Anticoagulants indications for use. Anticoagulants - effectiveness of direct and indirect acting drugs, new generation, indications and contraindications

Anticoagulants are one of the groups of drugs that affect the blood coagulation system, preventing the formation of blood clots in blood vessels. Depending on the mechanism of action, these drugs are usually divided into 2 subgroups: direct and non-direct anticoagulants. direct action. Below we will talk about the first group of anticoagulants - direct action.

Blood coagulation system: basic physiology

Blood coagulation is a set of physiological and biochemical processes aimed at stopping bleeding that began earlier. This defensive reaction body, preventing massive blood loss.

Blood clotting occurs in 2 stages:

  • primary hemostasis;
  • enzymatic coagulation.

Primary hemostasis

In this difficult physiological process 3 structures take part: the vascular wall, the central nervous system and platelets. When the wall of a vessel is damaged and bleeding begins, the smooth muscles located in it around the perforation site contract and the vessels spasm. Nature of this event reflex, that is, it occurs involuntarily, after a corresponding signal from the nervous system.

The next stage is adhesion (sticking) of platelets to the site of injury vascular wall and aggregation (gluing) of them together. Within 2-3 minutes the bleeding stops, since the site of injury is blocked by a blood clot. However, this thrombus is still loose, and the blood plasma at the site of injury is still liquid, so under certain conditions bleeding can develop with new strength. The essence of the next phase of primary hemostasis is that platelets undergo a series of metamorphoses, as a result of which 3 blood coagulation factors are released from them: their interaction leads to the appearance of thrombin and triggers a series of chemical reactions– enzymatic coagulation.

Enzymatic coagulation

When traces of thrombin appear in the area of ​​damage to the vessel wall, a cascade of reactions between tissue coagulation factors and blood clotting factors is triggered, and another factor appears - thromboplastin, which interacts with a special substance prothrombin to form active thrombin. This reaction also occurs with the participation of calcium salts. Thrombin interacts with fibrinogen and fibrin is formed, which is an insoluble substance - its threads precipitate.

The next stage is compression, or retraction, of the blood clot, which is achieved by compacting it, compressing it, as a result of which clear, liquid blood serum is separated.
AND last stage– dissolution, or lysis, of a previously formed thrombus. During this process, many substances interact with each other, and the result is the appearance in the blood of the enzyme fibrinolysin, which destroys fibrin strands and converts it into fibrinogen.
It is worth noting that some of the substances involved in coagulation processes are formed in the liver with the direct participation of vitamin K: a deficiency of this vitamin leads to disturbances in coagulation processes.

Indications and contraindications for the use of direct anticoagulants

Medicines from this group are used in the following situations:

  • to prevent the formation of blood clots or limit their localization in all kinds of surgical interventions ah, in particular, on the heart and blood vessels;
  • in case of progressive and acute;
  • with embolism and peripheral arteries, eyes, pulmonary arteries;
  • with disseminated intravascular coagulation;
  • to prevent blood clotting during a number of laboratory tests;
  • to maintain reduced blood clotting during or in artificial circulation machines.

Each of the direct-acting anticoagulants has its own contraindications for use, mainly:

  • hemorrhagic diathesis;
  • bleeding of any location;
  • increased vascular permeability;
  • subacute bacterial;
  • oncological pathology or ;
  • anemia – hypo- and;
  • acute cardiac aneurysm;
  • pronounced and kidneys;

It is recommended to be careful when prescribing these drugs to very malnourished patients, during pregnancy, in the first 3-8 days after childbirth or surgery, in case of high blood pressure.

Classification of direct anticoagulants

Depending on the characteristics of the structure and mechanism of action, drugs in this group are divided into 3 subgroups:

  • preparations of unfractionated heparin (Heparin);
  • low molecular weight heparin preparations (Nadroparin, Enoxaparin, Dalteparin and others);
  • heparinoids (Sulodexide, Pentosan polysulfate);
  • direct thrombin inhibitors – hirudin preparations.

Unfractionated heparin preparations

The main representative of drugs in this class is Heparin itself.
Antithrombotic effect this drug lies in the ability of its chains to oppress main enzyme blood clotting, thrombin. Heparin binds to the coenzyme antithrombin III, as a result of which the latter more actively binds to a group of plasma coagulation factors, reducing their activity. When heparin is administered in large dosages, it also inhibits the process of converting fibrinogen into fibrin.

In addition to those mentioned above, this substance has a number of other effects:

  • slows down the aggregation and adhesion of platelets, leukocytes and erythrocytes;
  • reduces the degree of vascular permeability;
  • improves blood circulation in adjacent vessels and collaterals;
  • reduces spasm of the vascular wall.

Heparin is produced in the form of a solution for injection (1 ml of solution contains 5000 units of the active substance), as well as in the form of gels and ointments, for local application.

Heparin is administered subcutaneously, intramuscularly and intravenously.

The drug acts quickly, but, unfortunately, for a relatively short time - with a single dose intravenous administration It begins to act almost immediately and the effect lasts for 4-5 hours. When administered into the muscle, the effect develops after half an hour and lasts up to 6 hours, when administered subcutaneously - after 45-60 minutes and up to 8 hours, respectively.

Heparin is often prescribed not alone, but in combination with fibrinolytics and antiplatelet agents.
Dosages are individual and depend on the nature and severity of the disease, as well as on its clinical manifestations and laboratory parameters.

The effect of heparin must be monitored by determining the APTT - activated partial thromboplastin time - at least once every 2 days during the first week of therapy, and then less often - once every 3 days.

Since the administration of this drug may lead to the development hemorrhagic syndrome, it should be administered only in a hospital setting under constant supervision medical personnel.
In addition to hemorrhages, heparin can provoke the development of thrombocytopenia, hyperaldosteronism, hyperkalemia, etc.

Heparin preparations for topical use are Lyoton, Linoven, Thrombophob and others. They are used for prevention, as well as in complex treatment chronic venous insufficiency: prevent formation in saphenous veins lower limbs blood clots, and also reduce, eliminate heaviness in them and reduce the severity of pain.


Low molecular weight heparin preparations

These are new generation drugs that have the properties of heparin, but have a number of advantageous features. By inactivating factor Xa, they reduce the risk of blood clots to a greater extent, while their anticoagulant activity is less pronounced, which means that hemorrhages are less likely to occur. In addition, low molecular weight heparins are absorbed better and last longer, that is, to achieve an effect, a smaller dose of the drug and a smaller frequency of administration are required. In addition, they cause thrombocytopenia only in exceptional cases, rarely.

The main representatives of low molecular weight heparins are Dalteparin, Enoxaparin, Nadroparin, Bemiparin. Let's look at each of them in more detail.

Dalteparin (Fragmin)

Blood clotting is slowed down slightly. Suppresses aggregation and has virtually no effect on adhesion. In addition, it has immunosuppressive and anti-inflammatory properties to a certain extent.

The drug is administered into a vein or subcutaneously. Intramuscular administration is prohibited. It is dosed according to the scheme, depending on the disease and the severity of the patient’s condition. When using dalteparin, a decrease in the level of platelets in the blood, the development of hemorrhages, as well as local and general allergic reactions is possible.
Contraindications are similar to those of other drugs of the direct-acting anticoagulant group (listed above).

Enoxaparin (Clexane, Novoparin, Flenox)

It is quickly and completely absorbed into the blood when administered subcutaneously. The maximum concentration is observed after 3-5 hours. The half-life is more than 2 days. Excreted in urine.

Available in the form of an injection solution. It is usually injected subcutaneously into the area abdominal wall. The administered dose depends on the disease.
Side effects are standard.
This drug should not be used in patients prone to bronchospasm.

Nadroparin (Fraxiparin)

In addition to the direct anticoagulant effect, it also has immunosuppressive and anti-inflammatory properties. In addition, it reduces the level of β-lipoproteins and cholesterol in the blood.
When administered subcutaneously, it is absorbed almost completely, the maximum concentration of the drug in the blood is observed after 4-6 hours, the half-life is 3.5 hours with the initial and 8-10 hours with repeated administration of nadroparin.

As a rule, it is injected into the abdominal tissue: subcutaneously. The frequency of administration is 1-2 times a day. In some cases, intravenous administration is used, under the control of blood coagulation parameters.
Dosages are prescribed depending on the pathology.
Side effects and contraindications are similar to those of other drugs in this group.

Bemiparin (Cibor)

It has a pronounced anticoagulant and moderate hemorrhagic effect.

When administered subcutaneously, the drug is quickly and completely absorbed into the blood, where its maximum concentration is observed after 2-3 hours. The half-life of the drug is 5-6 hours. There is currently no information regarding the withdrawal method.

Release form: solution for injection. Route of administration: subcutaneous.
Dosages and duration of therapy depend on the severity of the disease.
Side effects and contraindications are listed above.

Heparinoids

This is a group of mucopolysaccharides of semi-synthetic origin with the properties of heparin.
Drugs in this class act exclusively on factor Xa, regardless of angiotensin III. They have anticoagulant, fibrinolytic and hypolipidemic effects.

They are usually used to treat patients with angiopathy caused by increased level blood glucose: at . In addition, they are used to prevent thrombus formation during hemodialysis and during surgical operations. They are also used for acute, subacute and chronic diseases atherosclerotic, thrombotic and thromboembolic nature. They enhance the antianginal effect of therapy in patients with angina pectoris (that is, they reduce the severity of pain). The main representatives of this group of drugs are sulodexin and pentosan polysulfate.

Sulodexin (Wessel Due F)

Available in the form of capsules and solution for injection. It is recommended to administer intramuscularly for 2-3 weeks, then take orally for another 30-40 days. The course of treatment is 2 times a year or more often.
While taking the drug, vomiting, pain in the stomach, hematomas at the injection site, and allergic reactions are possible.
Contraindications are common for heparin preparations.

Pentosan Polysulfate

Release form: film-coated tablets and solution for injection.
The route of administration and dosage vary depending on the characteristics of the disease.
When taken orally, it is absorbed in small quantities: its bioavailability is only 10%, in the case of subcutaneous or intramuscular injection bioavailability tends to 100%. The maximum concentration in the blood is observed 1-2 hours after oral administration, the half-life is a day or more.
Otherwise, the drug is similar to other drugs in the anticoagulant group.

Hirudin preparations

Substance secreted salivary glands leeches - hirudin - similar to heparin preparations, has antithrombotic properties. Its mechanism of action is to bind directly to thrombin and irreversibly inhibit it. It also has a partial effect on other blood clotting factors.

Not so long ago, drugs based on hirudin were developed - Piyavit, Revask, Gyrolog, Argatroban, however wide application they didn't get it, so clinical experience on their use to date has not accumulated.

We would like to say separately about two relatively new drugs that have an anticoagulant effect - fondaparinux and rivaroxaban.

Fondaparinux (Arixtra)

Given medicine has an antithrombotic effect by selectively inhibiting factor Xa. Once in the body, fondaparinux binds to antithrombin III and enhances its neutralization of factor Xa several hundred times. As a result of this, the coagulation process is interrupted, thrombin is not formed, and therefore blood clots cannot form.

Quickly and completely absorbed after subcutaneous administration. After a single administration of the drug, its maximum concentration in the blood is observed after 2.5 hours. In the blood it binds to antithrombin II, which determines its effect.

It is excreted primarily in the urine unchanged. The half-life ranges from 17 to 21 hours, depending on the age of the patient.

Available in the form of an injection solution.

Route of administration: subcutaneous or intravenous. It is not used intramuscularly.

The dosage of the drug depends on the type of pathology.

Patients with reduced renal function require dose adjustment of Arixtra depending on creatinine clearance.

In patients with a pronounced decrease in liver function, the drug is used very carefully.
Should not be used concomitantly with drugs that increase the risk.

Rivaroxaban (Xarelto)

This is a drug that has a highly selective action against factor Xa, inhibiting its activity. It is characterized by high bioavailability (80-100%) when taken orally (that is, it is well absorbed into gastrointestinal tract when taken orally).

The maximum concentration of rivaroxaban in the blood is observed 2-4 hours after a single oral dose.

Excreted from the body half in urine, half in feces. The half-life ranges from 5-9 to 11-13 hours, depending on the age of the patient.

Release form: tablets.
Take orally, regardless of food intake. As with other direct-acting anticoagulants, the dosage of the drug varies depending on the type of disease and its severity.

Rivaroxaban is not recommended for patients receiving treatment with certain antifungal drugs or anti-inflammatory drugs, since they can increase the concentration of Xarelto in the blood, which can cause bleeding.

Patients with severe renal impairment require dose adjustment of rivaroxaban.
Women reproductive age Pregnancy should be reliably protected during treatment with this drug.

As you can see, the modern pharmacological industry offers a significant selection of direct-acting anticoagulant drugs. In no case, of course, should you self-medicate; all medications, their dosage and duration of use are determined only by the doctor, based on the severity of the disease, the patient’s age and other significant factors.

These are antithrombotic drugs and substances that prevent blockages from forming in the bloodstream. They provide the blood with an optimal liquid state, fluidity, subject to the integrity of the blood vessels. These substances are divided into several groups according to the formation factor: inside the body or synthetic medications. The latter are used by doctors as medicines.

Anticoagulants - what are they? These substances are divided into pathological and physiological. The latter are present in plasma normally, while the former are detected when a person has the disease. Natural or natural anticoagulants are divided into primary, which are produced by the body independently, they enter the blood, and secondary, which are formed during the breakdown of coagulation factors due to the process of formation and dissolution of fibrin.

Primary natural anticoagulants

It is described above what anticoagulants are and now you should understand their types and groups. As a rule, natural primary anticoagulants are divided into:

  • antithrombins;
  • antithromboplastins;
  • inhibitors of the fibrin self-assembly process.

If a person experiences a decrease in the level of these anticoagulants, there is a possibility of developing thrombosis. This group includes:

  1. Heparin. It is synthesized in mast cells and belongs to the class of polysaccharides. It is found in large quantities in the liver and lungs. With the growth of this substance, blood clotting decreases at all stages, which occurs due to the suppression of a number of platelet functions.
  2. Protein C. Produced by liver parenchyma cells, it is in the blood in an inactive state. Activity is driven by thrombin.
  3. Antithrombin III. Belongs to alpha2-glycoproteins, synthesized in the liver. Able to reduce the activity of some activated blood clotting factors and thrombin, but does not affect non-activated ones.
  4. Protein S. Synthesized by the liver parenchyma and endothelial cells, depends on vitamin K.
  5. Contact, lipid inhibitor.
  6. Antithromboplastins.

Secondary physiological anticoagulants

These substances are formed during the blood clotting process. They also appear during the dissolution of fibrin clots and the breakdown of coagulation factors, which lose their coagulation properties and acquire anticoagulant properties. What applies to anticoagulants of this type:

  • Febrinopuptids;
  • Antithrombin I, IX;
  • Antithromboplastins;
  • Metafactors XIa, Va;
  • PDF products.

Pathological anticoagulants

With the development of certain diseases, powerful immune inhibitors of blood clotting, which are specific antibodies, for example, lupus anticoagulant, sometimes accumulate in the plasma. They indicate one factor or another. These antibodies can be produced to combat any manifestation of blood clotting, but according to statistics, as a rule, these are inhibitors of factors VII, IX. Sometimes, with paraproteinemia and a number of autoimmune processes, pathological proteins that have an inhibitory or antithrombin effect can accumulate in the plasma.

Anticoagulant drugs

These are medications that affect the blood clotting function and are used to reduce the likelihood of a blood clot forming in the body. Due to blockage in blood vessels or organs, the following may develop:

  • ischemic stroke;
  • gangrene of the limbs;
  • thrombophlebitis;
  • inflammation of blood vessels;
  • cardiac ischemia;
  • atherosclerosis.

Direct and indirect anticoagulants are distinguished according to the mechanism of action, which help control blood clotting processes. They are often used to treat varicose veins, therapy autoimmune diseases. Anticoagulants have certain pharmacological properties and rules of admission, therefore they can only be prescribed by a doctor who is familiar with the patient’s medical history.

Direct anticoagulants

Therapy with these medications is aimed at inhibiting the formation of thrombin. Direct anticoagulants slow down the work of hyaluronidase, while the permeability of blood vessels in the brain and kidneys increases. Under the influence of drugs, the level of cholesterol and beta-lipoproteins decreases. There is an increase in lipoprotein lipase, and the interaction of T and B lymphocytes is suppressed.

Almost all direct anticoagulants are tested to determine their effectiveness in preventing internal bleeding. The most popular of the list of these medications is Heparin. Its effectiveness has been proven, but the formation of blood clots cannot be completely eliminated. This applies to blockages that have formed on an atherosclerotic plaque; the drug does not affect them. The medicine has a quick effect, but it lasts up to 5 hours after the end of administration. In addition to it, the following may be prescribed for use:

  • Hirudin;
  • Lepirudin;
  • Danaproid.

Indirect anticoagulants

The discovery of this medicine occurred due to events that are not directly related to medicine. In America at the beginning of the 20th century, large quantity cows started profuse bleeding. It was possible to find out that the cause was clover with mold, which was present in the feed. The first indirect anticoagulants were obtained from these raw materials. The medicine was then named Dicumarol. Since the middle of the last century, this medicine has been used to treat heart attacks.

The action of this group of anticoagulants is based on the inhibition of vitamin K. They interfere with the activation of proteins dependent on of this vitamin factors. The classification of drugs includes two main groups:

  1. Medicines based on Coumarin derivatives.
  2. Medicines derived from Indandione.

The latter have proven themselves poorly in clinical trials because the results are unstable and there is a risk allergic reaction. Therefore, coumarin-like drugs have become the most the best option. The most famous coumarin drug is Warfarin. Highlight the following readings for its use:

  • atrial fibrillation;
  • prevention of thromboembolism;
  • mechanical heart valve replacement;
  • acute venous thrombosis.

It is important to understand that the effects of anticoagulants can seriously affect a person's health. Taking them can lead to hemorrhagic complications. Medicines should be used only under the strict supervision of the attending physician, who can calculate exact dosage anticoagulants. If there is a risk of bleeding, then antiplatelet agents, which are safer for humans, should be used instead of these medications.

New generation oral anticoagulants

Drugs that thin the blood and prevent blood clots have become an indispensable tool to prevent ischemia, arrhythmia, heart attack, thrombosis, etc. Many effective medications have a number of unpleasant side effects, so developers continue to improve this group of medications. New oral anticoagulants should become universal remedy, which will be allowed for use by children during pregnancy. Modern drugs have the following positive aspects:

  • they are allowed for people for whom Warfarin is contraindicated;
  • reduced risk of bleeding;
  • thin the blood 2 hours after administration, but the effect ends quickly;
  • the influence of food consumed and other means is reduced;
  • inhibition is reversible.

Experts are constantly working to improve the next generation of blood thinning drugs, but they still have a number of negative properties, which include:

  • taking old options could be skipped, but new ones require strictly regular use;
  • there is a risk of bleeding in the gastrointestinal tract;
  • to prescribe a remedy, it is necessary to carry out many tests;
  • Some patients who had no problems with the old medications experience intolerance to the new anticoagulants.

Price for anticoagulants

The anticoagulant agent has strong action, which without medical control can lead to excessive internal bleeding. Therefore, you cannot buy this product in an online store. The exception is electronic representative offices of pharmacies. Medicines that thin the blood and prevent blood clots have different prices. The medicine catalog offers a wide range of derivatives. Below is a list of popular medications that can be ordered inexpensively:

  • Warfarin, 100 tablets – price from 100 rubles;
  • Curantil – price from 345 rubles;
  • Detralex – price from 640 rubles;
  • Antithrombin, capsules 75 mg – price from 225 rub.

Video: what are anticoagulant drugs

Anticoagulants - what they are and a list of drugs. The use of direct and indirect anticoagulants - all about medications and health on the site

  • heparinoids – traxiparin, enoxyparin

  • hirudinoids

  • complexone preparations (bind Ca) – Trilon-B (EDTA) and citrate-Na

indirect anticoagulants:

coumarin derivatives – neodicoumarin, syncumar, warfarin, fepromarone

indanedione derivatives – phenyline

  1. Fibrinolytics

    fibrinolysin

    streptokinase

    urokinase

Antiplatelet agents

  • aspirin (in small doses)

    trental (pentoxifylline)

  • clopidogrel (Plavix)

Mechanism of action of heparin:

Heparin is an acidic mucopolysaccharide containing a large amount of sulfuric acid residues with a negative charge. Acts on positively charged blood clotting factors.

Heparin

Pharmacological group: Direct acting anticoagulants.

Mechanism of action: antithrombotic effect, which is associated with its direct effect on the blood coagulation system. 1) Due to the negative charge, it blocks phase I; 2) By binding to antithrombin III in the blood plasma and changing the conformation of its molecule, heparin contributes to a significant acceleration of the binding of antithrombin III to the active centers of the factors of the blood coagulation system => inhibition of thrombus formation - disruption of the P phase;

3) disturbance of fibrin formation - III phase; 4) increases fibrinolysis.

Effects: reduces platelet aggregation, increases vascular permeability, stimulates collateral circulation, has an antispasmodic effect (adrenaline antagonist), reduces cholesterol and triglycerides in the blood serum.

Application: at acute heart attack myocardium, thrombosis and embolism of main veins and arteries, cerebral vessels, to maintain a hypocoagulable state of blood in artificial circulation machines and hemodialysis equipment. Side effects: hemorrhages, allergic reactions, thrombocytopenia, osteoporosis, alopecia, hypoaldosteronism.

Contraindicated in hemorrhagic diathesis, with increased vascular permeability, bleeding, subacute bacterial endocarditis, severe dysfunction of the liver and kidneys, acute and chronic. Leukemia, aplastic and hypoplastic anemia, venous gangrene.

Heparin antagonists include protamine sulfate, ubiquin, and tolluidin blue.

Antagonist of indirect anticoagulants: vitamin K (vicasol)

3. A patient with pneumonia with a body temperature of 37.8 started a course of antibiotic therapy. After 2 X injections, the patient’s condition improved, but then the fever intensified, body temperature reached 39 . The doctor did not cancel the antibiotic, but prescribed plenty of fluids, a diuretic, vitamin C, and prednisolone. The patient's condition improved. What antibiotic could the patient be treated with (only one answer is correct)?

Having a bactericidal effect

 mass death of bacteria with the release of endotoxins (pyrogens) heat

drinking plenty of fluids + diuretic  forced diuresis with the release of pyrogens from the body

vitamin C  - strengthening redox processes

- adaptability and resistance to infection has an antitoxic effect due to stimulation of the production of corticosteroids

    membrane permeabilityanti-inflammatory effect

prednisolone antitoxic effect:

    membrane stabilizing effect

     activity of liver enzymes involved in the destruction of endo- and exogenous substances

anti-inflammatory effect

    Disrupting bacterial cell wall synthesis:

    -lactam antibiotics:

    penicillins

    cephalosporins

    monobactams

    carbopenems

    vancomycin, ristomycin

    Permeability-impairing CPMs:

    aminoglycosides

    Anticoagulants are a group of drugs that suppress activity and prevent thrombus formation due to reduced fibrin formation. They affect biosynthesis certain substances in the body, changing and inhibiting clotting processes.

    Anticoagulants are used for therapeutic and prophylactic purposes. They are produced in various dosage forms: in the form of tablets, injections or ointments. Only a specialist can choose the right medicine and its dosage. Inadequate therapy can harm the body and cause serious consequences.

    High mortality from cardiovascular diseases is caused by the formation: in almost every second person who died from cardiac pathology, vascular thrombosis was discovered at autopsy. and venous thrombosis are the most common causes of death and disability. In this regard, cardiologists recommend starting to use anticoagulants immediately after diagnosing heart and vascular diseases. Their early use helps prevent the formation of a blood clot, its enlargement and clogging of blood vessels.

    Since ancient times in folk medicine used hirudin- the most famous natural anticoagulant. This substance is part of the saliva of leeches and has a direct anticoagulant effect that lasts for two hours. Currently, patients are prescribed synthetic drugs, not natural. More than a hundred names of anticoagulant drugs are known, which allows you to choose the most suitable one, taking into account individual characteristics body and the possibility of their combined use with other medications.

    Most anticoagulants do not affect the blood clot itself, but rather the activity of the blood coagulation system. As a result of a number of transformations, they are suppressed plasma factors blood clotting and the production of thrombin, an enzyme necessary for the formation of fibrin threads that make up a thrombotic clot. The thrombus formation process slows down.

    Mechanism of action

    Anticoagulants according to their mechanism of action are divided into drugs of direct and indirect action:


    Separately, there are drugs that suppress blood clotting, like anticoagulants, but by different mechanisms. These include " Acetylsalicylic acid", "Aspirin".

    Direct anticoagulants

    Heparin

    The most popular representative of this group is heparin and its derivatives. Heparin inhibits platelet aggregation and speeds up blood flow in the heart and kidneys. At the same time, it interacts with macrophages and plasma proteins, which does not exclude the possibility of thrombosis. The drug reduces blood pressure, has a hypocholesterolemic effect, increases vascular permeability, suppresses the proliferation of smooth muscle cells, promotes the development of osteoporosis, suppresses the immune system and increases diuresis. Heparin was first isolated from the liver, which determined its name.

    Heparin is administered intravenously in emergency cases and subcutaneously for prophylactic purposes. For local use, ointments and gels are used that contain heparin and have an antithrombotic and anti-inflammatory effect. Heparin preparations are applied thin layer onto the skin and rub in with gentle movements. Typically, the gels “Lioton” and “Hepatrombin”, as well as “Heparin ointment” are used for treatment.

    The negative effect of heparin on the process of thrombus formation and increased vascular permeability become the causes high risk bleeding during heparin therapy.

    Low molecular weight heparins

    Low molecular weight heparins have high bioavailability and antithrombotic activity, prolonged action, and a low risk of developing hemorrhoidal complications. Biological properties These drugs are more stable. Thanks to rapid absorption and long period excretion, the concentration of drugs in the blood remains stable. Medicines in this group inhibit blood coagulation factors, suppress thrombin synthesis, have a weak effect on vascular permeability, and improve rheological properties blood and blood supply to organs and tissues, stabilizing their functions.

    Low molecular weight heparins rarely cause side effects, which is why they are replacing heparin from therapeutic practice. They are injected subcutaneously into the lateral surface of the abdominal wall.

    When using drugs from the group of low molecular weight heparins, you must strictly follow the recommendations and instructions for their use.

    Thrombin inhibitors

    The main representative of this group is “Girudin”. The drug is based on a protein first discovered in saliva medical leeches. These are anticoagulants that act directly in the blood and are direct thrombin inhibitors.

    "Girugen" and "Ghirulog" are synthetic analogues of Hirudin, which reduce the mortality rate among people with heart pathology. These are new drugs in this group that have a number of advantages compared to heparin derivatives. Due to their prolonged action, the pharmaceutical industry is currently developing oral forms of thrombin inhibitors. Practical use"Girugena" and "Giruloga" are limited by their high cost.

    "Lepirudin"– a recombinant drug that irreversibly binds thrombin and is used for the prevention of thrombosis and thromboembolism. This is a direct thrombin inhibitor, blocking its thrombogenic activity and acting on thrombin located in the clot. It reduces mortality from and the need for heart surgery in patients with.

    Indirect anticoagulants

    Indirect anticoagulant drugs:

    • "Fenilin"– an anticoagulant that is quickly and fully absorbed, easily penetrates the histohematic barrier and accumulates in the tissues of the body. This medicine, according to patients, is considered one of the most effective. It improves blood condition and normalizes blood clotting parameters. After treatment, the general condition of patients quickly improves: cramps and numbness of the legs disappear. Currently, Phenilin is not used due to the high risk of undesirable effects.
    • "Neodicoumarin"- This is a drug that inhibits the process of thrombus formation. Therapeutic effect“Neodicoumarin” does not appear immediately, but after the accumulation of the drug in the body. It suppresses the activity of the blood coagulation system, has a hypolipidemic effect and increases vascular permeability. Patients are advised to strictly adhere to the time of administration and dose of the drug.
    • The most common drug in this group is Warfarin. This is an anticoagulant agent that blocks the synthesis of blood clotting factors in the liver, reducing their concentration in plasma and slowing down the process of thrombus formation. Warfarin has an early effect and rapid cessation undesirable consequences when reducing the dose or discontinuing the drug.

    Video: new anticoagulants and “Warfarin”

    Use of anticoagulants

    Taking anticoagulants is indicated for diseases of the heart and blood vessels:

    Uncontrolled use of anticoagulants can lead to the development of hemorrhagic complications. At increased risk If bleeding occurs, safer antiplatelet agents should be used instead of anticoagulants.

    Contraindications and side effects

    Anticoagulants are contraindicated for persons suffering from the following diseases:

    Anticoagulants should not be taken during pregnancy, lactation, menstruation, or early postpartum period, as well as elderly and elderly people.

    TO side effects anticoagulants include: symptoms of dyspepsia and intoxication, allergies, necrosis, rash, skin itching, kidney dysfunction, osteoporosis, alopecia.

    Complications of anticoagulant therapy - hemorrhagic reactions in the form of bleeding from internal organs: mouth, nasopharynx, stomach, intestines, as well as hemorrhages in muscles and joints, the appearance of blood in the urine. To prevent the development of hazardous health consequences, you should monitor basic blood counts and monitor general condition sick.

    Antiplatelet agents

    This pharmacological agents, by inhibiting platelet aggregation. Their main purpose is to enhance the effectiveness of anticoagulants and, together with them, prevent the process of thrombus formation. Antiplatelet agents also have antigout, vasodilator and antispasmodic effects. A prominent representative of this group is “Acetylsalicylic acid” or “Aspirin”.

    List of the most popular antiplatelet agents:

    • "Aspirin" is the most effective antiplatelet agent available today, produced in the form of tablets and intended for oral use. It inhibits platelet aggregation, causes vasodilation and prevents the formation of blood clots.
    • "Ticlopidine"– an antiplatelet agent that inhibits platelet adhesion, improves microcirculation and prolongs bleeding time. The drug is prescribed for the prevention of thrombosis and for treatment of ischemic heart disease, heart attack and cerebrovascular disease.
    • "Tirofiban"– a medicine that prevents platelet aggregation, leading to blood clots. The drug is usually used together with Heparin.
    • "Dipyridamole" expands coronary vessels, accelerates coronary blood flow, improves oxygen supply to the myocardium, rheological properties of blood and cerebral circulation, lowers blood pressure.

    Video: about drugs used in anticoagulant therapy

    IN drug therapy Anticoagulants are used to prevent blood clotting. For diseases directly or indirectly related to thrombus formation, they can be considered vital. The list of anticoagulant drugs includes direct and indirect drugs.

    Prescribed for treatment:

    • Acute venous and arterial thrombosis.
    • Pathologies associated with the release of large amounts of thromboplastic substances from tissues.
    • After previous operations to prevent the formation of blood clots.
    • As preventive measures in the presence of heart disease.

    What drugs are classified as anticoagulants? These medications have blood thinning properties and are also called anticoagulants. They are divided into two groups: direct and indirect action.

    List of direct anticoagulant drugs

    This group includes antithrombolic medications that reduce the clotting factor (thrombin) in the blood.

    1. Heparins for topical use (externally).

    These drugs related to anticoagulants are prescribed for internal inflammation veins with the formation of a blood clot in their cavity.

    Stop inflammatory process. Reduce platelet aggregate formation and thrombin activity. Relieves swelling. Activate tissue respiration. They help dissolve blood clots and gradually restore the lumen of the veins. Reduces painful sensations.

    The list includes direct anticoagulant drugs Russian production:

    1. Heparin ointment 25 g - 50 rubles.
    2. Heparin-Akrikhin 1000 gel 30 g - 224 rub.
    3. Trombless gel 30 g - 249 rub.
    4. Venolife 40 grams - 330 rub.
    5. Laventum 50 g - 290 rubles.

    For subcutaneous and intravenous administration

    Anticoagulant drugsare used in the treatment of deep vein thrombosis, pulmonary artery thrombolism, and angina pectoris. They are thrombin blockers. Prevents the formation of non-globular fibrin protein and platelet aggregation.

    As therapeutic therapy the doctor prescribes:

    1. Clexane (France). Main active ingredient enoxaparin sodium prevents blockage by a blood clot blood vessels and the formation of blood clots.

    • Syringes 0.2 ml 10 pcs. - 1700 rubles.

    2. Fraxiparine (France). Active substance nadroparin calcium has high factor Xa activity. Used to thin the blood when there is a risk of thrombosis.

    • Syringes 2850 ME 0.3 ml 10 pcs. - 2150 rub.

    3. Fragmin (USA). Prescribed to patients undergoing hemodialysis or hemofiltration. Effective drug blood anticoagulant. Active substance solution alteparin sodium has an anticoagulant effect. Reduces the rate of chemical reactions of blood clotting factor and thrombin.

    • Solution 2500 anti-Xa ME/0.2 ml 10 pcs. - 2100 rubles.

    Indirect anticoagulant drugs

    The active substances of medications included in this group disrupt the synthesis of prothrombin in the liver and slow down the blood clotting process. Prothrombin is a precursor to the enzyme thrombin. Refers to complex blood plasma proteins. Participates in blood clotting with the participation of vitamin K.

    List of anticoagulant drugs in tablets

    1. Warfarin (Russia). The most popular drug on the list indirect anticoagulants for the treatment of thrombosis of the venous system. Reduces the likelihood of thromboembolic complications.

    If you follow a diet, constantly monitor your blood for INR and dosage, therapy leads to positive results. Affordable price another significant advantage of the medication.

    • Tab. 2.5 mg 50 pcs. - 86 rubles.

    2. Fenilin (Russia). Another indirect drug anticoagulant effective remedy in tablet form. Active substance phenindione has anticoagulant properties.

    Prescribed for blockage of the walls of veins, vessels of the lower extremities and brain. It is used as a preventive measure after surgical interventions.

    • Packaging tab. 20 mg 30 pcs. - 120 rub.

    3. Sinkumar (Russia). The drug is included in the list of coumarin anticoagulant drugs. Prevents the synthesis of vitamin K in its active form, as a result of which the coagulation process is disrupted (formation blood clots). Suppresses the synthesis of blood clotting factors.

    • Packaging tab. 2 mg 50 pcs. - 470 rub.

    New generation anticoagulants

    A feature of the drugs is the ability not to constantly monitor the blood clotting index (INR). Judging by this property, the new drugs are superior to Warfarin in ease of use. However, the high price of drugs limits their availability, which is a significant drawback.

    The list of new generation anticoagulant drugs includes:

    1. Xarelto (Germany). Active component medicine is rivaroxaban. Clinical researches proved high efficiency this tool. Easy to use. Does not tie patients to constant testing.

    • Cost of 15 mg tablet 28 pcs. - 2700 rub.

    2. Eliquis (USA). Basics active substance apixaban restores vein patency. Used for the prevention of cardioembolic stroke. Does not require systematic monitoring of hemostasis.

    • Price of tablets 5 mg 60 pieces - 2400 rub.

    3. Pradaxa (Austria). The main component of the medicine dabigatran etexilate. Prescribed for venous and systemic thromboembolism, including lesions pulmonary artery after severe injuries and complex operations.

    Well tolerated. During drug therapy, practitioners note a low risk of bleeding.

    • Capsules 110 mg 30 pcs. - 1750 rubles.