40g Adrafinil

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Adrafinil (diphenylmethyl) sulfinyl-2 acetohydroxamic acid) is a synthetic compound with nootropic like effects. It is a prodrug of modafinil, both of which shares similar structure. As a prodrug, adrafinil increases the production of modafinil in the body. Researches have shown that adrafinil has the ability to activate behavioural arousal without causing any undesirable amphetamine-like effects. This exceptional characteristic is the primary reason why adrafinil has been grouped under the “eurgeroic” pharmaceutical category [1], [2], [3], [4].

Earlier clinical studies have shown that adrafinil is effective in treating memory problems, sleeping difficulties, arousal/vigilance deficits, depression and voluntary movement deficits amongst the elderlies. These studies however are mostly done in France and have not been replicated since on other countries [1]. Majority of studies undertaken to assess and evaluate the effects of adrafinil are done using non-human models such as rats, canines and monkeys [1], [2], [4].


Key findings


Promotes vigilance and arousal [1].

Increased locomotor activity [1], [4].

Increased learning [3].

Improved motivation [3].

Reduction of immobility [5].

Anti-depressant like effects [5].



In non-human studies, adrafinil is able to increase the arousal and locomotor activities of aged canines without causing any stereotypical activities usually seen on amphetamines (e.g. stereotypical behaviour, increased heart rate, high blood pressure, anxiety tolerance and dependence. Size discrimination was enhanced and adrafinil appears to cause prolonged electroencephalographic activity [1], [4]. In a similar test (open-field study) comparing adrafinil, nicergoline and propentofylline, only adrafinil demonstrated significant effects on alertness, behavioural, and memory improvement [9].

One clinical study comparing placebo and adrafinil revealed that the latter is able to effectively enhance learning. This was evidenced by the marked decrease of both trials and errors after doses of adrafinil as compared to placebo use [3].

Though the World Anti-Doping Agency bans both adrafinil and modafinil for athletes’ use during competitive sports, the US Food and Drug Administration (FDA) have approved modafinil as a treatment for narcolepsy or hypersomnolence. The US FDA also approved modafinil therapy for other sleep related disorders such as obstructed sleep apnoea (OSA)[10], [12].

Similar to adrafinil, modafinil is able to promote wakefulness and alertness amongst users as well as locomotor activities amongst non-human models [10], [11]. Some studies have also shown that it is effective in treating substance addiction and has neuroprotective properties[10], [12], [13], [14]. Modafinil is able to exert its effects without causing ensuing rebound hypersomnolence usually seen in caffeine and other amphetamines. Undesirable effects such as increased heart rate, stereotypical behaviors, dependence, tolerance, appetite problems, high blood pressure, anxiety and anorexia are unlikely to be seen with modafinil and adrafinil use [1], [11], [12].


How does adrafinil and modafinil works?


The mechanism of action for both adrafinil and modafinil is yet to be discovered. Theorists however hypothesized that both drugs have an antagonistic effect on the central nervous system’s (CNS) noradrenergic system. It is said to exert its impact on the post-synaptic alpha-1 receptors. Alpha-1 agonists function through decreasing or preventing the locomotor activities enhancing effects of adrafinil. Adrafinil helps in increasing hypocretin production in the hypothalamus. Hypocretin is a neurotransmitter that helps in the production of other critical neurotransmitter including norepinephrine, dopamine and histamine [4], [6], [7] . Other mechanism attributed to modafinil and adrafinil include the ability of these drugs to prevent gamma aminobutyric acid (GABA) release. Prevention of GABA passage and/or increased cerebral metabolism leads to alertness and wakefulness [1].

The properties of these novel compounds - modafinil and adrafinil as reflected in numerous studies and accounts show that both are potent nootropic compounds. However, further human and non-human studies are needed to further explore its potential benefits as well as ensure its safety and efficacy.


AdrafinilCited Sources

[1] http://www.ncbi.nlm.nih.gov/pubmed/11191710

[2] http://www.ncbi.nlm.nih.gov/pubmed/13679229

[3] http://www.ncbi.nlm.nih.gov/pubmed/10880682

[4] http://www.ncbi.nlm.nih.gov/pubmed/10880681

[5] http://www.ncbi.nlm.nih.gov/pubmed/3713198

[6] http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2654794/pdf/NDT-3-349.pdf

[7] http://www.ncbi.nlm.nih.gov/pubmed/11191710

[8] http://www.ncbi.nlm.nih.gov/pubmed/228945

[9] http://www.ncbi.nlm.nih.gov/pubmed/11108188

[10] http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2654794/pdf/NDT-3-349.pdf

[11] http://www.ncbi.nlm.nih.gov/pubmed/228945

[12] http://www.ncbi.nlm.nih.gov/pubmed/16142993

[13] http://www.ncbi.nlm.nih.gov/pubmed/9353396

[14] http://www.ncbi.nlm.nih.gov/pubmed/2906157


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