Modafinil

Modafinil is a prescription drug for narcolepsy, increases concentration and eliminates sleepiness also increases the perception and memory abilities. Modafinil as a dietary supplement takes pride of place among nootropics. Modafinil is a drug to get rid of sleepiness during the day and for the treatment of narcolepsy. Perhaps the improvement of perception by stimulating neurotransmitters in the brain, used to improve mental abilities.

Pharmacological group: stimulants; psychostimulants; nootropics. Mode of action: the treatment of narcolepsy, sleep apnea and other sleep disorders. The impact on the receptors: α1-adrenergic receptors (agonist) is also known as: 2- (diphenylmethyl) sulfinyl acetamide, Provigil, Modalert, Modapro, Alertex.

Not to be confused with Adrafinil!

In the US and Canada, modafinil is issued strictly on the recipe and get it not so easy, its distribution is strictly controlled in the United States.
• Belongs to nootropics

Modafinil: instructions for use
The standard dose is 100-200mg, or 4 mg per kilogram of body weight, take in the event of deliberate suppression of sleep or after waking up in the morning to maintain a cheerful state and without any harm to sleep at night.

In clinical use for the treatment of excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea, the recommended dosage usually ranging from 200 to 400 mg per day. The dose may be taken once in the morning or in two divided doses (morning and noon). When used to enhance physical performance, typical effective dosage is in the range of 100-400 mg. The drug is often taken for 2-3 hours before sporting events. Note that the side effects are dose dependent. Often advised to start using modafinil at the minimum effective dose and increase it by 50-100 mg per reception to establish optimum level. Areas of application of the drug are enormous and, in fact, include all kinds of sports, focusing on aerobic exercise or stamina. It is also great for athletes, performing exercises for strength or speed in short intervals repetitions (anaerobic load), such as the shot put, pole vault and long jump. Modafinil drug is not popular among builders, since it does not directly affect an increase in muscle or fat reduction levels in the body. Some, however, believe that the drug is effective stimulant before a workout, especially during periods of fatigue or loss of physical activity after hard work or because of other reasons.

Description pf Modafinil
Modafinil or benzhydrylsulfinylcetamid - central stimulant (psychostimulant). The substance approved by the FDA for the treatment of narcolepsy (a disease characterized by sudden and uncontrollable episodes of deep sleep, fatigue or excessive sleepiness), sleep apnea, and sleep disturbances caused by changes in the operation. quality tests were performed medication, including, as an agent for treating Alzheimer's disease, depression, and attention deficit disorder. Modafinil belongs to a group of drugs known as evgeroiki (stimulators) that promote mental alertness and attention. One of the known mechanisms of action of these drugs is agonism alpha 1-adrenoceptor, resulting in drugs have an influence on the mood, increasing the power by increasing dopamine release in the central nervous system. This also leads to changes in the levels of glutamate and GABA. In studies of modafinil were as stimulant drug shows advantages compared to amphetamine. To begin with, that the substance is supposed to have a much lower potential for abuse due to the fact that the impact does not cause the same euphoria. Moreover, the drug has minimal effect on peripheral CNS stimulation (i.e., exhibit less side effects), it has a minimal effect on the blood pressure does not cause sleep interruptions (without hangover or needs "catch" sleep), and, according to clinical trials, It has a more robust safety profile. The drug is used by the US armed forces even as an energy stimulant for pilots and soldiers required to operate for long periods of time without sleep. This is not as strange as it may seem at first glance, since the last military pilots and soldiers is widely used Dexedrine (Amphetamine) during long periods of sleep deprivation. Soldiers who use modafinil, often report that the drug helps them to maintain excellent cognitive function for up to 40 hours without sleep, and has fewer side effects than Dexedrine. Modafinil has been tested the last combat situations, such as Afghanistan and Iraq, and possibly in the future will receive official recognition as a special preparation for the military. Recently, modafinil became known among competitive athletes. They use it not only as a preparation for the "courage", and as a stimulant that increases the performance and endurance. Such use is likely to be a surprise for this drug developers, as it was reported earlier that the "soft" drug enhancing the vigilance does not have strong stimulatory effects, and can not improve athletic performance. Recent studies contradict these statements. A study in Canada found that taking modafinil can provide a pronounced sporting advantage. In a double blind study 15 male volunteers took the drug at a dose of 4 mg per kg body weight (equivalent to 200 mg for a person weighing 220 pounds) or placebo. Three hours after the meal held aerobic exercise on a cycle ergometer at 85% of maximal aerobic capacity, up to exhaustion. Taking modafinil men could exercise over a much longer periods of time (up to 30% longer), and used more oxygen intake during exercise. Also reported a decrease in the perceived intensity, whereby there is an increase in exercise performance. Please pay attention to Ladasten.

History of Modafinil
Modafinil was developed by Lafon Laboratories in France. In 1998, the drug was approved by the FDA for sale in the United States, where it is sold under the brand name Provigil. Modafinil is also found on the international market for this and certain other trade names, including Modiodal, Vigil, Alertec and Modasomil. Although the drug has a favorable safety profile in the United States for some time, he was considered a drug capable of provoking possible abuse. Currently Modafinil is included in Schedule IV controlled substance, along with Valium and Xanax. For example, its use for non-medical purposes is limited by significant legal sanctions on the import and possession of the drug. The drug has a fairly broad medical use, including sleep disturbances associated with changes in the operation. The drug is often prescribed prescription. In 2000-2004 Modafinil has become popular among competitive athletes before athletic regulatory authorities have not begun to show concern about the use of the drug. In 2004 he broke out the doping scandal involving the company VALCO, when it became known that many of the athletes who gave a positive result in the use of tetragidrogestrinona also used and Modafinil. After that, the IOC prohibits the use of modafinil, and through a series of research methodology of detection of this chemical in the urine was developed. Now that testing is part of the standard survey of athletes before the Olympic competition. Most other international sporting bodies followed the example of the IOC and the ban on testing of modafinil. Since then, the drug has lost its appeal as an "invisible" in tests, although still used by many athletes, not passing urine sample testing.

How Modafinil supplied
Modafinil often supplied as tablets of 100 mg and 200 mg each.

Structural Features
Modafinil is a central nervous system stimulant, close to adrafinilu. It has the chemical name 2 [(diphenylmethyl) sulfinyl] acetamide.

Structure and Properties of Modafinil
Origin
Modafinil is a drug for the treatment of diseases associated with sleep disorders and also improves the mental state during the long wakefulness.

Modafinil forms
The term "modafinil" refers to a racemic mixture of two isomers, R-S-modafinil and modafinil. R-isomer is referred armodafinilom. Modafinil is a racemic mixture of S-R-modafinil and modafinil, armodafinil while is represented only R-modafinil.

Pharmacology
serum
The half-life of modafinil is 13-15 hours, and serum concentration at steady state up to 2 days after the start of the reception. Half-life of S-isomer of modafinil is 4-5 hours, while the R-isomer of modafinil is longer period (15 hours) and thereby receiving substantially equivalent armodafinil receiving modafinil. These experiments showed that the concentration in the blood armodafinila 18% percent greater than in the case of modafinil (5.44 +/- 1.64mg / ml versus 4.61 +/- 0.73mg / mL) and accumulate in a shorter period of time (1.8 hours versus 2.5 hours) and the total concentration in urine armodafinila up 32-40%. Although both options modafinil (modafinil and armodafinil) have the same half-life, the effect on the body armodafinila is stronger (according to the content in the urine and blood).

Localization
According immunocytochemistry gene c-Fos (the gene responsible for the response to stimulation and detected by neural stimulation, or sleep deprivation), administration of modafinil to cats caused a sharp activation of the gene c-Fos in the anterior hypothalamic nucleus and the surrounding areas and weak in the suprachiasmatic nucleus, and the minimum gene activation in other areas such as the cerebral cortex or striatum. This activation of the hypothalamic-point was visible everywhere, in the process was involved and the amygdala. Studies in humans have shown clear differences between human exposure to modafinil, and amphetamine. In contrast to the effects of amphetamine or methylphenidate - excessive cheerfulness (which indicates a widespread neuronal activation), modafinil is selectively affects: the hypothalamus and amygdala.

Neurology
dopaminergic effects
Modafinil can increase the extracellular levels of dopamine in the prefrontal cortex of rats and in the caudate nucleus in dogs. Modafinil worked on dopamine and noradrenaline receptors (in the striatum) and the absence of such effects in mice has been linked with the disappearance of the effects associated with sleep, which confirmed the fact that the mechanism of action of modafinil really affects sleep. Recent research has shown the lack of influence of modafinil on the dopaminergic system, which may be associated with lower dosage used previously.

andrenergic impact
The invigorating effect of modafinil significantly weakened adrenergic receptor antagonists (group alpha and beta), but inhibition of the synthesis of catecholamine alpha-methyl-paratirozin does not diminish the impact.

Orexin-ergic effects
People deficient orexin (narcoleptics) modafinil shows good results, directly affecting the orexin neurons. This effect has the greatest impact on deficient mice, the effect of modafinil on the orexin system of healthy animals and humans is unknown. 3.5. Sedative and stimulating effect negative results of some studies about the effects of modafinil during the intentional deprivation of sleep, because the effect of 300 mg of modafinil during sleep deprivation is equivalent to receiving 20mg D-amphetamine. However, it was noted that the deterioration of self-control (the ability to accurately assess themselves and their surroundings) changes in the overconfidence (incorrect assessment of what is really capable of). The studies lasted for 64 hours (two nights without sleep) with a single dose of modafinil every 15 hours. Admission modafinil before sleep can seriously alter the sleep cycle and lead to subsequent lethargy, and can also cause side effects (worsening of mood and mental abilities). Recurrent hypersomnia - a phenomenon in which after the expiry of drugs against sleepiness sleepy more than to receive them. In contrast, preparations based on amphetamine modafinil not causes the phenomenon in cats, rats and mice. People who do not sleep for 64 hours and taken modafinil, this phenomenon also seen, in contrast to results with D-amphetamine reception. Modafinil does not cause recurrent hypersomnia. Exacerbation of attention observed in sleep deprivation for 10-12 hours after a single dose of 300 mg of modafinil, which is equivalent to 20 mg of D-amphetamine. The dose of modafinil 300mg of sleepiness is equivalent to 20 mg of the second dose of D-amphetamine. Brain sleep cycle is a balance of "ascending activating system" consisting of activating neurotransmitters (catecholamines, acetylcholine, orehina and so on.) And neurotransmitters (GABA, galanin), which inhibit the stimulation and promote sleep. Changing levels of activation and suppression of neurotransmitter generates a unique series of "switch-breaker." In general, regulation loop of vivacity and rest depends on the one hand, the circadian biorhythm from caused suprahiazimatic core and on the other - on the homeostatic need for sleep, which occurs during wakefulness. Modafinil is able to communicate with various stimulatory systems including serotonergic, noradrenergic, dopaminergic, glyutaminergic, histaminergic, oreksinergic and GABAergic pathways. While some studies modafinil used in the treatment of several other diseases and found that the side effect of insomnia lasted longer than in the placebo group, and Modafinil, adopted before bedtime, sleep did not give the participants of the experiment. Admission modafinil promotes mental stress.

The memory and thought processes
In healthy people, when receiving 100-200 mg of modafinil for 2 hours before the test (arithmetic test) improved storage properties, visual-spatial scheduling and rate of reaction. Short-term memory and accuracy of information processing improved after taking 200 mg of modafinil. In addition to the above, improvements are observed in the performance of tasks in general - increased motivation, enjoyment of the work done. In methamphetamine-dependent cognitive impairment dose of modafinil in a 400 g split into 3 days, can improve the properties of the short-term memory, which previously was not possible, however, a single dose of 200 mg of modafinil is not able to cause such effects.

Effects on appetite
Researchers condemning drug abuse is sometimes reported as a side effect of appetite in 16% (164cheloveka). Some researchers believe that this fact cause weight loss within one week, but no statistically.

Addiction
Modafinil is not able to activate the neural pathway that occurs in dependence, and is therefore considered that the drug has a relatively low threshold addiction other similar drugs. It is unlikely that modafinil will be used as a drug among addicts. Modafinil can help ease the breaking in methamphetamine-dependent, alcoholics and addicted to gaming, but the impact of the effect varies. Modafinil also reduces impulsivity drug-addicted, but this effect has effect only with subjects whose threshold impulsivity before experiments was already at a low level.

The impact of the Modafinil drug on people with certain diseases
multiple sclerosis
Disposable reception armodafinil (250 mg), patients with multiple sclerosis showed improvement mnemonic play, this effect was comparable to the placebo effect, but the fatigue, the ability to focus and speed of information processing the drug had no effect.

Precautionary measures. Toxicology
Tests revealed the following adverse effects of the drug - headache, dizziness, urine output, heart palpitations, tachycardia, anxiety, nervousness, gastrointestinal problems such as nausea and dry mouth, and abdominal pain. Apart from the above, modafinil is considered to be well-tolerated drug. Common side effects of modafinil include insomnia and decreased appetite.

Modafinil side effects
Side effects of modafinil, usually associated with stimulation of the central nervous system and may include nervousness, insomnia, tremors, euphoria, excitement and personality changes. The drug can also cause gastrointestinal symptoms such as nausea, vomiting, abdominal pain, dry mouth, anorexia and headache. Also, there may be high blood pressure, heart palpitations or abnormal heart rhythm. In rare cases it may occur an allergic rash, increased alkaline phosphatase, or in violation of the voluntary movements.

Availability:

Modafinil is currently to be found in more than two dozen countries. The drug, however, are not particularly popular on the black market and is not profitable target for counterfeiting. Modafinil available on medical prescription.