11 Jul 2018

Active substance

The active ingredient-Phenylpiracetam, N-carbamoylmethyl-4-phenyl-2-pyrrolidone, or 4-phenylpiracetam. Chemical formula С12Н14N2O2.

Mechanism of action

Nootropic effect of the drug is to activate the mental processes and concentration. In addition, Phenotropil has antiamnestic effect – improves memory, and eliminates t brain disorders, leading to its loss. The drug prevents the development of seizures. Under the action of Phenotropil improves mood. Psychostimulatory effect of the drug is to increase learning, to facilitate the assimilation and processing of new information. These effects are combined with the tranquilizing properties of Phenotropil. However, his tranquilizing activity is low. Under the action of Phenotropil increases visual acuity, improves color perception, expands the field of vision.

Phenotropil is a good adaptogen-increases resistance to stress in extreme conditions, eliminates the negative effects of physical and mental stress. Analgesic (analgesic) effect of the drug is to increase the threshold of pain sensitivity, to improve the tolerability of pain. It reduces the power of toxic effect on the brain of various chemical compounds, including ethyl alcohol. The drug has anorexigenic effect-reduces appetite, painful craving for high-calorie carbohydrate food.

Of the other effects, not related to the Central nervous system, it should be noted the stimulation of antibodies, and as a consequence - strengthening of immunity. It should be noted that the beneficial effect on the immune system is not accompanied by allergic reactions of immediate type. Phenotropil improves blood flow to the lower extremities, and has a weak diuretic effect.

Nootropic, psychostimulatory, anorexigenic effect is largely due to the facilitation of the transmission of impulses between the neurons of the brain. This is achieved by increasing the number of neurotransmitters (acetylcholine, dopamine, serotonin, norepinephrine) in the brain tissue. In this case, each of the neurotransmitters has a specific effect on the brain processes. For example, the acetylcholine allows the transmission of electric impulse through the synapses (contacts) between neurons. Dopamine, serotonin are hormones of happiness and satisfaction. They are responsible for good mood, motivation and focus.

And serotonin by affecting the peripheral centers of saturation in the hypothalamus reduces appetite. It should be noted that the reception of Phenotropil does not cause a painful state of euphoria and inadequacy. In addition, the drug improves blood circulation in the brain tissue, regulates the processes of excitation and inhibition in the brain structures. Under its action improves the transport of glucose and oxygen to the neurons of the brain, and in the opposite direction are removed toxins and waste products. As a result, the resistance of brain tissue to hypoxia is increased.

History of creation

The era of nootropics began in 1964 when employees of the Belgian pharmaceutical company UCBPharma was synthesized a new drug called Piracetam. This tool is a derivative of the organic compound of pyrrolidone, and belongs to the class of chemical compounds of racemates. In 1972, this drug called Nootropil appeared on the world pharmaceutical consumer market. However, its effectiveness in the treatment of cognitive (mental) disorders has not been confirmed by clinical trials.

Perhaps this is due to the fact that the tests were conducted on the elderly, many of whom suffered from Alzheimer's disease. And to achieve a nootropic effect, it is necessary to actively stimulate brain activity by obtaining and processing new information during training, mastering new skills. Only under this condition, acetylcholine is produced in the Central nervous system. However, many foreign scientists physiologists and clinicians hastened to declare piracetam placebo, dummy. For this reason, Piracetam, as well as other nootropics, are not included in the official list of drugs in the United States and in many countries of Western Europe.

In the early 90-ies of the last century in the Russian Institute of space biology and medicine was synthesized a new drug that in its effectiveness and ability to penetrate the blood-brain barrier ten times superior Piracetam or Nootropil. This action force was achieved by the fact that the structure of The nootropil molecule was introduced phenyl group.

A new tool has received the name Phenotropil (phenyl group + Nootropil). Initially, Phenotropil was conceived as an adaptogen for astronauts, a means of providing endurance, reaction and accuracy of action in extreme orbital conditions. In 2003 Phenotropil was officially entered in the state register of medicines of the Russian Federation. Since 2008, This tool is assigned to the Russian pharmaceutical manufacturer valent Pharmaceuticals. In 2010, who registered a drug under the international name Phenylpiracetam (Fonturacetam).

Phenylpiracetam Analogues

Currently, Phenotropil is produced by many Russian pharmaceutical companies in the form of tablets weighing 50 and 100 mg. Initially, the drug had a synonym for Carphedon. However, this name has not been fixed, and currently the drugs under this name are not officially registered in the Russian territory. Among other numerous analogs of Phenotropil – Cavinton, Cinnarizin, Mexidol, Glycine, Noopept, and many others. But this is not generics, namely analogues-drugs that have a similar effect, but with another active ingredient.

Its psychostimulatory properties and the ability to influence the level of neurotransmitters Phenotropil similar to amphetamines. However, unlike the latter, it does not cause painful addiction and drug dependence. Does not affect Phenotropil on the vasomotor and respiratory centers of the brain. However, this drug is officially included in the list of doping, and banned for use by athletes during the competition.

Indications

Among the indications for the using of Phenotropil:

Disorders of thinking and memory in various diseases of the Central nervous system due to vascular insufficiency, metabolic disorders, intoxication;

Increased depletion in neurotic disorders;

The balance of the sleep-Wake;

Poor learning ability;

Psycho-organic changes in schizophrenia with intellectual disabilities and thinking;

Mild to moderate depressive States;

Convulsive syndrome;

Various conditions associated with hypoxia of the brain;

Improving mental and physical performance in preparation for extreme activities.

In addition, Phenotropil is included in some programs to reduce body weight. It should be borne in mind that this drug does not burn excess calories, and does not affect carbohydrate and fat metabolism. It only reduces appetite, dulls hunger. Therefore, Phenotropil in weight correction is applicable only in combination with a low-calorie diet. If you do not abandon the old gastronomic habits, the effect will not be. Similarly, Phenotropil is not effective in those cases where obesity is not associated with overeating, and with severe metabolic disorders, dishormonal disorders.

Phenotropil is also used in alcoholism-it reduces the toxic effect of alcohol on the brain. This is expressed in a decrease in the degree of intoxication and severity of hangover. However, this does not mean that Phenotropil should be consumed with alcohol. On the contrary, it is impossible. This tool stimulates the metabolic processes in the brain. Because of this, neurons become more sensitive to the action of ethyl alcohol, and die faster.

Pharmacodynamics

The drug is absorbed into the gastrointestinal tract. Its bioavailability is 100%, and the maximum concentration in the blood is created within 1 hour after administration. The half-life of Phenotropil ranges from 3 to 5 hours. 40% of the drug is excreted by the kidneys, and 60% — through the sweat glands, and bile through the intestine. Moreover, the excretion is carried out in an unchanged form.

Psychostimulating and nootropic effects have different terms of appearance, and equally different duration. After 20-60 minutes after taking the pills, there is an improvement in vision, a sense of concentration, determination, thirst for action. Psychostimulating effect lasts 5-6 hours, no more. Nootropic properties are manifested later, 10-14 days, and last for the same 10-14 days. Weight loss with the use of Phenotropil on the background of a diet occurs after about 2 weeks. These facts suggest that Phenotropil, like other nootropics, should be taken as a course. Only then will the result.

Phenylpiracetam Dosage

A single dose of the drug is 100-200 mg, daily-200-300 mg, the maximum daily-750 mg. the Daily dose is divided into 2 doses. If the daily dose is 100 mg, the drug is taken once in the morning. Given the stimulating effect and the likelihood of insomnia, do not recommended to take Phenotropil after 15 h

Take the whole tablets without chewing, drinking water, during meals, or after meals. Welcome to the food undesirable because of the anorectic actions. The duration of the course in the treatment of various diseases and pathological conditions is from 2 weeks to 3 months, on average – 1 month. However, many experts recommend to take it no more than 3 weeks. Allegedly, long-term use of Phenotropil depletes reserves of neurotransmitters in the brain. But this view is controversial. In any case, the interval between courses of admission should be at least 1 month.

To improve mental and physical performance, the drug is taken 100-200 mg once for 2 weeks. Athletes to improve physical endurance during training enough 3-day morning reception of 100-200 mg. Phenotropil for weight loss is taken in the same dosage, and also in the morning for 1-2 months.

Phenylpiracetam Side effect

Cases of drug overdose are not described. Phenotropil non-toxic. The lethal dose is very high-800 mg / kg of body weight. Therefore, even taking 8 tablets of 100 mg per day in most patients does not entail any negative effects. However, some people after taking the drug noted insomnia, hyperactivity, increased blood pressure, redness of the skin and a feeling of heat throughout the body. Most of these side effects, with the exception of insomnia and high blood pressure, are short-lived, and independently take place within three days without medical correction.

Phenylpiracetam Contraindications

Individual intolerance to the components Phenotropil. In the appointment should be extremely careful with allergic reactions to Piracetam and other derivatives of pyrrolidone. Relative contraindications are severe liver and kidney disease, hypertension with high blood pressure numbers, severe cerebral atherosclerosis.

In patients with previously noted psychotic conditions, Phenotropil can cause psychomotor agitation and productive symptoms in the form of delusions and hallucinations. In some people with mental exhaustion due to fatigue, nervous stress, Phenotropil intake in the first day can increase the duration of sleep. In these cases, it is not recommended to prescribe the drug during work, performance of professional duties, and the beginning of the reception should fall on weekends.

Phenylpiracetam Interaction with other drugs

Phenotropil enhances the action of other nootropics, psychostimulants and antidepressants. The action of barbiturates and neuroleptics, on the contrary, are inhibited by Phenotropil.

Use in children

The effects of the drug on the child's body has not been well studied. Therefore, Phenotropil is not officially recommended for children under 14 years. In rare cases, it is still used for emotional exhaustion, mental retardation, depression, and poor learning in children. Among other indications-various brain disorders, accompanied by paresis and paralysis. The standard dosage is 50 mg 2 times a day. Duration of the course is 2-4 weeks. Indications for the use of Phenotropil in children are determined strictly individually. The main thing is that the risk of possible complications does not exceed the feasibility of prescribing this drug.

Pregnancy and lactation

The effect of Phenotropil on the body of the fetus and newborn has not been studied, and its teratogenic effect (the ability to cause deformities) is not excluded. For this reason, it is contraindicated in pregnancy and breastfeeding