Adrafinil is a wakefulness-promoting agent (eugeroic) and a mild behavioral stimulant. It is widely used as an over-the-counter nootropic (cognitive enhancer). While adrafinil is not approved by the FDA, its metabolite - modafinil - is a drug on its own and it is an approved treatment for narcolepsy, excessive daytime sleepiness, shift work sleep disorder, and other mental disorders.
Modafinil has been extensively studied and approved in many countries, but there is much less research examining the efficacy of adrafinil. The following is a scientific review of adrafinil that explains the basic facts about the mechanism of action and effects of this chemical drug.
If you don't wish to read the full paper, here are the key points:
- Adrafinil was developed in France by Louis Lafon Laboratories as a vigilance-promoting agent for people with sleeping disorders.
- The scientific name of the chemical is (diphenylmethyl)sulfinyl-2-acetohydroxamic acid. It was sold under the brand name Olmifon, which was discontinued in 2011.
- Clinical studies show that adrafinil enhances vigilance, alertness and mood in elderly subjects.
- The powder has a crystalline structure with a white, rosy or beige hue, and a sulfurous smell. Both color and odor may slightly vary from one manufacturer to another.
- The pure compound dissolves partially in water, and is fully soluble in methanol.
- Adrafinil is metabolized in the liver into modafinil, which is its primary active metabolite.
- Adrafinil has a half-life of 1 hour, while modafinil's half-life is 3 hours; according to one study.
- When administered orally, adrafinil takes about 1 hour to reach its peak levels in blood. Results start appearing after about 1 hour of ingestion and fade away after a few hours.
- Adrafinil itself does not have any pronounced therapeutic effects. It is only after it gets converted into its metabolite - modafinil - that it starts taking effect. This usually happens within 1-2 hours after administration, but may take longer for some users.
- The mechanism of action of both adrafinil and modafinil is not conclusively established. There are three possible mechanisms of action that have been investigated:
- Works as a selective alpha-1 adrenergic receptor agonist.
- Suppresses release of GABA and increases release of both dopamine and glutamate.
- Increases cerebral metabolism.
- Some studies suggest that adrafinil/modafinil may have neuroprotective effects, i.e. reduces damage to brain cells and promotes growth.
- Animal studies show that adrafinil may increase activity, motivation, wakefulness and learning.
- Most human studies of adrafinil were conducted in France on older subjects (45+ years old). Here are some of the clinical findings:
- Improvement in concentration, clarity, attention, memory, acuity, and vigilance after 45 days of treatment.
- Feeling happier, less sleepy and more energetic after 90 days of treatment.
- Improvement in patients with depression and anxiety after 3 months of treatment with 900mg/day.
- Adrafinil has more significant effects in patients with mild cognitive impairments like poor vigilance, lack of motivation, sleepiness, low energy, depression, and anxiety. It may not have significant benefits in healthy people.
- No significant side effects were reported in the cited studies. In rare cases, some participants experienced increased excitement, agitation, aggression and/or nausea.