ATC Group: N06B Psychostimulants, agents used for ADHD and nootropics

Adrafinil is a mild central nervous system stimulating drug typically employed to relieve excessive sleepiness and inattention in geriatric patients. It is also been used off-label to prevent fatigue or falling asleep for extended periods of time. Adrafinil is metabolized to modafinil.

Amphetamine is a potent central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. Amphetamine properly refers to a specific chemical, the racemic free base, which is equal parts of the two enantiomers, levoamphetamine and dextroamphetamine, in their pure amine forms. Historically, it has been used to treat nasal congestion and depression. Amphetamine is also used as an athletic performance enhancer and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant.

Aniracetam is a member of pyrrolidin-2-ones and a N-acylpyrrolidine. It is a compound with anti-depressive properties used as a mental performance enhancer.

Armodafinil is an indirect dopamine receptor agonist; both armodafinil and modafinil bind in vitro to the dopamine transporter and inhibit dopamine reuptake. Armodafinil (R-modafinil) has pharmacological properties similar to those of modafinil (a mixture of R- and S-modafinil), to the extent tested in animal and in vitro studies.

Atomoxetine is a highly selective and potent inhibitor of the pre-synaptic noradrenaline transporter, its presumed mechanism of action, without directly affecting the serotonin or dopamine transporters.

Caffeine is structurally related to the methylxanthines theophylline and theobromine. Caffeine’s main action is as a CNS stimulant.

Citicoline stimulates the biosynthesis of structural phospholipids of the neuronal membrane. Citicoline, through this action, improves the function of the membrane mechanisms, such as the functioning of the ionic exchange pumps and receptors inserted in the latter, the modulation of which is indispensable in the neurotransmission.

Amphetamines are non-catecholamine, sympathomimetic amines with CNS stimulant activity. Peripheral actions include elevations of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action.

Dexmethylphenidate is a CNS stimulant. It is the more pharmacologically active d-enantiomer of racemic methylphenidate. Methylphenidate blocks the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. The mode of therapeutic action in Attention Deficit Hyperactivity Disorder (ADHD) is not known.

Idebenone is an anti-oxidant assumed to be capable of transferring electrons directly to complex III of the mitochondrial electron transport chain, thereby restoring cellular energy (ATP) generation under experimental conditions of complex I deficiency. Similarly, in LHON idebenone can transfer electrons directly to complex III of the electron transport chain, thereby bypassing complex I which is affected by all three primary mtDNA mutations causing LHON, and restoring cellular ATP generation.

Lisdexamfetamine is rapidly absorbed from the gastrointestinal tract and hydrolysed primarily by red blood cells to dexamfetamine, which is responsible for the drug’s activity. Amfetamines are non-catecholamine sympathomimetic amines with CNS stimulant activity.

Meclofenoxate is a cholinergic nootropic with antianoxic effect whether anoxia is provoked by defect or misuse of oxygen. Meclofenoxate improves extraction and utilization of glucose from the brain which allows maintenance of storage of energy for the neuron even in case of O₂ deficiency or aging. In elderly patients, meclofenoxate has been shown to improve performance on certain memory tests. Meclofenoxate also increases cellular membrane phospholipids.

Methamphetamine is a sympathomimetic amine with CNS stimulant activity. Peripheral actions include elevation of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action.

Methylphenidate HCl is a mild central nervous system (CNS) stimulant. The mode of therapeutic action in Attention Deficit Hyperactivity Disorder (ADHD) is not known. Methylphenidate is thought to block the reuptake of noradrenaline and dopamine into the presynaptic neurone and increase the release of these monoamines into the extraneuronal space.

Modafinil promotes wakefulness in a variety of species, including man. The precise mechanism(s) through which modafinil promotes wakefulness is unknown.

Piracetam’s mode of action in cortical myoclonus is as yet unknown. Piracetam exerts its haemorrheological effects on the platelets, red blood cells, and vessel walls by increasing erythrocyte deformability and by decreasing platelet aggregation, erythrocyte adhesion to vessel walls and capillary vasospasm.

Solriamfetol is indicated to improve wakefulness in patients with excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea. Its mechanism of action has not been fully characterised. However, its efficacy could be mediated through its activity as a dopamine and norepinephrine (noradrenaline) reuptake inhibitor (DNRI).

Temgicoluril has an effect on the structure of limbic–reticular activity, particularly on hypothalamus emotional zone, as well as on all several basic neuromediator systems – γ aminobutyric acid (GABA), choline, serotonin, and adrenergic activity. It decreases brain norepinephrine levels and increases brain serotonin levels without modulating dopaminergic systems or cholinergic systems. Temgicoluril purportedly has anti-anxiety (anxiolytic) properties. It is also used to aid smoking cessation. In addition, temgicoluril may be useful in the treatment of adult attention-deficit/hyperactivity disorder (ADHD) symptoms.