedule 1, prohibiting most medical studies and applications. Notably, MDMA is also unique and very popular for its entactogenic properties. The stimulant effects of MDMA include hypertension
Hypertension
Hypertension or high blood pressure is a cardiac chronic medical condition in which the systemic arterial blood pressure is elevated. What that means is that the heart is having to work harder than it should to pump the blood around the body. Blood pressure involves two measurements, systolic and...
, anorexia
Anorexia (symptom)
Anorexia is the decreased sensation of appetite...
(appetite loss), euphoria
Euphoria
Euphoria is an emotional and mental state defined as a sense of great elation and well being.Euphoria may also refer to:* Euphoria , a genus of scarab beetles* Euphoria, a genus name previously used for the longan and other trees...
, social disinhibition, insomnia
Insomnia
Insomnia is most often defined by an individual's report of sleeping difficulties. While the term is sometimes used in sleep literature to describe a disorder demonstrated by polysomnographic evidence of disturbed sleep, insomnia is often defined as a positive response to either of two questions:...
(or enhanced wakefulness), improved energy, increased arousal, and increased perspiration, among others.
Cocaine
Cocaine is made from the leaves of the cocaCoca
Coca, Erythroxylum coca, is a plant in the family Erythroxylaceae, native to western South America. The plant plays a significant role in many traditional Andean cultures...
shrub, which grows in the mountain regions of South American countries such as Bolivia
Bolivia
Bolivia officially known as Plurinational State of Bolivia , is a landlocked country in central South America. It is the poorest country in South America...
, Colombia
Colombia
Colombia, officially the Republic of Colombia , is a unitary constitutional republic comprising thirty-two departments. The country is located in northwestern South America, bordered to the east by Venezuela and Brazil; to the south by Ecuador and Peru; to the north by the Caribbean Sea; to the...
, and Peru
Peru
Peru , officially the Republic of Peru , is a country in western South America. It is bordered on the north by Ecuador and Colombia, on the east by Brazil, on the southeast by Bolivia, on the south by Chile, and on the west by the Pacific Ocean....
. In Europe, North America, and in some parts of Asia, the most common form of cocaine is a white crystalline powder. Cocaine is a stimulant but is not normally prescribed therapeutically for its stimulant properties, although it sees clinical use as a local anesthetic, particularly in ophthalmology
Ophthalmology
Ophthalmology is the branch of medicine that deals with the anatomy, physiology and diseases of the eye. An ophthalmologist is a specialist in medical and surgical eye problems...
. Most cocaine use is recreational and its abuse potential is high, and so its sale and possession are strictly controlled in most jurisdictions. Other tropane
Tropane
Tropane is a nitrogenous bicyclic organic compound. It is mainly known for a group of alkaloids derived from it , which include, among others, atropine and cocaine. Both alkaloids contain tropinone from which tropane is a derivate...
derivative drugs related to cocaine are also known such as troparil and lometopane but have not been widely sold or used recreationally.
NRIs & NDRIs
These drugs inhibit the reuptake of norepinephrine and/or dopamine, resulting in increased extracellular levels and therefore enhanced neurotransmission, ultimately producing a stimulant effect. Many of these compounds are used as ADHD medications and antidepressants. The best-known NDRI is bupropionBupropion
Bupropion is an atypical antidepressant and smoking cessation aid. The drug is a non-tricyclic antidepressant and differs from most commonly prescribed antidepressants such as SSRIs, as its primary pharmacological action is thought to be norepinephrine-dopamine reuptake inhibition...
(Wellbutrin, Zyban), and the two best-known NRIs are atomoxetine (Strattera) and reboxetine
Reboxetine
Reboxetine is a drug marketed as an antidepressant for use in the treatment of clinical depression, panic disorder and ADD/ADHD, developed by Pharmacia . Its mesylate salt is sold under tradenames including Edronax, Norebox, Prolift, Solvex, Davedax or Vestra...
(Edronax). Many of these drugs have a considerably lower abuse potential in comparison to other stimulants like the amphetamines and cocaine.
Methylphenidate
MethylphenidateMethylphenidate
Methylphenidate is a psychostimulant drug approved for treatment of attention-deficit hyperactivity disorder, postural orthostatic tachycardia syndrome and narcolepsy. It may also be prescribed for off-label use in treatment-resistant cases of lethargy, depression, neural insult and obesity...
(MPH; Ritalin, Concerta, Metadate, or Methylin) is a drug
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...
approved for treatment
Therapy
This is a list of types of therapy .* Adventure therapy* Animal-assisted therapy* Aquatic therapy* Aromatherapy* Art and dementia* Art therapy* Authentic Movement* Behavioral therapy* Bibliotherapy* Buteyko Method* Chemotherapy...
of attention-deficit hyperactivity disorder
Attention-deficit hyperactivity disorder
Attention deficit hyperactivity disorder is a developmental disorder. It is primarily characterized by "the co-existence of attentional problems and hyperactivity, with each behavior occurring infrequently alone" and symptoms starting before seven years of age.ADHD is the most commonly studied and...
, postural orthostatic tachycardia syndrome
Postural orthostatic tachycardia syndrome
Postural orthostatic tachycardia syndrome is a condition of dysautonomia, more specifically orthostatic intolerance, in which a change from the supine position to an upright position causes an abnormally large increase in heart rate, called tachycardia...
, and narcolepsy
Narcolepsy
Narcolepsy is a chronic sleep disorder, or dyssomnia, characterized by excessive sleepiness and sleep attacks at inappropriate times, such as while at work. People with narcolepsy often experience disturbed nocturnal sleep and an abnormal daytime sleep pattern, which often is confused with insomnia...
. It belongs to the piperidine
Piperidine
Piperidine is an organic compound with the molecular formula 5NH. This heterocyclic amine consists of a six-membered ring containing five methylene units and one nitrogen atom...
class of compounds and increases the levels of dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
and norepinephrine
Norepinephrine
Norepinephrine is the US name for noradrenaline , a catecholamine with multiple roles including as a hormone and a neurotransmitter...
in the brain through reuptake inhibition
Reuptake inhibitor
A reuptake inhibitor , also known as a transporter blocker, is a drug that inhibits the plasmalemmal transporter-mediated reuptake of a neurotransmitter from the synapse into the pre-synaptic neuron, leading to an increase in the extracellular concentrations of the neurotransmitter and therefore an...
of the monoamine transporter
Monoamine transporter
Monoamine transporters are protein structures that function as integral plasma membrane transporters to regulate concentrations of extracellular monoamine neurotransmitters. Three major classes of MATs are responsible for the reuptake of their associated amine neurotransmitters...
s. It also increases the release of dopamine and norepinephrine. MPH possesses structural similarities to amphetamine
Amphetamine
Amphetamine or amfetamine is a psychostimulant drug of the phenethylamine class which produces increased wakefulness and focus in association with decreased fatigue and appetite.Brand names of medications that contain, or metabolize into, amphetamine include Adderall, Dexedrine, Dextrostat,...
, and, though it is less potent, its pharmacological effects are even more closely related to those of cocaine
Cocaine
Cocaine is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. The name comes from "coca" in addition to the alkaloid suffix -ine, forming cocaine. It is a stimulant of the central nervous system, an appetite suppressant, and a topical anesthetic...
.
Modafinil, Adrafinil, and Armodafinil
Modafinil (Provigil/Alertec/Modavigil) is an analeptic drug approved by the (FDA) for the treatment of narcolepsy, shift work sleep disorder, and excessive daytime sleepiness associated with obstructive sleep apnea.Modafinil, like other stimulants, increases the release of monoamines but also elevates hypothalamic histamine levels, leading some researchers to consider Modafinil a "wakefulness promoting agent" rather than a classic amphetamine-like stimulant.
Modafinil has been shown to be effective in the treatment of Attention-Deficit Hyperactivity Disorder (ADHD), depression, cocaine addiction, Parkinson's Disease, schizophrenia, shift workers' sleep disorder and disease-related fatigue.
Adrafinil
Adrafinil
Adrafinil is a mild central nervous system stimulant drug used to relieve excessive sleepiness and inattention in elderly patients...
is the prodrug of Modafinil, and is metabolized into it in about one hour, when taken on an empty stomach.
Armodafinil
Armodafinil
Armodafinil is a stimulant-like drug produced by the pharmaceutical company Cephalon Inc., which was approved by the FDA on June 15, 2007...
is a new version of Modafinil.
Ampakines
Recently, there have been improvements in the area of stimulant pharmacology, producing a class of chemicals known as ampakineAmpakine
Ampakines are a class of compounds known to enhance attention span and alertness, and facilitate learning and memory. The ampakines take their name from the glutamatergic AMPA receptor with which they strongly interact...
s, or eugeroic
Eugeroic
Eugeroics are a chemical class of psychoactive drugs which act as stimulants, and are also known as wakefulness-promoting agents. They are used mainly in the treatment of sleeping disorders, excessive daytime sleepiness and narcolepsy, though they are also used merely to counteract fatigue and...
s, (good arousal). These stimulants tend to increase alertness without the peripheral (body) effects or addiction/tolerance/abuse potential of the traditional stimulants. They have minimal effect on sleep structure, and do not cause rebound hypersomnolence or "come down" effects. Ampakines such as ampalex and CX717
CX717
CX717 is an ampakine compound created by Christopher Marrs and Gary Rogers in 1996 at Cortex Pharmaceuticals. It affects the neurotransmitter glutamate, with trials showing the drug improves cognitive functioning and memory.-Approval process:In 2005 the U.S...
have been developed but are still in clinical trials and have not yet been sold commercially. Another compound with similar effects to these drugs is carphedon
Carphedon
Phenotropil is a derivative of the nootropic drug -4-pheyl-2-pyrrolidon. It was developed in Russia, and a small number of low-scale clinical studies have shown possible links between prescription of carphedon and improvement in a number of encephalopathic conditions, including lesions of cerebral...
, which is sold as a general stimulant in Russia under the brand name Phenotropil.
Yohimbine
Yohimbine is a psychoactive drug of the tryptamineTryptamine
Tryptamine is a monoamine alkaloid found in plants, fungi, and animals. It is based around the indole ring structure, and is chemically related to the amino acid tryptophan, from which its name is derived...
chemical class with stimulant and aphrodisiac effects. Yohimbine is sometimes used to remedy Type-2 Diabetes
Diabetes mellitus type 2
Diabetes mellitus type 2formerly non-insulin-dependent diabetes mellitus or adult-onset diabetesis a metabolic disorder that is characterized by high blood glucose in the context of insulin resistance and relative insulin deficiency. Diabetes is often initially managed by increasing exercise and...
in animals and humans that carry the polymorphisms of the α2A-adrenergic receptor gene.
Abuse
AbuseDrug abuse
Substance abuse, also known as drug abuse, refers to a maladaptive pattern of use of a substance that is not considered dependent. The term "drug abuse" does not exclude dependency, but is otherwise used in a similar manner in nonmedical contexts...
of central nervous system
Central nervous system
The central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
stimulants is common. Addiction
Substance use disorder
Substance use disorders include substance abuse and substance dependence. In DSM-IV, the conditions are formally diagnosed as one or the other, but it has been proposed that DSM-5 combine the two into a single condition called "Substance-use disorder"....
to CNS stimulants can quickly lead to medical, psychiatric and psychosocial
Psychosocial
For a concept to be psychosocial means it relates to one's psychological development in, and interaction with, a social environment. The individual needs not be fully aware of this relationship with his or her environment. It was first commonly used by psychologist Erik Erikson in his stages of...
deterioration. Drug tolerance, dependence, sensitisation as well as a withdrawal
Withdrawal
Withdrawal can refer to any sort of separation, but is most commonly used to describe the group of symptoms that occurs upon the abrupt discontinuation/separation or a decrease in dosage of the intake of medications, recreational drugs, and alcohol...
syndrome can occur.