What is Adrafinil?

Adrafinil is a synthetic nootropic that is chemically very similar to Modafinil. In fact, Adrafinil works by increasing the levels of Modafinil in the body. Therefore, pharmacological effects of these two compounds are pretty much identical. Adrafinil was originally developed by a French pharmaceutical company and until 2011 marketed under the brand name of Olmifon. Adrafinil is a cognitive-enhancing therapeutic (CET) compound designed to relieve excessive daytime sleepiness and inattention in elderly patients. Modafinil (bioactive metabolite of Adrafinil) is an effective wakefulness promoting agent used by people with other disorders, such as Parkinson’s disease, multiple sclerosis, depression and obstructive sleep apnoea. Due to its effects, Adrafinil is often used to treat narcolepsy, sleep and attention disorders and is well-known for its ability to promote alertness and wakefulness. That is why Adrafinil is classified as an eugeroic (“the good arousal”) agent.

For example, Adrafinil is widely used by night shift workers who suffer from the Shift Work Sleep Disorder (SWSD) as it increases their overall productivity by improving cognitive performance, wakefulness and mood during the night shift. Most importantly, Adrafinil use does not result in the addictive potential and development of tolerance often associated with more traditional stimulants. Lack of undesirable effects has helped Adrafinil gain popularity as a very effective caffeine replacement. It is used by a wide range of people, including busy businessmen and soldiers.

Adrafinil has stimulant properties but is a unique wakefulness promoting agent as, unlike other stimulants that target the whole Central Nervous System (CNS), it only stimulates the circadian ‘clock’ of the brain. Further, it specifically targets the chemical processes within the brain thereby improving mental focus. Interestingly, it does so without affecting heart rate or blood pressure. This prevents side effects that are often associated with more common central nervous system stimulants (e.g. caffeine).

Although, Adrafinil is mainly used as a nootropic agent to improve alertness some other cognitive and physical benefits have been reported. Some users experience improvements in memory and learning capacity following its use. In addition, there are studies in the elderly showing its clinical efficiency as a mood-enhancing agent. Experimental animal models also demonstrate increases in activity following Adrafinil administration. Following improvements in psychometric tests and motor function in patients with mild cognitive impairments, it has been proposed by scientists to use Adrafinil in the treatment of age-associated memory impairment. It is important to note that Adrafinil does not have any anxiolytic effects.

Overall, Adrafinil is an effective agent to boost mental energy and increase alertness. This makes it a perfect compound to increase your productivity only when absolutely necessary as prolonged use of Adrafinil is not recommended (see below).

Adrafinil Key Benefits:

  • Increased alertness
  • Better mental focus
  • Higher energy levels
  • Increased motivation
  • Vigilance enhancement
  • Stimulates mental function
  • Feeling less lethargic
  • Reduced mental fatigue
  • Reduced daytime sleepiness

Adrafinil Mechanisms of Action:

The exact mechanism of action of Adrafinil is not yet fully understood. However, it is known that Adrafinil is converted to modafinil in the liver. With regards to specific mechanisms of action, a few hypotheses have been proposed.

Firstly, it has been suggested that Adrafinil is a central alpha 1-adrenergic agonist that acts on α-adrenergic receptors in the CNS. A stimulation of these receptors by Adrafinil increases alertness and wakefulness. The same receptors are stimulated by the adrenaline and noradrenaline. Secondly, Adrafinil may increase the brain metabolic rate by regulating energy substrates and various important neurotransmitters.2 Finally, Adrafinil may also play a role in the regulation of excitatory and inhibitory (i.e., GABA) amino acid neurotransmitters.2

Adrafinil Recommended Dosage:

The recommended daily dosage is between 150-300 mg. New users should start with the lowest dose and get used to it first before taking higher doses. Currently, there is very little to suggest that dosages higher than 300 mg per day will have more benefits as it is a potent nootropic compound. Due to its anti-sleep effects, Adrafinil should not be taken in the evening. However, if you accidently take Adrafinil late in the evening, it will not stop a good night’s sleep. Interestingly, evidence suggest that Adrafinil does not negatively affect a the quantity or quality of nocturnal sleep (i.e., normal sleep pattern). Adrafinil should not be taken more than three times a week, for longer than five months. Therefore, Adrafinil should be used on a non-continuous basis by taking it in cycles. Take Adrafinil strategically during the times when you need a great cognitive performance booster.

Compared to Modafinil, it takes slightly longer for Adrafinil and its effective metabolites to reach active levels in the bloodstream. Specifically, if taken on an empty stomach it takes around 45-60 minutes for Adrafinil capsules to start working. It has a half-life of around 5 hours.

Adrafinil Side Effects:

There are little to no side effects associated with Adrafinil if used at recommended dosages. Very few individuals may experience mild headaches or nausea.

References:

  1.     Mignot, E.J.M. 2012. A practical guide to the theraphy of narcolepsy and hypersomnia syndromes. Neurotherapeutics, 9, 739-752.
  2.     Milgram, N.W., Callahan, H. & Siwak, C. 1999. Adrafinil: a novel vigilance promoting agent. CNS Drug Reviews, 5 (3), 193-212.
  3.     Moreno, J.D. 2006. Juicing the brain. Scientific American Mind, 17(6), 66-73.
  4.     Scamell, T.E. et al. 2000. Hypothalamic arousal regions are activated during Modafinil-induced wakefulness. The Journal of Neuroscience, 20 (22), 8620-8628.
  5.     Schwartz, J.R.L. & Roth, T. 2008. Neurophysiology of sleep and wakefulness: basic science and clinical implications. Current Neuropharmacology, 6, 367-378.
  6.     Szabadi, E. 2006. Drugs for sleep disorders: mechanisms and therapeutic prospects. British Journal of Clinical Pharmacology, 61 (6), 761-766.
  7.     Walsh, J.K., Randzzo, A.C., Stone, K.L. & Schweitzer, P.K. 2004. Modafinil improves alertness, vigilance, and executive function during simulated night shifts. Sleep, 27, 434-439.