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Modafinil is a prescription medication which helps produce an increased state of alertness, awareness, and wakefulness.
The psychostimulant effects of this drug differ from the classic effects of other well-known stimulants. Modafinil is able to promote an awake and attentive mind in the user without producing the uncomfortable body sensations of jitters or agitation so often associated with amphetamines.
Originally, Modafinil was developed to treat patients who had been diagnosed with narcolepsy, a neurological disorder causing the patient to fall asleep without warning. Other prescribed uses for this drug are for obstructive sleep apnea and shift-worker sleep disorder.
Alertness
Mental Acuity
Focus- Stimulates wakefulness in the brain
- Promotes mental acuity & processing
- Enhances focus, motivation & energy
Modafinil History and Original Sleep Disorder Uses
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Modafinil was first developed at the French pharmaceutical company LaFon Laboratories (which has subsequently been bought by Cephalon) in 1976. Its discovery came about after the original discovery of a group of benzhydryl sulfinyl compounds, including the compound Adrafinil.
During studies trying to determine Adrafinil’s mechanism of action, it was discovered that the active compound in Adrafinil was Modafinil. Adrafinil is considered a prodrug of Modafinil. This means that after it is consumed it is broken down in the body into the active Modafinil, as well as the inactive modafinilic acid.
In original animal studies on Adrafinil and Modafinil, it was seen that Modafinil caused hyperactivity and vigilance. Consequently, the first human trials on both of these drugs was for treatment of the sleep disorder narcolepsy.
Narcolepsy is a sleep disorder that affects sleep and wakefulness states. People with narcolepsy can fall asleep randomly throughout the day, often have disrupted nighttime sleep, and experience excessive daytime sleepiness.
In multiple double-blind placebo-controlled research studies, it has been seen that Modafinil significantly reduces daytime sleepiness in people with narcolepsy compared to a placebo. Treatment with Modafinil has resulted in significantly improved scores on various sleep evaluations, including the Multiple Sleep Latency Test, the Maintenance of Wakefulness Test, and patient self-assessments using the Epworth Sleepiness Scale. In trials, it has been seen that after discontinuation of treatment with Modafinil, excessive daytime sleepiness returns to normal levels seen without the drug.
Another sleep disorder that Modafinil has been studied for is shift-work sleep disorder. This circadian rhythm disorder can occur in people who do shift work that is very late at night or overnight, and are consequently awake during normal sleep times (i.e. nighttime), and attempting to sleep during normal awake times (i.e. daytime). This disorder causes excessive sleepiness during awake times and sometimes insomnia when trying to sleep.
It has been seen that if these people are able to return to a normal asleep at night/awake during the day schedule then their bodies quickly readjust and the symptoms of the condition cease. However, many people who work these night shifts are unable to change their schedule, and must instead find ways to deal with this condition.
In multiple studies it has been seen that Modafinil improves wakefulness and reduces excessive sleepiness in people with shift-work sleep disorder. In one study, patients were given either a placebo or Modafinil before a nighttime shift. Comparing their performances on the Psychomotor Vigilance Test it was seen that patients who were given Modafinil has fewer and shorter lapses in attention than placebo patients.
The Modafinil patients reported that they still had some residual sleepiness even when taking the drug, though, prompting the researchers to conclude that even more effective treatments are still needed to be developed.
One more sleep disorder that Modafinil has been used as an adjunct treatment for is obstructive sleep apnea/hypopnea syndrome (OSAHS). In this medical condition, during sleep the muscles supporting the tongue and soft palate relax, allowing for the partial or total obstruction of the airway. Hypopnea occurs when there is partial obstruction causing shallow, labored breathing; while apnea occurs when this is a total obstruction of the airway, leading to the cessation of breath.
The treatment for OSAHS is typically using a continuous positive airway pressure (CPAP) machine to keep the airway open during sleep. Modafinil is therefore used as an adjunct treatment to help improve the symptoms of obstructive sleep apnea/hypopnea. People with this condition often have poor quality and interrupted sleep during to multiple episodes of poor breathing and waking throughout the night; this often leads to excessive daytime sleepiness. In multiple studies it has been seen that Modafinil significantly improves excessive daytime sleepiness in people with OSAHS compared to a placebo.
In the United States the FDA has approved Modafinil as a prescription drug. Its on-label approved uses are to treat narcolepsy, shift work sleep disorder, and obstructive sleep apnea-hypopnea. It is considered a prescription drug in most other countries around the world as well.
Modafinil and Sleep Cycles
For many individuals, Modafinil is used off-label for a variety of cognitive and productivity enhancement. Users experience an increase in motivation, improved ability to focus, enhanced learning function and reduction of fatigue during long work or study hours.
In addition, there are many reports stating that individuals have effectively utilized Modafinil to help with jet lag.
In clinical trials, Modafinil has been observed to improve cognitive performance on certain measurements that relate to accuracy of judgment, memory, and broad intelligence.
The U.S. airforce has even looked at using Modafinil for fatigued pilots who are required to stay awake for periods in excess of 30 to 40 hours at once.
Side effects, though not common, range from mild to serious. One of the moderate side effects associated with this drug is insomnia.
Because Modafinil works on systems within the brain which regulate wakefulness, it is important to be aware of the effect it can have on the sleep cycle. When taken later on in the day, many individuals have stated that it can be virtually impossible to fall asleep for 10-15 hours.
How does Modafinil affect sleep? Can Modafinil be taken without compromising a healthy sleep cycle? What is the best way to take Modafinil in order to avoid this? If it was developed to keep narcolepsy patients awake, how does it affect a normal person’s sleep/wake cycle?
- Increases energy, wakefulness and motivation
- Boosts mental performance and focus
- Supports memory and cognition
Effects in the Brain
In an average person’s brain, multiple neural systems work together to regulate our sleep/wake cycle. Brain chemicals like Glutamate work to keep us awake and mentally energized, while neurotransmitters like GABA work to calm the excitation and send signals to signal the need to sleep.
Modafinil has been found to alter the release and re-uptake of some of these neurotransmitters, and their receptors, to create a unique psycho-stimulation which reduces fatigue and produces a natural sense of being alert.
Instead of simply flooding the brain with dopamine and adenosine like most stimulants, Modafinil seems to be specifically targeting the brain’s sleep response. The drug has been hypothesized to be preventing the re-uptake of noradrenaline, a neurotransmitter related to the sleep-response triggering mechanism.
Perhaps more importantly, Modafinil seems to slow the release of the neurotransmitter GABA. This neurotransmitter interferes with the brain’s signaling of when it is time to go to sleep.
Some researchers speculate the most effective mechanism of action may be the effect Modafinil has on the brain’s energy chemical, Glutamate.
If it is correct that Modafinil may stimulate the action of Glutamate, it would produce an overall excited neural response, while at the same time blocking the sleepiness signaling of GABA.
What About Sleep Deprivation?
Many nootropic users do not use Modafinil on a consistent basis, but instead use it when there is a need to be alert and productive for an extended period of time due to the drug’s relatively long half-life.
Modafinil stays in the user’s system for approximately 10-15 hours; as a result users have shared that taking one dose first thing in the morning with their normal stack is usually enough to get through the day without fatigue.
To avoid sleep disruption, it is recommended that Modafinil be taken at least 10 hours before regular bed time.
Thresholds and Cautions
Sleep deprivation is a serious problem which can produce hallucinations, mania, paranoid delusions and extreme psychosis.
It is not recommended to go for any extended period of time without proper sleep. Both body and the mind require regular rest which has been shown to contribute to overall good health and longevity. It is recommended that this drug is not taken for an excessively long period of time without breaks.
Modafinil is thought to work by specifically targeting the brain processes related to sleep, thereby producing a sense of wakefulness and alertness which feels natural.
It can cause insomnia or varying degrees of sleep disruption in some users. If individuals experience sleep problems, it is recommended to seek the help of a health care professional.
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Article last updated on: March 13th, 2018 by Nootriment
1 Comment
Can Modafinil be administered safely 12 hours apart for a week?