Modafinil - instructions for use and composition, release form, indications and price

Hi all! You have long wanted underground information and today you will get it. We immediately warn you that our current substance has been poorly studied in humans and is currently being tested by the pharmaceutical company Cephalon.

This substance is Fluorenol or Hydrafinil! A worthy replacement for the legendary Modafinil, with a similar mechanism of action! (Link 1)

It is currently sold freely for research purposes.

I must say that there is really little information, even in the English-speaking segment. It is often written on the Internet that this substance is safer than modafinil and, moreover, is stronger in prolonging wakefulness in mice, but we did not find specific data in these studies (2). However, experienced users of modafinil in the West write about fewer side effects and a milder effect. And we move on to the proposed mechanisms of operation of Hydrafinil (3).

Instructions for use of Modafinil

The psychostimulant Modafinil is also known as diphenylmethylsulfinylacetamide. It belongs to a group of nootropics that treat narcolepsy, agitation or sleep apnea, and other sleep disorders. The drug is used for problems with concentration, memory and perception disorders. It belongs to the group of dietary supplements, is banned in a number of countries, and is considered sports doping.

Composition and release form

The drug is available only in tablet format; there are no other types of medication. The full composition depends on the type of tablet, because they are sold under different names. It is known that the concentration of the active substance of the same name in tablets is 100 or 200 mg per piece. Packages include blisters of 10 pieces, several blisters per pack.

Mechanism of action

The exact mechanism of interaction of Modafinil with brain transmitter neurons has not yet been clarified. Presumably, the active substance increases the release of monoamines, catecholamines, dopamine and norepinephrine from synaptic clefts. At the same time, the component increases the level of histamine in the hypothalamus, acting in a similar way to amphetamine stimulants. The drug is non-addictive, reduces the potential for abuse compared to traditional stimulants, while maintaining the anti-drowsy effect of the drug.

Pharmacodynamics and pharmacokinetics

Once in the body, modafinil increases the level of dopamine in the striatum and nucleus accumbens, norepinephrine in the hypothalamus, and serotonin in the amygdala of the brain. Under the influence of the inhibitor component, the glutamatergic chain is activated, and the transmission of the nerve signal under the influence of gamma-aminobutyric acid (GABA) is suppressed. It involves the neuropeptides orexin hypocretins, which are responsible for regulating wakefulness.

Activation of these neurons leads to an increase in histamine levels in the areas, reducing the desire for sleepiness. Presumably, the component enhances electrotonic coupling by increasing the efficiency of direct gap junctions between neurons. This allows the receptors to form direct diffusion through associated cells and increase resistance to action potential induction. Due to this, the gamma range of rhythms expands and the nootropic effect of the neurotransmitter manifests itself.

Pharmacokinetic data of modafinil: binds to plasma proteins by 60%, has 80% bioavailability, is an inducer of enzymes of the cytochrome system. The component reaches its maximum concentration 2.5 hours after ingestion, and is affected by food intake. The half-life is 11 hours, depending on the function of the liver and kidneys, the genotype of the enzymes. Excretion occurs in urine. The main metabolite of the substance, modafinilic acid, was detected in plasma, serum, and urine. The presence of the component can be confirmed by a doping test. It is unlikely to be detected by a test for amphetamines.

Indications for use

As a complex therapy, the drug is used as an addition to antidepressants. Indications for use are:

• suppression of the need for sleep;
• fight against general fatigue;
• pathological daytime sleepiness (hypersomnia);
• treatment of attention deficit hyperactivity disorder;
• deterioration of short-term memory;
• sleep deprivation;
• neurolepsy;
• slower reaction and accuracy (used by the military, astronauts, pilots);
• interruptions in circadian rhythms, decreased sleep quality.

Treatment for cocaine addiction

Experimentally, Modafinil can be used to treat cocaine addiction because their mechanisms of action on the brain are opposite. A double-blind study of the effectiveness of the two components found that addicts increased the number of consecutive days without cocaine use, but there was no effect on the rate of change in days without use. The patent was not received.

Weight loss

People even at a healthy weight can use the drug to reduce appetite and lose weight. According to month-long studies, users of the drug lose body weight and reduce calorie intake by 18% when taking 200 mg and by 38% when taking 400 mg/day compared to placebo. Scientists attribute the appetite-reducing effect to an amphetamine-like effect, but the drug in question does not increase heart rate. On the other hand, one of the companies has registered a drug under a patent for weight gain.

Cirrhosis of the liver

Chronic liver diseases, for example, cirrhosis, lead to excessive fatigue and daytime sleepiness in patients. Modafinil will help you cope with them. According to laboratory studies, two months of use of the drug helps to significantly reduce the symptoms of fatigue. The Epworth Sleepiness Scale was used to evaluate the analyses.

Treatment of mental disorders

The drug may be used off-label to treat mental disorders. It restores cognitive abilities in people who have undergone chemotherapy, alleviates memory impairment, alleviates depression in bipolar affective disorder (but sometimes provokes a manic phase), and reduces symptoms of neurological fatigue in multiple sclerosis. In pediatrics, the medication is used to a limited extent for the treatment of attention deficit disorder in children and adolescents aged 6-17 years (banned in a number of countries due to dermatological toxicity, no patent has been received).

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Content:

1. Modafinil: mechanism of action
2. Modafinil: effect on the body
3. Adverse reactions and complications
4. Overdose symptoms
5. Withdrawal syndrome

Modafinil is an analeptic, a central nervous system stimulant, used in the CIS countries, America and parts of Europe for the treatment of narcolepsy, schizophrenia and in the complex treatment of depression, attention deficit hyperactivity disorder. In the Russian Federation, modafinil is prohibited and included in the second “List of Narcotic and Psychotropic Drugs.” Despite restrictions on distribution and criminal liability, the illegal use of the substance is growing among students, scientists and the military as an stimulant that eliminates the need for sleep, enhances performance, endurance and brain activity during periods of increased mental stress.

Directions for use and dosage

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. To increase physical performance, 100-400 mg per day is indicated. To treat hypersomnia, take 200 mg per day once, in the morning. Therapy for drowsiness associated with shift shifts involves taking 200 mg tablets one hour before the start of the shift.

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.

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.

Side effects

Modafinil therapy is not without side effects. The most famous of them are:

• back pain;
• headaches, dizziness;
• nausea, diarrhea, dyspepsia;
• feeling of anxiety, restlessness, insomnia;
• nasal congestion;
• severe skin rash, severe allergic reactions, urticaria, blisters, skin peeling, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug fever with eosinophilia;
• damage to liver or blood cells;
• Quincke's edema, multiple organ sensitivity;
• mouth ulcers;
• heat;
• swelling of the face, throat, legs, eyes, tongue, lips;
• difficulty swallowing and breathing, shortness of breath;
• yellowing of the skin and whites of the eyes;
• darkening of urine.

According to clinical trials, taking 1200 mg of the drug per day for 7-21 days or a single dose of 4500 mg did not cause overdose symptoms or death. Possible symptoms of intoxication during a suicide attempt with large doses of medication include agitation, anxiety, insomnia, irritability, disorientation, tremor, vomiting, and diarrhea. A person may experience anxiety, aggressiveness, and nervousness. 5000 mg of the drug causes mild tachycardia and movement disorders.

Adrafinil - a workaround to Modafinil

Adrafinil is a drug that is a prodrug of Modafinil, that is, an agent that helps unlock the potential of the analeptic after it enters the body. Adrafinil is metabolized in the liver. Both drugs belong to the group of neurostimulants without the amphetamine effect.

Adrafinil stimulates the adrenergic system, promoting the release of adrenaline and hypocretin. The first neurotransmitter increases endurance and performance, the second stimulates the synthesis of norepinephrine and histamine, which allow you to maintain tone and level of intelligence for 6-8 hours. Adrafinil also releases glutamate, a neurotransmitter that restores and enhances the cognitive functions of the brain. In addition, the drug promotes the production of serotonin and dopamine, normalizing mood and emotions, and stress resistance.

The use of Adrafinil involves the development of the same side effects as with the use of Modafinil, namely:

• allergic reactions (due to increased histamine release)
• hyperstimulation of the central nervous system
• development of tolerance to the drug with long-term use
• liver dysfunction, etc.

Like Modafinil, Adrafinil is not recommended to be combined with alcoholic beverages and drugs. Fatalities have been reported when mixing high doses of neurostimulants with ethanol.

Analogues of Modafinil

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: mechanism of action

Modafinil is a powerful eugeroic that suppresses sleep and enhances cognitive functions. The pharmacological action has not been fully studied, and the mechanism of some of the reactions caused is unclear.

Application of Modafinil:

1. Produces the production of the neuropeptide orexin, the lack of which causes sleeping sickness - narcolepsy. Orexin levels regulate the sleep-wake cycle. The main function is to stimulate the production of histamine, which is responsible for transmitting signals to the immune system in response to an external irritant or stress. Histamine controls sleep and memory, enhances concentration and cognitive abilities, and is responsible for appetite, sexual behavior and motivation.
2. Increases dopamine levels by inhibiting receptors. As a result, the amount of neurotransmitter increases significantly. Dopamine is known as the “hormone of joy,” but in addition to increasing mood and pleasure, it is responsible for attention and motivation, activates the memorization of information, and exceeds the adaptive properties of the body.
3. Blocks the reuptake of serotonin and norepinephrine, which leads to a surge of energy, improved memory, attention and perception, faster movements and the thought process. At the same time, the feeling of happiness and self-confidence increases.
4. Increases glutamate concentration and blocks GABA. Glutamate is a neurotransmitter responsible for physical and mental arousal. GABA is responsible for functions opposite to glutamate - it inhibits and regulates excitation processes. Modafinil suppresses it, which enhances the stimulating properties.
5. Stimulates BDNF , a brain neurotropic factor responsible for neuroplasticity, growth and survival of nerve cells, recovery from injury and stress, and adaptation to new environmental conditions. BDNF also maintains and restores memory areas in the brain.

According to its effects, with long-term use it depletes all reserves of stimulated hormones, inhibiting their own production.

Modafinil price

In Russia, you can only buy the product through online stores, but this is illegal. The drug is not officially registered in our country and cannot be used for treatment. By purchasing a product, the patient takes responsibility for the treatment. Approximate prices will be:

Modafinil: effect on the body

The use of Modafinil increases performance and mental processes, suppresses the feeling of fatigue and the need for sleep. At the same time, it enhances concentration, logical and analytical thinking, and memorization of information.

Increases job satisfaction, motivation, self-confidence and self-confidence, and improves mood. Reduces feelings of anxiety, depression, depression and irritability.

Despite the fact that modafinil is banned in Russia, it is often used independently without medical indications, purchased from illegal distributors. It gained the greatest popularity among athletes, students and young people whose activities involve physical and psychological stress. It is used by users of methamphetamine and analogues to enhance the cognitive functions of the brain and is used for withdrawal symptoms.