The medicine belongs to the subgroup of nootropics. Phenotropil is intended to improve memory performance and facilitate the learning process, it helps concentration and memorization of material, and reduces the toxic effect of certain medications. The drug is responsible for improving mood, lowering the pain threshold, and increasing performance.
Contraindications
- hypersensitivity to the components of the drug.
The drug should be prescribed with caution to patients with severe organic damage to the liver and kidneys, severe arterial hypertension, and severe atherosclerosis; patients who have previously suffered panic attacks, acute psychotic states, accompanied by psychomotor agitation (as there may be an exacerbation of anxiety, panic, hallucinations and delusions); patients prone to allergic reactions to nootropic drugs of the pyrrolidone group.
And yet he exists: the strange story of Phenotropil
But in 2021, the cooperation between the company and the copyright holder - the author of the patent Valentina Akhapkina - ceased: she revoked the production license. Instead of the drug in pharmacies, consumers now found counterfeits, Chinese copies on iHerb (without proven equivalence) or fraudulent schemes on the Internet. According to Valentina herself, she made this decision due to the fact that the manufacturing company did not take active steps to further develop and research the drug, preferring to use existing data and developments. “The drug was not introduced into pediatric practice, new dosage forms were not developed and introduced,” she clarifies.
It is logical to assume that the story will end with Valentina Akhapkina creating her own company to produce the drug. She declared her foundation. 80% of the company’s shares belonged to Valentina herself, 10% each went to the second copyright holder, Roman Akhapkin, and the former general director of Valenta, Alexander Itin. But Phenotropil in their version never appeared on the shelves of pharmacies. A number of sites, such as this one, try to accept orders for the drug on behalf of the company. But they don’t inspire confidence at all. Reviews from angry anonymous people who paid money but never received their order also warn against them. And although angry comments, like advertising, may turn out to be fakes, this does not add credibility to the site.
Many other, no less dubious, sites, when asked whether Phenotropil will appear in pharmacies, without hesitation declare: “This will never happen.” This is explained by the fact that Valenta Pharm withdrew the drug from sale at the request of the copyright holder in 2021, which, as we found out, actually happened. But in fact, this story has a continuation.
Looking for a replacement
Since Valenta Pharm was a platform for the production of large quantities of the drug, and not the holder of a license, now the rights to the drug belong to Valentina Akhapkina. But, although this may seem paradoxical, this does not mean that no one else has the right to produce this substance. The fact is that the patent for Phenotropil allows the creation of generic drugs based on the same active substance called phenylpiracetam.
Indeed, on the website of the Russian Medicines Register you can see several similar analogues of the drug. “Entrop” from Latvia, which has the same active ingredient, is not imported to us, and Slim Story Prof from Teva, although registered in 2016, was never put into circulation. , “Mosmedpreparaty”, “Northern Star” at different times also conducted bioequivalence studies of their substances to show that their drugs are no worse than the original and act in the same way as it. Pharmstandard is now suing the Akhapkins for a patent.
Dosage
The dosage regimen is set individually.
Phenotropil is taken orally immediately after meals.
The average single dose is 100-200 mg, the average daily dose is 200-300 mg. The maximum daily dose is 750 mg. It is recommended to divide the daily dose into 2 doses. A daily dose of up to 100 mg should be taken 1 time/day in the morning; a daily dose of more than 100 mg should be divided into 2 doses. The duration of treatment can vary from 2 weeks to 3 months. The average duration of treatment is 30 days. If necessary, the course can be repeated after a month.
To improve performance, prescribe 100-200 mg 1 time/day in the morning for 2 weeks (for athletes - 3 days).
For nutritional-constitutional obesity - 100-200 mg 1 time/day in the morning for 30-60 days.
It is not recommended to take Phenotropil after 15 hours.
Overdose symptoms and manufacturer's instructions
If a large amount of Phenotropil is accidentally taken, the patient experiences signs of side effects. The patient is prescribed symptomatic treatment.
The abstract draws attention to the following nuances:
- Phenotropil is able to increase the effectiveness of drugs that affect the central nervous system, antidepressants and other nootropics;
- the medication can be used in the treatment of alcohol dependence due to the reduction in the toxic effect of ethanol on the body;
- the drug reduces appetite and increases physical activity, and is used as a means of helping to reduce body weight;
- the medicine is used during training; due to the increase in performance, it was included in the list of doping prohibited for professional athletes.
The effect of Phenotropil is incomparable to the effect of amphetamines, although many mistakenly believe that they give similar results. The nootropic does not provoke the development of withdrawal symptoms and addiction.
special instructions
It should be taken into account that with excessive psycho-emotional exhaustion against the background of chronic stress and fatigue, chronic insomnia, a single dose of Phenotropil on the first day can cause a sharp need for sleep. For such outpatient patients, it is recommended to start taking the drug on non-working days.
Use in pediatrics
Phenotropil is not recommended for use in children due to the lack of clinical data on the use of the drug in children.
Experimental results
Phenotropil is characterized by low toxicity, the lethal dose in an acute experiment is 800 mg/kg. Does not have a carcinogenic effect.
Effects of phenotropil
Why does phenotropil, aka phenylpiracetam, attract us all? Of course, it has a psychostimulating effect and improves memory! Some explained this by a certain affinity for dopamine receptors, some - to ionotropic glutamate receptors (for example, to NMDA or AMPA), but everything is much more interesting - this racetam was associated with nicotinic cholinergic receptors, which is responsible for its 2 main effects:
1) Psychostimulation - activation of nicotinic cholinergic receptors located on the surface of the dopaminergic neuron leads to the release of vesicles with dopamine. A similar process occurs outside the brain - the release of norepinephrine and adrenaline is triggered in the adrenal glands. Due to the fact that nicotinic cholinergic receptors are a “constructor” consisting of different subunits, which can be combined in different ways depending on the activity of certain genes in different populations of neurons. Phenylpiracetam had a greater affinity for H-cholinergic receptors in the brain, causing far fewer cardiovascular side effects.
2) Improving memory - in this case the mechanism is more complicated - prolonged activation of H-cholinergic receptors on the surface of glutamatergic neurons triggers an increase in the density of NMDA receptors (glutamate-dependent calcium channels), accordingly increasing the sensitivity of neurons to this excitatory neurotransmitter and “strengthening” this type of signal connections between nerve cells. This mechanism was described in the article “Phenotropil as a receptor modulator of synaptic neurotransmission” by the creator of the drug, V.I. Akhapkina, and is considered the main one.
pharmachologic effect
Nootropic drug. It has a pronounced anti-amnesic effect, activates the integrative activity of the brain, promotes memory consolidation, improves concentration and mental activity, facilitates learning processes, accelerates the transfer of information between the hemispheres of the brain, increases the resistance of brain tissue to hypoxia and toxic effects, has an anticonvulsant effect and anxiolytic activity , regulates the processes of activation and inhibition of the central nervous system, improves mood.
Phenotropil® has a positive effect on metabolic processes and blood circulation in the brain, stimulates redox processes, increases the body's energy potential through glucose utilization, and improves regional blood flow in ischemic areas of the brain. Increases the content of norepinephrine, dopamine and serotonin in the brain.
Does not affect the level of GABA content, does not bind to GABAA and GABAB receptors, and does not have a noticeable effect on the spontaneous bioelectrical activity of the brain.
Phenotropil® has no effect on the respiratory and cardiovascular systems. Has a mild diuretic effect. It has anorexigenic activity when used as a course.
Phenotropil® has a moderate activating effect on motor reactions, increases physical performance, has pronounced antagonism against the cataleptic effect of neuroleptics, and reduces the severity of the hypnotic effect of ethanol and hexenal.
The psychostimulating effect of Phenotropil predominates in the ideational sphere. The moderate psychoactivating effect of the drug is combined with anxiolytic activity. Phenotropil® improves mood, has an analgesic effect, increasing the threshold of pain sensitivity.
Phenotropil® has an adaptogenic effect, increasing the body's resistance to stress under conditions of increased mental and physical stress, fatigue, hypokinesia and immobilization, and low temperatures.
With the use of Phenotropil, there is an improvement in vision (increased sharpness, brightness and fields of vision).
Phenotropil® improves blood supply to the lower extremities.
Phenotropil® stimulates the production of antibodies in response to the introduction of an antigen, which indicates its immunostimulating properties, but at the same time does not cause the development of immediate hypersensitivity reactions and does not change the allergic inflammatory reaction of the skin caused by the introduction of a foreign protein.
With a course of use of Phenotropil, drug dependence and tolerance do not develop. When discontinuing the drug, no withdrawal syndrome was observed.
The effect of Phenotropil appears after a single dose, which is important when using the drug in extreme conditions.
Analogs
The appearance of non-standard symptoms during treatment requires replacing Phenotropil with a suitable medicine. The list of popular analogues is presented:
- Bravinton, Acefen, Carnicetine;
- Piracezin, Nooclerin, Semax;
- Piracetam, Olatropil, Phezam;
- Vinpocetine, Cerebrocurin, Cavinton Forte;
- Calcium Hopanthenate, Glutamic acid;
- Cephabol, Olanzapine, Cerebrolysate;
- Pramistar, Sidnocarb, Vinpotropil.
The drug has no complete analogues in structure. These nootropics have similar therapeutic effects. Common drug substitutes include Nootropil and Glycine.
The replacement and selection of a second drug is the responsibility of the attending physician. The specialist looks for an analogue based on laboratory diagnostic examination data and the reasons for rejecting the original.
Pharmacokinetics
Suction and distribution
After oral administration, it is quickly absorbed from the gastrointestinal tract, distributed in various organs and tissues, and easily penetrates the BBB. The absolute bioavailability of the drug when taken orally is 100%. Cmax in the blood is reached after 1 hour.
Metabolism and excretion
Phenylpiracetam is not metabolized in the body and is excreted unchanged. About 40% is excreted in urine, 60% in bile and sweat. T1/2 is 3-5 hours.
Indications for use of the drug
- diseases of the central nervous system of various origins, especially diseases of vascular origin or associated with metabolic disorders in the brain and intoxication (in particular, in post-traumatic conditions and phenomena of chronic cerebrovascular insufficiency), accompanied by a deterioration in intellectual and mnestic functions, a decrease in motor activity;
- neurotic conditions, manifested by lethargy, increased exhaustion, decreased psychomotor activity, impaired attention, memory impairment;
— violations of learning processes;
- depression of mild to moderate severity;
- psychoorganic syndromes, manifested by intellectual-mnestic disorders and apathetic-abulic symptoms, as well as flaccid apathetic states in schizophrenia;
- convulsive conditions;
— obesity (alimentary-constitutional origin);
— prevention of hypoxia, increasing resistance to stress;
— correction of the functional state of the body in extreme conditions of professional activity in order to prevent the development of fatigue and increase mental and physical performance;
— correction of daily biorhythm, regulation of the sleep-wake cycle;
— chronic alcoholism (in order to reduce symptoms of asthenia, depression, intellectual and mental disorders).
Reviews
On the forums you can find many positive reviews about Phenotropil:
- students talk about improved memory, increased performance, and easier preparation for exams;
- those losing weight – decreased appetite, rapid weight loss, improved mood and general condition;
- doctors report good results in improving memory and suppressing chronic fatigue syndrome.
Before using the medicine, consult a doctor. Attempts to lose weight without the supervision of a specialist using Phenylpiracetam can lead to the development of various diseases and deterioration of health.
