Adrafinil

What is Adrafinil?

Adrafinil, sold under the brand name Olmifon, is a wakefulness-promoting medication that was formerly used in France to improve alertness, attention, and mood, particularly in the elderly. It is considered a mild central nervous system stimulant. Adrafinil is a "prodrug," which means it is metabolized in the body into an active substance. In the case of adrafinil, it is primarily metabolized into modafinil, which is a prescription drug used to treat excessive sleepiness associated with conditions like narcolepsy, obstructive sleep apnea, and shift work disorder.

Because adrafinil is converted to modafinil in the liver, its effects are very similar to modafinil. However, since the body must first convert it, the onset of action is slower. Adrafinil was withdrawn from the market in France in 2011. It is not approved by the U.S. Food and Drug Administration (FDA) and is not a regulated substance in the United States.

Benefits and Side Effects

Potential Benefits:

• Increased Wakefulness and Alertness: Adrafinil is primarily known for its ability to promote wakefulness and combat fatigue. This is why it was used for conditions like excessive sleepiness.

• Improved Attention and Mood: The drug was also used to enhance attention and improve mood, particularly in elderly patients.

• Cognitive Enhancement (Nootropic effects): Some people use adrafinil off-label as a "nootropic" or "smart drug" to improve mental performance, focus, and productivity.

Potential Side Effects:

• Liver Concerns: Since adrafinil is metabolized in the liver, long-term or high-dose use may lead to elevated liver enzymes and potential liver damage. This is a significant concern, especially for individuals with pre-existing liver conditions.

• Cardiovascular Issues: As a stimulant, adrafinil can increase blood pressure and heart rate, which may be a risk for people with heart conditions or high blood pressure.

• Psychiatric and Neurological Effects: Adrafinil may cause or worsen psychiatric symptoms such as anxiety, nervousness, hallucinations, and aggression. It can also lead to headaches, dizziness, and insomnia.

• Skin Rashes: In rare cases, adrafinil (and its metabolite, modafinil) can cause severe and life-threatening skin reactions, such as Stevens-Johnson syndrome.

• Addiction and Dependence: Adrafinil has the potential for addiction and dependence, and anecdotal reports suggest that stopping its use can lead to withdrawal symptoms like reduced energy and depression.

Pros and Cons

Pros:

• Wakefulness Promotion: It is effective at promoting wakefulness and reducing fatigue.

• Cognitive Enhancement: It may improve focus and attention.

• Readily Available (as an unregulated substance): It is available as a dietary supplement or research chemical in some countries, but this also means there's no regulatory oversight.

Cons:

• Liver Toxicity: The risk of liver damage is a major drawback, especially with long-term use.

• Cardiovascular Risks: It can be dangerous for people with pre-existing heart conditions.

• Psychiatric Side Effects: The potential for mood and behavioral changes is a significant concern.

• Lack of Regulation: Because it's not a regulated medication, its quality, purity, and dosage can be inconsistent and unreliable.

• Legality: Adrafinil is a banned substance by the World Anti-Doping Agency (WADA) and is often not a legally recognized or approved medication.

Dosage and Frequency

There is no standardized medical dosage for adrafinil because it is not an FDA-approved drug. Information on dosage is largely based on anecdotal reports and some historical studies. Common dosages mentioned in non-medical sources range from 150 mg to 300 mg per day. Due to its long half-life and stimulating effects, it is usually taken once a day in the morning to avoid insomnia. It is crucial to note that these are not medical recommendations and the potential for side effects increases with higher doses.

Half-Life and Detection Time

• Half-life: The half-life of adrafinil is very short, approximately 1 hour. However, it is a prodrug that is metabolized into modafinil, which has a much longer half-life of 12-15 hours. The effects of adrafinil are tied to the accumulation of modafinil in the system.

• Detection Time: Adrafinil's metabolites, including modafinil acid, can be detected in urine for an extended period. The detection time for modafinil can be up to 11 days in urine, depending on the individual's metabolism, dosage, and frequency of use. Saliva tests can detect it for up to 48 hours, and blood tests for up to 24 hours.

Sterogenic, Progestogenic, and Prolactin Effects

Adrafinil is a wakefulness-promoting agent and not an anabolic-androgenic steroid. Therefore, it does not have significant sterogenic, progestogenic, or prolactin-related effects. It is not known to interact directly with steroid hormones like testosterone, estrogen, or progesterone. Its primary mechanism of action involves the central nervous system, particularly the dopamine and orexin pathways, to promote wakefulness.

Anabolic Androgenic Ratio

Anabolic androgenic ratio (AAR) is a metric used to compare the anabolic (muscle-building) effects of a substance to its androgenic (masculinizing) effects. This ratio is specifically relevant to anabolic-androgenic steroids (AAS), such as testosterone and its derivatives.

Adrafinil is not an anabolic-androgenic steroid and therefore has no anabolic androgenic ratio. It does not have anabolic or androgenic properties.