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CNS stimulants

What is CNS Stimulants?

Central nervous system (CNS) stimulants are medicines that stimulate the brain to speed up both mental and physical processes.

CNS stimulants increase energy, improve alertness and attention, and elevate heart rate, blood pressure, and respiratory rate. They decrease the need for sleep, improve concentration and confidence, reduce appetite, and lessen inhibitions.

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Stimulants can have different mechanisms. Many stimulants exert their effects through the manipulation of monoamine neurotransmission. Monoamines are a class of neurotransmitter that is relevant in motivation, reward, temperature regulation, and pain sensation that include norepinephrine, dopamine, and serotonin. Stimulants typically block the reuptake or stimulate the efflux of dopamine and norepinephrine resulting in increased activity of their circuits. Some stimulants, such as those with hallucinogenic and empathogenic effects change serotonergic neurotransmission. Interference with vesicular storage, reversing the flow of monoamine transporters, and activating TAAR1 may play a mechanism in the activity of the CNS stimulants. Adrenergic stimulants, such as ephedrine, may act by directly binding and activating the receptors that norepinephrine and epinephrine usually bind to, producing sympathomimetic effects. Some drugs, such as MDMA and its derivatives may lower regulatory capability by antagonizing adenosine receptors instead of directly acting on monoamines.

CNS stimulants may be useful to treat certain conditions characterized by symptoms such as inability to concentrate, prolonged fatigue, or excessive sleepiness. CNS stimulants may also be used to help with weight loss in people who are morbidly obese. CNS stimulants have been used for the following conditions:

  • Chronic lethargy
  • Attention deficit disorder
  • Narcolepsy
  • Postural orthostatic tachycardia syndrome
  • Neonatal apnea
  • Prolonged depression that does not respond to traditional antidepressants

Some people misuse CNS stimulants for their ability to increase energy levels. Some CNS stimulants may also create a feeling of euphoria or temporarily increase self-confidence.

The following are some notable stimulants:

Amphetamine

Amphetamine is a potent CNS stimulant of the phenethylamine class for the treatment of attention deficit hyperactivity disorder and narcolepsy. It refers to equal parts of the enantiomers: 50% levoamphetamine and 50% dextroamphetamine. Amphetamine is also used as a performance and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant.

Caffeine

Caffeine is a stimulant compound in the xanthine class of chemicals naturally found in coffee, tea, cocoa or chocolate.  It is an ingredient in many soft drinks and present in large amount in energy drinks. Caffeine is the world’s most widely used psychoactive drug and by far the most common stimulant. 

Ephedrine

It is a sympathomimetic amine similar in molecular structure to phenylpropanolamine and methamphetamine, as well as the neurotransmitter epinephrine. It is commonly used as a stimulant, concentration aid, appetite suppressant, and decongestant.

MDMA

Methylenedioxymethamphetamine, or MDMA or ecstasy, is a euphoriant empathogen, and stimulant of the amphetamine class. It is used as an adjunct to therapy, but has become popular recreationally.

MDPV

Methylenedioxypyrovalerone is a psychoactive drug with stimulant properties that act as a norepinephrine-dopamine reuptake inhibitor. It remained an obscure stimulant until around 2004 when it was reported to be sold as a designer drug. 

Mephedrone

It is a synthetic stimulant drug of the amphetamine and cathinone classes.

Methamphetamine

It is a neurotoxin and potent psychostimulant in the phenethylamine and amphetamine classes that is used to treat ADHD and obesity.