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Smart drugs and nutrients: Alertness and awakeness with adrafinil

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Smart drugs and nutrients: Alertness and awakeness with adrafinil

Strictly speaking, adrafinil (pronounced ad-ra-fin-l) is a Eugeroic rather than a Nootropic substance.  Eugeroics are wakefulness-promoting agents which are mainly used in the treatment of sleeping disorders, excessive daytime sleepiness (narcolepsy) and cataplexy (sudden fatigue).

Eugeroics

There are only a handful of drugs in this class and the principle ones of note are modafinil (Provigil®), armodafinil (Nuvigil®) and adrafinil (Olmifon®). Since the former two have become controlled substances in many countries, many people are looking to adrafinil, (which was the forerunner to modafinil) as the first choice.

Note: We fail to understand why some countries including Canada, the USA and Australia have listed modafinil as a controlled substance, especially since the Eugorics have failed to show any signs of dependence. Indeed, the conclusion of the Aerospace Medical Association, (Lyons TJ, French J; Modafinil the unique properties of a new stimulant” USAF School of Aerospace, Brooks TX, Science News Note 1991, 62 432-5) was the following:

“The development of modafinil brings to light a crucial social question. What would be the impediment for its use, if a compound such as modafinil is more like caffeine than amphetamine in terms of safety, and yet, as effective as the amphetamines?” 

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Figure: The molecular structure of adrafinil (left) and modafinil (right).

 

Adrafinil vs Modafinil

Adrafinil was discovered in the late 1970s by scientists working with the French pharmaceutical company Group Lafon. Initially it was a French military secret, used for example by the French Foreign Legion in insurgent operations. Then in 1986 it was first offered into the commercial French marketplace as a treatment for narcolepsy. In fact, it was Lafon who later developed modafinil, the primary metabolite of adrafinil.

Even though the exact mechanism of action is unclear, most investigators assume that adrafinil (and modafinil) both act as a α1-adrenergic receptor agonists, with modafinil having even greater affinity. This means that these receptors become more sensitive to the neurotransmitter noradrenaline, (also known as norepinephrine) and accordingly the individual feels a heightened sense of alertness, attention and wakefulness.

Adrafinil is primarily metabolized in-vivo into modafinil, resulting in nearly identical pharmacological effects. Unlike modafinil, however, it takes a little more time for the metabolite to accumulate to active levels in the bloodstream. Effects are usually apparent within approximately 45 minutes after taken orally on an empty stomach.

Adrafinil can affect liver enzymes in a small number of patients; that is if it is used continuously for 3-months or longer. If you have a need to take adrafinil on a daily basis then please ensure that you have some regular bloodwork undertaken; however for the majority of individuals whom may only need adrafinil on an intermittent basis, i.e., taken before a meeting or during an intense learning period etc., this should not be the case.

One thing is for certain, the advent of Eugorics such as adrafinil and modafinil have revolutionised the field of narcolepsy, since they can have the ‘uplifting’ effects of amphetamines, but without the downsides. Eugorics tend to keep the individual on an even level and despite hundreds of studies there is no evidence of addition or dependence.

Effectively, Eugorics have reduced the former alertness enhancing drugs to the trash can of medicine.

Adra-Pro™, the brand version of the latest version of adrafinil PLACED BY THE PRODUCT PHOTO