Direct anticoagulants drugs of a new generation. What are anticoagulants, which of them are referred to as drugs of direct and indirect action. New generation oral anticoagulants

Various vascular diseases lead to the formation of blood clots. This leads to very dangerous consequences, as, for example, a heart attack or stroke can occur. To thin the blood, the doctor may prescribe drugs that help reduce blood clotting. They are called anticoagulants and are used to prevent blood clots from forming in the body. They help block the formation of fibrin. Most often they are used in situations where blood clotting is increased in the body.

It can occur due to problems such as:

• Varicose veins or phlebitis;
• thrombi of the inferior vena cava;
• Thrombi in hemorrhoidal veins;
• Stroke;
• myocardial infarction;
• Arterial injury in the presence of atherosclerosis;
• Thromboembolism;
• Shock, trauma, or sepsis can also lead to blood clots.

To improve the state of blood clotting, anticoagulants are used. If earlier they used Aspirin, now doctors have abandoned this technique, because there are much more effective drugs.

What are anticoagulants, farm. Effect

Anticoagulants- these are blood thinning drugs, in addition, they reduce the risk of other thrombosis that may appear in the future. Distinguish anticoagulants of direct and indirect action.

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Direct and indirect anticoagulants

There are direct and indirect anticoagulants. The former quickly thin the blood and are excreted from the body within a few hours. The latter accumulate gradually, providing a therapeutic effect in a prolonged form.

Since these drugs reduce blood clotting, you can not lower or increase the dosage on your own, as well as reduce the time of admission. Medicines are used according to the scheme prescribed by the doctor.

Direct acting anticoagulants

Direct acting anticoagulants reduce thrombin synthesis. In addition, they inhibit the formation of fibrin. Anticoagulants are aimed at the work of the liver and inhibit the formation of blood clotting.

Direct anticoagulants are well known to everyone. These are local heparins and for subcutaneous or intravenous administration. In another article you will find even more information about.

For example, local action:

These drugs are used for thrombosis of the veins of the lower extremities for the treatment and prevention of the disease.

They have a higher degree of penetration, but have less effect than intravenous agents.

Heparins for administration:

• Fraxiparine;
• Clexane;
• Fragmin;
• Clivarin.

Typically, anticoagulants are selected to solve specific problems. For example, Klivarin and Troparin are used to prevent embolism and thrombosis. Clexane and Fragmin - for angina pectoris, heart attack, vein thrombosis and other problems.

Fragmin is used in hemodialysis. Anticoagulants are used at the risk of blood clots in any vessels, both in the arteries and in the veins. The activity of the drug persists for a whole day.

Indirect anticoagulants

Indirect anticoagulants are so named because they affect the creation of prothrombin in the liver, and do not directly affect clotting itself. This process is long, but the effect due to this is prolonged.

They are divided into 3 groups:

• Monocoumarins. These include: Warfarin, Sinkumar, Mrakumar;
• Dicoumarins are Dicoumarin and Tromexane;
• Indandiones are Phenylin, Omefin, Dipaksin.

Most often, doctors prescribe warfarin. These drugs are prescribed in two cases: with atrial fibrillation and artificial heart valves.

Often patients ask what is the difference between Aspirin cardio and Warfarin, and is it possible to replace one drug with another?

Experts answer that Aspirin cardio is prescribed if the risk of stroke is not high.

Warfarin is much more effective than Aspirin and is best taken for several months, if not for life.

Aspirin corrodes the stomach lining and is more toxic to the liver.

Indirect anticoagulants reduce the production of substances that affect clotting, they also reduce the production of prothrombin in the liver and are vitamin K antagonists.

Indirect anticoagulants include vitamin K antagonists:

• Sincumar;
• Warfarex;
• Fenilin.

Vitamin K is involved in the process of blood clotting, and under the influence of Warfarin, its functions are impaired. It helps to prevent the separation of blood clots and blockage of blood vessels. This drug is often prescribed after a myocardial infarction.

It is necessary to carefully consider taking this drug, as it has a lot of contraindications to food products that cannot be consumed simultaneously with these drugs.

There are direct and selective thrombin inhibitors:

Direct:

• Angioks and Pradaksa;

Selective:

• Eliquis and.

Any anticoagulants of direct and indirect action are prescribed only by a doctor, otherwise there is a high risk of bleeding. Anticoagulants of indirect action accumulate in the body gradually.

Apply them only inside orally. It is impossible to stop treatment immediately, it is necessary to gradually reduce the dose of the drug. Abrupt withdrawal of the drug can cause thrombosis. An overdose of this group may cause bleeding.

The use of anticoagulants

The clinical use of anticoagulants is recommended for the following conditions:

• Pulmonary and myocardial infarction;
• Stroke embolic and thrombotic (except hemorrhagic);
• Phlebothrombosis and thrombophlebitis;
• Embolism of vessels of various internal organs.

As a preventive measure, you can use it for:

• Atherosclerosis of the coronary arteries, cerebral vessels and peripheral arteries;
• Heart defects rheumatic mitral;
• Phlebothrombosis;
• Postoperative period to prevent the formation of blood clots.

Natural anticoagulants

Thanks to the process of blood clotting, the body itself made sure that the clot does not go beyond the affected vessel. One milliliter of blood can help clotting all the fibrinogen in the body.

Due to its movement, the blood maintains a liquid state, as well as due to natural coagulants. Natural coagulants are produced in the tissues and then enter the bloodstream, where they prevent the activation of blood clotting.

These anticoagulants include:

• Heparin;
• Antithrombin III;
• Alpha-2 macroglobulin.

Anticoagulant drugs - list

Direct-acting anticoagulants are absorbed quickly and their duration of action is not more than a day before re-introduction or application.

Anticoagulants
indirect action accumulate in the blood, creating a cumulative effect.

They should not be canceled immediately, as this may contribute to thrombosis. When taking them, gradually reduce the dosage.

Direct local anticoagulants:

• Lyoton gel;
• Hepatrombin;
• Trombless

Anticoagulants for intravenous or intradermal administration:

• Fraxiparine;
• Clexane;
• Fragmin;
• Clivarin.

Indirect anticoagulants:

• Girugen;
• Girulog;
• Argatroban;
• Warfarin Nycomed in tab.;
• Fenilin in tab.

Contraindications

There are quite a few contraindications to the use of anticoagulants, so be sure to check with your doctor about the appropriateness of taking the funds.

Cannot be used when:

• peptic ulcer;
• Parenchymal diseases of the liver and kidneys;
• Septic endocarditis;
• Increased vascular permeability;
• With increased pressure in myocardial infarction;
• oncological diseases;
• Leukemia;
• Acute aneurysm of the heart;
• Allergic diseases;
• Diathesis hemorrhagic;
• Fibromyomas;
• Pregnancy.

With caution during menstruation in women. Not recommended for nursing mothers.

Side effects

With an overdose of drugs of indirect action, bleeding may begin.

At
co-administration of Warfarin with aspirin or other non-steroidal anti-inflammatory drugs (Simvastin, Heparin, etc.) enhances the anticoagulant effect.

And vitamin K, laxatives or Paracetamol will weaken the effect of Warfarin.

Side effects when taking:

• Allergy;
• temperature, headache;
• Weakness;
• skin necrosis;
• Violation of the kidneys;
• Nausea, diarrhea, vomiting;
• Itching, abdominal pain;
• Baldness.

Before you start taking anticoagulants, you should consult a specialist for contraindications and side effects.

To avoid the occurrence of blood clots, like dangerous blood clots, there is a pharmacological group called anticoagulants in the classification of drugs - a list of drugs is presented in any medical reference book. Such medicines provide control of blood viscosity, prevent a number of pathological processes, and successfully treat certain diseases of the hematopoietic system. For recovery to be final, the first step is to identify and remove clotting factors.

What are anticoagulants

These are representatives of a separate pharmacological group, produced in the form of tablets and injections, which are designed to reduce blood viscosity, prevent thrombosis, prevent stroke, and in the complex therapy of myocardial infarction. Such medications not only effectively reduce the coagulability of the systemic blood flow, but also maintain the elasticity of the vascular walls. With increased platelet activity, anticoagulants block the formation of fibrin, which is appropriate for the successful treatment of thrombosis.

Indications for use

Anticoagulants are used not only for the successful prevention of thromboembolism, such an appointment is suitable for increased thrombin activity and the potential threat of the formation of blood clots dangerous for the systemic blood flow in the vascular walls. The concentration of platelets gradually decreases, the blood acquires an acceptable flow rate, the disease recedes. The list of drugs approved for use is extensive, and specialists prescribe them for:

• atherosclerosis;
• liver diseases;
• vein thrombosis;
• vascular diseases;
• thrombosis of the inferior vena cava;
• thromboembolism;
• blood clots of hemorrhoidal veins;
• phlebitis;
• injuries of various etiologies;
• varicose veins.

Classification

The benefits of natural anticoagulants are obvious, which are synthesized by the body and prevail in sufficient concentration to control blood viscosity. However, natural clotting inhibitors can be susceptible to a number of pathological processes, so there is a need to introduce synthetic anticoagulants into the complex treatment regimen. Before determining the list of drugs, the patient needs to contact the attending physician, to exclude potential health complications.

Direct acting anticoagulants

The list of such drugs is designed to suppress thrombin activity, reduce fibrin synthesis, and normal liver function. These are local heparins of subcutaneous or intravenous administration, necessary for the treatment of varicose veins of the lower extremities. The active components are efficiently absorbed into the systemic circulation, act throughout the day, and are more effective when administered subcutaneously than orally. Among low molecular weight heparins, doctors distinguish the following list of drugs intended for the administration of heparins locally, intravenously or orally:

• Fraxiparine;
• Lyoton-gel;
• Clexane;
• Fragmin;
• Hepatrombin;
• Sodium hydrocitrate (heparin administered intravenously);
• Clivarin.

Indirect anticoagulants

These are long-acting drugs that act directly on blood clotting. Anticoagulants of indirect action contribute to the formation of prothrombin in the liver, contain vitamins valuable for the body in the chemical composition. For example, Warfarin is prescribed for atrial fibrillation and artificial heart valves, while the recommended doses of Aspirin are less productive in practice. The list of drugs is represented by the following classification of the coumarin series:

• monocoumarins: Warfarin, Sincumar, Mrakumar;
• indandiones: Phenylin, Omefin, Dipaksin;
• Dicoumarins: Dicoumarin, Tromexane.

To quickly normalize blood clotting and prevent vascular thrombosis after a myocardial infarction or stroke, doctors strongly recommend oral anticoagulants containing vitamin K in the chemical composition. Prescribe this kind of medication for other pathologies of the cardiovascular system, prone to chronic course, relapses. In the absence of extensive kidney disease, the following list of oral anticoagulants should be highlighted:

• Sincumar;
• Warfarex;
• Acenocoumarol;
• neodicumarin;
• Fenilin.

NOAC anticoagulants

This is a new generation of oral and parenteral anticoagulants, which are being developed by modern scientists. Among the advantages of such an appointment, a quick effect, complete safety in terms of the risk of bleeding, and reversible inhibition of thrombin are distinguished. However, there are also disadvantages of such oral anticoagulants, and here is a list of them: bleeding in the digestive tract, the presence of side effects and contraindications. In addition, to ensure a long-term therapeutic effect, thrombin inhibitors must be taken for a long time, without violating the recommended daily doses.

The drugs are universal, but the effect in the affected organism is more selective, temporary, and requires long-term use. In order to normalize blood clotting without serious complications, it is recommended to take one of the declared list of new generation oral anticoagulants:

• Apixaban;
• Rivaroxaban;
• Dabigatran.

The price of anticoagulants

If it is necessary to reduce blood clotting as soon as possible, doctors strictly for medical reasons recommend taking anticoagulants - the list of drugs is extensive. The final choice depends on the pharmacological characteristics of a particular drug, cost in pharmacies. Prices are different, and more attention is required to the therapeutic effect. Below you can get acquainted with the prices in Moscow in more detail, but at the same time do not forget the main criteria for such a purchase. So:

Video

To date, there are many drugs that increase blood clotting. Such agents are called coagulants. They most often have only a positive effect on the body as a whole. With their help, even heavy bleeding can be stopped. Drugs that affect the increase in blood clotting are also called hemostatics. They can act on the body both directly and indirectly. However, their activity can also vary.

Direct coagulants are able to include biological components of the entire blood coagulation system. However, such drugs can only be used topically. Some medicines can only be administered to the body through injections.

• recent myocardial infarction;
• previously noticed increased rate of blood clotting;
• predisposition of the body to the formation of blood clots.

Indirect coagulants in their composition necessarily contain vitamin K. They also exhibit good hormonal properties. These medications are used either orally or by injection.

A drug such as Thrombin is most often used to increase blood clotting.

This drug is produced in the form of a powder placed in ampoules. Apply it in most cases only locally. Refer to coagulants of direct action.

To use Thrombin and really increase clotting, it must be properly diluted. To do this, the powder is poured into a physiological solution. As a result, the ampoule will contain a mixture consisting of prothrombin, calcium and thromboplastin.

Locally, this drug is used in cases of small bleeding from small vessels, as well as hemorrhages from parenchymal organs that do not pose a danger to human life. Quite often it is used for traumatic injuries during operations on certain organs.

In dentistry, Thrombin is also used topically for severe bleeding from the gums. To do this, use a hemostatic sponge, which is pre-impregnated with Thrombin.

However, there are cases when Thrombin needs to be used orally. Most often it is in demand in pediatrics. To do this, the powder must be dissolved in sodium chloride or in a special drug "Amben". Assign such a solution for severe intragastric bleeding. When bleeding occurs in the airways, Thrombin is administered by inhalation.

To increase blood clotting, many doctors also prescribe a medication such as Fibrinogen. It is produced in the form of special bottles in the form of a porous mass.

Fibrinogen has a systemic effect on the entire body.

Sometimes it is obtained from blood plasma from a donor. Quite often it happens that the active component of this drug can turn into fibrins, which increase the risk of blood clots.

1. Fibrinogen is used mainly for emergency therapy.
2. With heavy bleeding, the highest activity in the body of this drug is observed.
3. Fibrinogen is especially important in gynecology in case of bleeding during placental abruption, when a woman needs to save not only her life, but also try to save the child.

Most often, such a drug is prescribed in the form of droppers.

There are also cases of its use in severe bleeding of internal organs, when a fibrin film is applied to the bleeding area. In order to start the introduction of the drug into the body, it must first be dissolved in water. Fibrinogen is administered only by drip or jet intravenously, but always very slowly.

Vikasol and Phytomenadione

Vikasol is a coagulant that can be bought at almost any pharmacy. It is usually sold in the form of a solution for injection or tablets. Vikasol belongs to indirect coagulants. It has a synthetic origin and is considered an analogue of vitamin K. It is dissolved in water. This drug is used to accelerate the formation of fibrin clots.

By itself, Vikasol has practically no effect. Vitamins that are synthesized from it, especially vitamin K, cause effects that affect the body. Therefore, the results after taking such a medicine will be noticeable no earlier than 12 hours. However, with intravenous administration, the result can be seen within half an hour.

Most often, Vikasol is prescribed in case of a lack of vitamin K in the body or with a low value of the prothrombin index.

• long-term use of vitamin K antagonists;
• the use of sulfa drugs;
• prolonged therapy with broad-spectrum antibiotics;
• preventive measures taken to eliminate hemorrhagic pathology in infants;
• the presence of cystic fibrosis;
• frequent diarrhea in children;
• pregnancy complicated by some systemic diseases;
• hepatitis affecting clotting;
• heavy bleeding;
• preparatory stage before the operation.

But you need to remember that along with Vikasol, his antagonists can also be appointed. In this case, the effect of the drug is significantly reduced.

Phytomenadione is also used to increase blood clotting.

You can enter it intravenously. The ampoule contains 1 ml of such a drug. This tool can also be used in tablet form. The product is of synthetic origin.

• long-term use of anticoagulants;
• sulfonamide therapy;
• ulcerative colitis;
• antibiotic therapy;
• hemorrhagic syndrome;
• preparation for major surgery.

Quite often, in order to increase blood clotting, fibrinolysis inhibitors are prescribed. Aminocaproic acid can be attributed to improving this indicator. It is considered a drug of synthetic origin. It is usually produced in the form of a powder. When using such a drug, it is possible to slow down the process of converting plasminogen to plasmin. That is why fibrin clots persist for a longer time.

This drug also has a good anti-shock effect. Its toxicity is low. It is quickly excreted from the body along with urine.

1. Aminocaproic acid is introduced into the body during massive blood transfusions, when it is necessary to increase its coagulability.
2. Assign it almost always intravenously.
3. It is also used to prevent allergic reactions, but there is a possibility of developing a number of side effects.

A drug such as Amben has a good effect on blood clotting. This is a synthetic agent that has an antifibrinolytic effect.

However, you should always remember that the best remedy that will affect the increase in blood clotting is prescribed only by a doctor. In this case, self-medication is strictly prohibited, since bleeding can be life-threatening.

Therefore, if symptoms of bleeding were noticed, and especially from the internal organs, you should immediately seek help from a specialist. Only a doctor will be able to determine the cause that affects bleeding, and prescribe the most effective drugs that increase blood clotting to improve the condition in each individual case.

A complex enzymatic process of blood coagulation determines the normal functioning of internal organs, the natural cessation of bleeding and wound healing. The normal clotting process requires the protein fibrinogen, which is involved in the formation of fibrin clots. A healthy body with a normal aggregate state of blood and lymphatic fluid independently copes with small hemorrhages, forming blood clots, but a reduced concentration of fibrinogen leads to serious disorders. A person with poor blood clotting may have internal bleeding, and bruises appear on the skin even with minor exposure.

Means that increase blood clotting are prescribed exclusively by a specialist, but there are also folk methods that increase the amount of fibrinogen in the blood. The clotting index largely depends on what products a person consumes and what bad habits he has.

Causes of bleeding disorders

The main causes that affect the aggregate state of the blood are hidden in systemic disorders of the body.

• Reduced immunity, autoimmune diseases;
• Pathology of the liver, infection;
• Violation of the production of anticoagulants.

In an adult or child, a poor coagulation rate is accompanied by the following symptoms:

• the appearance of hematomas on the body with a slight impact;
• scratches on the skin bleed for a long time;
• there is bleeding gums;
• with an injury to the internal organs, life-threatening internal bleeding develops.

Drugs that increase the amount of fibrinogen

To remove the symptoms of bleeding and act directly on the cause of the disease, drugs of the hemostatic group, which can increase blood clotting, and eliminate the violation of the production of anticoagulants, can.

The list of such medicines includes:

1. Drugs that affect the increase in fibrinogen production (the impact directly on the causes of the pathology) are coagulants. These drugs can be direct action (Fibrinogen, Thrombin) or indirect (Vikasol).
2. Drugs of synthetic origin that improve clotting - Aminocaproic acid, Amien or animal origin - Pantrypin, Aprotinin.
3. Drugs that stimulate thrombosis - calcium chloride, serotonin adipate.
4. Drugs that affect the decrease in the permeability of the vascular wall. Allocate synthetic substances - Rutin, Adroxon and natural - arnica, yarrow, nettle.

Folk methods

Natural substances will be useful for people with poor blood clotting, in addition, they are safe for children and adults with contraindications to drug treatment.

1. Yarrow: indicated for poor clotting, affects the state of blood vessels, eliminates inflammatory processes, promotes rapid tissue regeneration. From this plant, you can prepare decoctions, infusions that will help in the rapid recovery of wounds, with nosebleeds. The plant is poisonous, therefore it can be used only after consulting a specialist;
2. Pine nut shells and extracts can be used to eliminate minor bleeding in the mouth or to regenerate a superficial skin injury.
3. Natural medicines that affect the level of fibrinogen include corn in their list, which needs to be supplemented with a diet, as well as prepare decoctions.
4. To cope with severe bleeding or a burn wound will help infusion of cudweed marshmallow. This natural plant is also used in medicine, helps to cope with circulatory disorders. Dried marshwort is used to prepare tinctures, decoctions and local compresses. Contraindications for use are high blood pressure, purulent skin lesions and thrombophlebitis.

Diet

The diet with reduced coagulability does not change dramatically, it is enough to include in the diet some foods that affect the fibrinogen index and contain vitamin K.

Products that improve blood clotting:

Important! The daily menu should include products from this list, but the diet should be varied.

Poor irregular nutrition, along with negative psychological factors, can provoke a violation of fibrinogen production, which will cause pathology, so treatment should be accompanied by normalization of the mental state, elimination of the stress factor and regular nutrition.

Violation of the aggregate state of the blood leads to a sign of serious problems, therefore, if specific symptoms appear, you should contact a hematologist for a blood test and the appointment of complex treatment.

The liquid state of the blood and the integrity of the bloodstream are necessary conditions for the vital activity of the organism. These conditions are created by the blood coagulation system, which keeps the circulating blood in a liquid state.

The blood coagulation system is part of a larger system - the system for regulating the aggregate state of blood and colloids (RASK system), which maintains the aggregate state of the internal environment of the body at a level that is necessary for normal life. The RASK system maintains the liquid state of the blood and restores the properties of the walls of blood vessels, which change even during their normal functioning. Thus, the body has a special biological system that, on the one hand, ensures the preservation of the liquid state of the blood, and, on the other hand, prevents and stops bleeding by maintaining the structural integrity of the walls of blood vessels and rapid thrombosis of the latter in case of damage. This system is called the hemostasis system.

There are vascular-platelet hemostasis, which ensures the cessation of bleeding from microcirculatory vessels by the formation of platelet thrombi (primary hemostasis), as well as coagulation enzymatic hemostasis, which ensures the stop of bleeding by the formation of a fibrin thrombus (stop bleeding in large vessels).

The liquid state of the blood is provided by the anticoagulant system. The trigger for blood clotting is damage to the blood vessels. Coagulation enzymatic hemostasis proceeds in three phases:

PHASE I Formation of prothrombinase (triggered by tissue

vym thromboplastin with subsequent formation

I eat blood (platelet and erythrocyte)

prothrombinase).

PHASE II The appearance of prothrombinase means the beginning of the

swarm phase of blood coagulation - education

thrombin (the process is instantaneous - 2-5 seconds

PHASE III Under the influence of thrombin in the third phase of pro

fibrinogen is converted to fibrin. About

fibrin formation and completes the formation

blood clot.

The aggregate (liquid) state of blood is provided by the dynamic balance of the potentials of the coagulation and anticoagulation systems. The liquid state of the blood is primarily maintained by the natural anticoagulants present in it.

gullants (anti-coagulant system). First of all, this is a group of antithromboplastins that inhibit the action of prothrombinase (antithrombin III, alpha-2-macroglobulin, or antithrombin IV). In addition, heparin is produced by mast cells and basophils.

There is also a third component - the fibrinolysis system, which begins to act simultaneously with clot retraction.

Fibrinolysis is the process of splitting fibrin, which forms the basis of a blood clot. The main function of fibrinolysis is the restoration of the lumen (recanalization) of a vessel clogged with a clot.

Fibrin is cleaved by the proteolytic enzyme plasmin, which is present in the plasma as plasminogen.

The pathology of blood coagulation in the clinic manifests itself either in the form of hemorrhages, or in the form of an increase in thrombus formation, a combination of both phenomena is also possible (with DIC - dissociated intravascular coagulation).

In the process of treating patients with these conditions, two main groups of drugs are used:

1. Anti-clotting drugs

blood, which means stopping bleeding (hemosta

2. Anti-clotting agents (antitrom

botic) or agents for thrombosis and for their

prevention.

Each of these groups is divided into subgroups that affect thrombus formation, the activity of the fibrinolytic system, platelet aggregation and the vascular wall in different directions.

I. HEMOSTATICS

1. Coagulants (agents that stimulate the formation

fibrin thrombi):

a) direct action (thrombin, fibrinogen);

b) indirect action (vikasol, phytomenadione).

2. Fibrinolysis inhibitors:

a) synthetic origin (aminocaprono

vaya and tranexamic acids,

b) animal origin (aprotinin, contri

cal, pantripin, gordoks "Gideon

Richter, Hungary);

3. Stimulants of platelet aggregation (serotonin

adipate, calcium chloride).

4. Means that reduce vascular permeability:

a) synthetic (adroxon, etamsylate, iprazoh

b) preparations of vitamins (ascorbic acid,

rutin, quercetin).

c) herbal preparations

you, yarrow, viburnum, water pepper,

arnica, etc.)

II. ANTI-COAGULATION DRUGS OR AN

TITHROMBOTICS:

1. Anticoagulants:

a) direct action (heparin and its preparations,

hirudin, sodium citrate, antithrombin III);

b) indirect action (neodicoumarin, syncumar,

phenylin, fepromarone).

2. Fibrinolytics:

a) direct action (fibrinolysin or plasmin);

b) indirect (plasminogen activators) action

(streptolyase, streptokinase, urokinase, ak

3. Antiplatelet agents:

a) platelets (acetylsalicylic acid,

dipyridamole, pentoxifylline, ticlopidine,

indobufen);

b) erythrocytes (pentoxifylline, reopoliglyu

kin, reogluman, rondex).

DRUGS THAT INCREASE BLOOD COAGULATION (HEMOSTATICS)

COAGULANTS

According to the classification, this group of drugs is divided into direct and indirect coagulants, but sometimes they are divided according to a different principle:

1) for topical application (thrombin, hemostatic sponge

chemical, fibrin film, etc.)

2) for systemic use (fibrinogen, vikasol).

THROMBIN (Trombinum; dry powder in amp. o, 1, which corresponds to 125 units of activity; in vials of 10 ml) is a direct-acting coagulant for topical use. Being a natural component of the blood coagulation system, it causes an effect in vitro and in vivo.

Before use, the powder is dissolved in saline. Usually the powder in the ampoule is a mixture of thromboplastin, calcium and prothrombin.

Apply only locally. Assign to patients with bleeding from small vessels and parenchymal organs (surgery on the liver, kidneys, lungs, brain), bleeding from the gums. Used topically in the form of a hemostatic sponge impregnated with a thrombin solution, a hemostatic sponge

lagenovy, or simply by applying a swab soaked in a solution of thrombin.

Sometimes, especially in pediatrics, thrombin is used orally (the contents of the ampoule are dissolved in 50 ml of sodium chloride or 50 ml of 5% amben solution, 1 tablespoon is prescribed 2-3 times a day) for gastric bleeding or by inhalation for bleeding from the respiratory tract.

FIBRINOGEN (Fibrinogenum; in vials of 1.0 and 2.0 dry porous mass) - used for systemic exposure. It is also obtained from the blood plasma of donors. Under the influence of thrombin, fibrinogen is converted into fibrin, which forms blood clots.

Fibrinogen is used as an ambulance. It is especially effective when its deficiency is observed in massive bleeding (placental abruption, hypo- and afibrinogenemia, in surgical, obstetric, gynecological and oncological practice).

Assign usually in a vein, sometimes locally in the form of a film applied to the bleeding surface.

Before use, the drug is dissolved in 250 or 500 ml of warm water for injection. Intravenously administered drip or slowly jet.

VIKASOL (Vicasolum; in tabs, 0.015 and in amp. 1 ml of 1% solution) is an indirect coagulant, a synthetic water-soluble analogue of vitamin K, which activates the formation of fibrin clots. Referred to as vitamin K3. The pharmacological effect is caused not by vikasol itself, but by the vitamins K1 and K2 formed from it, so the effect develops after 12-24 hours, with intravenous administration - after 30 minutes, with intramuscular injection - after 2-3 hours.

These vitamins are necessary for the synthesis in the liver of prothrombin (factor II), proconvertin (factor VII), as well as factors IX and X.

Indications for use: with an excessive decrease in the prothrombin index, with severe K-vitamin deficiency due to:

1) bleeding from parenchymal organs;

2) exchange transfusion procedure, if

poured (to the child) preserved blood;

and also when:

3) long-term use of vitamin K antagonists -

aspirin and NSAIDs (which disrupt platelet aggregation)

4) long-term use of broad-spectrum antibiotics

action (levomycetin, ampicillin, tetracyc

lin, aminoglycosides, fluoroquinolones);

5) the use of sulfonamides;

6) prevention of hemorrhagic disease of newborns;

7) prolonged diarrhea in children;

8) cystic fibrosis;

9) in pregnant women, especially in those suffering from tuberculosis

disease and epilepsy and receiving appropriate medication

10) overdose of indirect anticoagulants;

11) jaundice, hepatitis, as well as after injuries, blood

currents (hemorrhoids, ulcers, radiation sickness);

12) preparation for surgery and postoperative

ration period.

The effects can be weakened by the simultaneous administration of vikasol antagonists: aspirin, NSAIDs, PASK, indirect anticoagulants of the neodicoumarin group.

Side effects: hemolysis of erythrocytes when administered intravenously.

PHYTOMENADION (Phytomenadinum; 1 ml for intravenous administration, as well as capsules containing 0.1 ml of a 10% oil solution, which corresponds to 0.01 of the drug). Unlike natural vitamin K1 (trans compounds) is a synthetic drug. It represents a racemic form (a mixture of trans- and cis-isomers), and in terms of biological activity it retains all the properties of vitamin K1. It is rapidly absorbed and maintains a peak concentration of up to eight hours.

Indications for use: hemorrhagic syndrome with hypoprothrombinemia caused by a decrease in liver function (hepatitis, liver cirrhosis), with ulcerative colitis, with an overdose of anticoagulants, with prolonged use of high doses of broad-spectrum antibiotics and sulfonamides; before major operations to reduce bleeding.

Side effects: phenomena of hypercoagulability in case of non-compliance with the dosing regimen.

Of the drugs related to direct-acting coagulants, the following drugs are also used in the clinic:

1) prothrombin complex (VI, VII, IX, X factors);

2) antihemophilic globulin (VIII factor).

FIBRINOLYSIS INHIBITORS (ANTIFINOLITICS)

AMINOCAPRONIC ACID (ACC) is a powdered synthetic drug that inhibits the conversion of profibrinolysin (plasminogen) into fibrinolysin (plasmin) by acting on the profibrinolysin activator and thereby contributes to the preservation of fibrin thrombi.

In addition, ACC is also an inhibitor of kinins and some complement system factors.

It has anti-shock activity (inhibits proteolytic enzymes, and also stimulates the neutralizing function of the liver).

The drug is low toxic, quickly excreted from the body

with urine (after 4 hours).

They are used in the emergency clinic, during surgical interventions and in various pathological conditions, when the fibrinolytic activity of blood and tissues is increased:

1) during and after operations on the lungs, prostate, pancreas

glandular and thyroid glands;

2) with premature detachment of the placenta, prolonged

retention in the uterus of a dead fetus;

3) with hepatitis, cirrhosis of the liver, with portal gi

pertension, when using the device artificially

leg blood circulation;

4) at II and III stages of DIC, with ulcerative,

nasal, pulmonary bleeding.

ACC is administered during massive transfusions of canned blood, administered intravenously or orally.

Available: powder and bottles of 100 ml of sterile 5% solution in isotonic sodium chloride solution. AT

due to the fact that ACC has anti-shock activity, inhibits proteolytic enzymes and kinins, inhibits the formation of antibodies, the drug is used in shock reactions and as an anti-allergic agent.

Side effects: possible dizziness, nausea, diarrhea, mild catarrh of the upper respiratory tract.

AMBEN (Ambenum, aminomethylbenzoic acid) is also a synthetic drug, similar in chemical structure to para-aminobenzoic acid. White powder, poorly soluble in water. It is an antifibrinolytic agent. Amben inhibits fibrinolysis, the mechanism of action is similar to ACC.

Indications for use are the same. Assign intravenously, intramuscularly and inside. When injected into a vein, it acts quickly, but for a short time (3 hours). Release form: ampoules of 5 ml of 1% solution, tablets of 0.25.

Sometimes anti-enzymatic drugs are indicated, in particular, contrykal. It inhibits plasmin, collagenases, trypsin, chymotrypsin, which play an important role in the development of many pathophysiological processes. The drugs of this group have an inhibitory effect on the catalytic interaction of individual factors of fibrinolysis and blood coagulation processes.

Indications for use: local hyperfibrinolysis - postoperative and postportal bleeding; hypermenorrhea; generalized primary and secondary hyperfibrinolysis in obstetrics and surgery; the initial stage of DIC, etc.

Side effects: rarely allergies; embryotoxic action; With a quick introduction - malaise, nausea.

MEDICINES INCREASING PLATELET AGGREGATION AND ADHESION

serotonin. Its use is associated with stimulation of platelet aggregation, tissue swelling, changes in microcirculation, which contributes to the occurrence of platelet thrombi. Serotonin in the form of adipinate (Serotonini adipinatis in ampoules of 1 ml of 1% solution) is used intravenously or intramuscularly for hemorrhages associated with platelet pathology (thrombocytopenia, thrombocytopathy). This increases the number of platelets, shortens the bleeding time, increases the resistance of capillaries.

Used for von Willebrandt type I disease, hypo- and aplastic anemia, for Werlhof's disease, hemorrhagic vasculitis.

Do not use in case of kidney pathology, patients with bronchial asthma, with blood hypercoagulation.

Side effect: with a quick introduction - pain along the vein; pain in the abdomen, in the region of the heart, rise in blood pressure, heaviness in the head, nausea, diarrhea, decreased diuresis.

CALCIUM PREPARATIONS

CALCIUM is directly involved in platelet aggregation and adhesion, and also promotes the formation of thrombin and fibrin. Thus, it stimulates the formation of both platelet and fibrin clots.

Indications for use:

1) as a means of reducing vascular permeability,

with hemorrhagic vasculitis;

2) as a hemostatic agent for pulmonary,

gastric, nasal, uterine bleeding, and

also before the operation;

3) with bleeding associated with a decrease in calcium

in blood plasma (after transfusion of large coli

citrated blood, plasma substitutes).

Calcium chloride is used (intravenously and orally).

Side effects: with rapid administration, cardiac arrest, lowering blood pressure are possible; with intravenous administration, there is a feeling of heat ("hot injection"); with subcutaneous administration of calcium chloride - tissue necrosis.

DRUGS THAT DECREASE THE PERMEABILITY OF THE VASCULAR WALL

SYNTHETICS

ADROXONE (Adroxonum; in 1 ml amp. 0.025%) - a drug of adrenochrome, a metabolite of adrenaline. It does not increase blood pressure, does not affect the activity of the heart and blood clotting.

Its main effect is to increase the density of the vascular wall and activate platelet aggregation and adhesion. Therefore, adroxon has a hemostatic effect in capillary bleeding, when the permeability of the walls of these vessels is especially increased. However, with massive bleeding, the drug is not effective.

Indications for use:

1) with parenchymal and capillary bleeding;

2) in case of injuries and operations;

3) with intestinal bleeding in newborns;

4) with melena;

5) with platelet purpura.

Adroxon is applied topically (tampons, wipes), intramuscularly or subcutaneously. Etamzilat or dicynone (Ethamsylatum; in tab. 0.25 and in amp. 2 ml of 12.5% ​​solution) is a synthetic, a derivative of dioxybenzene. The drug reduces vascular permeability, reduces extravasation and exudation of the liquid part of the plasma, normalizes the permeability of the vascular wall and improves microcirculation, increases blood clotting, as it promotes the formation of thromboplastin (hemostatic effect). The last effect develops quickly - with intravenous administration after 5-15 minutes, the most pronounced - after 1-2 hours. In tablets, the effect is manifested after 3 hours. The drug is administered into a vein, subcutaneously or intramuscularly.

Indications for use:

1) platelet purpura;

2) intestinal and pulmonary bleeding (surgery);

3) hemorrhagic diathesis;

4) operations on ENT organs;

5) diabetic angiopathy (ophthalmology).

Side effect - sometimes there is heartburn, a feeling of heaviness in the epigastric region, headache, dizziness, flushing of the face, paresthesia of the legs, lowering blood pressure.

VITAMIN PREPARATIONS

To eliminate increased vascular permeability, especially in the presence of hemorrhages, vitamin C preparations (ascorbic acid) are used, as well as various flavonoids (rutin, ascorutin, quercetin, vitamin P), as well as vitamers, that is, semi-synthetic derivatives - venoruton and troxevasin in various medicinal products. forms (capsules, gel, solutions). Vitamin P preparations are used for intense extravasation of the liquid part of the plasma, for example, with swelling of the legs (thrombophlebitis). In addition, these drugs are prescribed for hemorrhagic diathesis, retinal hemorrhages, radiation sickness, arachnoiditis, hypertension, and an overdose of salicylates. Rutin and askorutin are used in pediatrics to eliminate intense trance.

administration in children with scarlet fever, measles, diphtheria and toxic influenza.

RUTIN is available in tablets of 0.02 (2-3 times per

day). ASKORUTIN - 0.05 each. VENORUTON - in capsules

0.3; ampoules of 5 ml of a 10% solution. Preparations from plants (infusions, extracts, tablets) have a weak hemostatic effect. Therefore, they are used for light bleeding (nasal, hemorrhoidal), for bleeding, hemoptysis, hemorrhagic diathesis, in obstetric and gynecological practice.

MEDICINES THAT REDUCE BLOOD COAGULATION (ANTITIS

ROMBOTIC MEANS)

ANTICOAGULANTS

1. Anticoagulants (drugs that disrupt the formation

fibrin thrombi):

a) direct anticoagulants (heparin and its preparations,

hirudin, sodium hydrocitrate, antitite concentrate

rhombin III) - cause an effect in vitro and in

b) anticoagulants of indirect action (derivatives

oxycoumarin: neodicoumarin, sincumar, pelentan

and etc.; indandione derivatives - phenyline, etc.)

Cause effect only in vivo.

HEPARIN (Heparinum; in a 5 ml vial containing 5,000, 10,000 and 20,000 IU per 1 ml, Gedeon Richter, Hungary) is a natural anticoagulant factor produced by mastocytes. Heparin is the collective name for a group of linear anionic polyelectrolytes distinguished by the number of sulfuric acid residues. There are high and low molecular weight heparins (average molecular weight -

Heparin is a novogalenic drug derived from the lungs and liver of cattle. It is the strongest organic acid due to the residues of its sulfuric acid and the presence of carboxyl groups, which gives it a very strong negative charge. Therefore, it, in fact, refers to anionic polyelectrolytes. Due to the negative charge, in the blood, heparin combines with positively charged complexes, is sorbed on the surface of the membranes of endothelial cells, macrophages, thereby limiting platelet aggregation and adhesion. The action of heparin largely depends on the plasma concentration of antithrombin III.

Pharmacological effects of heparin:

1) Heparin has an anticoagulant effect, so

how it activates antithrombin III and irreversibly

no clotting factors IXa, Xa, XIa and XIIa

2) moderately reduces platelet aggregation;

3) heparin reduces blood viscosity, reduces permeability

capacity of blood vessels, which facilitates and accelerates the flow of blood

vi, prevents the development of stasis (one of the facto

moat, contributing to thrombosis);

4) reduces the content of sugar, lipids and chylomicrons

in the blood, has an anti-sclerotic effect,

binds some components of a compliment, ugne

melts the synthesis of immunoglobulins, ACTH, aldosterone,

and also binds histamine, serotonin, showing,

thus, anti-allergic effect;

5) heparin has a potassium-sparing, anti-inflammatory

telny, analgesic effects. Besides,

heparin increases diuresis and reduces

vascular resistance due to the expansion of re

viscous vessels, eliminates spasm of coronary arteries

Indications for use:

1) with acute thrombosis, thromboembolism (acute in

myocardial infarction, pulmonary thrombosis, renal

veins, ileocecal vessels), thromboembolism in the

2) when working with artificial blood circulation devices

scheniya, artificial kidney and heart;

3) in laboratory practice;

4) for burns and frostbite (improvement of microcirculation

5) in the treatment of patients in the initial stages of DIC

roma (with lightning purpura, severe gastro

6) in the treatment of patients with bronchial asthma, rheumatism

mom, as well as in the complex therapy of patients with gloma

roll nephritis;

7) during extracorporeal hemodialysis,

hemosorption and forced diuresis;

8) with hyperaldosteronism;

9) as an antiallergic agent (bronchial

10) in the complex of therapeutic measures in patients with ate

rosclerosis.

Side effects:

1) development of hemorrhages, thrombocytopenia (30%);

2) dizziness, nausea, vomiting, anorexia, diarrhea;

3) allergic reactions, hyperthermia.

To eliminate complications (hemorrhages), heparin antidotes (protamine sulfate in the form of a 5% solution) are injected into the vein.

or POLYBREN; 1 mg of protamine sulfate neutralizes 85 units of heparin; enter slowly).

At one time, a patient with acute thrombosis, on average, is administered 10,000 IU intravenously. Up to 40,000 - 50,000 IU intravenously per day, administered slowly. It can be administered intramuscularly and subcutaneously (in the area of ​​least vascularization). In recent years, for the prevention of thrombosis, it is recommended to administer 5000 IU of heparin subcutaneously or intradermally every 6-8 hours. Heparin ointment is also available in tubes of 25.0 (2500 units). Inhalation in the form of an aerosol, as an antiallergic agent, the drug is administered using an ultrasonic inhaler at 500 IU / kg per day. Inhalations are carried out 2-3 times a week. A single dose is diluted in distilled water in a ratio of 1: 4.

HIRUDIN and its preparations (girudont, etc.) are a product of leeches. The anticoagulant and anti-inflammatory effects of these agents are used. They are prescribed topically (ointments and gels) for superficial inflammation of the veins, vein thrombosis, trophic ulcers of the leg, furunculosis, inflammation of the lymph nodes, to improve the healing of sutures after injuries and burns.

Side effect - allergic reactions (rash, itching, Quincke's edema).

SODIUM HYDROCITRATE is used only for blood preservation. The anion of citric acid combines with the calcium ion, which binds the activity of the latter. The substance is added in excess. The patient should not be used, since sodium hydrocitrate will block calcium ions and the patient will develop arrhythmia, possibly developing heart failure and cardiac arrest.

Sometimes prescribed orally to eliminate hypercalcemia and treat poisoning with cardiac glycosides.

If the patient is transfused up to 500 ml of canned blood, then this does not require any additional measures. If blood is transfused in a volume of more than 500 ml, then it is necessary to add 5 ml of a 10% solution of calcium chloride for every 50 ml in excess of 500 ml of transfused blood.

INDIRECT-ACTING ANTICOAGULANTS (PERO

RAL ANTICOAGULANTS)

Of the large number of anticoagulants, the most common drugs are the coumarin group. There are many drugs, but neodicoumarin (pelentan), sincumar, fepromarone, phenylin, amefin, farfavin are used more often than others.

NEODIKUMARIN (Neodicumarinum; in tab. 0.05 and 0.1), syncumar, dicumarin, fepromarone, omefin, phenylin are derivatives of phenylindanedione, very similar in pharmacodynamics. Their mechanism of action is related to the fact that they are antivitamins K, that is, they act as vitamin K antagonists.

By suppressing its activity, these drugs inhibit the synthesis of proconvertin (factor VII), prothrombin (factor II), as well as IX and X coagulation factors necessary for coagulation homeostasis, that is, for the formation of fibrin thrombi. These drugs do not act immediately, but after 8-24 hours, that is, they are slow-acting agents with cumulative properties. At the same time, different drugs of this group have different speed and strength of action, different degrees of cumulation. Another feature of their action is the high duration of action.

These drugs are used only inside, as they are well absorbed, then they are brought back to the intestine with the blood flow, released into its lumen and absorbed again (recirculation). All drugs enter into an unstable relationship with plasma proteins and are easily displaced from it by other drugs. They only work in vivo.

Indications for use:

1) to reduce blood clotting in order to pro

lactic and treatment of thrombosis, thrombophlebitis and

thromboembolism (myocardial infarction), embolic

strokes;

2) in surgery to prevent thrombus formation in

postoperative period.

Side effects are rarely recorded in the form of dyspeptic syndrome (nausea, vomiting, diarrhea, loss of appetite). In the course of pharmacotherapy with drugs such as neodicoumarin, there are complications in the form of bleeding due to an overdose, with a properly selected dose, but without taking into account drug interactions. For example, with the simultaneous appointment of neodicoumarin and butadione or salicylates. In this case, bleeding is also possible through an intact vascular wall, for example, in patients with peptic ulcer. Treatment should be carried out under constant monitoring of the level of prothrombin in the blood. In case of bleeding, a solution of vikasol, vitamin P, rutin, calcium chloride is administered, and 70-100 ml of the donor's blood is transfused.

Treatment with anticoagulants is a difficult task for the doctor. It is necessary to monitor the prothrombin index, which should be 40-50. Treatment is strictly individual.

There are a number of contraindications to the use of this group of funds:

1) open wounds, stomach ulcer;

2) endocarditis;

3) hepatitis, liver cirrhosis;

4) threatened abortion;

5) kidney disease.

FIBRINOLYTICS (THROMBOLYTICS)

1. Direct action - fibrinolysin (plasmin).

2. Indirect action (plasminogen activators: acti

lyse, streptokinase, streptodecase, urokinase).

FIBRINOLISIN (available as a powder in vials containing 10, 20, 30 and 40 thousand units) is an old drug that is a fibrinolytic. It is obtained from the blood plasma of a donor. As a proteolytic enzyme, it breaks down fibrin, acting on the surface of the thrombus. It eliminates only fibrin thrombi during the first days of their formation, dissolves only fresh fibrin strands in the veins, leading to vascular recanalization.

Fibrin degradation products have anticoagulant properties, as they inhibit the polymerization of fibrin monomers and the formation of thromboplastin.

Fibrinolysin is an emergency drug prescribed for thromboembolic conditions:

Peripheral vascular occlusion;

Thrombosis of the vessels of the brain, eyes;

IHD (myocardial infarction);

When removing a thrombus from a vascular shunt.

This drug has significant drawbacks: - it is very expensive (produced from donated blood); - not very active, poorly penetrates into the thrombus. Side effects with the introduction of fibrinolysin, a foreign protein, can be realized in the form of allergic reactions, as well as in the form of non-specific reactions to the protein (face flushing, pain along the vein, as well as behind the sternum and in the abdomen) or in the form of fever, urticaria.

Before use, the drug is dissolved in an isotonic solution at the rate of 100-160 IU of fibrinolysin per 1 ml of solvent. The prepared solution is poured intravenously drip (10-15 drops per minute).

FIBRINOLYTICS OF INDIRECT ACTION

STREPTOKINASE (streptase, avelizin; available in amps containing 250,000 and 500,000 IU of the drug) is a more modern drug, an indirect fibrinolytic. It is derived from beta-hemolytic streptococcus. This is a more active and cheaper drug. It stimulates the transition of the proactivator into an activator that transforms profibrinolysin into fibrinolysin (plasmin). The drug is able to penetrate into the thrombus (activating fibrinolysis in it), which distinguishes it favorably from fibrinolysin. Streptokinase is most effective in

action on a thrombus that formed no more than seven days ago. At the same time, this fibrinolytic is able to restore the patency of blood vessels, the breakdown of blood clots.

Indications for use:

1) in the treatment of patients with superficial and deep

thrombophlebitis;

2) with thromboembolism of the pulmonary vessels and vessels of the eye

3) with septic thrombosis;

4) with fresh (acute) myocardial infarction. Side effects

effects: 1) allergic reactions (antibodies to strep

tococcam); 2) hemorrhages; 3) drop in hemoglo

bina, erythrocyte hemolysis

(direct toxic effect);

4) vasopathy (formation of the CEC).

In our country, on the basis of streptokinase, STREPTODECASE has been synthesized, a similar drug with a longer duration of action. Allergic reactions are also possible to this drug.

Urokinase is a drug synthesized from urine. It is considered a more modern remedy, less allergic reactions than streptokinase.

General note: when a large number of fibrinolytics are used in the body, blood coagulation processes develop compensatory. Therefore, all these drugs must be administered together with heparin. In addition, using this group of agents, fibrinogen levels and thrombin time are constantly monitored.

DRUGS THAT PREVENT PLATELET AGGREGATION

(ANTIAGGREGANTS)

Antiplatelet agents - a group of anticoagulants:

1. Platelets (acetylsalicylic acid (ASA),

heparin, dipyridamole, ticlopidine, indobufen, pen

toxifylline).

2. Erythrocyte (pentoxifylline, reopoliglyukin).

ACETYLSALICYLIC ACID (Acidum acetylsalicylicum; in tab. 0, 25) is a vitamin K antagonist and can irreversibly block platelet cyclooxygenase. Due to this, the formation of arachidonic acid metabolites, in particular, aggregating prostaglandins and thromboxane A, which is the most powerful endogenous aggregant and vasoconstrictor, is rapidly reduced in them.

In addition to inhibition of platelet adhesion, ASA, being a vitamin K antagonist, disrupts the formation of fibrin clots in large doses.

It is necessary to note a number of very important points for the clinic:

1. Prevention of platelet aggregation ASA when using very low doses. The optimal dose for this effect is from 20 to 40 mg per day. Taking 30-40 mg of aspirin blocks platelet aggregation for 96 hours. A dose of 180 mg per day irreversibly inhibits the enzyme cyclooxygenase (COX). Large doses, equal to 1000-1500 mg of ASA per day, can suppress COX in the vascular wall, where another prostaglandin, prostacyclin J2, is formed. The latter prevents platelet aggregation and adhesion, and also causes vasodilation.

Thus, high doses of ASA cause COX inhibition both in platelets (which is desirable) and in the vascular wall (which is undesirable). The latter can provoke thrombosis.

2. ASA acts as an NSAID for several hours after administration. At the same time, the antiaggregation effect is long-term, as long as platelets live, that is, 7 days, since the inhibition of COX in them is an irreversible phenomenon, the enzyme is not synthesized again by the plate. After about a week, a new population of platelets is restored, with an appropriate supply of COX.

Taking into account these facts, one can understand why when taking small doses of ASA, clotting decreases, and bleeding does not occur.

Indications for the use of ASA (as an antiplatelet agent):

1) prevention of the occurrence of arterial blood clots;

2) with angina pectoris;

3) with hypertension;

4) with atherosclerosis.

As an antiplatelet agent, the drug is prescribed according to the scheme: the first day, 0.5 2 times, then 0.25 per day for several months, and sometimes years. To reduce the risk of ulcerogenesis, MICRISTIN has been released - a granular microcrystalline preparation of ASA, enclosed in a polyvinyl acetate shell.

For similar indications, indobufen, indomethacin are also prescribed.

DIPIRIDAMOL (Dypiridomalum; synonyms: chimes, persantyl; in a tablet or dragee at 0.025 and 0.075, as well as in 2 ml amps of a 0.5% solution) is an antianginal agent. Competitive inhibitor of phosphodiesterase and adenosine deaminase. Dipyridamole prevents platelet aggregation by limiting aggregating factors in them (cAMP accumulates in platelets) and potentiating the action of adenosine. The latter promotes vasodilating and antiaggregatory effects, a slight decrease in blood pressure. Thus, pre

Parat dilates the coronary vessels and increases the rate of blood flow, improves the supply of oxygen to the myocardium. In general, the drug is considered a weak antiplatelet agent.

Indications for use:

1) to prevent thrombosis;

2) in the treatment of patients with DIC (in combination

with heparin)

3) for the prevention of DIC in infectious

toxicosis, septicemia (shock);

4) with dehydration;

5) in patients with heart valve prostheses;

6) with hemodialysis;

7) with angina pectoris and myocardial infarction.

Side effects: short-term reddening of the face, tachycardia, allergic reactions. A modern antiplatelet agent is the drug TICLOPIDIN (Ticlopidinum; synonym - ticlid; in tab. 0, 25) - a new selective antiplatelet agent that is superior in strength to ASA.

Ticlid inhibits platelet aggregation and adhesion. The drug stimulates the formation of prostaglandins Pg E1, Pg D2 and Pg J2, improves microcirculation.

Indications for use:

1) ischemic and cerebrovascular diseases;

3) limb ischemia;

4) retinopathy (diabetes mellitus, etc.);

5) when bypassing blood vessels.

Side effects: stomach pain, diarrhea, rash, dizziness, jaundice, decrease in the number of leukocytes and platelets.

Plasma-substituting drugs based on dextran, that is, low molecular weight dextrans (glucose polymers), are also used as antiplatelet agents. These are, first of all, solutions of the medium molecular fraction of dextran: 6% solution of polyglucin, 10% solution of reopoliglyukin (especially this drug), as well as reogluman, Rondex. These funds "dilute" the blood, reduce its viscosity, envelop platelets and erythrocytes, which contributes to their antiplatelet effect, improve the movement of fluid from tissues to blood vessels, increase blood pressure, and have a detoxifying effect.

Indications for use: shock, thrombosis, thrombophlebitis, endarteritis, peritonitis, etc. (in order to improve capillary blood flow).

Side effects: allergic reactions.

Platelet antiaggregants are drugs from the group of methylxanthines: eufillin, as well as teonikol (xanthinol nicotinate, complavin, ksavin), etc.

THEONICOL (xanthinol nicotinate; in dragee 0, 15 and

amp. 2 and 10 ml of a 15% solution) has a vasodilating effect, improves cerebral circulation, and reduces platelet aggregation.

Indications for use:

1) spasms of the vessels of the extremities (endoarteritis, disease

2) trophic ulcers of the extremities.

Side effects: feeling of warmth, redness of the face, neck, general weakness, dizziness, pressure in the head, dyspepsia.

DRUGS THAT PREVENT erythrocyte aggregation

PENTOXYFILLIN or trental (Pentoxyphillinum; in pills of 0, 1 and in amps of 5 ml of a 2% solution) is a derivative of dimethylxanthine, similar to theobromine. The main effect of the drug is to improve the rheological properties of blood. It contributes to the bendability of erythrocytes, which improves their passage through the capillaries (the diameter of erythrocytes is 7 microns, and the capillaries are 5 microns).

Since trental increases the flexibility of erythrocytes, limits the aggregation of blood cells, reduces the level of fibrinogen, it ultimately reduces the viscosity of the blood and makes it more fluid, reducing the resistance to blood flow. Improving the rheological properties of blood is slow. The effect comes in 2-4 weeks.

Indications for use:

1) in violation of peripheral circulation:

Raynaud's disease;

Diabetic angiopathy;

Vascular pathology of the eye;

2) in violation of cerebral and coronary circulation

3) with circulatory shock.

Trental is contraindicated in pregnancy, patients with hemorrhages and myocardial infarction. Undesirable effects: nausea, anorexia, diarrhea, dizziness, redness of the face.

MEDICINES AFFECTING HEMATOPOISIS

ANTIANEMIC MEANS

Antianemic agents are used to enhance hematopoiesis and eliminate qualitative disorders of erythropoiesis.

Anemia can develop as a result of insufficiency of various hematopoietic factors:

Iron (iron deficiency anemia);

Some vitamins (B12-deficient, folic acid deficiency

cytic, E-deficient);

Proteins (protein deficiency).

In addition, the role of hereditary disorders of erythropoiesis, copper and magnesium deficiency is very significant. There are hypochromic and hyperchromic anemias. Hyperchromic anemia occurs with a deficiency of B vitamins (folic acid - Bc and cyanocobalamin - B12). All other anemias are hypochromic. The incidence of anemia is high, especially among pregnant women.

ANTIANEMIC MEDICINES USED IN

HYPOCHROMIC ANEMIA

Most often, hypochromic anemia is of iron deficiency origin. Iron deficiency can result from:

Inadequate intake of iron in the body of the fetus

and child;

Poor absorption from the intestines (mal

absorption, inflammatory bowel disease,

taking tetracyclines and other antibiotics);

Excessive blood loss (helminthic invasion, nasal and

hemorrhoidal bleeding);

Increased iron consumption (intensive growth, in

Iron is an essential component of a number of enzymes of both hemic and non-himine structures. Hemic enzymes: - hemo- and myoglobin;

Cytochromes (P-450);

Peroxidases;

Catalase.

Non-heminic enzymes: - succinate dehydrogenase;

Acetyl-CoA dehydrogenase;

NADH dehydrogenase etc.

With a lack of iron, the content of hemoglobin decreases (the color index is less than one), as well as the activity of respiratory enzymes in tissues (hypotrophy).

Iron is absorbed in the duodenum, as well as in other parts of the small intestine. Ferrous iron is well absorbed. The ferric iron received with food under the influence of hydrochloric acid of the stomach turns into ferrous iron. Calcium, phosphates contained in milk, especially cow's milk, phytic acid, tetracyclines prevent the absorption of iron. The maximum amount of iron (bivalent, which can enter the body per day, is 100 mg).

Iron is absorbed in two stages:

Stage I: iron is captured by mucosal cells.

This process is supported by folic acid

Stage II: transport of iron through the sli cell

zistoy and giving it to the blood. Iron in the blood

oxidized to trivalent, binds to

transferrin.

The more severe the iron deficiency anemia, the less saturated this protein is and the greater its capacity and ability to bind iron. Transferrin transports iron to the organs of hematopoiesis (bone marrow) or storage (liver, spleen).

For the treatment of patients with hypochromic anemia, drugs prescribed both orally and by injection are used.

Inside, ferrous iron preparations are mainly used, since it is better absorbed and less irritating to the mucous membrane.

In turn, drugs prescribed orally are divided into:

1. Organic iron preparations:

iron lactate; - ferrocal;

Hemostimulin; - ferroplex;

Conferon; - ferroceron;

Aloe syrup with iron; - ferramid.

2. Inorganic iron preparations:

ferrous sulfate;

iron chloride;

iron carbonate.

The most affordable and cheapest drug is the preparation of ferrous iron sulfate (Ferrosi sulfas; tab. 0.2 (60 mg of iron)) and powders in gelatin capsules of 0.5 (200 mg of iron)). In this preparation - a high concentration of pure iron.

In addition to this drug, there are many others. IRON LACTATE (Ferri lactas; in gelatin capsules of 0.1-0.5 (1.0-190 mg of iron)).

ALOE SYRUP WITH IRON (in 100 ml bottles) contains 20% ferrous chloride solution, citric acid, aloe juice. Use one teaspoon per dose in a quarter glass of water. Among the undesirable effects when taking this drug, dyspepsia is frequent.

FERROKAL (Ferrocallum; a combined official preparation containing in one tablet 0.2 ferrous iron, 0.1 calcium fructose diphosphate and cerebrolecithin). The drug is prescribed three times a day.

FERROPLEX - dragee containing ferrous sulfate and ascorbic acid. The latter sharply increases the absorption of iron.

FEFOL is a combination of iron and folic acid.

Prolongiro preparations are considered more modern.

bath action (TARDIFERON, FERRO - GRADUMET), made by a special technology on an inert plastic sponge-like substance, from which the gradual release of iron occurs.

There are many drugs, you can use any, but it must be remembered that the therapeutic effect does not develop immediately, but after 3-4 weeks of taking the medicine. Often repeated courses are required. This means that side effects are primarily associated with the irritating effect of iron ions on the gastrointestinal mucosa (diarrhea, nausea). In 10% of patients, constipation develops, since ferrous iron binds hydrogen sulfide, which is a natural irritant of the gastrointestinal tract. There is staining of the teeth. Poisoning is possible, especially in children (capsules are sweet, colored).

Clinic of iron poisoning:

1) vomiting, diarrhea (feces become black

2) blood pressure drops, tachycardia appears;

3) develops acidosis, shock, hypoxia, gastroenteroco

The fight against acidosis - gastric lavage (3% soda solution). There is an antidote, which is a complexone. This is DEFEROXAMINE (desferal), which is also used for chronic aluminum poisoning. It is prescribed orally, intramuscularly or intravenously by drip at 60 mg / kg per day. Inside is assigned 5-10 grams. If this drug is not available, then TETACIN-CALCIUM can be prescribed intravenously.

Only in the most severe cases of hypochromic anemia, in case of impaired iron absorption, are resorted to drugs for parenteral administration.

FERKOVEN (Fercovenum) is administered intravenously, contains ferrous iron and cobalt. When administered, the drug causes pain along the vein, thrombosis and thrombophlebitis are possible, pain behind the sternum, facial flushing may appear. the drug is highly toxic.

FERRUM-LEK (Ferrum-lec; in amps of 2 and 5 ml) is a foreign drug for intramuscular and intravenous administration containing 100 mg of ferric iron in combination with maltose. Ampoules for intravenous administration contain 100 mg of iron saccharate. The drug for intramuscular injection should not be used for intravenous administration. When prescribing the drug into a vein, the drug should be administered slowly, the contents of the ampoule must first be diluted in 10 ml of isotonic solution.

In the treatment of patients with hyperchromic anemia, vitamin preparations are used:

Vitamin B12 (cyanocobalamin);

Vitamin Bc (folic acid).

Cyanocobalamin is synthesized in the body by the intestinal microflora, and also comes with meat and dairy foods. In the liver, vitamin B12 is converted to coenzyme cobamamide, which is part of various reducing enzymes, in particular reductase, which converts inactive folic acid to biologically active folinic acid.

Thus, vitamin B12:

1) activates the processes of hematopoiesis;

2) activates tissue regeneration;

Cobamamide, in turn, is necessary for the formation of deoxyribose and contributes to:

3) DNA synthesis;

4) completion of erythrocyte synthesis;

5) maintaining the activity of sulfhydryl groups in

glutathione, which protects red blood cells from hemolysis;

6) improvement of myelin synthesis.

For the assimilation of vitamin B12 from food, the internal factor of Castle is needed in the stomach. In its absence, immature erythrocytes - megaloblasts - appear in the blood.

The preparation of vitamin B12 CYANOCOBALAMIN (Cianocobalaminum; vyp. in amp. 0.003%, 0.01%, 0.02% and 0.05% solution) is a means of replacement therapy, it is administered parenterally. In its structure, the drug has groups of cyan and cobalt.

The drug is shown:

In malignant megaloblastic anemia

dison-Birmer and after resection of the stomach, intestines;

With diphylobotriosis in children;

With terminal ileitis;

With diverticulosis, sprue, celiac disease;

With prolonged intestinal infections;

In the treatment of malnutrition in premature babies;

With radiculitis (improves myelin synthesis);

With hepatitis, intoxication (contributes to the formation

choline, which prevents the formation of fat in

hepatocytes);

With neuritis, paralysis.

It is used for hyperchromic anemia and folic acid (vitamin Bc). Its main source is the intestinal microflora. Comes with food (beans, spinach, asparagus, lettuce; egg white, yeast, liver). In the body, it turns into tetrahydrofolic (folinic) acid, necessary for the synthesis of nucleic acids and proteins. This transformation occurs under the influence of reductases activated by vitamin B12, ascorbic acid and biotin.

Especially important is the effect of folinic acid on cell division of rapidly proliferating tissues - hematopoietic and mucosal tissues.

mucosal lining of the gastrointestinal tract. Folinic acid is necessary for the synthesis of hemoproteins, in particular hemoglobin. It stimulates erythro-, leuko- and thrombopoiesis. In chronic folic acid deficiency, macrocytic anemia develops, in acute - agranulocytosis and aleukia.

Indications for use:

Necessarily together with cyanocobalamin with megalob

elastic anemia Addison-Birmer;

During pregnancy and lactation;

in the treatment of patients with iron deficiency anemia,

since folic acid is essential for normal

absorption of iron and its inclusion in hemoglobin;

With non-hereditary leukopenia, agranulocytosis,

some thrombocytopenias;

When prescribing to patients drugs that depress

intestinal flora that synthesize this vitamin (antibi

otiki, sulfonamides), as well as agents that stimulate

that neutralize the function of the liver (antiepileptic

tic agents: difenin, phenobarbital);

Children in the treatment of malnutrition (protein-synthesizing

function);

In the treatment of patients with peptic ulcer (regenerator

function).

DRUGS THAT STIMULATE LEUKOPOIESIS

Leukopoiesis stimulants are prescribed for various types of leukopenia, agranulocytosis (with radiation injuries, severe infectious diseases) and are contraindicated in malignant processes of the hematopoietic system.

SODIUM NUCLEINATE (produced in the form of powders. It is prescribed 0.5-0.6 three times a day after meals. The course of treatment is 10 days. Stimulates leukopoiesis, increases the activity of phagocytes, increases the body's resistance. There are practically no side effects.

PENTOXIL (in tablets of 0, 2). METHYLURACIL (powders, tablets 0.5 each, suppositories with methyluracil 0.5 each, 10% methyluracil ointment 25.0). Pentoxyl and methyluracil are derivatives of pyridine. The drugs have anabolic and anti-catabolic activity. They accelerate the processes of regeneration, wound healing, stimulate cellular and humoral protective factors. It is important that the compounds of this series stimulate erythropoiesis, but especially leukopoiesis, which is the basis for classifying these drugs in the group of leukopoiesis stimulants.

The drugs are shown:

With agranulocytic angina;

With toxic aleukia;

With leukopenia as a result of chemotherapy and radiation therapy

FDI of cancer patients;

With sluggish healing wounds, ulcers, burns, fractures

With a stomach ulcer and duodenal ulcer;

In infectious diseases occurring with a neutral

singing and inhibition of phagocytosis, in mild forms

leukopenia.

Pentoxyl is not used topically due to its irritant effect. A more modern tool refers to tools obtained using recombinant technology. In this regard, the best means of stimulating various hematopoiesis sprouts is the drug MOLGRAMOSTIM (Molgramostimum) or LEUKOMAKS. It is a recombinant human granulocyte-macrophage colony-stimulating factor that activates mature myeloid cells, stimulating the proliferation and differentiation of progenitor cells of the hematopoietic system. The drug leads to an increase in the content of granulocytes, monocytes and T-lymphocytes. After a single injection of leukomax, this effect appears after 4 hours and reaches a peak after 6-12 hours. Leukomax enhances the phagocytosis of neutrophils.

The drug is used for the prevention and correction of neutropenia:

In patients receiving myelosuppressive therapy

(oncology);

In patients with aplastic anemia;

In patients after bone marrow transplantation;

In patients with various infections, including HIV

When treating patients with cytomegalovirus with ganciclovir

Russian retinitis.