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

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.

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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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Pharmacological profile

The main active ingredient in all of the above analogues is modafinil. Additionally, they contain auxiliary components that enhance its properties. The subtleties of action and features that the nootropic possesses are not yet known to science. It is believed that its stimulating effect is based on the process of increasing serotonin levels in specific areas of the brain. This leads to an active release of monoamines, including norepinephrine and dopamine. In parallel, activation of a number of receptors is observed in response to the production of histamine by the hypothalamus.

Modafinil affects the functionality of several parts of the brain at once. After taking it, patients note a surge of vigor, increased concentration, improved and sharpened perception of the environment.

Individuals who take the product are able to better understand and absorb new information. Their memory is strengthened and their ability to memorize material increases. Additionally, consumers note a decrease in anxiety and improved mood. However, Modafinil is not classified as an antidepressant. The medicine does not provoke drug-induced euphoria and does not affect the psyche.

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.

Determination in biological fluids

Modafinil and its major metabolite modafinilic acid may be detected in plasma, serum or urine to monitor dosage in patients receiving the drug or to confirm the diagnosis of poisoning in hospitalized patients. Instrumental techniques used for these purposes include gas or liquid chromatography. As of 2011, the presence of modafinil is not specifically diagnosed by routine drug tests (with the exception of anti-doping tests) and is unlikely to cause false positives when detecting other chemically unrelated drugs such as amphetamines.

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.

Final Thoughts

Modafinil is certainly one of the most intriguing nootropics available today. There's a good reason for this: it allows you to perform physical and mental stress at peak levels for long periods, but without the typical nervousness, irritability, paranoia and ill-effects of sleep deprivation.

But based on reviews, user results with modafinil vary. While some consider it a modern miracle that can change your life, making you smarter and more productive, others warn that the experience of using modafinil is not equally rosy for everyone. Some users report disappointing or even unpleasant results.

As always, both sides of the story are important. There is no denying decades of research that has irrefutably proven that modafinil has enormous cognitive benefits and low addiction potential. But at the same time, there is no way around the fact that this is indeed a very powerful drug that can have some serious side effects, and that everyone reacts to differently.

The bottom line: Decades of research have shown modafinil to be a safe, effective and well-tolerated drug. But it is a regulated drug that cannot be legally purchased without a prescription in many countries. If you are interested in using modafinil to maximize your cognitive performance and minimize fatigue and drowsiness for limited periods, but do not want to risk ordering it from international pharmacies, you may want to look into adrafinil.

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.

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.

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.

Modafinilova's story

Modafinil was first developed in the LAFON laboratory in France in the late 1980s. Modafinil was discovered after the invention of a chain of other chemicals classified as benzhydryl sulfinyl. Most importantly, they included modafinil's precursor compound Adrafinil. Adrafinil was first found to improve wakefulness & alertness, it was later proposed for the treatment of people suffering from narcolepsy in 1986 in France.

Modafinil was discovered as the primary metabolite and active component for Adrafinil. It was observed that Modafinil had lesser side effects & greater strength than its predecessor. Although the use of modafinil is growing exponentially in countries such as the UK and US, Adrafinil is used as a replacement for modafinil as the drug is available without a prescription. Modafinil has been marketed in the United States since 1998, under the name Provigil, which is distributed by Cephalon Inc (parent company of Lafon since 2001).

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:

Reviews

Irina, 39 years old

My husband is constantly sleepy during the day, no matter what he tried. Colleagues advised me to get the drug Modafinil, which we do not sell. We barely found a remedy abroad, my husband started taking it. He is happy - he no longer feels sleepy during the day, his productivity has increased, and all this without any signs of side effects.

Mark, 49 years old

My son became addicted to cocaine two years ago, but I only found out about it recently. I decided to save him from addiction, but it turned out to be difficult - the habit drags him to the bottom. I researched many sources and one doctor told me that in the US they treat cocaine addiction with Modafinil. I ordered the drug, 5 months have passed, and my son is not addicted to the powder.

Alexander, 33 years old

I do long jumps, but not professionally—more like an amateur. As I grew older, I began to notice that the records were no longer what they were before. Fatigue appears, and sometimes apathy sets in. The trainer told me to take the drug Modafinil, and brought me the drug from another country. The pills really increase endurance, my performance has improved.

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Elena, 38 years old

My child has attention deficit hyperactivity disorder. I was already desperate to find an approach to him, I even tried to give him the hard-earned Modafinil. The latter also turned out to be toxic - my son developed an allergy, blisters and peeling began to appear on the skin. Only then did I read about these side effects, otherwise I wouldn’t have bought it.