Basic:
Amphetamine itself is a widely used psychostimulant drug and is the prototype off of which a series of amphetamine analogues have been built. It is a schedule 2 controlled substance in the US and is therefore used medicinally & illicitly. It is one of the most widely prescribed drugs in psychiatry practice. Amphetamine itself was first synthesized in 1887 Germany.
Use:
In the United States (and elsewhere), Amphetamine is used clinically for the following indications:
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Treatment of resistant cases of major depression.
Treatment of chronic fatigue syndrome & narcolepsy.
Emergency treatment of cardiac arrest & other types of acute cardiac failure.
As a nasal decongestant much like ephedrine or pseudoephedrine.
As an appetite suppressant, typically in obese individuals.
Chemistry:
Amphetamine is an analogue of the phenethylamine class and occurs as a racemic mixture. It is similar in structure to ephedrine & pseudoephedrine. Many analogues of amphetamine have been synthesized.
Pharmacology:
Amphetamine acts as a traditional stimulant, by producing sympathomimesis - i.e. arousing the fight or flight response of the sympathetic nervous system by modulating catecholamine neurotransmitters such as Adrenaline, Noradrenaline, and Dopamine. Amphetamine increases vital functions such as breathing & cardiac output and produces vasodilation.
Sympathomimetic agents act by either directly activating post synaptic receptor sites and mimicking neurotransmitters, or by enhancing the actions of the neurotransmitters themselves.Amphetamine works by the latter mechanism, specifically targeting reuptake of norepinephrine, dopamine, and serotonin.
Dopamine & Serotonin: Multiple theories have been proposed as to its exact mechanism. It is generally believed that amphetamine targets DAT and SERT - the presynaptic reuptake pumps for dopamine & serotonin; triggering a series of cellular changes which causes the transporter to function in reverse - i.e. rather than collecting excess dopamine from the synapse like a vaccum, it spits more dopamine or serotonin out into the synapse, basically flooding the synaptic cleft with the neurotransmitter.
The dopaminergic actions of amphetamine take place throughout the mesolimbic & mesocortical reward pathways of the brain - key areas of these pathways include the striatum, ventral striatum, ventral tegmentum, and the nucleus accumbens. The serotonergic actions of amphetamine seem to be limited to key areas of the brain - for instance, projections of serotonergic neurons which run from the VTA to the prefrontal cortex; in addition to other corticolimbic projections.
Norepinephrine: Amphetamine increases extrecellular concentrations of norepinephrine (i.e. noradrenaline). In this case it is believed to act as a norepinephrine reuptake inhibitor. NE activity is heavily associated with arousal of the sympathetic nervous system - i.e. the fight or flight response, and possibly to a lesser extent, reward.
Effects:
Excitement, euphoria, increased energy, alertness, wakefullness, insomnia.
Amphetamine & amphetamine type drugs tend to produce paradoxial effects in those with behavioral disorders such as ADHD - rather than causing excitation, they produce calmness, concentration, and promote pragmatism over a racing thought process.
Side effects include jitteriness, anxiety, agitation, fight or flight mode (adrenaline rush), hypertension, vasodilation, mydriasis (dilated pupils), bowel stimulation, diuresis. Overdose symptoms include irregular heartbeat, psychotic breaks, extreme confusion, slurred speech, aphasia (inability to speak), lazy eye or crossed-eyes, fear & panic, heart attack, stroke, cardiac arrest & death.
Amphetamine is a precursor to countless other psychostimulants just as morphine is to other narcotics (Image Below):
Methamphetamine:
Methamphetamine is the N-methyl analogue of amphetamine.
The methyl group is responsible for the potentiation of effects as compared to the related compound amphetamine, rendering the drug more lipophilic, more brain penetrable, and more resistant to destruction by monoamine oxidase enzymes. Methamphetamine, along with its main metabolite amphetamine, acts at dopamine, NE, and serotonin (5HT) transporters (via blockade) to inhibit presynaptic transmitter reuptake and reverse their direction of flow (i.e. phosphorylation).
Methamphetamine is administered by various routes and in various forms. It can be snorted as a powder, injected as a solution, indirectly heated and smoked in its crystallized form (known as ice or crystal meth), or taken orally in any form. Both insufflation and inhalation are effective as alternatives to injection, they allow good absorbtion and a fairly rapid onset.
In high doses, its effects are known to last up to 12 hours in recreational doses. Habitual or heavy users often stay awake for days at a time. Methamphetamine is known to be neurotoxic.
Ecstasy (MDMA):
MDMA is a popular recreational drug with empathogenic/enactogenic effects. It is a member of the amphetamine family, and is often referred to as ecstasy, X or molly.
Its effects include increased energy, increased sociability, a sense of affection and empathy, enhanced capacity for introspection and self-examination and recovery of repressed memories. Many of these properties have made MDMA extremely useful as a tool in psychotherapy, but it remains a schedule I controlled substance in the US and its therapeutic use has been criminalized.
It is available most commonly as an adulterated powder in a pressed tablet or capsule form for oral use. Effects of this drug are due to an increase in synaptic dopamine, norepinephrine and serotonin. MDMA promotes release of these transmitters and inhibits their reuptake by reversing the flow of monoamine transporters (i.e. reuptake pumps) - the latter process is known as phosphorylation. This drug elicits weak agonist activity at serotonin receptors and at the trace amine-associated (TAAR-1) receptor; involved in monoamine transported regulation. The active metabolite MDA contributes to its effects.
Its empathenogenic properties are believed to be related to both serotonin and the neuromodulator oxytocin, the latter of which serves as a hormone involved in the hard-wiring of emotional attatchments between a mother and fetus during pregnancy & childbirth.
Khat Leaf and Cathines:
Catha edulis is a flowering plant which commonly grows in the horn of Africa and the Arabian peninsula. Its leaves are rich with psychoactive alkaloids and are chewed for their stimulating effect. The leafy preparation is popularly known as Khat.
Cathine:
Cathine is an analogue of amphetamine and a precursor to cathinone. It is the primary naturally occurring alkaloid in "Khat". It differs from amphetamine with the presence of an OH group on the ethyl side chain. It is one optical isomer of phenylpropanolamine. Cathine acts as a sympathomimetic (stimulant) with similar effects to other amphetamines.
Cathinone:
Cathinone is a naturally occurring alkaloid of the substituted amphetamine class. It occurs as an isolated compound or as one of several alkaloids present in the "Khat" plant. It is popularly used for its psychostimulant properties.
Cathinone is chemically described as a substituted phenethylamine. It is a derivative of cathine where the side chain OH group has been oxygenated to a ketone. It is alternatively decribed as a beta keytone of amphetamine.
Its pharmacological profile is similar to amphetamine, both act as sympathomimetics. It acts by triggering an increased synaptic flow of catecholamines centrally and peripherally. Its rewarding & reinforcing effects are due to increased dopaminergic activity at the mesolimbic level.
Methcathinone:
Methcathinone is to cathinone as methamphetamine is to amphetamine. It is a psychostimulant drug of the substituted amphetamine family. Its sympathomimetic effects are similar to cathinone and methamphetamine; it acts by increasing synaptic concentrations, and thus neurotransmission, of catecholamines, both centrally and peripherally.
Mephedrone:
Known chemically as 4-methylmethcathinone. Mephedrone is the 4-methyl derivative of methcathinone and has been marketed as a popular research chemical; until being banned in the US in recent months. Its effects are similar to amphetamine and MDMA. Like other amphetamines, mephedrone increases the flow of catecholamines and serotonin throughout central and peripheral circuits, this is mediated by its action at monoaminergic and 5HT (serotonergic) transporters - specifically, it induces neurotransmitter release and inhibits presynaptic reuptake. Following administration of the drug, dopamine levels in the NA are increased up to 500% compared to baseline, while 5HT levels are increased by up to 950%.
Methedrone:
Known chemically as 4-methoxymethcathinone. Methedrone is the 4-methoxy derivative of methcathinone. It differs from mephedrone only with the presence of an oxygen linking the 4-ethyl group with the phenyl ring. It has been marketed as a popular research chemical. Like other amphetamines, methedrone increases the flow of catecholamines and serotonin throughout central and peripheral circuits, this is mediated by its action at monoaminergic and 5HT (serotonergic) transporters - specifically, it induces neurotransmitter release and inhibits presynaptic reuptake.
Methylone:
Methylone is a psychostimulant drug of the cathinone-amphetamine family. It possesses stimulant and empathogen properties. Methylone is a 3,4 methylenedioxy analogue of methcathinone, and differs from MDMA with the presence of the side chain ketone. It produces its effects by inducing release/inhibiting reuptake of 5HT and monoamine neurotransmitters. Its empathogenic effects are similar to ecstasy - due to its close structural similarity and its potent serotonergic properties. The drug has been marketed as a research chemical.
Amphetamine is a precursor to countless other psychostimulants just as morphine is to other narcotics (Image Below):
Methamphetamine:
Methamphetamine is the N-methyl analogue of amphetamine.
The methyl group is responsible for the potentiation of effects as compared to the related compound amphetamine, rendering the drug more lipophilic, more brain penetrable, and more resistant to destruction by monoamine oxidase enzymes. Methamphetamine, along with its main metabolite amphetamine, acts at dopamine, NE, and serotonin (5HT) transporters (via blockade) to inhibit presynaptic transmitter reuptake and reverse their direction of flow (i.e. phosphorylation).
Methamphetamine is administered by various routes and in various forms. It can be snorted as a powder, injected as a solution, indirectly heated and smoked in its crystallized form (known as ice or crystal meth), or taken orally in any form. Both insufflation and inhalation are effective as alternatives to injection, they allow good absorbtion and a fairly rapid onset.
In high doses, its effects are known to last up to 12 hours in recreational doses. Habitual or heavy users often stay awake for days at a time. Methamphetamine is known to be neurotoxic.
Ecstasy (MDMA):
MDMA is a popular recreational drug with empathogenic/enactogenic effects. It is a member of the amphetamine family, and is often referred to as ecstasy, X or molly.
Its effects include increased energy, increased sociability, a sense of affection and empathy, enhanced capacity for introspection and self-examination and recovery of repressed memories. Many of these properties have made MDMA extremely useful as a tool in psychotherapy, but it remains a schedule I controlled substance in the US and its therapeutic use has been criminalized.It is available most commonly as an adulterated powder in a pressed tablet or capsule form for oral use. Effects of this drug are due to an increase in synaptic dopamine, norepinephrine and serotonin. MDMA promotes release of these transmitters and inhibits their reuptake by reversing the flow of monoamine transporters (i.e. reuptake pumps) - the latter process is known as phosphorylation. This drug elicits weak agonist activity at serotonin receptors and at the trace amine-associated (TAAR-1) receptor; involved in monoamine transported regulation. The active metabolite MDA contributes to its effects.
Its empathenogenic properties are believed to be related to both serotonin and the neuromodulator oxytocin, the latter of which serves as a hormone involved in the hard-wiring of emotional attatchments between a mother and fetus during pregnancy & childbirth.
Khat Leaf and Cathines:Catha edulis is a flowering plant which commonly grows in the horn of Africa and the Arabian peninsula. Its leaves are rich with psychoactive alkaloids and are chewed for their stimulating effect. The leafy preparation is popularly known as Khat.
Cathine:
Cathine is an analogue of amphetamine and a precursor to cathinone. It is the primary naturally occurring alkaloid in "Khat". It differs from amphetamine with the presence of an OH group on the ethyl side chain. It is one optical isomer of phenylpropanolamine. Cathine acts as a sympathomimetic (stimulant) with similar effects to other amphetamines.
Cathinone:
Cathinone is a naturally occurring alkaloid of the substituted amphetamine class. It occurs as an isolated compound or as one of several alkaloids present in the "Khat" plant. It is popularly used for its psychostimulant properties.
Cathinone is chemically described as a substituted phenethylamine. It is a derivative of cathine where the side chain OH group has been oxygenated to a ketone. It is alternatively decribed as a beta keytone of amphetamine.
Its pharmacological profile is similar to amphetamine, both act as sympathomimetics. It acts by triggering an increased synaptic flow of catecholamines centrally and peripherally. Its rewarding & reinforcing effects are due to increased dopaminergic activity at the mesolimbic level.
Methcathinone:
Methcathinone is to cathinone as methamphetamine is to amphetamine. It is a psychostimulant drug of the substituted amphetamine family. Its sympathomimetic effects are similar to cathinone and methamphetamine; it acts by increasing synaptic concentrations, and thus neurotransmission, of catecholamines, both centrally and peripherally.
Mephedrone:
Known chemically as 4-methylmethcathinone. Mephedrone is the 4-methyl derivative of methcathinone and has been marketed as a popular research chemical; until being banned in the US in recent months. Its effects are similar to amphetamine and MDMA. Like other amphetamines, mephedrone increases the flow of catecholamines and serotonin throughout central and peripheral circuits, this is mediated by its action at monoaminergic and 5HT (serotonergic) transporters - specifically, it induces neurotransmitter release and inhibits presynaptic reuptake. Following administration of the drug, dopamine levels in the NA are increased up to 500% compared to baseline, while 5HT levels are increased by up to 950%.
Methedrone:
Known chemically as 4-methoxymethcathinone. Methedrone is the 4-methoxy derivative of methcathinone. It differs from mephedrone only with the presence of an oxygen linking the 4-ethyl group with the phenyl ring. It has been marketed as a popular research chemical. Like other amphetamines, methedrone increases the flow of catecholamines and serotonin throughout central and peripheral circuits, this is mediated by its action at monoaminergic and 5HT (serotonergic) transporters - specifically, it induces neurotransmitter release and inhibits presynaptic reuptake.
Methylone:
Methylone is a psychostimulant drug of the cathinone-amphetamine family. It possesses stimulant and empathogen properties. Methylone is a 3,4 methylenedioxy analogue of methcathinone, and differs from MDMA with the presence of the side chain ketone. It produces its effects by inducing release/inhibiting reuptake of 5HT and monoamine neurotransmitters. Its empathogenic effects are similar to ecstasy - due to its close structural similarity and its potent serotonergic properties. The drug has been marketed as a research chemical.
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