Antioxidant drugs in neurology. The use of antioxidant drugs in complex pathogenetic therapy of vascular cognitive disorders. What to eat to fight free radicals

Ivan Drozdov 13.04.2018

Neuroprotectors are a group of drugs that provide the protective function of the nervous system from adverse factors. Neuroprotectors include substances that ensure the functioning of the metabolic system, help maintain the integrity of nerve cells, protect them from death and improve oxygen supply. With their help, brain structures can quickly adapt to negative changes caused by pathological conditions such as senile dementia, Parkinson's syndrome and other neurological diseases.

Classification of drugs

Depending on the mechanism of action and composition, the following groups of neuroprotective drugs are distinguished:

  1. Nootropics – improve the functioning of the metabolic system and are used in the treatment of neurological and mental disorders.
  2. Antioxidants - designed to fight free radicals that appear under the influence of adverse factors.
  3. Vasoactive (vascular) drugs – reduce vascular permeability, help improve blood circulation:
  • anticoagulants – reduce blood viscosity;
  • angioprotectors – increase blood microcirculation in the walls of blood vessels, thereby reducing their permeability;
  • myotropes – help increase vascular tone and blood flow through the vessels;
  • drugs that affect metabolism (calcium channel blockers);
  • psychostimulants – provide nutrition to the brain.
  1. Combination drugs – combine several properties (for example, vasoactive and antioxidant).
  2. Adaptogens are neuroprotective drugs of plant origin.

The described neuroprotectors, depending on the diagnosis and state of health, can be combined during administration, while the range of drugs, as well as the treatment regimen, must be determined by the doctor.

Nootropic drugs

Nootropics are drugs that activate the interaction between nerve cells in the brain. Their action is aimed at:

  • improving memory, concentration and thought processes;
  • relieving nervous overexcitation;
  • elimination of depressive mood;
  • increasing the body's resistance to negative factors;
  • improving blood supply to the brain;
  • prevention of epileptic seizures and manifestations of Parkinson's syndrome.

Cerebrolysin

The hydrolyzate isolated from the pig brain quickly penetrates the brain cells through the blood and prevents the development of tissue necrosis caused by pathological conditions such as stroke, Alzheimer's disease, dementia, encephalitis, etc. In case of circulatory failure in the acute period due to stroke, brain infections, traumatic brain injuries, the drug is prescribed intravenously by drip infusion, dissolving it in special infusion solutions. In a state of sluggish circulatory disorders, Cerebrolysin is administered intramuscularly, without allowing it to be mixed in the syringe with substances that affect the functioning of the heart and vitamins.

Piracetam

The drug helps to increase the concentration of adenosine triphosphoric acid (ATP) in brain cells, which in turn has a positive effect on the functioning of the vascular system, restoration of cognitive, cerebral and metabolic functions. The action of the drug is aimed at protecting brain cells from damage caused by oxygen deprivation, intoxication, injury, and exposure to electric current.

Cerakson

Citicoline, which is the main active ingredient of the drug, has a beneficial effect on the membranes of brain tissue, protecting them from damage caused by traumatic brain injuries and strokes. It increases the speed of energy impulses between nerve cells, helps restore memory, concentration, awareness and thinking. Cerakson promotes a speedy recovery from post-traumatic and post-stroke coma, as well as a reduction in the severity of neurological symptoms characteristic of pathological conditions.

Antioxidants

The action of antioxidant drugs is aimed at neutralizing free radicals that have a negative effect on nerve cells and the body as a whole. Pharmaceuticals are prescribed if the body is exposed to such unfavorable factors as poor climate and ecology, work in harmful conditions, metabolic and endocrine system disorders, heart and vascular diseases. Taking them can increase the resistance of brain tissue to hypoxia, maintain energy balance, reduce the impact of long-term alcohol intoxication on nerve cells, and prevent the development of senile dementia.

Glycine

An amino acid that regulates metabolic processes in the central nervous system. A drug with a sedative and anti-stress effect is prescribed for increased nervous excitability, emotional exhaustion, neuroses, vegetative-vascular dystonia, and ischemic stroke. The cumulative effect of taking Glycine allows you to improve blood circulation, reduce the manifestations of psycho-emotional fatigue, and increase performance.

Mexidol

A powerful antioxidant used for acute attacks of impaired blood supply to the brain - epileptic seizures. The drug is also indicated for use in cases of decreased performance, loss of strength, nervous overexcitation, neuroses, alcohol intoxication, atherosclerotic disorders, and slowed down thinking processes characteristic of senile dementia.

Glutamic acid

A dicarboxylic amino acid that stimulates the metabolic system and the interconnection of neurons in brain structures. It ensures the resistance of brain tissue to oxygen deficiency and protects them from intoxications of various types - alcohol, chemicals, medications. The drug in combination with other antipsychotics is prescribed for mental disorders - psychosis, epilepsy, schizophrenia, as well as brain infections - encephalitis, meningitis. In childhood, glutamic acid is used to treat cerebral palsy, Down's disease, and polio.

Vascular drugs (vasoactive)

Pharmacological agents that have a beneficial effect on blood vessels and hematopoietic function are prescribed to improve blood supply to brain tissue and metabolic processes between neurons. Depending on the mechanism of action, they are divided into several types:

  • myotropic antispasmodics – improve vascular tone and blood flow through them to brain structures;
  • drugs that improve metabolism between nerve cells;
  • angioprotectors;
  • drugs that nourish nerve cells;
  • anticoagulants.

Cinnarizine

Myotropic antispasmodic with vasodilating properties. Under its action, blood fluidity is normalized, blood circulation improves, the resistance of nerve cells to oxygen starvation increases, and the bioelectrical exchange between them is activated. The drug relieves vasospasm and the symptoms accompanying this condition (,). It is prescribed for ischemic stroke, senile dementia, memory loss, Meniere's disease.

Vinpocetine (Cavinton)

The drug, which has antiplatelet, antihypoxic and vasodilating properties, accelerates metabolism in brain tissue, improves blood flow and oxygen delivery to them. Thanks to this, its use is effective in the acute stage of stroke, as well as in the progression of senile dementia. Taking Vinpocetine helps reduce the impact of neurological symptoms, improve memory, increase concentration and intellectual abilities.

Acetylsalicylic acid

An anti-inflammatory drug with antiplatelet properties. Taking it in large quantities helps suppress the biosynthesis process in platelets, due to which the blood clotting process slows down. Preparations containing acetylsalicylic acid are used in the post-stroke period to prevent the formation of blood clots.

Heparin

An anticoagulant with an effect aimed at preventing and treating diseases associated with the formation of blood clots - thrombophlebitis, thrombosis. The drug thins the blood and is administered intravenously in individual dosages. Contraindications to its use are bleeding disorders, the postoperative period, and gastrointestinal ulcers.

Combination drugs

Neuroprotectors of combined action have several properties that enhance each other, which makes it possible to achieve faster and more effective results in treatment by taking low doses of active substances.

Fezam

A drug based on Cinnarizine and Piracetam is prescribed to dilate blood vessels, increase the resistance of brain tissue and nerve cells to a lack of oxygen, and stimulate blood flow to areas of the brain that have been subject to ischemia. Phezam is also used to restore memory and thinking, improve emotional mood, eliminate intoxication syndrome and loss of strength.

Thiocetam

The drug is based on two main pharmaceutical agents - Thiotriazolin and Piracetam. Indications for the use of Thiocetam are cerebrovascular accidents and disorders caused by them, vascular diseases, brain, heart and liver diseases, as well as viral infections. Taking the drug helps strengthen the immune system and increase the resistance of brain cells to hypoxia.

Orocetam

A combined nootropic drug based on Piracetam and orotic acid improves liver function and its detoxification functions, accelerates the exchange of impulses between nerve cells. Thanks to these properties, Orocetam is effectively used for severe brain intoxication caused by infectious diseases and viruses, as well as alcohol and chemical poisoning.

Adaptogens

Herbal preparations that increase the body's resistance to harmful and pathological influences are called adaptogens. Substances in herbal remedies help adapt to stress and sudden climate change. They are effectively used during the recovery period for the treatment of infectious diseases of the brain, and intracranial injuries.

Ginseng tincture

The herbal product has a beneficial effect on the nervous, vascular and metabolic systems. It is prescribed as an adjuvant therapy for patients weakened by the disease, as well as in the presence of signs of physical and nervous exhaustion. Taking the infusion helps lower blood sugar, increase blood pressure during hypotension, improve metabolism, and eliminate bouts of vomiting.

Ginkgo biloba

The drug contains plant substances such as eleutherococcus and gotu kola. It is prescribed for intracranial hypertension, decreased brain function, nervous fatigue, vascular and endocrine diseases, and decreased transmission of impulses between nerve cells.

Apilak

A biostimulant based on dried royal jelly of bees is prescribed for low blood pressure, loss of strength, eating disorders, mental and neurological disorders. Apilak is not recommended for use in cases of adrenal dysfunction, as well as hypersensitivity or intolerance to bee products.

Indications and contraindications for the use of neuroprotectors

The action of neuroprotectors is aimed at improving metabolic processes between brain cells and their adaptation to changes caused by circulatory disorders. Their use is indicated for the following pathological conditions:

Taking neuroprotectors is contraindicated in the following cases:

  • hypersensitivity to substances included in the drug;
  • inflammatory and infectious processes occurring in the kidneys and liver;
  • when taking other sedatives and antidepressants;
  • heart failure;
  • pregnancy and lactation period.

Is something bothering you? Illness or life situation?

Neuroprotective drugs should also be discontinued if the patient experiences side effects after taking them - nausea, vomiting, allergic rash, increased breathing and heart rate, nervous overexcitation.

Antioxidants are substances that slow down oxidation processes by binding free radicals. The older a person is, the worse his antioxidant system copes with its tasks. This is especially true for people living in industrial centers and megacities. Antioxidant drugs from pharmacies are designed to help restore the body, improve health and prolong youth.

Main groups of antioxidants

Today, scientists know a huge number of different antioxidants, the number of which is growing every year, but they can all be divided into four categories:

  1. Vitamins. They can be fat- or water-soluble. The latter provide protection to ligaments, blood vessels and muscles, while fat-soluble ones protect fatty tissue in the body. The most powerful among the fat-soluble ones are vitamin A, beta-carotene and vitamin E. As for the water-soluble ones, the most powerful among them are vitamin C (ascorbic acid is an antioxidant) and B vitamins.
  2. Bioflavonoids. This type of antioxidant is also found in drugs, and is also found in red wine in the form of catechins, and in green tea in the form of quercetin. Bioflavonoids act on free radicals as a trap, suppressing their development.
  3. Enzymes. These antioxidant tablets act as catalysts that help neutralize free radicals. They are also produced by the body.
  4. Minerals. They are not synthesized by the body, but enter the body from the outside in the form of products and antioxidant drugs from the list. The most powerful are calcium, zinc and manganese.

Vitamin antioxidants

Such antioxidant preparations are sold in pharmacies without a prescription. These drugs are vitamin-mineral complexes. The list of antioxidants of this type includes the following pharmaceutical preparations:

Vitrum-forte Q10. The drugs help slow down the wear and tear of systems and organs by stimulating their blood supply and regulating the concentration of cholesterol in the blood.

Vitrum is an antioxidant. This antioxidant in the drug provides protection against the damaging effects of free radicals. The complex is prescribed to strengthen the immune system for colds and infections, as well as for the prevention of hypovitaminosis.

You can find out how antioxidant drugs from the vitamin-type group work in the instructions for a specific drug, choosing the best option for yourself.

Video

Omega-3 based drugs

This group of antioxidant drugs contains omega-3 fatty acids and includes such popular pharmaceutical products as:

  • fish fat;
  • Vitrum cardio;
  • Epadol;
  • Omacor;
  • Tecom and some others.

When omega-3 acids enter the body, they restore the normal balance of polyunsaturated fats. The strongest antioxidants in drugs in this group are:

Essentiale. A complex pharmaceutical antioxidant, which in addition to phospholipids contains vitamins with antioxidant properties. The drug is indispensable in the fields of obstetrics, pulmonology and cardiology.

Lipin. A powerful antioxidant drug of natural origin to restore the functional activity of the endothelium. It has immunomodulatory and membrane-protective properties, and also strengthens antioxidant defense in the body.

Berlition, Espa-Lipon. These antioxidants in medications are prescribed for hyperglycemia to lower blood glucose levels. Berlition is also used for diabetic neuropathy, and Espa-Lipon is a lipid-lowering agent, detoxifier and hepatoprotector.


Peptide and nucleic acid preparations

The most powerful antioxidant drugs on the list are pharmaceutical preparations and are used both in complex and mono-therapy.

Glutargin. It contains arginine and glutamic acid. It creates a hypoammonemic effect and is characterized by antioxidant, antihypoxic and cardioprotective activity. Prescribed for liver cirrhosis, hepatitis and other diseases.

Asparkam, Panangin. Popular antioxidant drugs stimulate the motility of the digestive system, the formation of ATP, normalize the functioning of blood vessels and the heart, and also tone skeletal muscles.

Kratal, Dibikor. These antioxidants from the pharmacy create a hypoglycemic and stress-protective effect on the human body. Prescribed for diabetes and other endocrine disorders, as well as for heart failure. Kratal can be used for vegetative neuroses.

Cerebrolysin. The main component of this antioxidant drug is a hydrolyzate of a substance from pig brain. The drug reduces the concentration of lactate in brain tissue, reduces the neurotoxic effects of certain amino acids, etc. The drug is prescribed for strokes and cerebrovascular disorders.

Actovegin. This antioxidant tablet is a thoroughly purified blood hemodialysate. It contains oligopeptides, nucleosides and other important components that increase the influx of potassium and stimulate phosphate metabolism. The product creates a powerful antioxidant effect and is used for damage to the central nervous system, organic eye damage and other diseases.


For quotation: Chukanova E.I., Chukanova A.S. The use of antioxidant drugs in complex pathogenetic therapy of vascular cognitive impairment // Breast Cancer. 2014. No. 10. P. 759

Over the past decades, vascular diseases of the brain have been one of the pressing problems in neurology. According to WHO, about 5 million people die every year from cerebrovascular diseases (CVDs). Chronic cerebral ischemia (CHI) is one of the most common clinical syndromes of CVD; it usually precedes the development of stroke and other cerebrovascular complications. One of the most common and earliest manifestations of CCI are vascular cognitive impairment (VCI), as well as emotional and motor disorders.

Despite the large number of fundamental and clinical works devoted to this topic, there are currently many unresolved issues related to both the pathogenetic and morphofunctional features of the course of acute and CCI.

Arterial hypertension (AH), atherosclerosis (lipohyalinosis) of small penetrating arteries and arterioles are the main etiological factor in the development of cerebral microangiopathy, which underlies the formation of CCI. In the absence of hypertension and lipohyalinosis, damage to small arteries may be associated with the course of senile arteriosclerosis, hereditary angiopathy, and inflammatory vasculopathies. These factors are closely associated with inflammation and endothelial dysfunction, destabilization of the atherosclerotic plaque and can be used as additional markers in assessing the risk of stroke.

The other most important risk factor for the development of endothelial dysfunction is genetic predisposition. In recent years, the attention of researchers has been drawn to the study of the functions of the vascular endothelium as one of the most important links in the pathogenesis of the development of vascular diseases. In the second half of the 20th century. The endothelium began to be considered as a metabolically active organ that influences the regulation of vascular tone and the course of various processes occurring within the vascular bed. Cerebral endothelium is one of the central links in the regulation of cerebral blood flow and is involved in the formation and functioning of the blood-brain barrier. In addition, under physiological conditions it is a tissue component of the system for regulating the aggregate state of blood (RAS), providing the tissue component of the anticoagulant status of the blood. The layer of endothelial cells on the inner surface of blood vessels and the heart is an active endocrine organ. Since endothelial cells secrete a large number of different substances into the blood and surrounding tissues, their complex can be considered as the largest endocrine system, diffusely scattered throughout all tissues and organs. The total mass of endothelium in humans is about 2000 g.

Cardiovascular risk factors, primarily hypertension, and the presence of metabolic syndrome disrupt the delicate balance between the most important functions of the endothelium, which is ultimately realized in the activation of the endothelium as an inflammatory response to stress factors, this is confirmed by the results of a number of studies. One of the consequences of endothelial activation is an increase in vascular permeability, as a result of which plasma proteins penetrate through the layer of endothelial cells into the vascular wall. The endothelium synthesizes prostacyclin, nitric oxide, atrial natriuretic factor, plasminogen activator, plasminogen activator inhibitor, endothelial growth factor and a number of other substances that are of great importance both for ensuring vasomotor reactions and for regulating the activity of free radical oxidation, intravascular thrombus formation, and the activity of local inflammatory and autoimmune reactions. Active substances released from endothelial cells affect both the cellular and plasma components of hemostasis, as well as smooth muscle cells and fibroblasts, triggering enzyme cascades that synthesize biogenic amines (adrenaline, norepinephrine, serotonin, etc.), nucleotides, eicosanoids, kinins and the conversion of angiotensin I (AI) to angiotensin II (AII).

Currently, some endothelial dilatation factors have been identified: endothelial hyperpolarizing factor, prostacyclin I2 (PGI2), nitrogen monoxide (NO), type C natriuretic peptide, adrenomedullin. Constriction factors include: thromboxane A2, prostaglandin F2a, endoperoxides, etc. Among the biologically active substances produced by the endothelium, the most important is nitric oxide - NO. Nitric oxide is present in all endothelial cells regardless of vascular size and function. But of the large number of biologically active substances secreted by the endothelium, it is nitric oxide that regulates the activity of other mediators. In this case, NO acts in most cases not directly, but by setting in motion a cascade of reactions inside cells indirectly, through many steps. NO is an important biological conductor capable of causing a large number of both negative and positive changes at the cellular level. NO, along with other free radical compounds, is involved in neuroregulation processes, being an additional risk factor for the development of oxidative stress.

The achievement of fundamental neurobiological sciences is the discovery of common mechanisms of neuron damage under various pathological conditions - excitotoxicity (from the English excite - excite) and oxidative stress.

The particular danger of developing oxidative stress in the central nervous system is determined by the significant intensity of oxidative metabolism in the brain, which accounts for 2% of the total mass of a person, but utilizes up to 50% of all oxygen consumed. The intensity of oxygen consumption by neurons is tens of times higher than the needs of other cells and tissues (350-450 μl O2/g /1 min/ compared to 70-90 μl for the heart, 1.6-2.4 μl for skeletal muscles, 9 -24 µl - for phagocytic leukocytes).

Additional factors for the development of oxidative stress in brain tissue are the high content of lipids (about 50% of dry matter), the unsaturated bonds of which constitute a substrate for lipid peroxidation (LPO); ascorbate (100 times more than in peripheral blood), participating as a pro-oxidant in non-enzymatic lipid peroxidation processes. The activity of enzymatic antioxidant systems (catalase, glutathione peroxidase) in the brain is significantly lower than in other tissues, which further increases the risk of developing oxidative stress.

Dysfunction of the endothelium sooner or later leads to impaired patency of vessels of various sizes and ischemia of the corresponding organ or tissue. The pathomorphological manifestation of damage to small vessels of the brain is the accumulation of hyaline and thickening of small perforating terminal arterioles located in the white matter; microatheromas are sometimes detected in small vessels.

With the development of microangiopathy, the deep parts of the white matter of the brain, located in the zone of adjacent blood supply to the carotid and vertebral-basilar basins, are primarily affected. Long-term hypertension, causing microangiopathy of penetrating arteries, leads to damage to the above-mentioned parts of the brain. The basal ganglia and deep parts of the white matter of the cerebral hemispheres are the most common localization of lacunar infarctions and leukoaraiosis, which are the morphological basis for the formation of cognitive impairment.

The basal ganglia, through which the association zones of the anterior and posterior parts of the cerebral cortex communicate with each other, are important for the cognitive activity of the brain. White matter damage also causes cognitive dysfunction because it disconnects the frontal lobes of the brain from its posterior cortical and subcortical structures. Clinical and psychological analysis indicates that dysfunction of the frontal lobes of the brain plays a key role in the formation of cognitive disorders in cerebrovascular insufficiency. If the process of circulatory disturbance develops acutely, focal damage occurs in the area of ​​​​the blood supply to the perforating arteriole - lacunar infarction; if the process of discirculation is more extended in time, then diffuse ischemic damage to the nervous tissue occurs - leukoaraiosis.

As we have already mentioned, cognitive impairment is one of the most important manifestations of cerebrovascular insufficiency, which occurs already in the early stages of vascular damage to the brain.

Currently, close attention is drawn to the intermediate stage of development of cognitive impairment, when it has not yet reached the level of dementia, but is already beyond the age norm. Currently, this condition is interpreted as the prodromal stage of dementia - “mild cognitive impairment” (mild, mild). In mild cognitive impairment (MCI), intellectual changes are expressed both in memory loss and in the limitation of other cognitive abilities, but do not lead to loss of everyday independence.

The incidence of MCI is 2-4 times more common than dementia (15-25%). Moreover, the mortality rate of patients with MCI significantly exceeds the mortality rate of the group of patients without MCI. Within 6 years, 1/3 of patients with MCI die due to the development of somatic complications, more often from cardiovascular diseases. However, it must be remembered that 20-40% of patients with MCI may experience improvement in cognitive function.

The criteria for diagnosing MCI, according to the European Alzheimer's Association, are: complaints of decreased memory of the patient himself or those around him; indications from people who know the patient of a decline in cognitive function or functional ability over the past year; moderate cognitive deficits on neuropsychological examination (memory, language, visuospatial, regulatory or other functions); presence of a preserved level of intelligence; no impact of cognitive defect on daily activities (some difficulty in performing the most complex activities) and no clinical signs of dementia.

Clinical signs of MCI are: decreased attention and/or absent-mindedness; fast fatiguability; irritability; decreased memory for current events; inability to remember new names; inability to retell what you just read; impaired orientation in unfamiliar areas; difficulty finding words when speaking; difficulties with counting operations; weakening of the patient’s sense of time; limiting the range of interests.

One of the ways to influence the course of CCI, as well as prevent the development of stroke, is to eliminate or reduce the influence of risk factors for the development of CVD, which can help interrupt the pathological biochemical cascade that underlies the formation of morphofunctional changes in the brain.

The main groups of drugs that improve cognitive function are drugs acting on the neurotransmitter systems of the brain (dopaminergic/noradrenergic, cholinergic, glutamatergic), as well as drugs with neurometabolic, neurotrophic and vasoactive effects.

Currently, much attention is paid to studying the effect of neuroprotectors in the treatment of patients with acute and chronic forms of cerebrovascular pathology. Protective protection of the brain in chronic cerebrovascular insufficiency may be one of the most effective methods of treating patients with this pathology. The administration of neuroprotectors helps prevent the development of cerebral metabolic disorders in patients with an increased risk of cerebral ischemia, i.e., when the reserves of cerebral hemodynamics and metabolism are limited. Their administration can prevent severe and irreversible damage to neurons.

Medicines that improve cerebral blood flow include ergot derivatives (nicergoline, vasobral), periwinkle derivatives (vincamine, vinpocetine), pentoxifylline, nicotinic acid derivatives, ginkgo biloba preparations, combination drugs - instenon, cinnarizine. Piracetam and its derivatives, cerebrolysin, citicoline, choline alfoscerate, g-aminobutyric acid, as well as drugs with a pronounced antioxidant effect that have a multifactorial effect on brain tissue, such as solcoseryl, actovegin, α-lipoic acid preparations, are used as metabolic and neurotransmitter agents. (thioctic acid, etc.), carnitine chloride and succinic acid preparations (Mexiprim).

Mexiprim (ethylmethylhydroxypyridine succinate), belonging to the group of heteroaromatic antioxidants and direct-acting hypoxants, has a wide spectrum of pharmacological activity, occurring at two levels - neuronal and vascular. The drug has a wide range of pharmacological activity: it increases the body’s resistance to stress, exhibits an anxiolytic effect that is not accompanied by a muscle relaxant effect; has nootropic properties, prevents and reduces learning and memory disorders that occur with aging and exposure to various pathogenic factors; has an anticonvulsant effect; exhibits antioxidant and antihypoxic properties; increases concentration and performance; weakens the toxic effect of alcohol.

Such a wide range of clinical effects of Mexiprim is associated with its ability to improve the metabolism of brain tissue, microcirculation and rheological properties of blood, and reduce platelet aggregation. Mexiprim stabilizes the membrane structures of blood cells (erythrocytes and platelets). It has a hypolipidemic effect, reduces the content of total cholesterol and LDL. Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action is due to its antioxidant and membrane protective effect. It inhibits lipid peroxidation, increases superoxide oxidase activity, lipid-protein ratio, reduces membrane viscosity, and increases its fluidity. Modulates the activity of membrane-bound enzymes (calcium-independent PDE, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, helps preserve the structural and functional organization of biomembranes, transport of neurotransmitters and improve synaptic transmission. Mexiprim increases dopamine levels in the brain. Causes an increase in compensatory activation of aerobic glycolysis and a decrease in the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in the content of ATP and creatine phosphate, activation of the energy-synthesizing functions of mitochondria, stabilization of cell membranes.

When taking Mexiprim orally, the time to reach the maximum concentration in the blood plasma is 0.46-0.5 hours. Mexiprim quickly passes from the bloodstream into organs and tissues and is quickly eliminated from the body. When administered intramuscularly, the drug is detected in the blood plasma for 4 hours after administration. The time to reach maximum concentration, as with oral administration, is 0.45-0.5 hours. Mexiprim in the human body is intensively metabolized with the formation of its glucuron-conjugated product.

In case of acute cerebrovascular accidents, Mexiprim is prescribed as part of complex therapy in the first 2-4 days intravenously in a stream or drip for adults at 200-300 mg 1 time per day, then intramuscularly at 100 mg 3 times per day. The duration of treatment is 10-14 days.

For CCI in the decompensation phase, Mexiprim is prescribed intravenously in a stream or drip at a dose of 100 mg 2-3 times a day for 14 days. Then they switch to intramuscular administration of the drug at 100 mg/day over the next 2 weeks.

For course prophylaxis of CCI, the drug is administered to adults intramuscularly at a dose of 100 mg 2 times a day for 10-14 days.

For mild cognitive disorders in elderly patients and in cases of anxiety, the drug is administered intramuscularly in a daily dose of 100-300 mg for 14-30 days.

An extremely important aspect of the action of Mexiprim is its compatibility with psychotropic drugs; Mexiprim enhances the effect of benzodiazepine anxiolytics, anticonvulsants, in particular carbamazepine, antiparkinsonian drugs (levodopa). Mexiprim increases the antianginal activity of nitro drugs. This drug does not affect the conduction system of the heart, which is especially important for elderly patients, does not cause tachycardia, dizziness, daytime sleepiness, and is also compatible with drugs of other pharmacological groups.

Side effects (nausea, dry oral mucosa, drowsiness, lack of coordination, allergic reactions, headache, fluctuations in blood pressure) when taking Mexiprim are extremely rare, which has been repeatedly confirmed in clinical studies.

Thus, improving care for patients with cerebrovascular insufficiency is one of the priorities of modern medicine. Drugs with antioxidant effects, in particular Mexiprim, can be recommended as an effective treatment for mild and moderate cognitive disorders as part of complex therapy due to their effect on the main pathobiochemical links in the development of CCI.

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Antioxidants, antioxidants (preservatives, antioxidants) - molecules with a negatively charged electron, oxidation inhibitors, synthetic or natural substances that can slow down the oxidation process.

Antioxidants are substances that slow down oxidation processes by binding free radicals. The older a person is, the worse his antioxidant system copes with its tasks. This is especially true for people living in industrial centers and megacities. Antioxidant drugs from pharmacies are designed to help restore the body, improve health and prolong youth.

Main groups of antioxidants

Today, scientists know a huge number of different antioxidants, the number of which is growing every year, but they can all be divided into four categories:

  1. Vitamins. They can be fat- or water-soluble. The latter provide protection to ligaments, blood vessels and muscles, while fat-soluble ones protect fatty tissue in the body. The most powerful among the fat-soluble ones are vitamin A, beta-carotene and vitamin E. As for the water-soluble ones, the most powerful among them are vitamin C (ascorbic acid - an antioxidant) and B vitamins.
  2. Bioflavonoids. This type of antioxidant is also found in drugs, and is also found in red wine in the form of catechins, and in green tea in the form of quercetin. Bioflavonoids act on free radicals as a trap, suppressing their development.
  3. Enzymes. These antioxidant tablets act as catalysts that help neutralize free radicals. They are also produced by the body.
  4. Minerals. They are not synthesized by the body, but enter the body from the outside in the form of products and antioxidant drugs from the list. The most powerful are calcium, zinc and manganese.

Vitamin antioxidants

These antioxidants are sold in pharmacies without a prescription. These drugs are vitamin-mineral complexes. The list of antioxidants of this type includes the following pharmaceutical preparations:

Vitrum-forte Q10. The drugs help slow down the wear and tear of systems and organs by stimulating their blood supply and regulating the concentration of cholesterol in the blood.

Vitrum is an antioxidant. This antioxidant in the drug provides protection against the damaging effects of free radicals. The complex is prescribed to strengthen the immune system for colds and infections, as well as for the prevention of hypovitaminosis.

You can find out how antioxidants from the group of vitamin-type drugs work in the instructions for a specific drug, choosing the best option for yourself.

Omega-3 based drugs

This group of antioxidant drugs contains omega-3 fatty acids and includes such popular pharmaceutical products as:

  • fish fat;
  • Vitrum cardio;
  • Epadol;
  • Omacor;
  • Tecom and some others.

When omega-3 acids enter the body, they restore the normal balance of polyunsaturated fats. The strongest antioxidants in drugs in this group are:

Essentiale. A complex pharmaceutical antioxidant, which in addition to phospholipids contains vitamins with antioxidant properties. The drug is indispensable in the fields of obstetrics, pulmonology and cardiology.

Lipin. A powerful antioxidant drug of natural origin to restore the functional activity of the endothelium. It has immunomodulatory and membrane-protective properties, and also strengthens antioxidant defense in the body.

Berlition, Espa-Lipon. These antioxidants in medications are prescribed for hyperglycemia to lower blood glucose levels. Berlition is also used for diabetic neuropathy, and Espa-Lipon is a lipid-lowering agent, detoxifier and hepatoprotector.

Peptide and nucleic acid preparations

Antioxidants of this group of drugs are used both in complex and mono-therapy. The most powerful antioxidants in tablets from the list are pharmaceutical preparations:

Glutargin. It contains arginine and glutamic acid. It creates a hypoammonemic effect and is characterized by antioxidant, antihypoxic and cardioprotective activity. Prescribed for liver cirrhosis, hepatitis and other diseases.

Asparkam, Panangin. Popular antioxidant drugs stimulate the motility of the digestive system, the formation of ATP, normalize the functioning of blood vessels and the heart, and also tone skeletal muscles.

Kratal, Dibikor. These antioxidants from the pharmacy create a hypoglycemic and stress-protective effect on the human body. Prescribed for diabetes and other endocrine disorders, as well as for heart failure. Kratal can be used for vegetative neuroses.

Cerebrolysin. The main component of this antioxidant drug is a hydrolyzate of a substance from pig brain. The drug reduces the concentration of lactate in brain tissue, reduces the neurotoxic effects of certain amino acids, etc. The drug is prescribed for strokes and cerebrovascular disorders.

Actovegin. This antioxidant tablet is a thoroughly purified blood hemodialysate. It contains oligopeptides, nucleosides and other important components that increase the influx of potassium and stimulate phosphate metabolism. The product creates a powerful antioxidant effect and is used for damage to the central nervous system, organic eye damage and other diseases.

Unfortunately, you can only be forever young and beautiful in your avatar. In life, everything is different: with age, wrinkles and diseases appear. And free radicals are to blame for all these troubles. To combat them, you can use natural products and artificial antioxidants - drugs that are sold in pharmacies. We will talk about them.

How to protect yourself from “agents of old age”?

Free radicals are molecules that are missing one electron. These are found both in products and in the environment. Everything would be fine, but when they find themselves in the body, they intensively try to make up for their “defect” and look for material for themselves to “complete”, taking it away from other cells. By damaging them, they cause premature aging. After 30 years, almost a third of all protein compounds suffer from free radical attacks.

To stop their destructive effects, there are drugs - antioxidants. What are they and what do they contain? These are special substances that neutralize oxidation processes and are created in laboratories. They increase cell endurance, prolong youth and increase human life expectancy.

Certain foods can also introduce them into the body. But why are synthetic antioxidants better than natural products? Nothing really. The best option is to get such beneficial substances through food. But not everyone has the opportunity to eat fully and properly. In addition, the quality of the products themselves today leaves much to be desired: they contain nitrates and other harmful components. Therefore, in order to protect yourself from cancer, heart disease, preserve vision and avoid early aging, it is advisable to take artificial antioxidants - drugs that can be found in pharmacies.

The best antioxidants for age-related diseases

If you have already felt the harmful effects of “evil” radicals and are determined to give a decisive rebuff to illness and old age, then use “pure” antioxidants. Drugs (the list of them is quite impressive) of this spectrum are available, but they must be prescribed by a doctor: if you act on your own, you can harm your well-being.

The most powerful antioxidants are used in complex and monotherapy. Among the best are the following pharmaceuticals:

  • Glutargin. Includes glutamic acid and arginine. It has not only antioxidant, but also antihypoxic (improves oxygen metabolism) and cardioprotective activity (positively affects heart function). This drug is prescribed for cirrhosis, hepatitis and other serious ailments;
  • Asparkam and Panangin. These are fairly well-known drugs from the range of synthetic antioxidants. They have a beneficial effect on the functioning of the digestive organs, heart and blood vessels, maintain skeletal muscle tone, stimulate ATP synthesis;
  • Dibikor, Kratal. Produces stress-protective and hypoglycemic effects. They are prescribed for diabetes and other endocrine pathologies. They are also indicated for those who have insufficient pumping function of the heart. Kratal becomes a real salvation for VSD;
  • Actovegin. A drug that is, as they say, “well known.” The main active ingredient of this antioxidant is purified blood hemodialysate. It also contains other valuable elements that replenish potassium reserves and stimulate phosphate metabolism. The medicine effectively resists free radicals and is used for lesions of the central nervous system and pathologies of the organs of vision;
  • Cerebrolysin. A medicine with an impressive “experience”. Its antioxidant effect is based on the presence of a special substance from pig brain. It reduces the lactate content in brain tissue and suppresses the neurotoxic effects of certain amino acids. It is usually included in the list of prescriptions for strokes and other pathologies of the nervous system.

Antioxidants without a prescription: how to prolong your youth?

If you don’t have any special health problems, but signs of age are already making themselves felt, then it’s better to start with vitamin-mineral complexes. The following multivitamins lead the list of such antioxidants:

  • Vitrum-forte Q10. A product that slows down the natural wear and tear of all organs, improves their blood supply and normalizes the content of “bad” cholesterol;
  • Vitrum is an antioxidant. Qualitatively blocks the oxidative process, thereby reducing the danger of pest radicals. Can be used both for prophylactic purposes (to prevent vitamin deficiency) and to strengthen the immune system (for frequent ARVI);
  • Essentiale. This is a complex antioxidant. Its peculiarity is that it contains phospholipids and vitamins;
  • Lipin. Considered the most powerful antioxidant of natural origin. Restores endothelial activity, increases the protective forces and antioxidant capabilities of cells;
  • Espa-Lipon, Berlition. Agents that reduce glucose concentrations.

The range of antioxidant drugs is quite large, but you need to pay attention to this feature: in order for vitamins and microelements to neutralize the negative effects of free radicals, you should increase their daily dose by 2-3 times and drink them for at least a year.

What to eat to fight free radicals?

As already mentioned, you can help your body resist insidious radicals not only with pills. Products can also perform this task. These are vegetables and fruits (grapes), vegetable oils, sprouted grains, green tea, coffee (good quality), chocolate, spices (cinnamon and cloves). The only pity is that most of them contain an impressive amount of calories, so consuming them in large quantities simply won’t work.

So are antioxidants the miracle cure that will stop aging? Scientists have not yet come to a consensus. The healing effect of these elements on the body has not yet been proven by science. But one thing is certain: proper and balanced nutrition and well-chosen vitamin complexes will help avoid many diseases and prolong youth.

Should neuroprotective drugs be used in clinical practice?

Kuznetsov A.N. National Medical and Surgical Center named after N.I. Pirogov, Moscow

The debate regarding the appropriateness of neuroprotective therapy is currently one of the most heated. Several dozen substances have demonstrated a neuroprotective effect in experimental studies, but none of them have confirmed their effectiveness and safety in clinical randomized controlled trials (RCTs). In this regard, in all modern clinical guidelines for the treatment of acute neurological diseases, neuroprotective therapy is not recommended for use. On the other hand, based on empirical experience, as well as within the framework of their own protocols in many medical institutions, and in Russia - in the vast majority of them, drugs with supposed neuroprotective activity are widely used. Why are neuroprotective agents that have proven their effectiveness in experimental studies not subsequently confirmed in clinical trials? Most experts agree that the reason is significant design flaws in the RCTs conducted:

  • selection of an inadequate “therapeutic window”;
  • lack of targeted patient selection;
  • use of obviously insufficient dosages of the drug;
  • selecting endpoints with low sensitivity and overestimating the magnitude of the possible effect.
Although in experimental studies neuroprotective agents were used immediately after ischemic or traumatic injury (usually within 90 minutes), RCTs enrolled patients within 24 to 48 hours of the acute event. In addition, when selecting patients with stroke, there was no upper and lower threshold for stroke severity, the subtype of ischemic stroke was not taken into account, and the presence or absence of recanalization of the affected artery was not taken into account, while in experimental studies, in almost all cases, neuroprotective therapy was carried out in conditions restored perfusion. This approach to selecting patients and choosing a “therapeutic window” was dictated by the desire to include as many patients as possible in the study, with deliberate disregard for extrapolating the results of experimental studies to the clinical situation, which ultimately led to negative results from RCTs. The use of dosages of drugs in RCTs that were much lower than in the experiment was aimed at minimizing side effects. Treatment efficacy was assessed using clinical endpoints, scales with insufficient clinical sensitivity (eg, Glasgow Coma Scale) were used, and the study design was modeled for a clinically significant effect. Differences of about 10-15% were assumed for the primary endpoints, that is, the effect obtained for thrombolytic therapy within a 3-hour “therapeutic window”, which was obviously an unrealistic result. Statistical calculations show that, using a single neuroprotective agent and clinical endpoints, an effect of 3-5% can be calculated by enrolling 3000-4000 patients using a 3-hour “therapeutic window” and using dosages similar to the experimental ones. An effect of 1-2% is realistically achievable. In any case, these should be large or very large studies in terms of the number of patients included. But in this case the question arises: who will be able to pay for such research? And even if an effect of 1-2% is achieved: who will pay for an expensive drug with minimal effect? Possible ways to overcome this situation are:
  • use of surrogate endpoints;
  • the use of several neuroprotective drugs with different points of application;
  • use of combined thrombolytic and neuroprotective therapy.
Surrogate, that is, non-clinical, endpoints have recently become more and more widely used in RCTs. The most commonly used results are magnetic resonance neuroimaging, which can monitor the extent of damage and serve as a predictor of recovery. But the most promising seems to be the use of combined thrombolytic and neuroprotective therapy in the case of ischemic stroke. Recanalization of an occluded artery will ensure maximum delivery of a neuroprotective agent to the site of damage and, thus, approach the conditions for conducting experimental studies. On the other hand, neuroprotective therapy will help to expand the “therapeutic window” for thrombolysis, as well as reduce reperfusion injury. It should be noted that the experimental studies also had significant shortcomings that contributed to the negative results of the RCT:
  • the “therapeutic window” was not precisely defined;
  • the dose range that ensures maximum effectiveness and safety of the substance has not been precisely determined;
  • the set of markers for the effectiveness of the substance has not been precisely defined.
The main groups of neuroprotective drugs are:
  • calcium channel blockers;
  • NMDA and AMPA receptor antagonists;
  • glutamate release inhibitors;
  • GABA receptor agonists;
  • adenosine receptor agonists;
  • membrane-stabilizing drugs;
  • neurotrophic (growth) factors;
  • nitric oxide inhibitors;
  • antioxidants;
  • anti-inflammatory drugs;
  • other drugs.
The action of so-called calcium antagonists or calcium channel blockers (nimodipine (NimotopR) is the most well known in Russia) is aimed at one of the key mechanisms of cell death, both through the mechanism of necrosis and the mechanism of apoptosis - excessive calcium entry into the cell. Drugs in this group block voltage-gated calcium channels, but do not affect calcium channels controlled through receptors (NMDA, AMPA), so their effectiveness is limited. In addition, calcium antagonists have significant side effects, in particular vasodepressor effects. In this regard, numerous RCTs have had negative results. The effectiveness of nimodipine has been demonstrated only in relation to the prevention of vasospasm in subarachnoid hemorrhage. NMDA and AMPA receptor antagonists block receptor-gated calcium channels and thus interrupt the basal flow of calcium into the cell. Receptor activation occurs due to the release of excitotoxic amino acids (mainly glutamate). Substances with high affinity for NMDA receptors (for example, MK-801) showed in RCTs serious psychotomimetic and neurotoxic side effects, since they caused a complete blockade of the receptors, inhibiting their normal physiological activity. Promising drugs are drugs with low affinity for NMDA receptors (memantine, amantadine sulfate, magnesium sulfate and others). An additional important mechanism of action of memantine demonstrated experimentally is the inhibition of hyperphosphorylation of the tau protein and thus the process of neurodegeneration. Some other excitotoxic amino acids, in particular glycine, also cause activation of NMDA receptors, so glycine antagonists have been studied in RCTs, but have not yet confirmed their effectiveness. Currently, RCTs are ongoing to study the effectiveness and safety of AMPA receptor antagonists. The experiment demonstrated the effectiveness of substances that prevent the release of glutamate from presynaptic terminals (lubeluzole), but RCTs have not confirmed their effectiveness. RCTs are ongoing to study the effectiveness of new classes of neuroprotectors - GABA and adenosine receptor antagonists. Among drugs with membrane-stabilizing effects, the effectiveness and safety of cytidine diphosphocholine (cyticholine) is currently being studied in RCTs. A drug used in Russia with a similar mechanism of action is choline alfoscerate (GliatalinR). It should be noted that the effectiveness and safety of this drug have not been studied in RCTs. Great hopes are associated with the use of neurotrophic (growth) factors. One such drug, fibroblast growth factor, was studied in RCTs, but the results were negative. At the same time, the results of experimental studies show the effectiveness of such substances (in particular, the drug CerebrolysinR) in blocking both necrotic and apoptotic neuronal death by inhibiting the calcium-dependent protease calpain. Clinical studies of the neuroprotective activity of antioxidants are ongoing. RCTs of the drug ebselen are currently being conducted. In Russia, antioxidant drugs are used quite widely (MexidolR, CarnitineR and others), but their effectiveness and safety have not been studied in RCTs. Currently, an RCT study of the neuroprotective activity of piracetam, a drug that has been widely used in Russia for a long time, is being conducted. Nitric oxide inhibitors and anti-inflammatory drugs have not yet demonstrated their effectiveness and safety in RCTs. There is no doubt that new RCTs, the design of which will be carried out taking into account previously existing shortcomings, as well as the emergence of new, safer neuroprotective agents, will make it possible to prove the clinical effectiveness of neuroprotection. In this case, the high expectations that the medical community has regarding neuroprotective therapy, as well as the high costs that pharmaceutical companies incurred when creating drugs, will be justified. However, this takes time, so what to do now? The way out of this situation is the use of drugs with supposed neuroprotective activity and known symptomatic effects. Such drugs can also be considered as means that increase the effectiveness of early rehabilitation of patients with severe acute neurological pathology. Early rehabilitation, as is known, is one of the integral components of complex treatment of such patients. Among the drugs used in Russia:
  • amantadine sulfate (PC-MerzR) has demonstrated its effectiveness in restoring motor functions; has an awakening effect;
  • memantine (AkatinolR) has been shown to improve cognitive function in RCTs;
  • CerebrolysinR promotes the restoration of cognitive functions;
  • choline alfoscerate (GliatilinR) has an awakening effect;
  • piracetam (PiracetamR, NootropilR, LucetamR) helps improve cognitive functions and has also shown its effectiveness in restoring impaired speech.
It should be noted that one of the areas where neuroprotective drugs can demonstrate their effectiveness is the prevention of neurological complications during surgical interventions that are aggressive to the nervous system (surgeries and manipulations on the heart and cerebral vessels, neurosurgical interventions). Today, when we are on the verge of creating Russian recommendations for the treatment of acute neurological diseases, there is a need to invite Russian specialists to a broad discussion regarding the advisability of using neuroprotective drugs.

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