Modafinil is a prescription drug for patients with narcolepsy, increases concentration and eliminates drowsiness, and also enhances perception and memory abilities. Modafinil as a biologically active additive takes pride of place among nootropic drugs. https://Stop-sleepiness-meds.com is a drug that relieves drowsiness in the daytime and for the treatment of narcolepsy. It is possible to improve perception by stimulating neurotransmitters in the brain, used to improve mental abilities.
Pharmacological group: stimulants; psychostimulants; nootropics. Pharmacological action: treatment of narcolepsy, sleep apnea, and other sleep disorders. Effects on receptors: α1-adrenergic receptors (agonist) Also known as: 2- (diphenylmethyl) sulfinyl acetamide, Provigil, Modalert, Modapro, Alertex.
Do not confuse with Adrafinil!
In the USA and Canada, modafinil is prescribed strictly according to the prescription and it is not so easy to obtain it; in the USA its distribution is strictly controlled.
Belongs to • Nootropic drugs
Modafinil: instructions for use
The standard dosage is 100-200 mg, or 4 mg per kilogram of weight, taken in case of targeted suppression of sleep, or after sleep in the morning to maintain a wakeful state and without harm to sleep at night.
When used clinically to treat excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea, the recommended doses are usually between 200 and 400 mg per day. The dose can be taken once in the morning or in two doses (morning and noon). When used to enhance physical performance, typical effective dosages range from 100-400 mg. The drug is often taken 2-3 hours before a sporting event. Please note that side effects may be dose dependent. It is often advised to start using Modafinil at the minimum effective dose, and increase it by 50-100 mg per dose until the optimal level is established. The areas of application of the drug are huge and, in essence, include any sports that focus on aerobic exercise or endurance. The drug is also great for athletes performing strength or speed exercises in short reps (anaerobic exercise), such as shot put, pole vaulting or long jump. Modafinil is not a popular drug among bodybuilders, since it does not directly affect muscle gain or a decrease in body fat. Some, however, believe that the drug is an effective stimulant before training, especially during periods of fatigue or loss of physical activity after hard work or due to other reasons.
Modafinil or benzhydrylsulfinylacetamide is a central stimulant (psychostimulant). The substance is approved by the FDA for the treatment of narcolepsy (a disease characterized by sudden and uncontrolled attacks of deep sleep, fatigue or excessive drowsiness), sleep apnea, and sleep disturbances caused by changes in working hours. Tests of the quality of the drug were conducted, including as a tool for the treatment of Alzheimer’s disease, depression and attention deficit disorder. Modafinil belongs to a group of drugs known as euroheics (stimulants) that promote mental alertness and attention. One of the known mechanisms of action of these drugs is alpha-1-adrenoreceptor agonism, as a result of which drugs affect mood, increasing energy by enhancing the release of dopamine in the central nervous system. It also leads to changes in the levels of GABA and glutamate. In studies of modafinil as a stimulant, the advantages of the drug compared to amphetamines were shown. To begin with, the substance is supposed to have a much lower potential for abuse due to the fact that its effect does not cause the same euphoria. In addition, the drug has a lesser effect on peripheral CNS stimulation (that is, it has fewer side effects), has a minimal effect on blood pressure, does not cause sleep interruptions (without a hangover or the need to “catch up” sleep), and, in accordance with clinical trials, has a more reliable security profile. The drug is even used by the US armed forces as an energy stimulant for pilots and soldiers, necessary for working for long periods of time without sleep. This is not at all as strange as it might seem at first glance, since in the past military pilots and soldiers used dexedrine (amphetamine) extensively during long periods of lack of sleep. Soldiers using modafinil often report that the drug helps them maintain excellent cognitive function for up to 40 hours without sleep, and has fewer side effects than dexedrine. Modafinil has been tested in recent combat situations, such as Afghanistan and Iraq, and may in the future receive official recognition as a special drug for the military. Modafinil recently gained fame among competitive athletes. They use it not just as a preparation for “vitality,” but as a stimulant that increases performance and stamina. Such use is likely to be a surprise for the developers of this drug, as it was previously reported that this “mildly” vigilant drug does not have strong stimulatory effects, and cannot improve athletic performance. Recent studies contradict these claims. A study in Canada showed that taking modafinil can provide pronounced athletic benefits. In a double-blind study, 15 male volunteers took the drug at a dose of 4 mg per kg of body weight (which equates to 200 mg for a person weighing 220 pounds), or a placebo. Three hours after eating, aerobic exercises were performed on a bicycle ergometer at 85% of maximum aerobic power, until exhaustion. By taking modafinil, men could exercise for significantly longer periods of time (up to 30% longer), and used more respirable oxygen during exercise. A decrease in subjectively perceived tension has also been reported, resulting in an increase in performance during training.
History of occurrence
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 was sold under the Provigil brand name. Modafinil is also found on the international market under this and some other trade names, including Modiodal, Vigil, Alertec and Modasomil. Although the drug has favorable safety indicators, in the United States for some time it was considered a drug that can provoke possible abuse. Modafinil is currently on the list of IV controlled substances, along with Valium and Xanax. So, its use for non-medical purposes is limited by significant legal sanctions on the possession and import of the drug. The drug has a fairly wide medical use, including for sleep disorders associated with changes in the mode of operation. The drug is often prescribed by prescription. In 2000-2004, Modafinil became popular among competitive athletes, before the sports regulatory authorities began to show concern about the use of the drug. In 2004, a doping scandal erupted with BALCO, when it became known that many of the athletes who tested positive for tetrahydrogestrinone also used Modafinil. After that, the IOC forbids the use of Modafinil, and with the help of a number of studies, a methodology for detecting this chemical in urine has been developed. Now this testing is part of a standard survey of athletes before the Olympic competition. Most other international sports bodies have followed the IOC’s ban on testing and testing Modafinil. Since then, the drug has lost its attractiveness as “invisible” in tests, although it is still used by many athletes who do not pass random urine testing.
How is supplied
Modafinil most often comes in the form of tablets of 100 mg and 200 mg each.
Modafinil is a central nervous system stimulant similar to adrafinil. It has the chemical name 2 [(diphenylmethyl) sulfinyl] acetamide.
Structure and properties
Modafinil is a medicine for the treatment of diseases associated with sleep disorders, and also improves mental state during long-term wakefulness.
Forms of Modafinil
The term “modafinil” refers to a racemic mixture of two isomers, R-modafinil and S-modafinil. The R-isomer is called armodafinil. Modafinil is a racemic mixture of S-modafinil and R-modafinil, while armodafinil is only R-modafinil.
The half-life of modafinil is 13-15 hours, and the concentration in the blood serum in equilibrium reaches 2 days after the start of administration. The half-life of the S-isomer of modafinil is 4-5 hours, whereas for the R-isomer of modafinil, the term is longer (15 hours) and thus taking armodafinil is almost equivalent to taking modafinil. The experimental data showed that the concentration of armodafinil in the blood is 18% higher than in the case of modafinil (5.44 +/- 1.64 mg / ml versus 4.61 +/- 0.73 mg / ml) and accumulates in a shorter period of time (1.8 hours) versus 2.5 hours), and the total concentration of armodafinil in urine is 32–40% higher. Although both variants of modafinil (modafinil and armodafinil) have the same half-life, the effect of armodafinil on the body is more pronounced (according to the content in the urine and blood).
According to immunocytochemistry of the c-Fos gene (the gene responsible for the response to stimulation and is detected by neural stimulation or sleep deprivation), the introduction of modafinil to cats caused a sharp activation of the c-Fos gene in the anterior hypothalamic nucleus and adjacent areas and was weak in the suprachiasmatic nucleus, and minimal gene activation in other areas, for example, in the cerebral cortex or striatum. A similar point activation of the hypothalamus was visible everywhere; the amygdala was also involved in the process. Human studies have shown clear differences between human exposure to modafinil and amphetamine. Unlike the effects of amphetamine or methylphenidate – excessive vigor (which indicates widespread neural activation), modafinil acts selectively: on the hypothalamus and amygdala.
Modafinil is able to increase extracellular dopamine levels in the prefrontal cortex in rats and in the caudate nucleus in dogs. Modafinil acted on dopamine and norepinephrine receptors (in the striatum), and the absence of such an effect in mice was associated with the disappearance of sleep-related effects, which confirmed the fact that the mechanism of action of modafinil really affects sleep. Recent studies have shown an insufficient effect of modafinil on dopaminergic systems, which may be associated with a dosage less than previously used.
The invigorating effect of modafinil is significantly attenuated by antagonists of adrenergic receptors (subgroup alpha and beta), however, inhibition of catecholamine synthesis by α-methyl paratyrosine does not reduce the effect.
In people with a deficiency of orexin (nakoleptikov) modafinil shows good results, directly affecting orexin neurons. This effect had the greatest effect on deficient mice; the effect of modafinil on the orexin system of healthy individuals and humans is unknown. 3.5. Sedative and stimulating effect Some studies have negative results regarding the effects of modafinil during intentional sleep deprivation, since the effect of 300 mg modafinil during sleep deprivation is equivalent to taking 20 mg of D-amphetamine. However, it was noted that the deterioration of self-control (the ability to accurately assess yourself and your environment) changes towards excessive self-confidence (incorrect assessment of what you are really capable of). These studies continued for 64 hours (two nights without sleep) with a single dose of modafinil every 15 hours. Taking modafinil before bedtime can seriously change the sleep cycle and lead to subsequent lethargy, and can also cause side effects (worsening mood and mental abilities). Recurrent hypersomnia is a phenomenon in which, after the end of the action of drugs against drowsiness, it puts you to sleep even more than before taking them. Unlike amphetamine-based drugs, modafinil does not cause this phenomenon in cats, rats, and mice. In people who did not sleep for 64 hours and took modafinil, this phenomenon is also not visible, in contrast to the results when taking D-amphetamine. Modafinil does not cause recurrent hypersomnia. An increase in attention is observed with sleep deprivation for 10-12 hours after a single dose of 300 mg of modafinil, which is equivalent to 20 mg of D-amphetamine. A dose of 300 mg of modafinil from drowsiness is equivalent to a 20 mg dose of D-amphetamine. The brain’s sleep cycle is the balance of the “ascending activating system”, consisting of activating neurotransmitters (catecholamines, acetylcholine, nut, etc.) and neurotransmitters (GABA, galanin), which inhibit stimulation and contribute to falling asleep. Changing the levels of activation and suppression of neurotransmitters forms a kind of “on-off switch” cycle. On the whole, the regulation of the cycle of vivacity and rest depends, on the one hand, on the daily biorhythm caused by the suprachiasimatic nucleus, and on the other hand, on the homeostatic need for sleep that occurs during wakefulness. Modafinil is able to contact various stimulatory systems, including serotonergic, noradrenergic, dopaminergic, glutaminergic, histaminergic, orexinergic and GABAergic metabolic pathways. In some studies, modafinil was used in the treatment of a number of other diseases, and it was found that the side effect of insomnia lasted longer than in the placebo group, and that modafinil, taken before bedtime, did not allow the participants to sleep. Taking modafinil promotes mental stress.
Memory and thought processes
In healthy people, when taking 100-200 mg of modafinil 2 hours before testing (arithmetic test), the memory properties, spatial-visual planning, and reaction rate improved. Short-term memory and accuracy of information processing improved after taking 200 mg modafinil. In addition to the above, improvements are observed during the performance of the task as a whole – increased motivation, enjoyment of the work done. In methamphetamine-dependent patients with cognitive impairment, a 400g dose of modafinil, divided into 3 days, can improve the properties of short-term memory, which was previously not possible, but a single dose of 200mg of modafinil is not able to cause such an effect.
Impact on appetite
Researchers condemning the drug sometimes report anorexia as a side effect in 16% (164 people). Some researchers consider this fact to be the cause of weight loss during the week, but statistically
Modafinil is not able to activate the neural pathways of metabolism, which occurs with addiction, and therefore it is believed that the drug has a low tolerance threshold relative to other similar drugs. Modafinil is unlikely to be used as a drug among drug addicts. Modafinil can help weaken the withdrawal of methamphetamine-dependent, alcoholics and gamers, but the effect is different. Modafinil also reduces the impulsivity of nakrozavisimy, however, this effect has an effect only with subjects whose threshold of impulsivity before the experiments was already at a low level.
The effect of the drug on people with certain diseases
A single dose of armodafinil (250 mg) in patients with multiple sclerosis showed improved mnemonic reproduction, this effect was comparable to the placebo effect, but the drug did not affect fatigue, the ability of purposeful activity and the speed of information processing.
Precautionary measures. Toxicology
Tests revealed the following adverse effects of taking the drug – headache, dizziness, diuresis, palpitations, tachycardia, anxiety, nervousness, gastrointestinal problems such as nausea, as well as dry mouth and abdominal pain. In addition to the above, modafinil is considered a well-tolerated drug. Common side effects of modafinil include insomnia and decreased appetite.
Modafinil side effects
Side effects of Modafinil are usually associated with stimulation of the central nervous system and may include nervousness, insomnia, trembling, euphoria, personality changes, and arousal. The drug can also cause gastrointestinal upsets, such as nausea, vomiting, abdominal pain, dry mouth, anorexia, and headache. Hypertension, heart palpitations, or abnormal heart rhythms may also occur. In rare cases, an allergic rash, an increase in alkaline phosphatase, or a disturbance in voluntary movements may occur.
Modafinil can now be found in more than two dozen countries. The drug, however, is not particularly popular on the black market and is not a profitable target for fakes. Modafinil is a prescription.