Armodafinil is a Nootropic smart drug used to increase alertness and wakefulness, resulting in overall enhanced mental performance.

Armodafinil is sold as a prescription drug under the names Waklert and Nuvigil and has been approved in the USA by the FDA since 2007.

According to its manufacturers Cephalon, Inc., an estimated 1.6 million users have purchased Armodafinil in the last three years.

The drug itself is actually a derivative of Modafinil with many similar effects but a slightly higher potency level.

Which one you use is a matter of personal preference, but many people think that Armodafinil provides a better stimulant effect and that it lasts longer.

The clinical uses for Armodafinil are extensive, but it is also commonly used for off-label purposes as a cognitive enhancer by the nootropic community.

What is Armodafinil, how does it work and should you get a prescription for this drug from your doctor?

History

Armodafinil is a eugeroic, or wakefulness promoting compound. It is related to the compounds Adrafinil and Modafinil, both of which were developed in the 1970s.

In 1974, scientists at the pharmaceutical company Lafon Laboratories in France developed a group of benzhydryl sulfinyl compounds. One of these compounds was Adrafinil. During tests to determine how Adrafinil works in the body, Modafinil was discovered.

When it is ingested, Adrafinil travels through the bloodstream to the liver, where it is broken down into its component parts modafinilic acid and Modafinil. Modafinil is the primary active compound in Adrafinil which causes the effects of this drug.

In initial animal trials, both Adrafinil and Modafinil showed stimulant-like effects, increasing alertness and locomotor activity. Because of these effects, they were first tested for use in humans for treating the sleep disorder narcolepsy.

Both Adrafinil and Modafinil were seen to significantly reduce the excessive daytime sleepiness of narcolepsy and improve wakefulness. Adrafinil was approved as a drug for this purpose in France in 1986, and Modafinil in 1994. Modafinil was also approved in the United States in 1998.

Once it had gone through testing and approval and it was possible to synthesize Modafinil on its own, then the need for Adrafinil diminished. Eventually production of this less potent compound ceased (although it is now made today by other manufacturers).

In 2001 Cephalon Inc bought Lafon Laboratories. Cephalon continued making the original name brand version of Modafinil created by the Lafon scientists, called Provigil.

A few years before the exclusivity patent expired on Provigil, Cephalon scientists were tasked with developing a new version of the compound that would help the company maintain a good position in the market. This led to the development of Armodafinil.

Modafinil is composed of two stereoisomers of the same molecular structure that are mirror image copies of each other (like a left and right hand). These are known as enantiomers, and there is R-Modafinil and S-Modafinil.

In compounds like this, some times one of the enantiomers causes most of the effects, while the other is largely inactive, or possibly is the source of most negative effects. In research it was determined that the R-enantiomer is the most pharmacologically active, stable, and longer-acting of the two isomers.

By isolating the R-enantiomer alone, the scientists developed an enantiopure version of Modafinil, that they called Armodafinil, from R-Modafinil. The brand name version of Armodafinil produced by Cephalon was and is called Nuvigil.

In 2011, Cephalon was acquired by Teva Pharmaceutical Industries. Cephalon still operates as a subsidiary of Teva, and to this day they produce the original name brand versions of Modafinil and Armodafinil, Provigil and Nuvigil respectively.

How Armodafinil Works in the Body

The original intent for developing Armodafinil was as a more potent version of Modafinil, to be used as wakefulness enhancer in individuals who suffer from excessive daytime sleepiness.

It is useful in the treatment of sleep apnea/hypopnea syndrome, narcolepsy, and in promoting higher levels of alertness for people with shift work sleep disorder and other individuals with irregular sleep patterns.

Although early clinical trials were inconclusive, there is still the thought that this pharmaceutical might be helpful in the treatment of attention-deficit hyperactivity disorder (ADHD), depression and schizophrenia.

The FDA has declined to approve this supplement as a treatment for jet leg, but many experts still believe it to be effective in this area.

One of the reasons why Armodafinil has become so popular is because of the powerful energy boost it provides without the kind of negative side effects that other drugs can cause.

The Armodafinil experience is completely unlike caffeine or other traditional stimulants. Most users report that they feel a more ‘natural’ sense of being awake and alert which lasts longer and enables them to be more focused and productive.

Most users will also typically not experience any jitters, anxiety, restlessness, or changes in blood pressure with anywhere near the frequency as seen with traditional stimulants.

Many researchers think Armodafinil helps to somehow alter how the brain perceives or communicates tiredness to the rest of the body.

Like its predecessor Modafinil, the exact mechanism of action of Armodafinil is still unknown. However, similar to Modafinil, Armodafinil has been observed to interact with a large variety of neurotransmitters in the brain and central nervous system, including Dopamine, Serotonin, Epinephrine (Adrenaline), Norepinephrine (Noradrenaline), Orexin (Hypocretin), and Histamine.

Armodafinil has been observed to act as a Dopamine transport inhibitor and a reuptake inhibitor. This allows for more circulating Dopamine.

While it has not been studied directly with Armodafinil, it is believed that many of Modafinil’s effects stem from its interactions with Orexin and Histamine. Is is reasonable to extrapolate the effects seen with Modafinil to Armodafinil’s effects as well, as the two compounds work in very similar ways.

Modafinil activates Orexin neurons and Orexin-secreting neurons in the brain. Orexin is a neuropeptide that plays a role in wakefulness, arousal, and appetite. The Orexin in turn stimulates the release of Histamine, a neurotransmitter that is involved in the same effects in the body.

It is thought that through the action of these two compounds Modafinil and Armodafinil have most of their wakefulness promoting effects.

Armodafinil for Sleep Disorders

Just like Modafinil before it was is used to treat serious sleep disorders, Armodafinil is used in the same way. Armodafinil has been categorized by the Food and Drug Administration (FDA) as a Schedule IV prescription only drug, that is approved as a treatment for narcolepsy and shift-work sleep disorder, and as an adjunct treatment for obstructive sleep apnea/hypopnea syndrome.

Narcolepsy is a neurological sleep disorder that causes excessive daytime sleepiness and bouts of falling asleep randomly and often without warning throughout the day. In multiple double-blind placebo-controlled clinical trials, Modafinil and Armodafinil have been seen to significantly improve wakefulness and reduce excessive daytime sleepiness in narcoleptics compared to placebo.

In one study, patients were given either a placebo or Armodafinil. It was observed that the Armodafinil patients had significantly improved mean sleep latency times on the Maintenance of Wakefulness Test compared to a decrease seen in placebo patients.

Shift work sleep disorder is a condition that some people develop when their work schedule forces them to be awake and working at night, and sleeping during the day, either on a consistent or intermittent basis. This causes excessive sleepiness while awake at night, and can cause insomnia when trying to sleep during the day.

In one study, mean sleep latency times on the Multiple Sleep Latency Test were significantly improved in Armodafinil patients compared to placebo patients. Patient diaries also reported reduced sleepiness on the Epworth Sleepiness scale during nighttime work shifts, lab testing shifts, and during commutes at night.

Obstructive sleep apnea/hypopnea syndrome is a medical condition that affects breathing during sleep. Using a nasal continuous positive airway pressure (nCPAP) machine at night is the most common treatment for this condition. Even with treatment though, some people still experience some excessive daytime sleepiness, and Armodafinil is used in these cases.

In one study, Armodafinil was seen to improve mean sleep latency times from baseline on the Maintenance of Wakefulness tests significantly compared to placebo times. Patient estimated wakefulness was improved, and fatigue was decreased.

Cognitive Enhancer

While many people who take Armodafinil do in fact have a medical need for the drug, it is also uses as a brain booster in non-clinical settings.

If you have been experiencing consistent fatigue or even brain fog, then Armodafinil could be a major help for you.

This is due to a wide range of cognitive enhancing effects. Taking Armodafinil is known to greatly improved concentration and focus.

People who use this drug also report that they experience improved reasoning and the ability to create mental connections faster. Some say it puts them into flow-like state where they are able to accomplish just about anything they set their minds to.

Enhanced mood and higher levels of confidence and motivation are additional benefits.

Testing has not been done directly studying the cognitive effects of Armodafinil, but these effects have been measured in studies that focused on sleep disorders, specifically narcolepsy and shift-work sleep disorder.

In a study on narcolepsy, evaultions of cognitive performance were done using the Cognitive Drug Research battery of tests. It was seen that patients given Armodafinil has improved scores on tests of attention and memory compared to placebo patients.

Similar results were seen in a study on shift-work sleep disorder, where results improved on standardized tests of memory and attention in the Armodafinil patients compared to placebo patients.

Additional Benefits Of Armodafinil

Armodafinil has also been found effective as an appetite suppressant. Combined with the increased energy it produces, Armodafinil may be successfully used as a diet pill to help you lose weight.

Bodybuilders and athletes have also discovered that it helps them to push harder through their pain barrier to allow for more intense workouts.

The compound may even be effective in treating attention deficit disorders in adults or children, especially for those who have already built up a tolerance to other medications.

Side Effects

While generally well tolerated in adults when taken at doctor recommended dosages, there are some common mild side effects reported with Armodafinil use. The side effects associated with Armodafinil are similar to those linked to Modafinil. These include headaches, nausea, anxiety/nervousness, dizziness, diarrhea, indigestion, insomnia, dry mouth, depression, and fatigue.

Less common side effects include allergic reactions to the supplement like hives, swelling of the lips, face, tongue, or even difficulty breathing. Cardiovasular effects are also fairly rare, but can include heart palpitations, chest paint, and lowered blood pressure.

Some people experience side effects during the first few weeks they start taking a new medication as their body adjusts to the drug. This is normal, and typically subsides in about 2-3 weeks. If your symptoms last longer than this, then speak to your doctor about potentially trying a lower dosage to help reduce side effects.

Insomnia is a commonly reported side effect of Armodafinil that in most people is not a true adverse reaction to the drug, but rather is normally a matter of poor dosage timing. Because of the long half-life of Armodafinil – between 12-15 hours – the effects of the drug are active for many hours after it is ingested.

Because of this, taking your dosage early in the day is key to helping avoid sleep disturbances. It is recommended that dosages be taken as soon in the morning as possible, and before noon at the latest.

There is a possibility of developing some rare, but very serious cutaneous reactions when taking Armodafinil, including Stevens-Johnson syndrome. There is strong evidence that some people have certain human leukocyte antigens that given them a genetic susceptibility to developing these conditions.

Symptoms of Stevens-Johnson syndrome include a fever, flu-like symptoms such as body aches and sore throat, and a red or purple rash that spreads and blisters, and is primarily centered on the mouth, eyes, nose, and genitals.

If any of these effects are present it is best to immediately discontinue use and even seek medical attention. In most cases, if you are taking this drug properly and following the recommendations of your doctor then Armodafinil is unlikely to cause serious adverse effects.