Adrafinil is a stimulant of central nervous system, which can be used to fight sleepiness and concentration loss. It is classified as a eugeroic, or wakefulness-promoting agent. The feature of eugeroics is that they increase alertness without overstimulation and adverse effects typical to other stimulants like amphetamines. Adrafinil mostly used to combat fatigue by night time workers, and other people who need to stay alert for a long time.
The drug was discovered in 1974 in France by Louis Lafon Laboratories. After clinical trials done in both animals and humans, Adrafinil hit the market in 1984 under brand “Olmifon.” The most known eugeroic Modafinil, which is the active metabolite of Adrafinil, was discovered two years later after its prodrug.
Adrafinil effects and usage
Adrafinil is Modafinil prodrug, that means it is metabolized in the body into Modafinil, thus having almost identical pharmacological effects. In contradistinction to Modafinil, it takes more time to take effect. Adrafinil effects usually occur in one hour after taken orally on an empty stomach.
Since it’s a wakefulness-promoting agent, the main indication for use is the treatment of narcolepsy, daytime sleepiness, and shift work sleep disorder.
Adrafinil increase both mental and physical performance. Some athletes use it as a stimulant or pre-workout supplement. However, the usage in sports limited because Adrafinil is banned by World Anti-Doping Agency.
Most common off-label usage is concentration increase. The ability of Adrafinil to improve attention and learning ability is just what many people needs.
Mechanism of action
Adrafinil acts as a α1-adrenergic receptors agonist. Adrenergic receptor antagonists, such as Yohimbine or Dibenzyline block Adrafinil effects. The drug also affects the release of inhibitory and excitatory neurotransmitters. Studies found that Modafinil inhibits the release of GABA in hypothalamic structures, striatum, and neocortex which in turn increases the dopamine levels. Adrafinil also showed to increase the glutamate release in various brain structures.
Compared to other Nootropics, Adrafinil pretty harmful to health. The reason of that is that it is toxic to the liver. To avoid liver damage, you should cycle Adrafinil correctly with proper dosage. Suggested dosage is 600-1200mg one-three times a week, maximum for five months. You can also use milk thistle to restore liver after a course.
The other possible side effects include:
- Skin redness.
Adrafinil is effective yet not a completely harmless wakefulness-promoting agent. The biggest advantage of Adrafinil is that it is sold OTC as a supplement. So you can experience benefits of Modafinil like noticeable and fast concentration increase with the stimulant effect, without having a prescription. But the downside is that it will harm your liver more than Modafinil. Phenotropil at this point seems like a better OTC Modafinil alternative.