Performance-enhancing drugs

Drugs that increase performance help to cope with temporary physical and mental overload, relieve fatigue, stabilize and harmonize the psycho-emotional state of a person - that is, significantly improve his well-being.

In addition, there are many pharmacological agents for increasing the body's adaptive capabilities in situations where, under the influence of certain external negative factors, there is a failure of the autonomic and neuroendocrine regulation of natural physiological processes.

However, it is important to keep in mind that - in order to avoid negative consequences - performance enhancing drugs should only be used on the recommendation of a doctor, since many of these drugs have contraindications and serious side effects.

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Indications for the use of drugs that enhance performance

A decrease in a person's performance is a clear indication that his body, as they say, has accumulated fatigue from long-term physical work or (much more often) constant mental stress, from experiencing or suppressing strong emotions, from an irrational regime (in particular, lack of sleep), an unhealthy lifestyle, etc. When the feeling of fatigue does not disappear even after rest, doctors state a very common painful condition of modern man - chronic fatigue syndrome. And the indications for the use of drugs that increase performance, first of all, concern this syndrome, that is, they are aimed at increasing resistance to physical and mental stress.

Drugs that improve mood and performance are also prescribed for vegetative neuroses and asthenic disorders, depression, loss of strength and muscle weakness, in cases of pathological decrease in the ability to concentrate during work or study. Medicines of this pharmacological group are effective in cases of cerebrovascular disorders, which are accompanied by dizziness, memory and attention impairment; in states of anxiety, fear, increased irritability; in somatovegetative and asthenic disorders associated with alcohol withdrawal syndrome.

It is almost impossible to list all the names of drugs that increase performance, but we will look at their main groups and discuss the use of some of them in more detail.

To increase physical endurance and eliminate the consequences of many painful conditions that reduce the body's adaptability to external factors, drugs of the adaptogen group are used. In order to improve memory and increase mental performance, nootropics (neurometabolic stimulants) are widely used in clinical practice. In both cases, doctors prescribe vitamin preparations that increase performance - B vitamins.

Drugs that enhance mental performance: pharmacodynamics and pharmacokinetics

There is a wide variety of drugs that increase mental performance, which belong to the nootropic group. These are Piracetam, Deanol aceglumate, Picamilon, Calcium hopantenate, Phenotropil, Cereton and many others.

The pharmacodynamics of performance enhancing drugs is based on the ability of their active substances to activate nucleic acid metabolism, release serotonin from sensory neurons, and stimulate the synthesis of dopamine, norepinephrine, acetylcholine, and the main source of intracellular energy - adenosine triphosphate (ATP). In addition, drugs of this group increase the synthesis of RNA and proteins in cells. The result of such therapeutic effects is an improvement in the energy state of neurons, increased transmission of nerve impulses, and more intense glucose metabolism in the cerebral cortex, subcortical nerve nodes, cerebellum, and hypothalamus.

Also, the pharmacodynamics of drugs that increase performance directly affects the normalization of the structure of neuronal cell membranes, and in hypoxia, it helps reduce the need for oxygen in nerve cells. In general, these drugs make nerve cells more resistant to various negative effects.

The pharmacokinetics of performance enhancing drugs depend on the biochemical properties of their specific components. Since nootropics are predominantly amino acids and their derivatives, their bioavailability reaches 85-100%. After oral administration, they are well absorbed in the stomach and enter various organs and tissues, including the brain. At the same time, they do not bind to blood plasma proteins, but penetrate the BBB and placenta, as well as into breast milk. The maximum concentration in blood plasma is from 1 to 5 hours, and the time during which the highest concentration of drugs in cells is reached ranges from 30 minutes to 4 hours.

Most performance enhancing drugs are not metabolized and are excreted from the body through the kidneys (in urine), the biliary system (in bile), or through the intestines (in feces).

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Piracetam

Piracetam (synonyms - Nootropil, Piramem, Piratam, Cerebropan, Ceretran, Cyclocetam, Cintilan, Dinacel, Oxiracetam, Eumental, Gabatset, Gericitam, Merapiran, Noocephal, Noocebril, Norzetam, etc.) is available in the form of capsules (0.4 g), tablets (0.2 g), 20% injection solution (in 5 ml ampoules), and granules for children (2 g piracetam).

It is recommended to take Piracetam tablets 3 times a day, and capsules - 2 pieces per day (before meals). After the condition improves, the dosage is reduced to 2 tablets per day. The course of treatment is from 6 to 8 weeks (it can be repeated after 1.5-2 months). Method of administration and dosage of Piracetam in granules for children (after 1 year, with cerebrosthenic disorders): 30-50 mg per day (in two doses, before meals).

Deanol aceglumate

The release form of the drug Deanol aceglumate (synonyms - Demanol, Nooclerin) is a solution for oral administration. This drug, which improves mood and performance, has a positive effect on the state of brain tissue, improves well-being in asthenia and depression. Its use is justified in the case of the need to facilitate the processes of memorization and reproduction of significant amounts of information. As experts note, Deanol aceglumate has a positive effect on elderly patients in a number of neurotic conditions caused by organic brain damage or traumatic brain injury.

Method of administration and dosage of Deanol aceglumate: adults should take the drug orally one teaspoon (5 ml of solution contains 1 g of the active substance) 2-3 times a day (the last dose should not be later than 18 hours). The average daily dose is 6 g (with the maximum permissible dose being 10 g, i.e. 10 teaspoons). The course of treatment with this drug lasts from one and a half to two months (2-3 courses can be taken during the year). During treatment, special care should be taken when driving vehicles or operating machinery.

Picamilon

Nootropic drug Picamilon (synonyms - Amilonosar, Picanoil, Pikogam; analogues - Acefen, Vinpocetine, Vinpotropil, etc.) - tablets of 10 mg, 20 mg and 50 mg; 10% solution for injections. The active substance nicotinoyl gamma-aminobutyric acid increases brain performance and improves memory by dilating blood vessels and activating cerebral circulation. In case of strokes, Picamilon improves the condition of patients with movement and speech disorders; it is effective for migraines, vegetative-vascular dystonia, asthenia and senile depression. For preventive purposes, it can be prescribed to people who are in extreme conditions - to increase resistance to both physical and mental stress.

Method of administration and dosage of Picamilon: it is recommended to take 20-50 mg of the drug twice or three times a day (regardless of food); the maximum daily dose is 150 mg; the duration of therapy is 30-60 days (a repeat course of treatment is carried out after six months).

To restore working capacity, a 45-day course of treatment is indicated - 60-80 mg of the drug (in tablets) per day. In severe cases, a 10% solution of the drug is administered intravenously - 100-200 mg 1-2 times a day for two weeks.

Calcium hopantenate

To restore performance under increased loads, as well as in asthenic syndrome in adults, the drug Calcium hopantenate (in tablets of 0.25 g) should be taken one tablet three times a day (20-25 minutes after meals, in the morning and afternoon).

This medicine is also widely used in the complex therapy of disorders of brain functions and congenital brain dysfunction in children with developmental delay (oligophrenia), in the treatment of cerebral palsy and epilepsy. The dosage in these cases is 0.5 g 4-6 times a day (treatment continues for at least three months).

When treating with Calcium hopantenate (trade names - Pantocalcin, Pantogam), it is not allowed to simultaneously prescribe other nootropic drugs or agents that stimulate the central nervous system.

Phenotropil

The drug Phenotropil - release form: tablets of 100 mg - a nootropic with the active substance N-carbamoyl-methyl-4-phenyl-2-pyrrolidone. Its use is recommended to increase the resistance of brain cells and stimulate its cognitive (cognitive) functions, as well as to improve concentration and mood. The drug, like all nootropics, stimulates blood supply to the brain, activates intracellular metabolism and normalizes impaired oxidation-reduction reactions in the nervous tissue associated with the breakdown of glucose.

Doctors prescribe Phenotropil (Fonturacetam) depending on the individual characteristics of the pathology and the condition of the patients. The average single dose is 100 mg (1 tablet), the tablets are taken 2 times (after meals, in the morning and in the afternoon, no later than 15-16 hours). The average daily dose should not exceed 200-250 mg. The duration of the course of therapy is on average 30 days.

Cereton

The therapeutic effect of Cereton (generics - Gleacer, Noocholine Rompharm, Gliatilin, Delecite, Cerepro, Holitylin, Choline alfoscerate hydrate, Choline-Borimed) is provided by its active substance choline alfoscerate, which supplies choline (vitamin B4) directly to the brain cells. And choline is necessary for the body to produce the neurotransmitter acetylcholine. Therefore, the drug Cereton not only normalizes the functioning of receptors and brain cells, but also improves neuromuscular transmission and helps to increase the elasticity of neuronal cell membranes.

Indications for use of this drug include dementia (including senile) and cognitive impairment, attention deficit, encephalopathy, consequences of stroke and cerebral hemorrhage. In these cases, Cereton capsules are taken one at a time 2-3 times a day (before meals). Treatment can last from 3 to 6 months.

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Drugs that enhance physical performance

Preparations that increase physical performance include such agents for increasing the overall tone of the body and activating its adaptive abilities as acetylaminosuccinic acid, melatonin, calcium glycerophosphate, pantocrine, alcohol tinctures of ginseng, eleutherococcus and other medicinal plants.

The release form of Acetylaminosuccinic acid (succinic acid) is 0.1 g tablets. The general tonic effect of this product is based on its ability to stabilize and simultaneously stimulate neuroregulatory processes of the central nervous system. Due to this, taking succinic acid relieves fatigue and eliminates the state of depression associated with it.

Method of administration and dosage of Acetyl amino succinic acid: the usual dose for an adult is 1-2 tablets per day (only after meals, with a glass of water). Children under 6 years of age are prescribed 0.5 tablets per day, after 6 years - a whole tablet (once a day).

The drug Melatonin increases the content of gamma-aminobutyric acid (GABA) and serotonin in the brain and hypothalamus, and also acts as a powerful antioxidant. As a result, this drug is used in the complex therapy of depressive states and CNS disorders, insomnia, and decreased immunity.

Melatonin is prescribed to adults 1-2 tablets before bedtime. During its use, it is forbidden to drink alcohol and smoke. This medicine is contraindicated for children under 12 years old; children over 12 are given one tablet per day (immediately before bedtime).

Calcium glycerophosphate (0.2 and 0.5 g tablets) is used as a drug that increases performance, due to the fact that this substance can enhance protein synthesis, and more active anabolic processes in the body's tissues, in turn, increase the tone of all its systems. Therefore, doctors recommend taking Calcium glycerophosphate for general loss of strength, chronic fatigue and nervous exhaustion. In addition, calcium is very useful for strengthening bones.

The drug should be taken one tablet three times a day (before meals), but it should not be combined with acidic foods and drinks, as well as with milk.

Pantocrin is a liquid alcohol extract of young (non-ossified) antlers of maral, red deer and sika deer. It is a central nervous system stimulant and is used for asthenic conditions and low blood pressure. Method of administration and dosage: orally, 30-40 drops 30 minutes before meals (2-3 times during the day). The course of treatment lasts 2-3 weeks, repeated courses are carried out after a break of 10 days.

For many decades, classic preparations that increase physical performance have included tinctures of ginseng (root), eleutherococcus, Manchurian aralia and Chinese magnolia vine.

The presence of triterpene glycosides in the composition of these biogenic stimulants, which affect energy processes in the body, explains their absolute effectiveness in regulating glucose metabolism. Doctors recommend taking these tinctures for physical and mental fatigue, increased drowsiness and low blood pressure.

The release form of drugs based on these medicinal plants is an alcohol tincture. Method of administration and dosage: ginseng tincture - 10-20 drops (dissolved in a small amount of water at room temperature) 2-3 times a day (for 1-1.5 months); eleutherococcus tincture - a teaspoon twice a day (before meals); Manchurian aralia tincture - orally 30-40 drops 2-3 times a day; Chinese magnolia vine tincture - 20-25 drops twice a day.

Contraindications to the use of performance enhancing drugs

It should be immediately noted that the use of drugs that enhance performance during pregnancy, as well as during lactation, is contraindicated, although in many cases the tyratogenic and embryotoxic effects of the listed drugs have not been studied by their manufacturers.

Contraindications to the use of performance enhancing drugs are as follows:

• The drug Piracetam is not used in children under 1 year of age;
• the drug Deanol aceglumate is not used in case of hypersensitivity, infectious diseases of the brain, febrile conditions, blood diseases, renal and hepatic insufficiency, epilepsy;
• the drug Picamilon is contraindicated in case of individual intolerance, acute and chronic forms of kidney pathologies;
• The drug Cereton cannot be prescribed to patients under 18 years of age, or in the acute stage of stroke;
• Acetylaminosuccinic (succinic) acid is not used for angina and glaucoma;
• The drug Pantocrin is contraindicated in atherosclerosis, organic heart pathologies, increased blood clotting, inflammatory kidney diseases (nephritis), and bowel disorders (diarrhea).
• Tinctures of ginseng, eleutherococcus and Manchurian aralia are not used to treat children, acute infectious diseases, bleeding, hypertension, epilepsy, a tendency to convulsions, insomnia and liver pathologies.

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Side effects of performance enhancing drugs

When prescribing to patients, doctors should take into account the side effects of drugs that increase performance. Namely: Piracetam can cause dizziness, headache, mental agitation, irritability, sleep disorders, pain in the stomach, nausea, vomiting, diarrhea, decreased appetite, convulsions; Deanol aceglumate can provoke headaches, sleep disorders, constipation, weight loss, itching, and in elderly patients - depression.

Side effects of the drug Picamilon are expressed in the form of dizziness and headache, irritability, agitation, anxiety, as well as nausea and skin rash with itching. For some, the use of Phenotropil is fraught with insomnia, irritability, dizziness and headache, unstable mental state (tearfulness, anxiety, as well as the appearance of delirium or hallucinations).

The drug Cereton has the following possible side effects: nausea, headache, convulsions, dry mucous membranes, urticaria, insomnia or drowsiness, increased irritability, constipation or diarrhea, convulsions, anxiety.

However, the side effects of Melatonin are quite rare and are expressed in the form of headaches and discomfort in the stomach area.

Interactions of performance enhancing drugs with other drugs

The use of any nootropic or adaptogen must be coordinated with the use of drugs of other pharmacological groups. Here are the main characteristics of the interaction of drugs that increase performance with other drugs:

• Piracetam increases the effectiveness of thyroid hormones, neuroleptic drugs, psychostimulants and anticoagulants;
• Picamilon reduces the effect of sleeping pills and enhances the effect of narcotic analgesics;
• Calcium hopantenate prolongs the action of hypnotics and may also enhance the effects of anticonvulsants and CNS stimulants;
• Taking acetylaminosuccinic acid with sedatives (sedative antidepressants and tranquilizers) can significantly reduce their effects.
• The use of tinctures of ginseng, eleutherococcus and Manchurian aralia enhances the effect of psychostimulant drugs, as well as cordiamine and camphor-containing drugs. And the simultaneous use of tonic tinctures with tranquilizers or anticonvulsants completely blocks the therapeutic effect of the latter.

Overdose of the above drugs may lead to undesirable consequences. In particular, there may be insomnia, increased irritability, trembling of the limbs (tremor), and in patients over 60 years of age - attacks of heart failure and sharp fluctuations in blood pressure.

The storage conditions for performance enhancing drugs are almost identical and require storing them in a dry, dark place at room temperature (not higher than +25-30°C). A mandatory condition: their storage location must be inaccessible to children.

And the manufacturers, as expected, indicate the expiration date of these drugs on the packaging.