Glycosaminoglycans sulfated trade name. Treatment and prevention of osteoarthritis: drugs of choice (part 2). Chemical properties and classification

Glycosaminoglycans synthesized in the human body have attracted particular interest of scientists. These compounds were obtained artificially and became part of some medicines and dietary supplements, which are currently widely used in medicine. However, the opinion of doctors in the use of such drugs is ambiguous, especially for chondroprotectors - drugs for maintaining and restoring cartilage tissue. Let's consider the topic in detail.

Glycosaminoglycans are natural formations of heteropolysaccharides, which are most often located in the substance between the cells of human tissues and organs. They can be found in human connective tissue and in synovial fluid. Glycosaminoglycans are composed of repeating disaccharide units. Previously, they were called mucopolysaccharides.

These organic compounds tend to bind water molecules quite firmly in a significant amount, so the substance located between the cells can take on a jelly-like appearance.

Glycosaminoglycans are not found in free form, they are obtained by chemical processing from biomass, consisting of cartilage and bone marrow of young animals or fish.

Physico-chemical properties and classification

There are several types of these substances that solve specific problems. Classification of glycosaminoglycans:

  1. Hyaluronic acid.
  2. Keratan sulfates.
  3. Heparin.
  4. Chondroitin sulfates.
  5. Dermatan sulfate.
  6. Heparan sulfate.

Glycosaminoglycans are part of the intercellular substance of the connective tissue and are an essential component of the extracellular matrix. They are able to hold a large number of water molecules, due to which they form viscous solutions in the body. These compounds have a negative charge, which determines their physical and chemical properties such as viscosity and resistance to compression (compression).

Hyaluronic acid is found in large quantities in the human skin, it also acts as a lubricant in the joints.

Keratan sulfates are found in the intervertebral disc, cartilage and bone tissue.

Dermatan sulfate is found in the skin and in the intercellular substance of cartilage. The liver, lungs and vascular wall contain a component such as heparin.

Chondroitin sulfate is found in ligaments, tendons and arteries.

Thanks to these substances, a number of important processes are carried out in the body. Heparin prevents blood clotting and affects the state of the immune system. Proteoglycans are necessary for the repair of cartilage tissue, and they are also responsible for the circulation of water in the synovial fluid. Chondroitin sulfate stimulates the synthesis of proteoglycans and collagen. Chondroitin inhibits the activity of specific enzymes that cause the destruction of cartilage and promotes the deposition of calcium in bone tissue.

Thus, glycosaminoglycans are involved in the following processes in the body:

  1. ion exchange.
  2. immune reactions.
  3. tissue differentiation.
  4. in cell renewal.
  5. in the base function.
  6. In fertilization.

Indications

Glycosaminoglycans are widely used in various branches of medicine: in ophthalmology, cosmetology, rheumatology. Some sulfated glycosaminoglycans are part of chondroprotectors, which are recommended for joint diseases. Chondroprotectors prevent the destruction of cartilage tissue. Indications for the appointment of these drugs are as follows:

  • treatment of arthrosis of any localization, including osteochondrosis;
  • prevention of the development of arthrosis after injuries and operations;
  • with chronic arthritis.

However, numerous clinical studies have shown that chondroprotectors have no effect on cartilage. In a number of patients, a decrease in pain syndrome was observed while taking these drugs. Repeated studies have shown that chondroprotectors do not affect the pain syndrome. Most of the time it's just a placebo effect.

Interesting to know. There are no chondroprotectors in international and Russian standards for the treatment of joints.

In cosmetology, glycosaminoglycans are used to fight wrinkles, tissue regeneration, skin softening, eyelash and hair growth. Subcutaneous injections of hyaluronic acid help produce collagen and elastin, which improves the nutrition and appearance of the skin.

Contraindications

Like any compound introduced into the body from the outside, glycosaminoglycans have their own contraindications. For chondroprotectors, these are:

  1. Individual intolerance.
  2. Severe diseases of the gastrointestinal tract.
  3. Age up to 12 years.
  4. Pregnancy and lactation.
  5. Advanced stages of arthrosis (ankylosis).
  6. Thrombophlebitis.

Contraindications for the use of cosmetics or procedures with glycosamiglycans in cosmetology:

  1. Allergy to components.
  2. Pregnancy and lactation.
  3. Acute infections.
  4. malignant formations.
  5. Tendency to form scars on the skin.
  6. Viral diseases.
  7. Problems with blood clotting.

Overview of popular drugs

« Chondroitin sulfate"is available as a solution in ampoules for intramuscular injection. It is recommended for, helps to restore the cartilaginous surface of the joints, the production of synovial fluid, which improves joint mobility and reduces pain. Preparations that also contain sulfate include Structum, Mukosad, Chondroxide and others.

« Rumalon» in the form of an active substance contains an extract of cartilage and bone marrow of young animals. It enhances the synthesis of sulfated mucopolysaccharides and stimulates the regeneration of articular cartilage. It is prescribed for degenerative changes in the joints, administered intramuscularly according to the scheme.

"" consists of glucosamine sulfate and excipients. Available in sachets for oral administration and in ampoules for intramuscular injections. Glucosamine sulfate inhibits the development of degenerative processes in the joints, restores their function, reducing joint pain, and facilitates the normal deposition of calcium in bone tissue.

« Angioflux"consists of a mixture of glycosaminoglycans - a heparin-like fraction and dermatan sulfate. The drug is administered intravenously drip. The main indications for admission are angiopathy, in which there is a high risk of thrombosis, microangiopathy, which includes nephropathy, retinopathy, neuropathy, and macroangiopathy in diabetes mellitus.

« Hyaluronic acid Evalar"Contains 150 mg of the drug in one capsule. Refers to and is recommended for solving age-related problems associated with a lack of natural moisture in the tissues of the skin, joints, eyes.

Conclusion

Glycosaminoglycans are part of many organs and tissues of the human body and perform a number of important functions. They are used to treat burns, eye diseases and for tissue repair.

In rheumatology, drugs containing mucopolysaccharides still cause a lot of controversy about their effectiveness in affecting the cartilage tissue of the joints. You should not take such drugs on your own without consulting your doctor, who will be able to choose an adequate treatment regimen.

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Glycosaminoglycans are natural formations of heteropolysaccharides, which are most often located in a substance located in the space formed between human tissue cells and its organs. In addition, they can be found in human connective tissue and in synovial fluid.

Glycosaminoglycans are found in relatively small amounts in cartilage and skin.

In its direct combination with elastin and a certain amount of collagen fibers, a fairly strong and stable base is created, which is called the matrix.

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Irina Martynova. Graduated from the Voronezh State Medical University. N.N. Burdenko. Clinical intern and neurologist of BUZ VO \"Moscow Polyclinic\".

Biological significance, role in the human body

Glycosaminoglycans have the ability to quite strongly bind various water molecules in a significant amount, so the substance located between the cells can take on a jelly-like appearance. This group of chemicals can be attributed to the so-called heparin. This substance found in human heart tissue and in the lungs.

Heparin can have a fairly strong effect as an anti-clotting agent and is considered an anticoagulant for its actions.

Structure of matter and types


Glycosaminoglycans are made up of disaccharide units having specific repeats. In any of them, in addition to a certain content of hyaluronic acid, there is a certain residual number of monosaccharides in its direct combination with an O-sulfate or N-sulfate group. In the human body, polysaccharides cannot be formed in a free form, therefore, over time, they bind to the protein in the human body. The total composition of glycosaminoglycans contain a certain amountglucose or a residual amount of galactosamine.

Another important monomer of such a substance located in the human body are acids: D-glucuronic and L-iduronic. Almost all polysaccharides present in the human body have different molecular sizes and differ in their mass and spatial distribution.

They can be attributed to polyelectrolytes, which have a negative self-charge.

Biosynthesis and localization

Glycosaminoglycans are able to form in various tissues of the human body, as well as organs in direct proportion to their specific type.

Chondroitin-6-sulfate is located in the skin of the human body in a fairly significant number.

In the lungs of the human body is an element such as heparin.

Chemical properties and classification

In cartilage, it is possible to detect a relatively small number of different substances. According to their classification, drugs are divided into:

  • Dermatan sulfates.
  • Chondroitin-4-sulfate.
  • Chondoroitin-6-sulfates.
  • Keratan sulfate.
  • Heparins.
  • Heparan sulfates.

Hyaluronic acid

The spectrum of use of this drug divided into several distinct types: non-cosmetological use - pediatric, as well as gerontological.

Drug synonyms:

  • Ostenil.

The modern market of medical preparations offers various forms of release of hyaluronic acid, one of which is injections.

Dermatan sulfates

The drug is considered an antithrombotic agent, as well as a fairly reliable way to prevent thrombosis. It is sufficiently effective in the treatment or prevention of disseminated coagulation syndrome. In some cases, it can be used to treat and prevent a heart attack.

Dermatan sulfate is described as having a characteristic viscosity of about 0.8 per 100 ml/g, or in some cases higher with an Ubbelone viscometer.

The tool is quite successfully used now, because it has high rates of efficiency and reliability in use.

Chondroitin-4-sulfate

This drug takes its direct participation in the appearance of the main substance of the cartilage tissue of the human body. It sufficiently improves calcium metabolism. In addition, the effect of the drug reduces the aging process of the body tissue, and also effectively inhibits various elements in the human body that disrupt the articular cartilage.

Chondoroitin-6-sulfates

This substance is produced by the cartilage tissue of the human body and performs the function of one of the main elements of the synovial fluid. It ensures the work of the joints, while sufficiently preventing the drying process and other negative effects.

When using this drug, these effects are quickly neutralized, which is very effective and reliable.

Keratan sulfate

Heparins

The action begins almost immediately after taking it. It sufficiently activates blood circulation and reduces the effect of certain elements.

Synonyms:

  • Heparin J
  • Heparin Sodium
  • Heparin Akrikhin
  • Heparin Sodium Brown
  • Heparin Ferein
  • Lavenum
  • Lyoton
  • Trombless

Prescribe the drug after a heart attack and thrombosis.


Heparan sulfates

The main action of the presented drug begins almost immediately after its direct entry into the human body. It activates blood circulation, and also reduces the effect of certain elements. Its appointment after a heart attack, because it sufficiently reduces the number of deaths.

The tendons of the human body in their main composition have a fairly high content of dermatan sulfate. Bone contains keratan sulfate. The spinal discs contain relatively small amounts of chondroitin-4-sulfate.

The breakdown of polysaccharides is carried out with the direct participation of hydrolytic elements in this process.

In violation of the metabolism of glycosaminoglycans, which in some possible cases occurs for hereditary reasons, can lead to a significant accumulation of these substances in the human body. This, over a certain period of time, can lead to quite severe and chronic diseases, which are called mucopolysaccharidosis.

Diseases of such pathologies of a hereditary nature are quite complex clinical signs and difficult to treat. With such human diseases, the appearance of:

  1. Problems of mental development.
  2. Various diseases that are associated with cloudy eyes.
  3. Various vascular diseases and pathologies.

Now, the most common in practice are several specific types of mucopolysaccharidosis.

In some possible cases, in order to be able to establish the fastest and most accurate diagnosis, the patient needs to identify an indicator of the action of lysosomal hydrolases. In the presence of various hypovitaminosis in their composition, one can also meet a violation of the metabolism of such substances in the human body. In a person who is completely healthy and has a balanced metabolism, the indicator of glycosaminoglycans in the blood has an approximate value of 50-60 mg per 100 ml. Over a certain period of time and under different circumstances, the total concentration of a given substance in the human body may vary to some extent.

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Glycosaminoglycans are drugs that were previously called mucopolysaccharides. In the body, these substances are covalently bound to proteoglycans and do not occur in free form. In total, today it is customary to distinguish 7 main types, of which 6 are similar in structure. This:

  1. Dermatan sulfate.
  2. Chondroitin-4-sulfate.
  3. Chondoroitin-6-sulfate.
  4. Heparin.
  5. Heparan sulfate.

As for the seventh type, this is keratan sulfate, which is slightly different from the above. In the body, all these substances are part of the connective tissue of the intercellular substance, are found in bone tissue and synovial fluid, as well as in the vitreous body and the cornea of ​​the eye. Genetic pathologies of the breakdown of glycosaminoglycans end in the development of such a hereditary disease as mucopolysaccharidosis.

Artradol

One ampoule of this drug contains 100 mg of chondroitin sulfate sodium. When administered intramuscularly, it is easily absorbed and after 15 minutes it is found in the synovial fluid. The highest concentration is observed one hour after administration, then it gradually decreases over two days.

During the treatment period, the drug is used at 100 mg every other day. The dry matter must first be diluted in 1 ml of water for injection. The full course of treatment is 25-35 injections, after 6 months the course can be repeated.

The main indications for taking the drug are primary arthrosis, osteoarthritis with damage to the largest joints and intervertebral osteochondrosis.

Artron Chondrex

This is a modern tablet preparation based on chondroitin sulfate, and each tablet contains 750 mg of the active substance. It is used in the treatment of various diseases:

  1. Osteopathy.
  2. Periodontopathies.
  3. Osteochondrosis.
  4. Degenerative diseases of cartilage and joints.

One to two tablets should be taken per day. After the desired effect is achieved, the dosage is reduced to a maintenance dose of 750 mg per day.

Angioflux

The active substance of this drug is a natural product, which consists of a mixture of glycosaminoglycans - a heparin-like fraction and dermatan sulfate. The drug is administered intravenously by drip, dissolving the contents of the ampoule in 150-200 ml of saline. The course of parenteral administration is 15-20 systems, after which you should switch to taking capsules.

The main indications for admission are angiopathy, in which there is a high risk of thrombosis, microangiopathy, which includes nephropathy, retinopathy, neuropathy, and macroangiopathy in diabetes mellitus.

Wessel Due F

The drug is produced in capsules and in solution for intramuscular and intravenous administration, and refers to direct-acting anticoagulants. At the beginning of treatment, the drug is administered intravenously, after which they switch to taking capsules. The duration of treatment is 30 - 40 days. The full course is held twice a year. The main indications for use include:

  1. Angiopathy with an increased risk of thrombosis.
  2. Ischemic stroke.
  3. vascular dementia.
  4. Phlebopathy.
  5. Thrombophlebic conditions.
  6. Heparin-induced thrombotic thrombocytopenia.

During the treatment period, constant monitoring of peripheral blood is required, as well as bleeding time and clotting time.

Mukartrin

Mukartrin is a drug that belongs to the stimulators of cartilage tissue regeneration. The drug has good anti-inflammatory activity, has an antithrombotic effect, lowers the level of lipids in the blood, helps to restore damaged connective tissue and cartilage cells.

Before starting treatment with any drug from the group of glycosaminoglycans, you should consult a specialist, as there may be some contraindications, and for all 7 types of these substances they can be very different, since the drugs act differently.

Drugs that also belong to this group include:

  1. Structum.
  2. Chondrogard.
  3. Chondroitin.
  4. Chondroxide.
  5. Rumalon.

What can be associated with a lack of glycosaminoglycans? This may be a consequence of diets or vegetarianism, metabolic disorders that lead to disease, excessive stress on the body and age-related changes. Therefore, in some cases, preparations containing glycosaminoglycans may be prescribed for prophylaxis.

Glycosaminoglycans are used as components for skin rejuvenation. They combine a class of substances, among which there is such a substance known to all beauties as hyaluronic acid.

Mucopolysaccharides help restore epidermal cells, provide structural support to the skin, increase turgor and accelerate hair growth. All substances are originally present in the human body and are natural. Therefore, their use usually does not cause allergic reactions or side effects.

Glycosaminoglycans: classification

Glycosaminoglycans and proteoglycans are found in the intercellular fluid and help in the creation of the connective tissue matrix. These substances are involved in immune metabolism, tissue differentiation and ion exchange.

Proteoglycans are found on the surface of cells and are involved in the immune response, ion exchange, and tissue differentiation. They are high molecular weight compounds that consist of glycosaminoglycans and protein.

Glycosaminoglycans look like repeating chain units that can be sulfated or non-sulfated. The first have a high holding capacity and give the intercellular substance the form of a gel.

Sulfated are divided into:

  • Keratan sulfate;
  • Chondroitin-6 sulfate;
  • Dermatan sulfate;
  • Heparan sulfate;
  • Chondroitin sulfate.

Non-sulfated include hyaluronic acid, which is often used as a means for mesotherapy. Subcutaneously injected preparations help produce collagen and elastin, thereby improving trophism and the appearance of the skin.

In medical practice, drugs that have these substances in their composition are used to treat burns, eye pathologies and to restore tissues. Hyaluronic acid is one of the most popular subcutaneous injection components in this series. It is considered the safest substance in cosmetology.

Glycosaminoglycans: effect on the body

Glycosaminoglycans (mucopolysaccharides) are produced in the human body, so the use of these substances does not cause serious side effects. They enter the skin along with cosmetic or medicinal preparations, after which they form an integral matrix and increase the protective function of the epidermis.

Mucopolysaccharides form a natural barrier that prevents moisture from escaping and bacteria from entering. Thanks to this, the skin becomes smooth and elastic, dryness and irritation disappear.

Entering the body through drugs or injections, these components improve the quality of collagen and contribute to its production. Under their action, hair growth is accelerated, tissues are restored faster and wounds heal.

It is possible to distinguish such an effect of mucopolysaccharides on human skin:

  • Healing;
  • protective;
  • Anti-inflammatory;
  • anti-aging;
  • Moisturizing.

Cosmetic preparations, which contain glycosaminoglycans, return the normal level of hydration to the epidermis and help prevent age-related signs of skin aging. Therefore, in cosmetology, such drugs are used to fight wrinkles, to regenerate tissues, to soften the skin, to grow eyelashes and hair.

Mucopolysaccharides are found in anti-aging cosmetics and repair creams. They can be combined with peptides, antioxidants or vitamins.

These drugs are obtained from natural sources or by synthesis in the laboratory.

Hyaluronic acid

Hyaluronic acid (sodium hyaluronate) is a member of the group of mucopolysaccharides and is used in cosmetic practice as a rejuvenation agent. One of the main useful properties of this substance is its increased viscosity.

Sodium hyaluronate helps bind together bundles of collagen and fibrils to cells. In the body, this substance is located in the intercellular fluid and envelops small vessels. Its main function is to protect tissues from the action of a mechanical factor.

In its action, this substance works like a sponge, because one acid molecule holds 500 water molecules near it.

Action of hyaluronic acid:

  • Antioxidant;
  • Immunostimulating;
  • Firming;
  • Moisturizing.

With age, the content of hyaluronic acid decreases, the skin becomes drier and tissue elasticity is lost. Therefore, it is recommended to introduce this component artificially through injections or cosmetics.

In the cosmetology field, hyaluronic acid obtained by a biosynthetic method is used, and acid of animal origin is also used. Indications for its use are age-related changes in the skin, hypotrophic and atrophic scars.

The substance is injected once a week or a month into the middle layers of the skin, accompanying the procedure with a light massage. Preventive sessions are recommended every 6 months or more often, depending on the condition of the skin. After injections, tissue swelling or redness may occur, which disappears after a couple of days.

Hyaluronic acid is sold in syringes or bottles of different volumes. As a method of skin rejuvenation, injections with hyaluronic acid are most often used. So the drug gets directly deep into the skin to the cells and has a direct effect.

Before starting the procedure, the cosmetologist must determine the presence or absence of contraindications in the patient and select the optimal course of mesotherapy.

Indications for mesotherapy using hyaluronic acid:

  • Mimic wrinkles;
  • Nasolabial folds;
  • Acne rashes;
  • skin pigmentation;
  • Scars, scars.

Contraindications

It is forbidden to use cosmetics or carry out mesotherapy with mucopolysaccharides in the presence of such contraindications:

  • Allergy to components;
  • Pregnancy and lactation;
  • acute infections;
  • Malignant formations;
  • Tendency to form scars on the skin;
  • Viral diseases;
  • Problems with blood clotting.

If the patient has an allergic reaction to egg white, after the introduction of hyaluronic acid, an individual intolerance reaction may occur:

  • Redness of the skin;
  • Runny nose;
  • Edema and others.

With the use of glycosaminoglycans in cosmetic products or through mesotherapy, it is possible to achieve a rejuvenating effect and restore youth and beauty to the skin. The classification of these substances includes sulfated and non-sulfated glycosaminoglycans. The most famous of them is hyaluronic acid, which is widely used in cosmetology for beauty injections. It should be noted that the procedure has many contraindications.

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