Modafinil - analogues in Russia, instructions for use, what it is

Modafinil side effects

1. Armodafinil increases dopamine and histamine levels in the hypothalamus. This increases extracellular dopamine concentrations and enhances neurophysiological activity. Increased dopamine leads to physical and psychological arousal. Increases cognitive function and motivation. [R]

2. Armodafinil increases levels of norepinephrine, serotonin and orexin. Norepinephrine provides a sharp surge of energy. Serotonin is responsible for emotional stability and mood. Stimulation of orexin receptors (OX1 and OX2) increases physical energy. And orexin deficiency leads to fatigue and drowsiness. [R]

3. Armodafinil activates glutamatergic circuits and inhibits GABA. Glutamate is the main excitatory neurotransmitter, and GABA is its opposite (the main inhibitory one). As a result, the level of physical and mental energy increases sharply. [R]

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 application areas of the drug 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.

Side effects of Modafinil are generally associated with stimulation of the central nervous system and may include nervousness, insomnia, tremors, euphoria, personality changes and agitation. The drug may also cause gastrointestinal problems such as nausea, vomiting, abdominal pain, dry mouth, anorexia and headache.

The psychostimulant Modafinil can be sold under such commercial names as Modalert, Modiodal, Modafil, Vigia, Karim, Alertek. Most often, this remedy is replaced with Modafinil Provigil tablets. These pills are also banned in Russia, so it is very difficult to purchase them.

This medication is approved in the USA. In Russia, the drug is prohibited, so it is impossible to buy it in a pharmacy. The only way out is to order medicine online. The cost of Modafinil Provigil tablets ranges from 4.5-8 thousand rubles per 100 pieces. This comes out cheaper than the drug to which the article is devoted.

Most of all Modafinil is sold in tablet form. So, some desperate individual, in the hope of achieving his base selfish goals, eats 300 mg of the substance, which was then used to make a book, a film and a TV series about a pill for the brain. In the stomach/intestines, this magical substance is absorbed and enters the blood.

The action itself is not fully understood. And some of the drug's effects remain unclear. Like the butterfly effect, according to research we see action here and here, but what the hell, why does something work here too?

What is known almost 100%:

1. The reuptake of dopamine, norepinephrine and glutamate is partially blocked, and their production is enhanced. (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2696807/) For those who do not know these substances, read the relevant articles. Action in the style of drugs such as cocaine/amphetamine. In the short term, the combination of release and reuptake inhibition of these catecholamines indicates frantic drive, stimulation, tunnel vision, where you find it easy to concentrate on one thing even when everything around you is moving/jumping/flashing. In simple terms, such a person is difficult to distract; he is collected and concentrated. However, this way you can become paranoid and concentrate, at least believe in Pokemon.

2. Increases histamine levels. No sleep. (https://www.ncbi.nlm.nih.gov/pubmed/22640618) Probably few people know that most medications for allergies and rashes are antihistamines. Histamine develops and enhances the body’s reaction to an irritant; it seems to say: “You ate or smelled this in vain - now you have a rash on your arms and a couple of pimples on your back. Your great-grandfather almost died from this bullshit, this information was encoded in a special gene so that you, a fool, would not repeat the mistakes. Nothing personal!". Antihistamines, as the name suggests, suppress it. On the contrary, Modafinil enhances its production, making the body more sensitive and irritable. And the increased level of histamine completely destroys all drowsiness. That is why it is believed that modafinil is primarily for narcoleptics who constantly want to sleep.
3. Increased IQ. And here is the link (https://www.ncbi.nlm.nih.gov/pubmed/16140369). This is one of those effects that is understudied. IQ is related to Acetylcholine, but modafinil has little or no effect on acetylcholine. Perhaps there is a substance that changes under today's drug, causing an indirect improvement in the functioning of the brain, its cognitive functions. And it’s hard to say what this might mean in 30-40 years. IQ increases especially strongly in people with low brain development.

Reading a major study of modafinil on IQ (English) - https://emilkirkegaard.dk/wp-content/uploads/Cognitive-effects-of-modafinil-in-student-volunteers-may-depend-on-IQ.pdf

1. Improving short-term memory. On this point, most likely, the truth lies in the influence of the dopaminergic system. After all, it is dopamine and its receptors that are responsible for the so-called “focus,” concentration, and attentiveness.
2. Suppression of GABA secretion. (https://www.ncbi.nlm.nih.gov/pubmed/22640618) This property is designed to completely kill all calm, serenity and tranquility.

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.

Overdose

The standard dosage of tablets is 4 mg/kg of human weight. This is approximately 100-200 mg/day. This dose helps with targeted suppression of sleep or for invigorating in the morning or at night. For the treatment of narcolepsy or sleep apnea (breath holding) take 200-400 mg/day once or in the morning and at noon.

Athletes take 50-100 mg tablets per dose, gradually increasing the dose. The drug is used 2-3 hours before sports competitions. It is indicated for aerobic exercise, endurance exercise, shot put, pole vault or long vault. For bodybuilders, the use of the drug is not justified because it does not affect muscle gain or fat loss.

- Cardiopalmus.

- Nervous excitement.

– Increased blood pressure.

In case of overdose, the patient should urgently call an ambulance.

— Modafinil is a controversial substance. A strong nootropic with frequent side effects.

— The basis of its action, its effects is an increase in dopamine, norepinephrine, histamine, incomprehensible understudied effects.

— The most common side effects: headache and decreased resistance to allergies. It is much safer than narcotic psychostimulants, but it is far from “glycine”.

— In some countries it is sold without problems, you can look for it at the resorts where you vacation, in the Russian Federation it has been banned since 2012.

It’s difficult to be “not a romantic” when it comes to nootropics; you want to try everything, but maybe sometimes you should choose the “blue” pill and move on with your life. If it’s “red”, then you are responsible for yourself!

Good luck!

Drug interactions

Before starting therapy, the patient should notify the doctor about the medications he is taking, because the combination of Modafinil with other drugs may have unpredictable effects. It reduces the effectiveness of birth control pills, which leads to the development of unwanted pregnancy, so during therapy it is better to use barrier methods of contraception. The drug, in combination with yohimbine (included in potency enhancing drugs), increases the heart rate and increases blood pressure to dangerous levels. Combination with alcohol is prohibited.

Description

Modvigil 200

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.

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:

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.

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.

Legal psychostimulants

Rice. 1: Legal psychostimulants

• atomoxetine
• synephrine
• ephedrine
• nicotine

Other stimulants include bupropion, amineptine, tranylcypromine, and selegiline. They are often included among psychostimulant agents, but they have too little psychotropic effect.

Psychostimulants can cause mental dependence, insomnia, anorexia, irritability, sometimes tachycardia and increased blood pressure. Taking drugs with a pronounced sympathomimetic effect can lead to diseases of the cardiovascular system; one of the most dangerous complications is pulmonary hypertension.”

Atomoxetine

Atomoxetine is a legal "amphetamine" that belongs to the group of selective norepinephrine reuptake inhibitors and is also used for ADHD. Unlike other drugs, the effect of the drug appears only after a few weeks. Atomoxetine does not cause addiction and is not prohibited in the Russian Federation.

Possible side effects include gastrointestinal discomfort, headache, fatigue and rapid heartbeat. There was also an increase in aggressive behavior, suicidal ideation, and suicide in children. Symptoms should be monitored very carefully, especially at the beginning of treatment. If thoughts of suicide occur, the drug should be stopped.

Potent central nervous system stimulants are prohibited by law in most countries of the world. Exceptions are methylphenidate and modafinil. Cathinone is approved in some countries, but is not used for therapeutic purposes.

Methylphenidate

Methylphenidate, an amphetamine analogue whose tablets are used to treat attention deficit hyperactivity disorder (ADHD), is prohibited in the Russian Federation. When taken as directed by a physician, no cases of dependence have been observed with methylphenidate. The drug has the potential to develop dependence if used incorrectly.

Research has shown that children and adolescents with ADHD are at increased risk of developing addictions to substances such as alcohol, nicotine, or opioids. Further research shows that methylphenidate reduces the risk of developing such addiction.

The active substance should only be used in the case of a confirmed diagnosis of ADHD and in combination with other treatment methods (eg psychotherapy, cognitive behavioral therapy). Side effects occur frequently at the beginning of treatment.

Common side effects include stomach upset, headache, and loss of appetite. If the dosage is too high, anxiety and internal tension arise. At very high doses, the drug retards human growth.

Cathinone

Cathinone is an amphetamine analogue that enhances motor, speech and cognitive activity, and also causes mild euphoria. Metabolites of cathinone, cathine and norepinephrine also stimulate the central nervous system, but less pronounced than the parent substance. The leaves of the khat plant are plucked from the stem and then chewed. Chewing releases juices, including cathinone.

Cathinone absorption occurs in different places:

• buccal mucosa
• stomach
• in the small intestine

Approximately 2.3 hours after chewing the leaves, the maximum concentration of cathinone in the blood plasma is reached and, therefore, the most powerful psychotropic effect. The half-life of cathinone from the human body is 1.5 ± 0.8 hours.

Other Applications

Due to its ability to stimulate cognitive functions, its general activating effect and impact on performance, modafinil has found its wide application in various fields. This use of the product is called “off-label” - use for indications that do not have an evidence base and, accordingly, are not officially approved. Among these indications are the following:

• ADHD;
• depressive episodes;
• multiple sclerosis;
• asthenia in the hyposthenic stage;
• drug addiction;
• derealization, depersonalization.

In the treatment of endogenous depression, modafinil is used by some doctors in conjunction with antidepressants to enhance the severity of their effect. This use of the drug is limited due to the risk of increased suicidal tendencies as a result of stimulation of mental processes against the background of a persistent affective disorder.

In some clinical situations, the drug has shown effectiveness in the development of withdrawal syndrome as a result of drug addiction or addiction to medications that have a hypnotic or stimulant effect. The active component facilitates the manifestation of vegetative, somatoneurological symptoms and residual psychological disorders during abstinence.

In the treatment of patients with multiple sclerosis, modafinil is used to reduce fatigue during the day. Placebo-controlled studies conducted by the manufacturer in 2000 showed that a single dose of 200 mg of the drug significantly reduced fatigue, drowsiness and other neurological manifestations of increased fatigue.

The drug is used as a cognitive stimulant during periods of increased mental stress, which is why modafinil is often called “the drug of choice for students, entrepreneurs and managers.” The use of many stimulants goes beyond the direct prescriptions of doctors; the use of modafinil is also widespread in order to increase memory, attention, and productivity during the study process.

The use of the drug is common among athletes performing anaerobic exercise and endurance, and there are frequent cases of its use in competitive sports. The drug is included by the International Olympic Commission in the list of stimulants prohibited in competitions; standard examination of athletes necessarily includes a test for modafinil.

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 price

This remedy is quite expensive. The price of the drug is influenced by such factors as the manufacturer, the number of tablets in the package, and the speed of delivery of the order. It is impossible to find Modafinil in a pharmacy, since in Russia these pills have been included in the list of narcotic drugs and psychotropic substances since 2012. Therefore, our country has limited the circulation of the drug.

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.

Denial of responsibility

This description of the drug Modvigil 200 should not be taken as instructions for use, much less as a guide to action. The description may contain inaccuracies and may contain false or outdated information. Taking the drug is indicated exclusively for medical reasons and strictly according to the prescription. Before purchasing Modvigil 200, be sure to visit your doctor for advice and a prescription. The administration is not responsible for risks and damage to health as a result of self-medication and uncontrolled use.