Modafinil - is it so effective and is it possible to buy a “smart” nootropic in Russia?

Under the mysterious name “Smart drugs” hide neurometabolic stimulants, also known as nootropics.

It is believed that such pharmaceutical drugs can significantly improve memory functions, concentration, and also have a stimulating effect on the nervous system, allowing you to increase performance and temporarily get rid of the need for sleep.

Among a very large group of nootropics, Modafinil (aka Alertek, Provigil and Modalert), which is banned in Russia, but is widely used abroad, is of particular interest.

Primary characteristics of a psychostimulant

Modafinil is a psychostimulant developed in the seventies of the twentieth century.
The authorship of this product belongs to the French-American manufacturer - Cephalon Corporation, which was looking for an effective remedy to combat narcolepsy. Despite the fact that, according to statistics, such an ailment is quite rare (diagnosed in about 0.025% of the US population), a person suffering from it may fall asleep unnoticed while driving or in other situations requiring high concentration. Therefore, the problem is much more serious than it might seem at first glance, and requires competent treatment.

The US Food and Drug Administration (FDA) considers Modafinil a relatively safe pharmaceutical that is an excellent alternative to caffeine, amphetamine and other popular synthetic stimulants. The medicine contains, in addition to the main active ingredient (modafinil), a number of auxiliary components.

Composition and release form

The active ingredient is diphenylmethylsulfinylacetamide (modafinil). Modafinil is an equivalent mixture of two enantiomers called R-modafinil and S-modafinil, which have the same physical properties. Enantiomers are a pair of stereoisomers, that is, substances that have an identical chemical composition, but a different orientation of the molecule in space (a mirror image of each other). The substances are insoluble in water and slightly soluble in most organic solvents. They are homogeneous white crystals.

The only release format is tablets containing 200 mg of the active substance, placed in foil packaging (blister). Used orally. In addition to diphenylmethylsulfinylacetamide, the composition contains excipients in the form of lactose, talc and others.

Pharmacological profile

Little is known today about the exact mechanism of action of Modafinil on the human body. As a result of large-scale clinical studies, scientists have found that the drug increases the level of serotonin in the anterior cortex and amygdala and stimulates increased release of dopamine, norepinephrine and other monoamines from synoptic clefts.

Under the influence of the drug, the hypothalamus intensively produces histamine, which entails the activation of alpha-1 receptors.

Modafinil affects different parts of the brain. One of the most important and pronounced effects is considered to be an increase in vigor, concentration, ability to remember, comprehend and assimilate new information. With the help of medicine, a person is able to control his voluntary attention, as well as improve his perception of the surrounding reality.

Although Modafinil is not an antidepressant and does not cause euphoria like some other illicit stimulants, it may well restore a good mood and reduce anxiety.

Experts in foreign languages ​​will be interested in:

Description

Modafinil or benzhydrylsulfinylacetamide is a central stimulant (psychostimulant). The drug is FDA approved for the treatment of narcolepsy (a condition characterized by sudden and uncontrollable episodes of deep sleep, fatigue, or excessive sleepiness), sleep apnea, and sleep disorders caused by changes in daily routine. The quality of the drug was tested, including as a treatment for Alzheimer's disease, depression and attention deficit disorder. Modafinil belongs to a group of drugs known as eugeroics (stimulants) that promote mental alertness and attention. One of the known mechanisms of action of these drugs is alpha-1 adrenergic receptor agonism, whereby the drugs have an effect on mood by increasing energy by increasing the release of dopamine in the central nervous system. This also leads to changes in GABA and glutamate levels. Studies of modafinil as a stimulant have shown advantages over amphetamines. To begin with, the substance is supposed to have a much lower potential for abuse due to the fact that its effects do not cause the same euphoria. In addition, the drug has less impact on peripheral CNS stimulation (i.e., fewer side effects), has minimal effects on blood pressure, does not cause sleep disruption (no hangover or need to catch up on sleep), and, according to clinical trials, has a more robust security profile. The drug is even used by the US military as an energy booster for pilots and soldiers to work for long periods of time without sleep. This is not at all as strange as it may seem at first glance, since in the past, military pilots and soldiers widely used Dexedrine (an amphetamine) during long periods of sleep deprivation. 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 specific drug for the military. Recently, modafinil has gained popularity among competitive athletes. They use it not just as a drug for “vigor,” but as a stimulant that increases performance and endurance. This use will likely come as a surprise to the drug's developers, as it has previously been reported that this "mild" alertness-enhancing drug does not have strong stimulant effects and may not improve athletic performance. Recent research contradicts these claims. A study conducted in Canada found that taking modafinil may provide significant athletic benefits. In a double-blind study, 15 male volunteers took the drug at a dose of 4 mg per kg of body weight (equivalent to 200 mg for a 220-pound person) or a placebo. Three hours after the meal, aerobic exercise was performed on a bicycle ergometer at 85% of maximum aerobic power until exhaustion. While taking modafinil, men were able to exercise for significantly longer periods of time (up to 30% longer), and used more inhaled oxygen during exercise. A decrease in subjectively perceived tension has also been reported, resulting in increased performance during exercise.

Scope of application

As mentioned above, Modafinil was originally developed as an effective treatment for narcolepsy and obstructive sleep apnea. It was also supposed to be used to get rid of chronic lack of sleep and drowsiness resulting from the transition to summer/winter time and the subsequent shifts in the work schedule.

Unlike amphetamine, which causes euphoria, as well as side effects such as a hangover and addiction, Modafinil can significantly increase concentration, vigor and performance without side effects.

For experimental purposes, the drug was used and continues to be used to this day for military and space applications. Scientists from Canada have published a detailed report that the nootropic was able to demonstrate very positive results during the long stay of a group of astronauts on the ISS.

In the American army, the use of Provigil by pilots of fighter planes and military helicopters is acceptable, which allows them to maintain a high degree of concentration for up to a day and a half after a single dose of a high dose (600 mg or more).

Some scientists have suggested that the drug could be used to treat addiction to cocaine and some other addictive stimulants. A double study involving patients suffering from a similar problem showed that the drug can alleviate cocaine withdrawal, but a positive result is not guaranteed and depends on a number of psycho-emotional and other related factors.

Based on the results of numerous clinical trials, it was established that the medication reduces appetite and promotes intensive weight loss. Amphetamine, taken for similar purposes, significantly increases the heart rate and can cause tachycardia and a number of other undesirable effects.

Modafinil also shows outstanding results in the treatment of cognitive impairment, is used to improve memory and eliminate excessive daytime fatigue and sleepiness that are caused by primary biliary cirrhosis.

Tablets with a higher dose of the main active ingredient have been used since 2004 to treat adolescents and children suffering from hyperactivity and attention deficit disorder.

Provigil and its analogues are currently used to relieve symptoms of multiple sclerosis, such as neurological fatigue and depression.

After clinical trials of the R-isomer of Modafinil, it has proven itself very positively as an effective treatment for bipolar affective disorder.

Modafinil: analogues

Other drugs with the same composition and therapeutic effect can replace a nootropic drug. These include:

• Modalert – stimulant of concentration;
• Modiodal - the drug is produced in a number of European countries and South American countries, serves as a nootropic;
• Modafil is an Australian medicine;
• Vigia is a nootropic originally from Colombia;
• Karim - produced in South American countries, for the treatment of narcolepsy;
• Alertek - Canadian and Ecuadorian tablets to improve memory quality.

Modafinil. A more common version is armodafinil, with an almost identical chemical structure. Has the same similarities to Adderall, but with less stimulation. The biggest difference from armodafinil is the strength of the drug, modafinil is weaker. Modafinil can be taken for longer periods with less risk of tolerance.

Adrafinil. Precursor modafinil. A stimulant used to maintain wakefulness and reduce fatigue. Metabolized in the liver to modafinil.

Methylphenidate. Reduces fatigue and is used to treat narcolepsy and daytime sleepiness. Stimulates the central nervous system, which helps improve cognitive function. Research has shown that methylphenidate is effective in treating ADHD. Alcohol and vitamin C products may reduce effectiveness.

Contraindications for use

The use of the medicine is prohibited in the following cases:

• individual intolerance or hypersensitivity to the components included in the composition;
• previous vascular or heart diseases;
• the presence of phobias, nervous disorders and obsessive depression.

The use of Provigil is contraindicated during pregnancy and breastfeeding. The medication cannot be combined with alcoholic beverages and can significantly reduce the effectiveness of contraceptives. In case of cirrhosis and serious liver damage, using the drug is strictly prohibited.

You also need to know that Alertek gives a positive result if you undergo a doping test before a sports competition.

Modafinil Dosage

A sample size of 31 patients consuming Provigil showed that 200mg followed by 50mg are the most common dose';s. Patients chose to go against mentioning if they had any condition, symptoms they were taking it for and it';s perceived effectiveness. We will be releasing a graph that will allow us to know the intent based on the type of stack from, based on manual inspection of the stacks, most are for “Cognitive Enhancement.”

What dosage is right for you? Modafinil usually comes in two sizes, 100 mg and 200 mg. This is sales of 200 mg from the rank of 100 mg. For the most part, your doctor will prescribe you the correct dosage based on any medical conditions you may or may not have. In general, if taken for mental performance, 25mg is a good starting point to determine if the desired effect is felt, unless you can increase the dose the day after. It doesn't matter if you take it on an empty stomach or not. One easy way to tell if you've taken too many headaches.

The generally recommended dosage of modafinil is 200mg, that is, once a day, often in the morning, some people claim that it takes up to 3 hours to “kick in”; (see chart below) and thus it may be advisable to take it immediately upon waking as you will feel alert by the time you get to work.

Best Modafinil Dose for You

First things first, Modafinil is not for children, Children shouldn't take it at all -; especially given the FDA's disapproval based on testing.

If you are taking Modafinil to resist shift work sleep disorder (excessive sleepiness as a result of irregular work hours or schedules) then you should consider taking Modafinil only one for three hours before starting your shift. If you're working for 8 hours, and even if the drug takes 2 hours to take effect, based on the graph on the left you can see that the blood concentration remains high enough for you to get through your work effectively.

Important Motor Neuron

Some people believe that Modafinil should be taken according to body weight; However, there is only little evidence out there to prove that Modafinil is only necessary for the average user. Every supplement or drug has it's pros and cons, risk-reward ratio, and Modafinil is no different. Even though modafinil is considered a safe drug to take, several possible side effects may be associated with taking it. Side effects such as nausea, nervousness, headaches, insomnia, dizziness, anxiety, back pain, rhinitis and diarrhea.

In placebo-controlled studies, 8% of subjects had to stop taking the drug due to adverse side effects. The most frequently reported side effects were headache. Patients on our site have noted that lowering the dose and then taking it for 2 sessions reduced or removed headaches. Please consult a doctor or healthcare professional if any side effects occur. When you decide to take the drug, start with a small dose and observe for a week. If there are no negative effects, you can increase the dosage. You can also learn more about Modafinils successor, Armodafinil, or Nuvigil here.

Recommendations

1 2 https://www.ncbi.nlm.nih.gov/pubmed/24247883

Features of use - recommended dosages

To treat drowsiness and narcolepsy, the medicine is taken once a day in the morning in an amount of 200-300 mg.

A dosage of 400 mg may lead to difficulty falling asleep at night. In studies involving airplane and helicopter pilots, a dosage of 600 mg, divided into several doses, allowed maintaining high accuracy, good reaction and concentration for one and a half days.

In the case of patients suffering from multiple sclerosis, increasing the dose from 200 to 400 mg did not show a noticeable difference in results.

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 an alert state and without harm to sleep at night.

When used clinically to treat excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea, recommended doses are generally 200 to 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 are in the range of 100-400 mg. The drug is often taken 2-3 hours before sporting events

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 drug's applications are vast and essentially include any sport that focuses on aerobic exercise or endurance.

It is also great for athletes performing short-repetition strength or speed exercises (anaerobic exercise), such as shot put, pole vault, or long jump. Modafinil is not a popular drug among bodybuilders as it does not directly increase muscle gain or reduce body fat levels. Some, however, find the drug to be an effective pre-workout stimulant, especially during periods of fatigue or loss of physical activity after strenuous work or due to other reasons.

Overdose and side effects

The most common side effects that occur with an overdose of the drug are headache and nausea.

Today, Provigil is considered a safer stimulant than amphetamine and even caffeine. However, according to a large-scale study by the Canadian Department of Health, it was possible to establish the following information regarding side effects and possible complications:

• the use of the drug is contraindicated in persons suffering from clinically significant mitral valve prolapse that has developed due to the use of stimulants;
• The use of a nootropic is prohibited in the presence of various mental disorders and abnormalities;
• hypersensitivity to the components of the drug can cause rash, dermatitis, toxic necrolysis and a number of life-threatening skin reactions;
• The medication can cause shortness of breath, a feeling of heat, mouth ulcers and hives.

In rare cases, an overdose can lead to anaphylactic shock, dyseptic disorders, nasal congestion, lumbar pain and Quincke's edema.

Provigil should not be used by children despite the fact that studies have shown the drug to be relatively safe for adolescents and children aged 9 to 17 years.

People's opinions about a drug banned in Russia

The medication "Modafinil" has minor reviews. This is due to the fact that the drug is prohibited in Russia and Ukraine. Many people have not encountered this remedy, since doctors do not prescribe it. However, there are still isolated responses from those people who were treated with this medicine. Those men and women who have used this drug write on forums that thanks to the pills the thought process becomes accelerated, the mood improves, the person becomes focused and balanced. This drug helps a person stay alert throughout the day. People also note that there are minimal side effects from it, and it is not addictive. Also, after it there are no hallucinations or euphoria.

People who lived in the USA for some time and then returned to their homeland - Russia, note that in America the drug "Modafinil" and its analogues are sold in any pharmacy. This medicine is taken both by students during sessions and by people who want to improve their performance. Even police officers use it during long work shifts to improve their concentration. And in Canada, this drug is even in the first aid kit of astronauts in order to optimize performance during fatigue. Elderly people also cannot do without this product.

Drug or not?

Despite the fact that the World Anti-Doping Agency has classified Alertek and its analogues as prohibited stimulants, the drug does not cause dependence or severe withdrawal symptoms.

Therefore, it cannot be called a drug in the classical sense of the term.

In France and England, debates continued for a long period of time about whether to withdraw the drug from free sale, since many cases of inappropriate use were recorded among young people actively visiting nightclubs and entertainment venues.

In the spring of 2012, Modafinil and its derivatives were included in the list of psychotropic and narcotic drugs of the Russian Federation with limited circulation; accordingly, it cannot be purchased in pharmacies. The official status of the legality of this drug in Russia is such that any citizen of the country who has at least one tablet falls under Article 228 of the Criminal Code, which implies liability in the form of serving a sentence of at least 3 years.

Invention and legal status

Modafinil was developed and patented in 1990 by the French company Lafon Laboratories. It was soon registered in the United States as a drug for the treatment of narcolepsy. To date, the medicine has been officially approved and allowed for sale in more than 20 countries, including England, France, India, and Ukraine.

In Russia, due to an incomprehensible misunderstanding, modafinil is banned and included in the group of narcotic substances. Most likely, this decision is associated with lobbying for the interests of the domestic drug Phenotropil. The sale, storage of analogues and generics of modafinil - Modapro, Provigil, Modalert, Alertek and others on the territory of the Russian Federation is prohibited by law and is subject to criminal prosecution.

About the advantages and disadvantages

Modafinil has a minimal number of side effects with a noticeable effect, which is expressed in increased performance, improved concentration and lack of need for sleep.

That is why today many military departments in different countries are raising the question of completely replacing the traditional Amphetamine, present in the first aid kit of special forces soldiers, with Modafinil. Due to its outstanding qualities, the drug is actively used among astronauts, pilots and even law enforcement officers.

For example, in some American states, police officers receive 200 mg of Modalert daily to increase productivity and improve the reaction required when catching criminals.

On the other hand, in cases of abuse or excess dosage, the following may be observed: dehydration, diarrhea, vomiting, nausea and a number of other unpleasant symptoms.

Since this pharmaceutical drug increases histamine levels, people prone to allergic reactions should avoid using it. Buyers from some countries also consider the high cost of the drug and a certain complexity associated with its acquisition as disadvantages.

Since you can’t buy it, it means you need to replace it with something.

Drugs under the registered trade names Provigil, Modalert and Alertek in fact do not differ significantly from Modafinil. One tablet of any of the listed drugs contains 200 mg of active substance with the addition of excipients.

On the modern European and American market there are numerous generics that are positioned as a budget option for Modafinil.

In fact, no clinical trials of such pharmaceuticals have been conducted, so their use is associated with an unjustified health risk. A more potent analogue of Modafinil is Methylphenidate (aka Ritalin), but this drug can cause psychological dependence and has a large number of side effects.

Currently, Provigil and any of its analogues are prohibited in the Russian Federation. Accordingly, it is not possible to purchase it with or without a prescription.

Among the closest analogues of this drug is Phenotropil, which was developed in the Soviet Union specifically for pilots, astronauts and cosmonauts. However, this nootropic is in many ways inferior to Provigil, while having a large number of side effects.

To increase concentration, get rid of drowsiness, improve memory and perception abilities, nootropic drugs or psychostimulants are used. They stimulate brain activity and relieve sleep problems. One of the well-known drugs of this type is Modafinil. Read its instructions for use, find out about the indications, permission for use in the Russian Federation.

Real stories of real people

Stories - reviews of people who have used or are using Modafinil with varying degrees of success.

The first time I came across Modalert was when one of my good friends very persistently began to recommend it to me. She took the drug in a single dosage of 200 mg on days of increased responsibility and stress at work.

After consulting with my doctor, I decided to order one package for myself. Half an hour after taking a dosage of 0.2 g, drowsiness disappeared, while there was no rapid pulsation, euphoria and other qualities inherent in amphetamine-type substances.

Increasing the dosage to 0.5 g increased my performance so much that the night passed without sleep productively editing videos (my main occupation).

It is worth noting the complete lack of appetite and desire to sleep. Perception became clearer, and concentration also increased. Absent-mindedness has decreased, and productivity can be judged by the project completed by morning, which I planned to complete no earlier than in a few days. The effect of the drug on physical strength, endurance and coordination can only be assessed indirectly.

Eugene

I had the opportunity to become acquainted with Modafinil while on vacation in the Indian state of Goa. There it can be purchased at virtually any pharmacy where it is sold without a prescription.

The reason for taking it was severe fatigue resulting from a long flight and acclimatization. About 30 minutes after taking 300 mg of the drug, I felt a surge of energy, and this was clearly not a placebo effect.

The drowsiness immediately disappeared, and no tachycardia or dizziness was observed. The effect from a single dose lasted for about eight hours. The only mistake was drinking the Red Bull energy drink, which resulted in a slight headache and nausea.

Andrey, Moscow

Harm of modafinil, its danger

- Side effects. Remember our old axiom: “The stronger the effects, the more side effects.” Modafinil exhibits side effects relatively more often than most other nootropics, however, it is also stronger in action than most. The most common side effect is headache, accounting for approximately 34% of all modafinil side effects.

- Exhaustion of the body. Regular lack of sleep and treatment with modafinil can lead not only to an imbalance in the body, but also to various depressions and psychoses. We know that everything is learned by comparison, so a study was conducted, I would call it “The Dream of a Drug Addict” (https://www.ncbi.nlm.nih.gov/pubmed/10607161). The bottom line: 3 groups of people, 1st received a placebo, 2nd received modafinil at a dosage of 300 mg, 3rd received amphetamine (d-isomer) at a dosage of 20 mg.

In the group with our current substance and with amphetamine, short-term memory, logical thinking and reaction were noticeably improved, compared with placebo. The frequency of side effects was the highest with amphetamine (so don’t snort this rubbish), much more often than with modafinil. But modafinil was also more painful than placebo.

Doctor Review

This drug has certain indications, and its use for other purposes or exceeding recommended dosages is an unjustified risk to one’s own health.

Despite the fact that Modafinil was synthesized relatively long ago, and more than two dozen large-scale clinical studies have already been carried out, it is impossible to declare the complete safety of this medication.

Any stimulant depletes the nervous system, so I would recommend using the medicine in one-time cases when it is really necessary. It is best to find a “legal” energy drink and tonic for yourself that does not deplete serotonin and dopamine reserves, such as sports, creativity or sex.

Likhachev Pavel, specialist in neurosurgery

Modafinil withdrawal symptoms

People who take modafinil on a regular basis sooner or later think about stopping its use. There can be many reasons for this - from a banal lack of money, to the development of strong tolerance to the drug and the inappropriateness of its further use. This is where stimulant withdrawal symptoms come into play:

• Problems with concentration and fatigue.
• Depression.
• Dyspnea.
• Cognitive decline.
• Headache.
• Liver dysfunction.
• Hypertension.
• Fatigue.
• Nausea.
• Nervousness, etc.

Interesting Facts

Modafinil and its analogues are currently actively used in bodybuilding. Among fans of weightlifting, there is an opinion that the drug not only increases IQ, but also miraculously increases the efficiency of training in the gym.

In fact, it allows you to provide the utmost level of concentration, allowing you to focus as much as possible on the training process.

The active component of the drug is part of various pre-workout complexes designed to improve performance and “pumping”.

Modalert and Provegil are also often used by American and European students, since with their help you can prepare for a test in a matter of days, and assimilate information much more effectively.

Doctors' opinions

In Russia, the drug “Modafinil” has mixed reviews from specialists. Since this remedy is prohibited in our country, many doctors naturally criticize it and note that it is not worth taking. After all, as experts explain, this medicine can be compared to taking painkillers. That is, if a patient has a headache for a week and does not take any pills, then he will definitely find the cause of the disease. The same applies to Modafinil: if a person feels a lack of energy and vigor, then you should not increase their level through any medications. You need to get enough sleep, have a good rest, plan your time, and then you won’t need to take any medications. Doctors note that you should not once again poison your body with any chemicals.

At the same time, there are doctors in Russia who, although they do not directly advise their patients to take Modafinil, do not deny this possibility. Thus, those specialists who have visited Europe and America note that this drug simply must be used by people whose work is associated with stress.

Be that as it may, this medication is currently prohibited in Russia, so we will not recommend it. However, people should know that in other countries it is sold in many pharmacies and is considered an effective remedy against drowsiness, narcolepsy.