Nootropic drugs are used to promote memory, focus and learning, and particularly to prevent cognitive deficits associated with some types of dementia. Their mechanism of action depends on each drug, and although they haven’t been accepted to be used for a wide audience, their use has been researched in animal models mainly and both the benefits and risks have been characterized. Modafinil has been used to treat daytime sleepiness and narcolepsy. It is well tolerated with little side effects, and has gained increasing interest for its reputation to improve attention and mood. But its off-label use has directed the attention of consumers towards non-prescription nootropics as brain-boosting supplements, and the N-hydroxy derivative of modafinil is a popular alternative, called adrafinil (2-((diphenylmethyl)sulfinyl-N-hydroxyacetamide). It is a pro-drug metabolized in the liver to a bioactive substance: modafinil.
Benefits and Pharmacological Effects
Studies show that oral administration of adrafinil increases activity with effects being time- and dose-dependent. It does not seem to induce anxiety, and the effect is described as an increase in wakefulness rather than an amphetamine-like effect. Trials in ambulatory patients aged 65 years and older with vigilance problems show a marked improvement in measures of confusion, attention, power of recall, concentration, vigilance, and fatigue after taking 3 doses of adrafinil daily over 90 days.
Adrafinil has also been tested as a treatment for depression, showing statistically significant improvements in depression rates, with a higher efficacy on psychomotor retardation and without any significant undesirable side effects. Additionally, studies have found that treatment with modafinil, the active metabolite of adrafinil, reduces dopamine cell loss in the striatum, creating a neuroprotective effect at low doses, maybe as a result of preventing cell death or through a neurotrophic effect that promotes additional growth.
Risks and Safety Information
When studying adrafinil as a stimulating drug in animal trials, there have been instances of hyperactivity and stereotypical behavior in dogs with doses ranging from 50 to 200 mg/kg administered over 2 months, and lower doses administered over 3 months. Higher doses may increase the likelihood of side effects, with injury and even death reported in animal trials.
Another study described no harmful side effects, tolerance or dependence after long-term use (over 3 years) of modafinil, the bioactive substance of adrafinil. However, a case report following a patient with adrafinil treatment for 10 months described the development of orofacial dyskinesia; an adrafinil-induced involuntary facial movement disorder.
The drug is not yet approved to be used as treatment by the FDA, it’s not regulated by the DEA, and has been banned by the World Anti-Doping Agency. There is not enough information about the safety of adrafinil because modafinil is used instead in most cases as it is an approved prescription-only drug.
Off-Label Use
Although originally developed to treat certain conditions including narcolepsy and daytime sleepiness, most consumers today take adrafinil as a nootropic aid to increase mental energy and focus.
You should keep in mind that adrafinil is not approved by the FDA and doctors won't prescribe it to their patients, unlike modafinil which is an approved medication. Using drugs off-label is not recommended, but still many people believe it is worth the risk.
Adrafinil capsules and formulas are not commonly found at local retailers, but you can easily get it online. Amazon is one of the favorite places to buy supplements, but adrafinil was recently banned by Amazon, together with a bunch of other nootropic drugs. Remember that this is a drug not a dietary supplement, so a lot of places may choose not to carry it to avoid potential legal trouble, especially when the product comes with health claims.
Summary
Adrafinil is considered a novel drug, used as a vigilance-enhancing agent with studies mainly performed in France. There is credible clinical evidence of improvement in attention, vigilance and memory. It can also improve symptoms of depression and provide a neuroprotective effect. Modafinil is the most widely studied metabolite of adrafinil with similar pharmacological effects and does not show development of tolerance or dependence within standard dosages.
While there is very little information about the long-term safety of adrafinil, studies so far have provided reasonable evidence to say that its harmful effects and toxicity levels are low, with a known case of orofacial dyskinesia described in the literature.
If you are interested, feel free to read more about adrafinil and its benefits and side effects before you rush to buying something that won't do much good for you.
References:
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