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Neuroprotectors – types, purpose, mechanisms of action

The category of neuroprotectors includes substances that prevent damage to neurons in the brain and nervous system as a result of exposure to negative factors.
Neuroprotective drugs protect, adapt and improve the activity of neurons, stimulate mental activity, and increase cognitive functions. It is impossible to call “better neuroprotectants”, because this is an extensive list of substances with different structures and mechanisms of action. The list of neuroprotectors is conventionally divided into several groups:

Neuroprotectors: list of drugs, action and review of effectiveness – Chest pain

Soldatenkov Ilya Vitalievich, general practitioner

Neuroprotectors are a group of pharmaceuticals that protect cells of the nervous system from the effects of negative factors. They help brain structures quickly adapt to pathological changes that occur in the body during stroke, TBI, and neurological diseases.

Neuroprotection allows you to preserve the structure and function of neurons. Under the influence of neuroprotective drugs, metabolism in the brain is normalized and the energy supply to nerve cells is improved. Neurologists have been actively prescribing these drugs to patients since the end of the last century.

Neuroprotectors are cytoprotective drugs, the action of which is ensured by the correction of membrane stabilizing, metabolic and mediator balance. Any substance that protects neurons from death has a neuroprotective effect.

Nootropic drugs

Nootropics are drugs that stimulate metabolism in nervous tissue and eliminate neuropsychic disorders. They rejuvenate the body, prolong life, activate the learning process and speed up memorization. The term “nootropic” literally means “change the mind” when translated from ancient Greek.

Piracetam is the most famous representative of nootropic drugs, widely used in modern traditional medicine for the treatment of psychoneurological diseases. It increases the concentration of ATP in the brain, stimulates the synthesis of RNA and lipids in cells. Piracetam is prescribed to patients during the rehabilitation period after acute cerebral ischemia. The drug is the first nootropic that was synthesized in Belgium in the last century. Scientists have found that this medicine significantly increases mental performance and perception of information.
Cerebrolysin is a hydrolysate obtained from the brain of young pigs. It is a partially degraded whey protein enriched with amino peptides. Due to its low molecular weight, Cerebrolysin quickly penetrates the blood-brain barrier, reaches brain cells and exerts its therapeutic effect. This medicine is of natural origin, due to which it has no contraindications and rarely causes side effects.
"Semax" is a synthetic neuropeptide complex that has a pronounced nootropic effect. It is an analogue of a fragment of adrenocorticotropic hormone, but does not have hormonal activity and does not affect the functioning of the adrenal glands. "Semax" adapts brain function and promotes the formation of resistance to stress damage, hypoxia and ischemia. This medicine is also an antioxidant, antihypoxant and angioprotector.
"Cerakson" is prescribed to patients who have had a stroke. It restores damaged membranes of nerve cells and prevents their further death. For patients with TBI, the drug allows them to quickly recover from post-traumatic coma, reduces the intensity of neurological symptoms and the duration of the rehabilitation period. In patients, after active therapy with the drug, clinical signs such as lack of initiative, memory impairment, difficulties in the process of self-care disappear, and the general level of consciousness increases.
“Picamilon” is a drug that improves cerebral circulation and activates metabolism in brain tissue. The medicine has the properties of an antihypoxant, antioxidant, antiplatelet agent and tranquilizer at the same time. In this case, depression of the central nervous system does not occur, drowsiness and lethargy do not occur. "Picamilon" eliminates symptoms of fatigue and psycho-emotional overload.

Vascular drugs

Classification of the most used vascular drugs: anticoagulants, antiplatelet agents, vasodilators, calcium channel blockers.

Anticoagulants: Heparin, Sincumarin, Warfarin, Phenilin. These drugs are anticoagulants that disrupt the biosynthesis of blood clotting factors and inhibit their properties.
Acetylsalicylic acid has an antiplatelet It inactivates the enzyme cyclooxygenase and reduces platelet aggregation. In addition, this drug has indirect anticoagulant properties, realized by inhibiting blood clotting factors. "Acetylsalicylic acid" is prescribed for prophylactic purposes to persons with cerebrovascular accidents who have suffered a stroke or myocardial infarction. "Plavix" and "Tiklid" are analogues of "Aspirin". They are prescribed in cases where their “Acetylsalicylic acid” is ineffective or contraindicated.
“Cinnarizine” improves blood fluidity, increases the resistance of muscle fibers to hypoxia, and increases the plasticity of erythrocytes. Under its influence, brain vessels dilate, cerebral blood flow improves, and the bioelectrical ability of nerve cells is activated. "Cinnarizine" has an antispasmodic and antihistamine effect, reduces the reaction to certain vasoconstrictors, reduces the excitability of the vestibular apparatus, without affecting blood pressure and heart rate. It relieves spasms of blood vessels and reduces cerebroasthenic manifestations: tinnitus and severe headaches. The medication is prescribed to patients with ischemic stroke, encephalopathy, Meniere's disease, dementia, amnesia and other pathologies accompanied by dizziness and headache.
Vinpocetine is a semi-synthetic vasodilator that eliminates hypoxia and increases the resistance of neurons to oxygen deficiency. It reduces platelet aggregation and increases cerebral blood flow, mainly in ischemic areas of the brain. Vinpocetine and Cinnarizine are indirectly acting antihypoxants. Their therapeutic effect is due to the transfer of the body to a lower level of functioning, allowing it to perform full-fledged physical and mental work. The antihypoxic effect of these drugs is considered indirect.
"Trental" dilates blood vessels, improves microcirculation and cerebral blood flow, provides brain cells with the necessary nutrition, and activates metabolic processes. It is effective for osteochondrosis of the cervical spine and other diseases accompanied by a significant deterioration in local blood flow. The main active ingredient of the drug causes relaxation of the smooth muscle walls of blood vessels, increases their diameter, improves the elasticity of the walls of red blood cells, due to which they calmly pass through the vessels of the microvasculature. The drug dilates mainly the blood vessels of the heart and brain structures.

Drugs with combined effects

Neuroprotective drugs of combined action have metabolic and vasoactive properties that provide the fastest and best therapeutic effect when treated with low doses of active substances.

"Tiocetam" has a mutually potentiating effect of "Piracetam" and "Tiotriazolin". Along with cerebroprotective and nootropic properties, the drug has antihypoxic, cardioprotective, hepatoprotective, and immunomodulatory effects. Thiocetam is prescribed to patients suffering from diseases of the brain, heart and blood vessels, liver, and viral infections.
Phezam is a drug that dilates blood vessels, improves the body's absorption of oxygen, and helps increase its resistance to oxygen deficiency. The medicine contains two components: Piracetam and Cinnarizine. They are neuroprotective agents and increase the resistance of nerve cells to hypoxia. Phezam accelerates protein metabolism and glucose utilization by cells, improves interneuronal transmission in the central nervous system and stimulates blood supply to ischemic areas of the brain. Asthenic, intoxication and psychoorganic syndromes, disorders of thinking, memory and mood are indications for the use of Phezam.

Neuroprotectors – stimulants

These are neuroprotective drugs that stimulate the activity of the central nervous system. The most well-known stimulant of the central nervous system is caffeine. It also stimulates the cardiovascular system, constricts blood vessels and has a mild diuretic effect. Caffeine has a beneficial effect on the respiratory system and increases intellectual and physical functionality. This is the most popular neuroprotector for eliminating drowsiness.

Cerebrovascular

Vascular agents form the basis for the systemic correction of many processes: from hypertension to chronic encephalopathies, disorders of normal nutrition of cerebral structures.

They are universal compared to nootropics, but they give much more side effects. The group is heterogeneous and includes a number of subtypes, which are combined based on the mechanisms of beneficial effects on the patient’s body.

Restoring blood flow. By reducing the rate of synthesis of certain specific substances, those that disrupt the tone of large arteries. There are also other routes of direct exposure; the biochemical characteristics depend on the specific name and subgroup.
Normalization of rheological properties of blood. Liquefaction, increased fluidity. Which becomes a factor in eliminating eating disorders. Although not always.
Correction of the condition of vascular walls. Reducing the rate of oxidation, restoring elasticity. This preventive effect of neuroprotective agents helps prevent many problems: including reducing the likelihood of hemorrhagic stroke or cerebral aneurysms in the future.

Indirectly, cerebrovascular medications improve mental activity, memory, attention and relieve symptoms of neurological deficits: from headaches to others.

If we talk about specific names of such cerebroprotectors:

They disrupt the process of platelet aggregation. Essentially, this effect provides an increase in blood fluidity. Many medications of this kind have a mild effect, therefore they create a minimum of danger with a high therapeutic ability.

Classic names include products based on acetylsalicylic acid: Aspirin, Thrombo ass. More modern types that do not have this substance in the structure and composition: Clopidogrel, Ticlopidine and others. Use strictly according to indications.

The group of antiplatelet agents is described in detail in this article.

A much more powerful pharmacological group. Capable of disrupting the synthesis of coagulation factors. These medications have many more side effects. Use is only possible in a limited number of cases. Anticoagulant drugs with heparins of different weights are presented.

Read a detailed review of anticoagulant agents here.

The combined drug allows you to solve a group of problems at once: normalize blood fluidity due to minimal antiplatelet activity, relieve spasms of the brain arteries, restore blood pressure, intellectual abilities, and thinking capabilities.

The medicine has relatively few side effects, but if used incorrectly, it provokes obvious asthenic phenomena - fatigue, decreased performance. This must be taken into account when prescribing treatment.

Available in the form of tablets and ampoules for injection. Has a specific effect. Functions as a vasodilator. That is, it dilates blood vessels, helps improve the nutrition of brain tissue (a group of vasodilator drugs is described in detail here).

On the other hand, the medication helps reduce the oxygen demand of neurons and helps optimize the functioning of cerebral structures. It is used in a wide range of cases.

Neuroprotective therapy includes not only nootropics or cerebrovascular ones; as a rule, several types of different types are used to solve specific treatment problems. Of which there are usually many, especially in patients with ischemic disorders.

Neuroprotectors – antioxidants

Many antioxidants act as neuroprotectors, as they inhibit the reactions of non-enzymatic free radical oxidation of proteins, fats and other substances, providing a membrane-protective effect. These substances help preserve the functional properties of neurons.

An example is the neuroprotector glycine, which has an “inhibitory” effect on “exciting” amino acids like glutamic acid and at the same time stimulates the synthesis of GABA, the most important neurotransmitter of the brain, normalizing the sleep-wake cycle, improving cognitive functions and eliminating mental arousal.

Classification of plant neuroprotectors (Reviews)

Key words: neuroprotectors, medicinal plants, complex therapeutic effect
Neuroprotectors are classified as mixed-type nootropic drugs with a wide range of effects. The therapeutic effect of nootropic drugs is based on several mechanisms: improvement of the energy state of neurons (increased ATP synthesis, antihypoxic and antioxidant effects); activation of plastic processes in the central nervous system due to increased RNA synthesis; strengthening of synaptic transmission processes in the central nervous system; improved glucose utilization; membrane-stabilizing effect [4].

Neuroprotection involves mainly antioxidant, anti-excitotoxic (preventing cell death), blocking calcium ions and neurotrophic effects.

Substances with neuroprotective effects are mainly:

antioxidants (enzyme and non-enzyme ROS inactivation systems),
calcium channel blockers (calcium antagonists, Ca2+),
substances affecting the GABA system (GABA receptor modulators),
brain metabolism activators,
cerebral vasodilators,
substances of various groups.

Under physiological conditions, the formation of reactive oxygen species (ROS) and free radical oxidation (FRO) is necessary for normal cell functioning; in particular, free radical nitric oxide (NO) is an essential mediator of vasorelaxation, and its deficiency leads to hypertension. Some ROS serve as mediators in cellular signaling pathways. SRO determines the structural features of the phospholipid layer of biological membranes, membrane receptors, energy and plastic supply of cells, synthesis of prostaglandins, nucleic acids, lipolysis, transport of metabolites, excitability of CNS cells, correction of other metabolic processes.

However, if the concentrations of ROS - superoxide anion (O-2), hydrogen peroxide (H2O2), hydroxyl ion (OH-), singlet (atomic) oxygen (O2) - reach critical values, then pathological processes develop under conditions of excessive intensification of FRO. According to modern concepts, FRO is one of the universal mechanisms of cell damage and a universal pathological factor in many diseases [10]. In clinical medicine, free radical pathology with all its features is called oxidative or oxidative stress.

During oxidative (oxygen) stress, free radical metabolites (FRM) and oxygen-containing radical metabolites (OCRM), such as peroxide and nitroxide radicals, as well as lipid peroxidation (LPO) products accumulate. Oxidative damage to biological molecules is generated mainly by free radicals. Neurodegenerative diseases, a number of inflammatory diseases, atherosclerosis, cataracts, cardiovascular diseases, cancer, and the aging process are increasingly associated with the consequences of SRO [16,85]. Severe forms of oxidative stress are an important pathogenetic factor leading to severe consequences (myocardial infarction, ischemic stroke, diabetes mellitus, hypertension, etc.), a complex of which clinicians refer to as metabolic syndrome [10].

To prevent oxidative damage to biological molecules by free radicals, natural antioxidant systems with different principles of action can be used - ascorbic acid, tocopherols, carotenoids, substances of polyphenolic nature (flavonoids, proanthocyanidins, tannins, substances containing phenolic hydroxyl groups), polyenes (compounds with several unsaturated bonds) [1, 2, 3, 8, 81].

The possibility of using natural modulators is currently being studied in many laboratories. Moreover, the range of substances is very wide – from human hormones to medicinal plant extracts.

Understanding the molecular mechanisms of neuroprotection, oxidative stress and immune function helps to simplify the possible prevention of neurodegenerative diseases by diet, food products with the addition of medicinal plants and plant extracts [15]. The dietary factor is a modulator of physiological functions (including brain function), as a result, an increase in the economic productivity of the population is derived from the health of the population.

Table

conclusions

Neuroprotectors of plant origin belong to various groups of chemical compounds:
- alkaloids,
tannins,
phenolic acids and their derivatives,
terpenoids (aliphatic monoterpenoids, monocyclic, bicyclic, quinones),
diterpenoids (quinones, lactones, acids, alcohols),
triterpenoids,
polyacetylene alcohols,
neurotransmitter amino acids,
L-theanine,
xanthine derivatives,
vitamins (tocopherols, ascorbic acid).
The variety of compounds is due to the fact that neuroprotectors are nootropic compounds with a wide range of effects.
The primary direction of protective therapy of neuroprotectors includes interrupting the rapid mechanisms of necrotic cell death - reactions of the glutamate-calcium cascade (blockade of calcium channels). These include vincamine, 6-methylapigenin, taxifolin, patuletin, axillarin, resveratrol (activator of sirtuins, the SIRT1 protein responsible for chromosome integrity); GABA.
The secondary direction of protective therapy of neuroprotectors includes interruption of delayed mechanisms of cell death - oxidative stress, accumulation of ROS in mitochondria, imbalance of cytokines (mediators of neuroinflammatory processes), local inflammation, apoptosis, impaired neurotrophic function, etc. These include catechins, oligomeric proanthocyanidins, flavones, flavonols, isoflavones, biflavonoids, sesquiterpenoids and others.

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Adaptogens with neuroprotective properties

These are substances with a neuroprotective effect that increase the body’s nonspecific resistance to negative influences caused by environmental factors - stress, poor ecology, unbalanced nutrition.

An example is ginseng extract, it stimulates physical and mental performance, helps fight chronic fatigue syndrome and overwork. This effective neuroprotector stabilizes the functioning of the central nervous system, has a beneficial effect on cardiac activity, and suppresses nervousness and depression. Ginseng eliminates thirst and stimulates appetite.

Neuroprotectors: list of drugs, mechanism of action and review of cerebroprotectors

From the article you will learn the features of neuroprotective drugs, indications and contraindications for the use of drugs, side effects.

Neuroprotectors are drugs that improve metabolic processes in the brain, which can be disrupted as a result of traumatic brain injuries, neurological pathologies, and hypoxia.

Indications for use

Neuroprotectors are recommended for use in cases of toxic or hypoxic encephalopathies, problems with falling asleep and waking up, during the rehabilitation period after a stroke, chronic fatigue syndrome, fatigue, and also:

dizziness;
loss of orientation in space;
consequences of inflammatory processes in the central nervous system.

In children, drugs are used for speech delay, psychomotor development, poor learning ability, and cerebral palsy.

Treatment with neuroprotective agents is today considered the most promising direction in medical practice for brain hypoxia and impaired nutrition of neurocytes.

The peculiarity of medicines is the speed of effect and the duration of the achieved result.

This is explained by the fact that the preparations contain a large number of amino acids and vitamins, which, in conjunction with neuropeptides, guarantee the desired result.

Reception features

When choosing medications, the doctor uses an individual approach to the patient, taking into account his physiological characteristics and the severity of the pathological condition.

To diagnose hemodynamic disorders, a complete clinical and laboratory examination and consultations with specialists are prescribed. In addition, constant monitoring of the effectiveness of the prescribed therapy is required, especially in the first few days from the date of prescription of the medications.

A distinctive feature of neuroprotectors is their maximum effectiveness when administered through a dropper, when the infusion lasts at least an hour. Intravenous and intramuscular administration of drugs, as well as the use of capsule and tablet forms for courses of up to six months, are also effective. It all depends on the diagnosis given to the patient and the degree of damage to neurocytes.

Classification

Neuroprotective drugs belong to different pharmacological groups. There are 5 types of drugs with neuroprotective properties:

nootropics – correctors of metabolism and neuropsychic pathologies, activate memory;
antioxidants – remove free radicals, rejuvenating every cell, balancing redox reactions in the body;
vascular (cerebrovascular or cerebroprotectors) drugs are divided into several subclasses: anticoagulants and antiplatelet agents - control blood viscosity, prevent the formation of blood clots, calcium antagonists - restore heart rhythm, reduce the load on the myocardium, pulmonary artery, control regional blood flow;
adaptogens - help brain neurons adapt to the proposed conditions;
combined (mixed type) drugs perform the entire complex of the listed tasks.

Neuroprotectors are prescribed by a doctor who selects the drug in accordance with the minimum side effects, maximum efficiency, and calculates the required dose.

Characteristics of drugs of different groups

The quality of human life is correlated with brain function. Over time, neurocytes age, which means we need drugs that can support brain cells and slow down their decline. This is precisely the problem that neuroprotectors solve; every year there are more and more drugs on the pharmacological market.

The task of neuroprotectors is to protect brain cells from various types of influences and damage. The work of all medicines is aimed at solving this issue, and each group of drugs has its own characteristics, treatment regimen, dosage, and method of administration.

Nootropics

Nootropic drugs are a whole group of medications that support neurocytes in negative conditions. The drugs are recommended for use in short courses; in exceptional cases, long-term use is possible under the control of laboratory parameters (therapy effectiveness). The therapeutic effect is based on:

the ability to activate the synthesis of mediators that carry out nerve impulses along nerve fibers;
stimulation of regenerative processes;
restoration of gas exchange, correction of hypoxia;
restoration of memory and cognitive abilities.

High doses cause many side effects. The presence of brain tumors is an absolute contraindication for use.

Picamilon

Picamilon is an inexpensive but effective nootropic that improves blood circulation and eliminates fatigue.

Produced in the form of injections and tablets, prescribed parenterally for the treatment of: asthenia; VSD, migraine, traumatic brain injury, enuresis, stress, emotional overexcitation, neuroinfections, visual impairment, to relieve alcohol intoxication; in order to restore functionality. Price – 85 rubles.

Complete analogues of Picamilon are the following drugs: Pikogam (70 rubles), Picanoyl (3858), Amylonosar (84).

Actovegin

Actovegin is a neuroprotector based on calf blood with a wide spectrum of action due to the ability of the drug to saturate any cells of the body with glucose and oxygen.

It is prescribed as a neuroprotector for strokes, discirculatory encephalopathies, and brain injuries. It is administered parenterally, taken in tablet form. Price – 549 rubles.

Cortexin

The nootropic Cortexin is a complex of protein fractions isolated from the brain of pigs and cattle. It is a neuroprotector with excellent tolerability.

The drug is approved for use by adults and children in courses of 10 days. The downside is the fact that Cortexin is administered only intramuscularly (there are no other forms of release yet). Cost – 766 rubles.

Fenotropil

Phenotropil is a neuroprotector with an almost immediate effect, the effect is felt after a single dose. The ability to remember, concentrate, and speed of thinking accelerates. The drug improves mood and increases the body's resistance to stress. There are currently no complete analogues of the drug. Cost – 455 rubles.

Encephabol

Encephabol is a neuroprotector approved for use from birth (suspension). Prescribed for the treatment of memory impairment, mental retardation, dementia syndrome, and pathological thinking.

The result is achieved with long-term use. Take in the morning (provokes insomnia). Doses and regimen are individual. Side effects are extremely rare. Price – 859 rubles.

Gliatilin

Gliatilin is a precursor to the neurotransmitter acetylcholine and phospholipids that make up cell membranes. The drug is indicated for the treatment of acute conditions (stroke, trauma) and chronic processes: encephalopathy, cognitive dysfunction. Price – 517 rubles. Complete analogues of Gliatilin are Cereton and Cerepro (265 rubles).

Source: https://sosudy.info/nejroprotektory

Other neuroprotectors

oic lecithin is necessary for the formation of intercellular space; it is involved in ensuring the normal functioning of the nervous system and brain cells, as well as in the process of cellular regeneration.

The vitamin-like substance choline is also a neuroprotective drug; it protects cell membranes from destruction and has an antidepressant and calming effect. Choline is involved in lipid metabolism and stabilizes cholesterol levels.

Gingko biloba extract is a natural neuroprotector that combines the properties of an antioxidant and nootropic. It improves memory and increases mental concentration, helps restore psychomotor coordination, and improves blood supply to tissues and organs.

Please note that neuroprotectors with a nootropic effect, neuroprotectors - antioxidants and other types of supplements in this group do not belong to medications and cannot be used to treat diseases. Individual contraindications and intolerances are possible; it is recommended to consult a medical specialist before taking it.

Nootropic medications

This group of drugs is used as a supportive measure. It is mainly prescribed in short courses, but long-term systematic use is possible. The question remains at the discretion of the doctor.

The pharmacological effect is based on several abilities:

Acceleration of the synthesis of specific substances that ensure normal conduction of nerve fibers. This is the main quality of such names.
Stabilization of regenerative properties, increasing the intensity of all healing processes. This is mainly required for patients after emergency conditions such as stroke or hematoma or injury.
Restoring normal gas exchange. Nootropic drugs help correct the oxygen supply to nerve tissues. Considering that the brain is extremely demanding of O2 concentration, this effect is observed almost from the first doses.

In addition, indirectly, nootropics provide normal mental activity and are able to restore memory and cognitive abilities in a short time. However, when using and prescribing in general, caution must be exercised.

High dosages cause side effects. In addition, it is worth keeping in mind that the presence of brain tumors of any location is an absolute contraindication for the use of nootropics. Because there is a high probability of accelerated growth of neoplasia. Including benign, up to a typical pituitary adenoma. This is a direct path to mental and organic disorders.

There are many names of neurotropic drugs for restoring metabolic processes in the brain. Let's consider those that are especially popular in the medical environment.

Perhaps the very first of the medications of this type. It is used in a wide range of situations and is a kind of universal name. Mainly prescribed as a measure of prevention or treatment of chronic ischemic processes in the brain.

A fairly long course is required to correct cognitive abilities and brain nutritional disorders.

It has a minimum of side effects, therefore, despite its long existence, it still retains its position in the conditional ratings of neurologists.

It has a narrow scope of use, restores the membranes of nerve cells and prevents their further death. Indications include previous injuries of any nature, as well as ischemic and hemorrhagic strokes.

It makes sense to use such a drug throughout the entire rehabilitation period.

Refusal occurs gradually until the condition returns to normal. In the future, other medications are prescribed as secondary prevention.

Approximately equal in intensity to the neuroprotective effect of Piracetam. It is created on the basis of a pig brain preparation and is available in the form of an injection solution. It has a natural, natural origin. Therefore, there are minimal contraindications, as well as the likelihood of side effects.

However, you should not take the medicine at your own discretion. The consequences are unpredictable.

It is a mixed neuropeptide that not only accelerates neurometabolism, but also restores adequate blood flow. Refers to synthetic, universal products, used at the discretion of specialists.