Adrafinil

What is adrafinil?

Adrafinil is a synthetic compound primarily used to improve alertness, wakefulness and attention in people suffering from a lack thereof. [3] Adrafinil is a prodrug, which means it is used by the body to convert into a different substance. One of those being: modafinil. Both drugs have very similar chemical structures and effects. Since modafinil can also be synthesized directly, it was tested as an alternative to adrafinil and appeared to be more potent. Therefore it was favored over adrafinil which got discontinued in 2011.[4]

Where does adrafinil come from?

As any synthetic compound, it is synthesized by a pharmaceutical company. This was first done by Assous and Gombert from the french company Laboratoires Lafon in 1974.[1] It wasn’t until later they discovered it could increase activity levels in mice. [2] After studies on various animals showed similar effects it was tested on humans in 1977. It reached the market in france some seven years later in 1984[1]

What are the effects of adrafinil?

Adrafinil works mainly by influencing the neurotransmitters orexin and glutamate. Orexin has a role in regulating arousal, wakefulness and appetite.[9] Glutamate is involved in plethora of bodily functions including learning and memory.[10] Adrafinil’s metabolite modafinil was also found to influence dopamine transport in the body which may explain all of its effects.[5][6] Notable effects include improved focus, learning and memory. When taken orally, the effects of adrafinil usually can be felt after an hour and last for six to twelve hours. Adrafinil has a low addictability [7] and people using it are unlikely to build up tolerance. [8]

Cognitive

  • Reduced fatigue
  • Increased wakefulness
  • Increased memory
  • Increased focus

Physical

  • Increased activity

How to use adrafinil?

Like most synthetic drugs adrafinil is available in powder and pill form both having different pros and cons. Pills tend to be easier to use and more available but offer less possibilities in the way of really fine-tuning your preferred dosage. Powders on the other hand, might offer more versatility and fine tuning but can be less user-friendly.

How much adrafinil to use?

When trying out new supplements it is wise to start with a lower dose and–depending on the experienced effects–increase or decrease the dosage accordingly

There are varying reports on how much adrafinil to take. When it was used as a medicine to treat narcolepsy 600 mg was prescribed twice daily. A study on user reports indicated dosages ranged from 50 mg to 2700 mg. [11] When trying out adrafinil for the first time it can be wise to start with a lower dose of 300 mg and, depending on the experienced effects, increase or decrease the dosage accordingly.

What are the side effects of adrafinil?

There are potential unwanted effects of adrafinil, ranging from mild to serious. Less than 10% of users experience a headache, nausea and decreased appetite. Some people experience more serious side effects like anxiety, insomnia or diarrhea.

Cognitive

  • Anxiety

Physical

  • Dehydration
  • Headache
  • Dizziness
  • Nausea

Interactions of adrafinil

Most nootropics are relatively safe to use on their own. Combining them with other substances may cause them to suddenly become dangerous or life-threatening.

Adrafinil is metabolized into modafinil which decreases the efficacy of opioids. Potentially leading to withdrawal symptoms. It is also used popularly in combination with noopept.

References

  1. [1] Guglietta, A. (2014). Drug Treatment of Sleep Disorders. Springer Publishing.
  2. [2] Duteil, J., Rambert, F. A., Pessonnier, J., Gombert, R., & Assous, E. (1979). A possible α-adrenergic mechanism for drug (CRL 40028)-induced hyperactivity. European Journal of Pharmacology, 59(1–2), 121–123. https://doi.org/10.1016/0014-2999(79)90033-5
  3. [3] Milgram, N. W., Callahan, H., & Siwak, C. (2006). Adrafinil: A Novel Vigilance Promoting Agent. CNS Drug Reviews, 5(3), 193–212. https://doi.org/10.1111/j.1527-3458.1999.tb00100.x
  4. [4] Denis, F. (2021). Smart drugs et nootropiques. Socio-Anthropologie, 43, 97–110. https://doi.org/10.4000/socio-anthropologie.8393
  5. [5] Zolkowska, D., Jain, R., Rothman, R. B., Partilla, J. S., Roth, B. L., Setola, V., Prisinzano, T. E., & Baumann, M. H. (2009). Evidence for the Involvement of Dopamine Transporters in Behavioral Stimulant Effects of Modafinil. Journal of Pharmacology and Experimental Therapeutics, 329(2), 738–746. https://doi.org/10.1124/jpet.108.146142
  6. [6] Reith, M. E., Blough, B. E., Hong, W. C., Jones, K. T., Schmitt, K. C., Baumann, M. H., Partilla, J. S., Rothman, R. B., & Katz, J. L. (2015). Behavioral, biological, and chemical perspectives on atypical agents targeting the dopamine transporter. Drug and Alcohol Dependence, 147, 1–19. https://doi.org/10.1016/j.drugalcdep.2014.12.005
  7. [7] Mignot, E. J. M. (2012). A Practical Guide to the Therapy of Narcolepsy and Hypersomnia Syndromes. Neurotherapeutics, 9(4), 739–752. https://doi.org/10.1007/s13311-012-0150-9
  8. [8] Mitler, M. M., Harsh, J., Hirshkowitz, M., & Guilleminault, C. (2000). Long-term efficacy and safety of modafinil (PROVIGIL®) for the treatment of excessive daytime sleepiness associated with narcolepsy. Sleep Medicine, 1(3), 231–243. https://doi.org/10.1016/s1389-9457(00)00031-9
  9. [9] Sakurai, T. (2007). The neural circuit of orexin (hypocretin): maintaining sleep and wakefulness. Nature Reviews Neuroscience, 8(3), 171–181. https://doi.org/10.1038/nrn2092
  10. [10] McEntee, W. J., & Crook, T. H. (1993). Glutamate: its role in learning, memory, and the aging brain. Psychopharmacology, 111(4), 391–401. https://doi.org/10.1007/bf02253527
  11. [11] Lowe, D. W., Dobson, E., Jewett, A. G., & Whisler, E. E. (2021). Adrafinil: Psychostimulant and Purported Nootropic? American Journal of Psychiatry Residents’ Journal, 17(1), 7–9. https://doi.org/10.1176/appi.ajp-rj.2021.170105
Summary
NameAdrafinil
EffectsFocus
ConsumptionSporadically
Dosage
100
300
600