Modafinil

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Modafinil

Medical use

Modafinil is a stimulant. It was developed at the end of the 1980s for the treatment of narcolepsy, which causes people to suddenly falling asleep during daytime.  Modafinil is in use in about 20 countries. In Finland modafinil doesn’t have a trading license, but Fimea has given a special permit for the treatment of narcolepsy with modafinil in Finland.

Modafinil is used also for treatment of conditions other than narcolepsy that also cause daytime sleepiness. In addition, it’s sporadically used for the treatment of memory and attention deficit disturbances, Alzheimer’s disease, and depression [1].

Abuse

Modafinil is classified as a doping substance. Its effect on performance is not researched, but on the basis of its effects, it is assumed that it improves endurance and explosiveness. In connection with bodybuilding, modafinil is known to be used to decrease fatty tissues because of its appetite suppressing effect.

Properties and mechanism of action

The action mechanism of modafinil differs from the mechanism of action of amphetamine and ephedrine or other similar stimulants. Modafinil is also not produced in the body from the amphetamine or ephedrine derivatives. Adrafinil, older than modafinil, is a similar medical substance as modafinil, in terms of its structure and effects.

Modafinil affects many different locations in the brain [2]. Probably the most important is increasing mental agility, an effect that is applied to the bottom of the interbrain, the hypothalamus, where it activates nerve tracks that use orexin (hypocretins) that are important for regulating waking-sleeping states, as their mediating substances.

It also activates the sympathetic alfa-1-receptors of the central nervous system; increases the activity of stimulating glutamine and histamine transmitters; and strengthens the effects of serotonin in the cerebral cortex. In addition, it decreases the activity of those inhibitory nerve cells that use gamma-aminobutyric acid as their transmitters. Modafinil doesn’t excite the dopamine system of the central nervous system, which is the most important effect of amphetamines.

Adverse effects

Modafinil can cause pleasure and addiction but to a much lesser degree than amphetamine. It is well tolerated when used in medical doses, but side effects can include insomnia, headaches, nervousness, anxiety, aggressiveness, increased blood pressure, and heart symptoms [1, 2, 3].

Timo Seppälä
Medical Director
The Finnish Antidoping Agency FINADA

[1] Kumar (2008): Approved and investigational uses of modafinil: an evidence-based review.  Drugs 68(13):1803-39.

[2] Minzenberg & Carter (2008): Modafinil: a review of neurochemical actions and effects on cognition. Neuropsychopharmacology 33(7):1477-502.

[3] Spiller, Borys, Griffith, Klein-Schwartz, Aleguas, Sollee, Anderson & Sawyer (2009): Toxicity from modafinil ingestion. Clinical Toxicology (Philadelphia) 47(2):153-6.

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