Summary

Adrafinil is a nootropic supplement with a difference: it’s a CNS stimulant that can prevent fatigue, increase energy, and enhance wakefulness, but it doesn’t cause anxiety or other typical stimulant side effects.[1] It may also improve mood, focus, and learning ability,[2][3] and may even help keep your brain healthy.[4]

Adrafinil is also different in that it’s a prodrug, a biologically inactive compound that is converted to an active drug inside the body. When Adrafinil is metabolized, it is converted to modafinil,[5] a stimulant that increases wakefulness and has a pronounced eugeroic effect without the corresponding increase in anxiety and hyperactivity that is typical of amphetamine stimulants.[6][7]

Because modafinil is the active form of adrafinil, the pharmacological actions and effects of the two compounds are basically identical; however, only a portion of adrafinil is converted to modafinil, so a larger dose of adrafinil is required to create the same effect.

Adrafinil was discovered by Lafon Laboratories in 1974 and the same company isolated modafinil two years later.  Modafinil was selected for further clinical development (and is now available by prescription under the brand names Alertec, Modavigil, and Provigil) but both forms of the compound reached the market. Adrafinil was sold throughout Europe as the prescription drug Olmifon from 1986 until it was discontinued in 2011.

It remains unregulated in the US, Canada, and the UK and can be legally purchased in those countries, but it has been banned as a prohibited stimulant by the World Anti-Doping Association.[8]

It is widely used off-label to fight fatigue and enhance energy, and it is thought by many to be an effective cognitive enhancing nootropic.

Adrafinil has a low incidence of side effects and appears to have a low potential for dependence, tolerance, or addiction.[9]

The body of research centering on adrafinil is relatively limited, with most human studies focusing instead on its active form, modafinil.

Benefits and Effects

Wakefulness Without Stimulant Side Effects

Adrafinil’s eugeroic or wakefulness-promoting properties are the most thoroughly studied and documented of its effects. Extensive animal testing indicates that adrafinil definitely increases both wakefulness and locomotion, and is particularly effective during periods when the research subjects would ordinarily be asleep.[10][11][12]

Testing also confirms that while Adrafinil’s wakefulness-promoting properties are on a par with amphetamine, it doesn’t trigger the anxiety, hyperactivity, elevated heart rate, and other negative side effects associated with amphetamines.[13]

Research on adrafinil’s wakefulness effects on human subjects is limited, but the animal study findings are confirmed by tests in which human subjects were given modafinil, adrafinil’s active form. Modafinil has been proven effective against excessive daytime sleepiness in humans with sleep disorders.[14][15]

A US Army test indicated that modafinil significantly diminished the effects of sleep deprivation among healthy subjects as well. Aviators who took modafinil during a period of two days and one night without sleep demonstrated the ability to perform highly demanding tasks, reduced slow-wave EEG activity, and lessened self-reported problems with mood and alertness in comparison to placebo.[16]

Cognitive Enhancement

In addition to promoting wakefulness and increasing energy, adrafinil may improve the speed of learning and enhance overall cognition. Tests on aged canines showed that treatment with adrafinil produced substantial improvement in learning, as indicated by a decrease in errors and an increase in successful task completion.[17]

While there are relatively few studies on adrafinil’s effect on human cognition, those that have been conducted suggest that adrafinil has significant nootropic potential.[18] A double-blind placebo-controlled study of 100 patients aged 65 and over, all of whom had vigilance problems severe enough to disrupt daily life, showed that those who took adrafinil felt happier and less sleepy than those on placebo and also had improved concentration, attention, and power of recall. In a similar test on 548 patients with attention and concentration problems, those who took adrafinil showed significant improvement in daily activities, attention, orientation, and memory.

Clinical trials and research reviews of modafinil, adrafinil’s active form, further confirm the potential for cognitive enhancement.[19][20][21]

Antidepressant Potential

Adrafinil is widely believed to have potential as an antidepressant. Animal studies suggest that adrafinil may contribute to a significant improvement in aging and neurodegenerative disorders that involve depression,[22] and though human studies on this aspect of adrafinil are limited, the ones that exist indicate that it may alleviate depressive symptoms. A two-month study involving 70 depressed patients showed that adrafinil treated depressive symptoms as effectively as clomipramine, a known antidepressant, but caused fewer undesirable somatic or psychological side effects.

In a 28-day study of 81 non-institutionalized patients, those who took adrafinil demonstrated significantly lowered depression and reduced apathy.[23]

Neuroprotectant

Adrafinil’s active form has been shown to act as a potent neuroprotectant, helping keep brain cells healthy and intact and even slowing the degenerative process associated with Parkinson’s disease.[24]

It has also been shown to counteract neuroinflammatory processes caused by methamphetamine use,[25] and preliminary studies suggest its neuroprotective capability could play a role in the treatment of multiple sclerosis.[26]

How it Works

Though the exact chemical mechanisms of adrafinil are not entirely understood, researchers hypothesize that in its metabolized form it acts primarily in two specific areas of the brain, the hypothalamus and amygdala; this sets it apart from amphetamine and other psychostimulants that induce wakefulness by general widespread neuronal activation. This selective neuronal activation is thought to be key to adrafinil’s ability to promote wakefulness without triggering negative side effects typical of CNS stimulants.

One of the ways in which metabolized adrafinil promotes wakefulness is by stimulating the brain’s orexin/hypocretin system, which is responsible for regulating wakefulness, arousal, and appetite. Lack of orexin is the cause of the most common form of narcolepsy, and modafinil (adrafinil’s active metabolite) is believed to address this by acting directly on orexin neurons. This stimulation, in turn, increases the production of histamines, which also play an important role in the regulation of the sleep-wake cycle.[27]

Metabolized adrafinil is also known to act on the adrenergic system, the part of the nervous system that releases adrenaline. It is believed to replicate the energy and alertness of an adrenaline release by acting as an adrenergic receptor agonist, boosting levels of adrenergic neurotransmitters in the brain.[28]

Another important brain chemical modulated by metabolized adrafinil is dopamine, an important neurotransmitter associated with the brain’s reward/pleasure responses. Rather than directly stimulating dopamine release to create the rapid and highly amplified rise in dopamine levels typical of CNS stimulants, adrafinil’s active metabolite works more gradually by blocking the receptors that remove dopamine from the synapses, effectively elevating the amount of dopamine available for immediate use in the brain. This gradual and somewhat indirect action on the dopamine system is an important feature of how modafinil works because it reduces the “rush” type of euphoria that is associated with addiction.[29]

Adrafinil is also believed to positively modulate levels of two important excitatory neurotransmitters, glutamate and norepinephrine. Increased availability of these neurotransmitters can result in enhanced neuronal communication, which may improve memory and focus and enhance general cognitive function.

Concentrations of adrafinil in the blood appear to peak at about one hour after ingestion, but because the conversion to its active form takes some time, neurological effects are generally not noted until after concentration peaks. There is no available data on adrafinil’s half-life in humans, but animal studies suggest it has a half-life of about five hours.

Dosage

Dosage recommendations vary, but a range of 150 to 300 mg daily is widely accepted as safe and effective. It is a very powerful nootropic, so it’s a good idea to give the body a chance to adjust by starting with a lower dose and gradually increasing it as needed.

Adrafinil should be ingested on an empty stomach. Because of its potent wakefulness-inducing properties, it should be taken in the morning to allow for normal night’s sleep. Effects can typically be felt within an hour, and the duration of a single dose can be 3-4 hours.

Taking adrafinil on a long-term basis is inadvisable, as it could potentially affect liver function. Using adrafinil in a cycle (for instance, two weeks on, one week off) is preferable. If you do plan to take adrafinil for an extended period, it’s important to have your liver function closely monitored by a medical professional.

Stacking

Adrafinil works efficiently on its own, but it also stacks very well with other nootropics, such as piracetam, phenylpiracetam, and Noopept.

Adrafinil and Noopept Stack

Stacking adrafinil with Noopept is a popular combination that is suited for extended periods of mental work where focus and attention are needed.

As Needed (not more than once per day)

Side Effects

Adrafinil is generally well tolerated when taken responsibly in moderate doses. However, some potential side effects have been documented, and they range from mild to serious.

The most common side effects of adrafinil are headaches, dizziness, nausea, and insomnia.

The most serious side effects are related to liver function, and there is potential for increased risk of high blood pressure and heart problems, particularly when taking higher doses of adrafinil. If you have a history of or are undergoing treatment for liver or cardiovascular problems it is important to consult a medical professional before taking Adrafinil.

If you experience any side effects when taking adrafinil, you should stop taking it and seek medical advice.

Where to Buy

Adrafinil is legal for purchase in the USA, Canada, and the UK. For other countries, please research the laws in your country.

There are only a handful of suppliers for adrafinil, and it is advised to only purchase from reputable sellers. We recommend ordering adrafinil online via PureNootropics.net as they are a trusted seller of nootropics and their supplements are all verified by 3rd party labs to ensure purity.

Closing Thoughts

Adrafinil is a powerful nootropic that can fight fatigue, increase energy, improve mood, and may provide a significant cognitive boost. Its unique combination of mental and physical benefits could make it a valuable supplement for anyone who needs or wants more energy, stamina, and mental acuity.

References   [ + ]

Planning to start a new supplementation regimen? See our medical disclaimer.