Anticoagulants: basic drugs. Anticoagulants - what they are and list of drugs

The liquid state of the blood and the integrity of the bloodstream are necessary conditions for the life of the body. These conditions are created by the blood coagulation system, which keeps 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 (RAS 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 ensures the maintenance of the liquid state of the blood and restoration of the properties of the walls of blood vessels, which change even during their normal functioning. Thus, the body has a special biological system that ensures, on the one hand, the preservation of the liquid state of the blood, and on the other, the prevention and stopping of bleeding by maintaining the structural integrity of the walls of blood vessels and the 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 through the formation of platelet thrombi (primary hemostasis), as well as coagulation enzymatic hemostasis, which ensures the cessation of bleeding through the formation of a fibrin thrombus (stopping bleeding in large vessels).

The fluid state of the blood is ensured by the anticoagulant system. The trigger for blood clotting is damage to blood vessels. Coagulation enzymatic hemostasis occurs in three phases:

PHASE I Formation of prothrombinase (triggered by tissue

high thromboplastin with subsequent formation

I eat blood (platelet and erythrocyte)

prothrombinase).

PHASE II The appearance of prothrombinase means the beginning of second

swarm of blood coagulation phase - formation

thrombin (the process occurs instantly - 2-5 sec

PHASE III Under the influence of thrombin in the third phase

fibrinogen is converted into fibrin. About

fibrin formation and completes the formation

blood clot.

The aggregate (liquid) state of blood is ensured 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.

gulants (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 a third component - the fibrinolysis system, which begins to act simultaneously with clot retraction.

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

The breakdown of fibrin is carried out by the proteolytic enzyme plasmin, which is found in the plasma in the form of plasminogen.

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

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

1. Medicines that promote clotting

blood, which means stopping bleeding (hemostasis)

2. Drugs that reduce blood clotting (antithrom

botic) or drugs for thrombosis and for their

prevention.

Each of these groups is divided into subgroups that have different effects on thrombus formation, the activity of the fibrinolytic system, platelet aggregation and the vascular wall.

I. HEMOSTATICS

1. Coagulants (agents that stimulate the formation

fibrin thrombi):

a) direct action (thrombin, fibrinogen);

b) indirect action (vicasol, phytomenadione).

2. Fibrinolysis inhibitors:

a) synthetic origin (aminocaprono

va and tranexamic acids,

b) animal origin (aprotinin, contri

feces, pantripin, gordox "Gideon"

Richter", Hungary);

3. Stimulators of platelet aggregation (serotonin

adipate, calcium chloride).

4. Agents that reduce vascular permeability:

a) synthetic (adroxon, etamsylate, iprazox

b) vitamin preparations (ascorbic acid,

rutin, quercetin).

c) herbal preparations (crappie

you, yarrow, viburnum, water pepper,

arnica, etc.)

II. ANTI-CLOTTING DRUGS, OR ANTI-CLOTTING DRUGS

TITHROMBOTIC DRUGS:

1. Anticoagulants:

a) direct action (heparin and its preparations,

hirudin, sodium citrate, antithrombin III);

b) indirect action (neodicoumarin, syncumar,

phenyline, fepromarone).

2. Fibrinolytics:

a) direct action (fibrinolysin or plasmin);

b) indirect (plasminogen activators) action

(streptolyase, streptokinase, urokinase, ac

3. Antiplatelet agents:

a) platelet (acetylsalicylic acid,

dipyridamole, pentoxifylline, ticlopidine,

indobufen);

b) erythrocyte (pentoxifylline, reopoliglu

kin, reogluman, rondex).

DRUGS THAT INCREASE BLOOD CLOTTING (HEMOSTATICS)

COAGULANTS

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

1) for local use (thrombin, hemostatic sponge

chelic, fibrin film, etc.)

2) for systemic use (fibrinogen, Vicasol).

TROMBIN (Trombinum; dry powder in amp. 0.1, which corresponds to 125 units of activity; in bottles 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 solution. Typically, the powder in the ampoule is a mixture of thromboplastin, calcium and prothrombin.

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

Lagenova, or simply applying a tampon soaked in thrombin solution.

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 a 5% Ambien solution, administered 1 tablespoon 2-3 times a day) for gastric bleeding or by inhalation for bleeding from the respiratory tract.

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

Fibrinogen is used as an emergency medicine. It is especially effective when there is a deficiency in cases of massive bleeding (placental abruption, hypo and afibrinogenemia, in surgical, obstetric, gynecological and oncological practice).

It is usually prescribed into 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 warmed water for injection. It is administered intravenously by drip or slow stream.

VICASOL (Vicasolum; in tablets, 0.015 and in amps, 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 not caused 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 administration - 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 vitamin K deficiency caused by:

1) bleeding from parenchymal organs;

2) the procedure of exchange blood transfusion, if

they poured canned blood onto (the child);

and also when:

3) long-term use of vitamin K antagonists -

aspirin and NSAIDs (impairing platelet aggregation

4) long-term use of broad-spectrum antibiotics

action (chloramphenicol, ampicillin, tetracycline

lin, aminoglycosides, fluoroquinolones);

5) use of sulfonamides;

6) prevention of hemorrhagic disease of newborns;

7) prolonged diarrhea in children;

8) cystic fibrosis;

9) in pregnant women, especially those suffering from tuberculosis

lesis and epilepsy and receiving appropriate treatment

10) overdose of indirect anticoagulants;

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

diseases (hemorrhoids, ulcers, radiation sickness);

12) preparation for surgery and post-operation

tion period.

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

Side effects: hemolysis of red blood cells when administered intravenously.

PHYTOMENADIONE (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), it is a synthetic preparation. It is 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 quickly absorbed and maintains peak concentration for up to eight hours.

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

Side effects: hypercoagulation phenomena if the dosage regimen is not followed.

Among the drugs related to direct-acting coagulants, the clinic also uses the following drugs:

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

2) antihemophilic globulin (factor VIII).

FIBRINOLYSIS INHIBITORS (ANTIFIBRINOLYTICS)

AMINOCAPRONIC ACID (ACA) 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 clots.

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

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

The drug is low-toxic and is quickly eliminated from the body

with urine (after 4 hours).

Used in emergency clinics, 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

breast and thyroid glands;

2) with premature placental abruption, long-term

retention of a dead fetus in the uterus;

3) for hepatitis, cirrhosis of the liver, for portal hypertension

hypertension, when using the device artificially

low blood circulation;

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

nosebleeds, 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. IN

Due to the fact that ACC has anti-shock activity, inhibits proteolytic enzymes and kinins, inhibits the formation of antibodies, the drug is used for shock reactions and as an antiallergic 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. Ambien inhibits fibrinolysis, its mechanism of action is similar to ACC.

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

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

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

Side effects: rarely allergies; embryotoxic effect; With rapid administration - malaise, nausea.

DRUGS THAT INCREASE PLATELET AGGREGATION AND ADHESION

SEROTONIN. Its use is associated with stimulation of platelet aggregation, tissue swelling, and changes in microcirculation, which contributes to the formation of platelet thrombi. Serotonin in the form of adipate (Serotonini adipinatis in ampoules of 1 ml of 1% solution) is used intravenously or intramuscularly for hemorrhages associated with pathology of blood platelets (thrombocytopenia, thrombocytopathy). At the same time, the number of platelets increases, the bleeding time is shortened, and the resistance of capillaries increases.

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

It should not be used in case of kidney pathology, in patients with bronchial asthma, or in cases of blood hypercoagulation.

Side effect: with rapid administration - pain along the vein; pain in the abdomen, in the heart area, increased 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 blood clots.

Indications for use:

1) as a means of reducing vascular permeability,

with hemorrhagic vasculitis;

2) as a hemostatic agent for pulmonary,

stomach, nose, uterine bleeding, and

also before surgery;

3) for bleeding associated with a decrease in calcium

in blood plasma (after transfusion of large coli

quality of citrated blood, plasma substitutes).

Use calcium chloride (intravenously and orally).

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

DRUGS THAT REDUCE VASCULAR WALL PERMEABILITY

SYNTHETIC PREPARATIONS

ADROXONE (Adroxonum; in amp. 1 ml 0.025%) is a preparation 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 during capillary bleeding, when the permeability of the walls of these vessels is especially increased. However, in case of massive bleeding, the drug is not effective.

Indications for use:

1) with parenchymal and capillary bleeding;

2) for injuries and operations;

3) with intestinal bleeding in newborns;

4) with melena;

5) with platelet purpura.

Adroxon is used topically (tampons, wipes), intramuscularly or subcutaneously. ETHAMSYLAT or dicinone (Ethamsylatum; in tablets of 0.25 and in amps of 2 ml of 12.5% solution) is a synthetic derivative of dioxybenzene. The drug reduces vascular permeability, reduces transudation 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 latter effect develops quickly - with intravenous administration after 5-15 minutes, the most pronounced - after 1-2 hours. In tablets, the effect appears 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 effects - sometimes there is heartburn, a feeling of heaviness in the epigastric region, headache, dizziness, facial flushing, parasthesia of the legs, decreased blood pressure.

VITAMINS PREPARATIONS

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

dation in children suffering from scarlet fever, measles, diphtheria and toxic flu.

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

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

0, 3; ampoules of 5 ml of 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.

ANTI-COLOTTING MEDICINES (ANTITIS)

RHOMBOTIC DRUGS)

ANTICOAGULANTS

1. Anticoagulants (drugs that interfere with the formation of

fibrin thrombi):

a) direct anticoagulants (heparin and its preparations,

hirudin, sodium hydrogen citrate, antit concentrate

rhombin III) - cause an effect in vitro and in

b) indirect anticoagulants (derivatives

oxycoumarin: neodicoumarin, syncumar, pelentan

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

Cause effect only in vivo.

HEPARIN (Heparinum; 5 ml bottle containing 5000, 10000 and 20000 IU per 1 ml, Gedeon Richter, Hungary) is a natural anticoagulant factor produced by mast cells. Heparin is a collective name for a group of linear anionic polyelectrolytes that differ in the number of sulfuric acid residues. There are high and low molecular weight heparins (average molecular weight -

Heparin is a new galenic drug obtained from the lungs and liver of cattle. It is the strongest organic acid due to its sulfuric acid residues and the presence of carboxyl groups, which gives it a very strong negative charge. Therefore, it, in fact, belongs to anionic polyelectrolytes. Due to its negative charge, in the blood heparin combines with positively charged complexes and is sorbed on the surface of the membranes of endothelial cells and macrophages, thereby limiting the aggregation and adhesion of platelets. The effect 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

does not disappear IXa, Xa, XIa and XIIa coagulation factors

2) moderately reduces platelet aggregation;

3) heparin reduces blood viscosity, reduces permeability

blood vessels, which facilitates and accelerates blood flow

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

dits that promote thrombus formation);

4) reduces the content of sugar, lipids and chylomicrons

in the blood, has an antisclerotic effect,

connects some components of a compliment,

the synthesis of immunoglobulins, ACTH, aldosterone melts,

and also binds histamine, serotonin, showing

thereby, antiallergic effect;

5) heparin is potassium-sparing and anti-inflammatory

telny, analgesic effects. Besides,

heparin increases diuresis and reduces

vascular resistance due to expansion of re

positive vessels, eliminates spasm of coronary arteries

Indications for use:

1) for acute thrombosis, thromboembolism (acute in

myocardial infarction, thrombosis of the pulmonary artery, renal

veins, ileocecal vessels), thromboembolism in the

2) when working with artificial blood circulation devices

breastfeeding, artificial kidney and heart;

3) in laboratory practice;

4) for burns and frostbite (improving microcirculation

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

Roma (with fulminant purpura, severe gastrointestinal

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

mom, as well as in complex therapy of patients with glome

roll nephritis;

7) when performing extracorporeal hemodialysis,

hemosorption and forced diuresis;

8) with hyperaldosteronism;

9) as an antiallergic agent (bronchial

10) in a complex of therapeutic measures for 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; inject slowly).

At one time, on average, 10,000 units are administered intravenously to a patient with acute thrombosis. Per day up to 40,000 - 50,000 units intravenously, administered slowly. Can be administered intramuscularly and subcutaneously (in the area of least vascularization). In recent years, to prevent thrombosis, it has been recommended to administer 5000 units 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 units/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 (hirudont, etc.) is a product of leeches. The anticoagulant and anti-inflammatory effects of these drugs are used. 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 citric acid anion combines with the calcium ion, which binds the activity of the latter. The substance is added in excess. The patient should not use it, since sodium hydrogen citrate 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 a patient is transfused with up to 500 ml of canned blood, this does not require any additional measures. If blood is transfused in a volume of more than 500 ml, then for every 50 ml in excess of 500 ml of the volume of transfused blood, add 5 ml of a 10% calcium chloride solution.

INDIRECT ACTION ANTICOAGULANTS (PERO

RAL ANTICOAGULANTS)

Of the large number of anticoagulants, the most common are drugs of the coumarin group. There are many drugs, but the most commonly used are neodicoumarin (pelentan), syncumar, fepromarone, phenylin, amefine, and farfavin.

NEODICUMARIN (Neodicumarinum; in tablets 0.05 and 0.1), syncumar, dicoumarin, fepromarone, omefin, phenyline - phenylindandione derivatives, very similar in pharmacodynamics. Their mechanism of action is due 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 blood clotting factors IX and X, which are necessary for coagulation homeostasis, that is, for the formation of fibrin clots. These drugs do not act immediately, but after 8-24 hours, that is, they are slow-acting agents with cumulative properties. Moreover, different drugs in this group have different speeds and strengths of action, and different degrees of accumulation. Another feature of their action is their long duration of action.

These drugs are used only orally, as they are well absorbed, then they are brought back to the intestine through the bloodstream, released into its lumen and absorbed again (recirculation). All drugs form a weak bond with plasma proteins and are easily displaced from it by other drugs. Act only in vivo.

Indications for use:

1) to reduce blood clotting for professional purposes

lactation and treatment of thrombosis, thrombophlebitis and

thromboembolism (myocardial infarction), embolic

strokes;

2) in surgery to prevent thrombosis in

postoperative period.

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

1) open wounds, stomach ulcers;

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).

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

Fibrin degradation products have anticoagulant properties because 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 blood vessels in the brain, eyes;

IHD (myocardial infarction);

When removing a blood clot from a vascular shunt.

This drug has significant disadvantages: - it is very expensive (it is made from donor blood); - not very active, does not penetrate well into the blood clot. Side effects from the administration of fibrinolysin, a foreign protein, can occur in the form of allergic reactions, as well as nonspecific reactions to the protein (facial hyperemia, 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 units of fibrinolysin per 1 ml of solvent. The prepared solution is poured intravenously (10-15 drops per minute).

INDIRECT ACTION FIBRINOLYTICS

STREPTOKINASE (streptase, avelysin; available in amps containing 250,000 and 500,000 units of the drug) is a more modern drug, an indirect fibrinolytic. It is obtained from beta-hemolytic streptococcus. This is a more active and cheaper drug. It stimulates the transition of the proactivator to the activator, transforming profibrinolysin into fibrinolysin (plasmin). The drug is able to penetrate inside the blood clot (activating fibrinolysis in it), which distinguishes it favorably from fibrinolysin. Streptokinase is most effective when

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

3) with septic thrombosis;

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

effects: 1) allergic reactions (antibodies to strep

tokokkam); 2) hemorrhages; 3) drop in hemoglobin level

bina, red blood cell hemolysis

(direct toxic effect);

4) vasopathy (formation of CEC).

In our country, based on streptokinase, STREPTODECASE was synthesized, a similar drug with a longer-lasting effect. Allergic reactions to this drug are also possible.

UROKINASE is a drug synthesized from urine. It is considered a more modern remedy and produces less allergic reactions than streptokinase.

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

MEDICINES INTERPEDING PLATELET AGGREGATION

(ANTIAGREGANTS)

Antiplatelet agents - a group of anticoagulants:

1. Platelet (acetylsalicylic acid (ASA),

heparin, dipyridamole, ticlopidine, indobufen, pen

toxifylline).

2. Erythrocyte (pentoxifylline, rheopolyglucin).

ACETYLSALICYLIC ACID (Acidum acetylsalicylicum; in tablets of 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, quickly decreases in them.

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

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

1. Prevention of platelet aggregation by ASA when using very small 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 the formation of another prostaglandin - prostacyclin J2. The latter prevents platelet aggregation and adhesion, and also causes vasodilation.

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

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

Taking these facts into account, one can understand why, when taking small doses of ASA, coagulation is reduced 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) for hypertension;

4) with atherosclerosis.

As an antiplatelet drug, the drug is prescribed according to the following 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, MIKRISTIN was released - a granular microcrystalline preparation of ASA, enclosed in a polyvinyl acetate shell.

For similar indications, indobufen and indomethacin are also prescribed.

DIPIRIDAMOLE (Dypiridomalum; synonyms: chimes, persantyl; in tablets or tablets of 0.025 and 0.075, as well as in amps of 2 ml of 0.5% solution) - 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 antiaggregation effects and a slight decrease in blood pressure. Thus pre

Parat dilates the coronary vessels and increases the speed 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 syndrome (in combination

with heparin);

3) for the prevention of DIC syndrome during infectious diseases

toxicosis, septicemia (shock);

4) during dehydration;

5) in patients with prosthetic heart valves;

6) during hemodialysis;

7) for angina pectoris and myocardial infarction.

Side effects: short-term redness of the face, tachycardia, allergic reactions. A modern antiplatelet agent is the drug TICLOPIDINE (Ticlopidinum; synonym - ticlid; in tablets of 0.25) - a new selective antiplatelet agent that is superior in potency to ASA.

Tiklid 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) ischemia of the limbs;

4) retinopathy (diabetes mellitus, etc.);

5) when shunting blood vessels.

Side effects: stomach pain, diarrhea, rash, dizziness, jaundice, decreased white blood cell and platelet counts.

Plasma replacement 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 reopolyglucin (especially this drug), as well as reogluman, rondex. These agents “dilute” the blood, reduce its viscosity, envelop platelets and red blood cells, which contributes to their antiplatelet effect, improve the movement of fluid from tissues to vessels, increase blood pressure, and have a detoxification effect.

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

Side effects: allergic reactions.

Platelet antiplatelet agents are drugs from the methylxanthine group: aminophylline, as well as teonicol (xanthinol nicotinate, complavin, xavin), etc.

TEONIKOL (xanthinol nicotinate; in tablets 0, 15 and

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

Indications for use:

1) vascular spasms 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.

MEDICINES INTERPENDING RED CYTE AGGREGATION

PENTOXYPHYLLINE or trental (Pentoxyphillinum; in tablets of 0, 1 and in amps of 5 ml of 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 promotes the bendability of red blood cells, which improves their passage through the capillaries (the diameter of red blood cells is 7 microns, and the diameter of capillaries is 5 microns).

Since trental increases the bendability of red blood cells, limits the aggregation of blood cells, and reduces the level of fibrinogen, it ultimately reduces the viscosity of the blood and makes it more fluid, reducing resistance to blood flow. Improvement in the rheological properties of blood occurs slowly. The effect occurs after 2-4 weeks.

Indications for use:

1) for peripheral circulatory disorders:

Raynaud's disease;

Diabetic angiopathy;

Vascular pathology of the eye;

2) for disorders of the cerebral and coronary blood flow

3) with circulatory shock.

Trental is contraindicated during pregnancy, in patients with hemorrhages and myocardial infarction. Undesirable effects: nausea, anorexia, diarrhea, dizziness, facial flushing.

DRUGS AFFECTING BLOODOOSIS

ANTIANEMIC DRUGS

Antianemic drugs 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 deficiency, folate deficiency

cit, E-deficient);

Protein (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 due to 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 DRUGS USED FOR

HYPOCHROMIC ANEMIA

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

Insufficient supply of iron to the fetus

and child;

Poor absorption from the intestine (mal syndrome

absorption, inflammatory bowel disease,

taking tetracyclines and other antibiotics);

Excessive blood loss (helminthic infestation, nasal and

hemorrhoidal bleeding);

Increased iron consumption (intensive growth, in

Iron is an essential component of a number of enzymes of both hemin and non-hemin structures. Hemin enzymes: - hemo- and myoglobin;

Cytochromes (P-450);

Peroxidases;

Catalase.

Non-heme enzymes: - succinate dehydrogenase;

Acetyl-CoA dehydrogenase;

NADH dehydrogenase etc.

With a lack of iron, the hemoglobin content 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. Trivalent iron received from food is converted into divalent iron under the influence of hydrochloric acid of the stomach. Calcium, phosphates contained in milk, especially cow's milk, phytic acid, tetracyclines interfere with the absorption of iron. The maximum amount of iron (ferrous that 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 cell

zistoy and release it into the blood. Iron in the blood

oxidizes 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 hematopoietic organs (bone marrow) or storage organs (liver, spleen).

To treat patients with hypochromic anemia, drugs are used, prescribed both orally and by injection.

Preferably ferrous iron preparations are used internally, as 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;

Gemostimulin; - ferroplex;

Conferon; - ferrocerone;

Aloe syrup with iron; - ferramide.

2. Inorganic iron preparations:

Ferrous sulfate;

Ferric chloride;

Iron carbonate.

The most accessible and cheapest drug is ferrous iron sulfate (Ferrosi sulfas; tablets of 0.2 (60 mg iron)) and powders in gelatin capsules of 0.5 (200 mg iron)). This preparation contains a high concentration of pure iron.

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

ALOE SYRUP WITH IRON (in 100 ml bottles) contains a 20% solution of ferrous chloride, 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 common.

FERROCAL (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 is a dragee containing ferrous sulfate and ascorbic acid. The latter sharply increases iron absorption.

The drug FEFOL is a combination of iron and folic acid.

Prolongiro drugs are considered more modern

bath action (TARDIFERON, FERRO - GRADUMET), manufactured using a special technology on an inert plastic sponge-like substance, from which iron is gradually released.

There are many drugs, you can use any, but you must remember that the therapeutic effect does not develop immediately, but after 3-4 weeks of taking the medicine. Repeated courses are often required. This means that side effects are primarily associated with the irritating effect of iron ions on the gastrointestinal mucosa (diarrhea, nausea). 10% of patients develop constipation because 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 (sweet, colored capsules).

Iron Poisoning Clinic:

1) vomiting, diarrhea (stool turns black

2) blood pressure drops, tachycardia appears;

3) acidosis, shock, hypoxia, gastroenterocco develops

The fight against acidosis is 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 at a dose of 60 mg/kg per day. 5-10 grams are prescribed orally. If this drug is not available, then you can prescribe TETACIN-CALCIUM intravenously.

Only in the most severe cases of hypochromic anemia, when iron absorption is impaired, do they resort to drugs for parenteral administration.

FERKOVEN (Fercovenum) is administered intravenously, contains divalent iron and cobalt. When administered, the drug causes pain along the vein, thrombosis and thrombophlebitis are possible, chest pain and facial hyperemia may appear. the drug is very toxic.

FERRUM-LEK (Ferrum-lec; in amp. 2 and 5 ml) is a foreign drug for intramuscular and intravenous administration containing 100 mg of ferric iron in combination with maltose. The ampoules for intravenous administration contain 100 mg of iron sucrose. The drug for intramuscular injection cannot 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 an isotonic solution.

When treating patients with hyperchromic anemia, vitamin preparations are used:

Vitamin B12 (cyanocobalamin);

Vitamin BC (folic acid).

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

Thus, vitamin B12:

1) activates hematopoietic processes;

2) activates tissue regeneration;

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

3) DNA synthesis;

4) completion of red blood cell synthesis;

5) maintaining the activity of sulfhydryl groups in

glutathione, which protects red blood cells from hemolysis;

6) improvement of myelin synthesis.

To absorb vitamin B12 from food, intrinsic Castle factor is needed in the stomach. In its absence, immature red blood cells appear in the blood - megaloblasts.

Vitamin B12 preparation CYANOCOBALAMIN (Cianocobalaminum; dispensed in 1 ml amps of 0.003%, 0.01%, 0.02% and 0.05% solution) is a means of replacement therapy, administered parenterally. In its structure, the drug has cyanide and cobalt groups.

The drug is indicated:

For malignant megaloblastic anemia

Dison-Biermer and after resection of the stomach and intestines;

With diphylbothriasis in children;

With terminal ileitis;

For diverticulosis, sprue, celiac disease;

For long-term intestinal infections;

In the treatment of malnutrition in premature infants;

For radiculitis (improves myelin synthesis);

For hepatitis, intoxication (promotes the formation of

the presence of choline, which prevents the formation of fat in

hepatocytes);

For neuritis, paralysis.

Folic acid (vitamin Bc) is also used for hyperchromic anemia. Its main source is intestinal microflora. It also comes from food (beans, spinach, asparagus, lettuce; egg whites, yeast, liver). In the body, it is converted 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.

The influence of folinic acid on the division of cells of rapidly proliferating tissues - hematopoietic and blood cells - is especially important.

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

Indications for use:

Mandatory together with cyanocobalamin for megalob

plastic Addison-Birmer anemia;

During pregnancy and lactation;

When treating patients with iron deficiency anemia,

since folic acid is necessary for normal

absorption of iron and its inclusion in hemoglobin;

For non-hereditary leukopenia, agranulocytosis,

some thrombocytopenias;

When prescribing drugs to patients that depress

intestinal flora that synthesizes this vitamin (antibi

otics, sulfonamides), as well as agents that stimulate

neutralizing liver function (antiepileptic

tic agents: diphenin, phenobarbital);

For children in the treatment of malnutrition (protein synthesizing

function);

In the treatment of patients with peptic ulcer (regenerator

function).

DRUGS STIMULATING LEUKOPOIESIS

Stimulators of leukopoiesis 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 (available in the form of powders. 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, suppositories with methyluracil 0.5, 10% methyluracil ointment 25.0). Pentoxyl and methyluracil are pyridine derivatives. The drugs have anabolic and anti-catabolic activity. They accelerate the processes of regeneration and wound healing, stimulate cellular and humoral protection factors. An important fact is that compounds of this series stimulate erythro-, but especially leukopoiesis, which is the basis for classifying these drugs into the group of leukopoiesis stimulants.

Drugs are indicated:

For agranulocytic sore throat;

For toxic aleukia;

For leukopenia as a result of chemotherapy and radiation therapy

PI for cancer patients;

For slow healing wounds, ulcers, burns, fractures

For stomach and duodenal ulcers;

For infectious diseases occurring with neutro

singing and inhibition of phagocytosis, in mild forms

leukopenia.

Pentoxyl is not used topically due to its irritating effect. A more modern remedy is one obtained using recombinant technology. In this regard, the best means of stimulating various germs of hematopoiesis is the drug MOLGRAMOSTIMUM or LEUCOMAX. This is a recombinant human granulocyte-macrophage colony-stimulating factor that activates mature myeloid cells, stimulating the proliferation and differentiation of precursor 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 Leucomax, this effect appears after 4 hours and reaches its peak after 6-12 hours. Leucomax 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-in

When treating patients with cytomegalovir with ganciclovir

Russian retinitis.

Drugs that increase blood clotting are called coagulants. They have their own characteristics in use, have a positive effect on the body, and help prevent and stop bleeding. Modern pharmacological companies produce a wide variety of products that allow you to cope with the problem as quickly as possible.

General information

Drugs that increase blood clotting are also called hemostatics. Their action can be direct or indirect, and their activity in the body also varies. Some drugs exhibit it exclusively inside the body. Medicines differ in the specifics of their effects.

The inclusion of biological components of the blood coagulation system is characteristic of the group of direct coagulants. This series contains drugs that are intended exclusively for local use. Some drugs are injected into the blood only by injection. There are direct contraindications to therapy.

Among them are:

high blood clot formation in humans;
myocardial infarction;
history of increased blood clotting.

A group of drugs based on vitamin K is made up of coagulants with indirect action. It also includes some drugs with hormonal properties. These drugs are taken orally. These can be tablets or injections.

Any medications that affect the blood system are prescribed by a doctor. Medicines are used only under his supervision, so you should not self-medicate.

Drug Thrombin

Increasing blood clotting is performed through medication in the form of a dry powder in ampoules. Activity is 125 units. The medication is a direct-acting coagulant for local use.

Since the drug is a natural component of the blood coagulation system, it is able to provoke effects in vivo and in vitro.

Before the therapeutic effect on the body begins, the product must be properly prepared. The powder is added to the saline solution. The ampoule contains a mixture that includes:

calcium;
thromboplastin;
prothrombin.

The medication is prescribed exclusively for local use to patients who have bleeding from small vessels and parenchymal organs. These may be cases of traumatic exposure during operations on the kidneys, lungs, brain, liver. Used for bleeding gums. Application is indicated using a hemostatic or collagen sponge, which is soaked in Thrombin solution. You can also apply a swab moistened with liquid to the desired area.

Cases of using Thrombin orally are not excluded. This is often found in pediatrics. The contents of the ampoules are dissolved in sodium chloride (50 ml) or Ambien 5% (50 ml). The drug is prescribed 2 or 3 times a day for gastric bleeding. Another option for therapy is inhalation, when bleeding through the respiratory tract is observed.

Fibrinogen

How to increase blood clotting? Patients are often prescribed Fibrinogen. It is sold in bottles that contain a porous mass. A medication is prescribed to provide a systemic effect on the body. It can be obtained from the blood plasma of a donor. After administration, the active component of the drug can be converted into fibrin, which forms blood clots.

The drug Fibrinogen is used for surgical treatment of the body and emergency therapy. The maximum degree of effectiveness is visible when there is a lack of substance in the body, if massive bleeding is observed. We are talking about placental abruption, with afibrinogenemia.

The medicine is actively used in the practice of oncologists, obstetricians, and gynecologists.

To increase blood clotting, the drug is preferably administered into a vein. Local use as a film, which is applied to the bleeding area of the surface, is possible. Before use, the composition is dissolved in 250-500 ml of water to perform the injection. Patients are shown drip or jet intravenous administration at a slow pace.

Effective Vikasol

If necessary, a medication can be used to increase blood clotting, which can be purchased at pharmacies in the form of tablets or as a solution in ampoules. The drug is an indirect coagulant. This is an analogue of vitamin K, which is of synthetic origin. It is water soluble. With its help, it is possible to improve the process associated with the formation of fibrin blood clots. In medicine, the drug is referred to as vitamin K3.

It is possible to obtain a pharmacological effect thanks not to Vikasol itself, but to the vitamins that are synthesized from it. These are connections K1, K2. For this reason, the result is noticeable within 12-24 hours. If the drug is administered intravenously, the effect is observed after half an hour. Intramuscular use allows you to see a positive effect after 2-3 hours. The need for the mentioned vitamins is noted in the process of synthesis of prothrombin, proconvertin and other factors of liver function.

The medication is prescribed for an excessive reduction in the prothrombin index or for severe vitamin K deficiency. Elimination of the last deviation is carried out when it is provoked by a replacement blood transfusion or bleeding from parenchymal organs. Other reasons:

long-term use of vitamin K antagonists;
carrying out long-term therapy using antibacterial drugs with a wide spectrum of action;
use of sulfonamides;
prevention of hemorrhagic disease in infants;
prolonged diarrhea in childhood;
cystic fibrosis;
pregnancy in a woman who suffers from epilepsy, tuberculosis and receives symptomatic therapy;
overdose of anticoagulants with indirect action;
hepatitis, jaundice, wounds, bleeding;
preparation for surgical intervention, postoperative period.

The effectiveness of therapy with the drug Vikasol is sometimes weakened if the patient is simultaneously prescribed antagonists of the drug. These are NSAIDs, indirect anticoagulants included in the neodicoumarin group, PAS, aspirin. Treatment with the drug is carried out in strict compliance with the doctor’s prescriptions and instructions. Vikasol may cause side effects. For example, hemolysis of red blood cells when the drug is administered intravenously.

The drug Phytomenadione

Increased blood clotting is achieved with the help of this medication. For intravenous administration, a dose of 1 ml is used. Tablets (capsules) contain 0.01 substances. They contain an oil solution of 10%. Compared to natural vitamin K1, the drug is a synthetic product. It has a racemic form, but within the framework of biological activity it retains the entire set of properties inherent in the mentioned vitamin. Absorption of the active component occurs quickly. Peak concentration levels can be maintained for 8 hours.

Phytomenadione, which improves blood clotting, is prescribed in a number of cases:

ulcerative colitis;
overdose of anticoagulants;
hemorrhagic syndrome with hypoprothrombinemia, which is provoked by a deterioration in the functioning of the liver;
long-term treatment with antibiotics that have a broad spectrum of action;
long-term therapy with sulfonamides;
before major surgery on the body to eliminate the high risk of bleeding.

Since the medicine allows you to improve blood clotting, it is in demand. However, you need to pay attention to the presence of side effects on the body.

This is a phenomenon of hypercoagulation when the dosage prescribed by the doctor is not followed.

Other agents that affect coagulation and are classified as direct-acting coagulants are antihemophilic globulin, prothrombin complex. In folk medicine, after consultation with a doctor, special medicinal herbs are used, since in some cases they can cause harm. Pharmacies sell medicines that are of plant origin. They may contain nettle, yarrow, viburnum, and water pepper. They allow you to get positive results.

Other medicines

Fibrinolysis inhibitors may be prescribed to increase blood clotting. Aminocaproic acid is a synthetic drug in powder form that is highly effective. It helps to inhibit the conversion of plasminogen to plasmin. The manipulation is carried out due to the influence on the activator profibrinolysin. Due to this, fibrin blood clots are preserved.

This drug is an inhibitor of kinins, individual provocateurs of the compliment system. In addition to increasing blood clotting, the drug has antishock activity. The drug is characterized by low toxicity and rapid elimination from the body. It occurs along with urine after 4 hours.

The use of the drug is very extensive. ACC is administered during a massive transfusion to increase the clotting of preserved blood. It is usually prescribed orally or intravenously. ACC can be used for therapy as an antiallergic agent. During treatment, side effects are likely to develop.

Ambien affects blood clotting. The drug is synthetic, the chemical structure is similar to para-aminobenzoic acid. Antifibrinolytic drug. Ambien inhibits fibrinolysis. The mechanism of action is similar to ACC.

A medication that increases blood clotting can be prescribed orally, intramuscularly, or intravenously. Produced in the form of tablets, 1% solution in ampoules. An increased volume of the drug on its own can provoke the development of side effects.

In some cases, antienzyme agents are prescribed. For example, Kontrikal. It is indicated for use in local hyperfibrinolysis, postoperative, post-portal bleeding, etc. Side effects are likely to develop. If the composition is administered quickly, nausea and malaise may occur. In rare cases, patients develop allergies.

Only the attending physician can prescribe the best drug. He knows the characteristics of the body and the clinical picture of the disease. It is strictly contraindicated to choose a remedy or change the dosage on your own. If the medication causes side effects, you can contact your doctor to replace the medication with a similar one.

In contact with

Anticoagulants are a group of drugs that inhibit blood clotting and prevent blood clots by reducing the formation of fibrin.

Anticoagulants affect the biosynthesis of certain substances that inhibit clotting processes and change blood viscosity.

In medicine, modern anticoagulants are used for preventive and therapeutic purposes. They are available in different forms: as ointments, tablets or injection solutions.

Only a specialist can choose the right medications and select their dosage.

Improperly administered therapy can harm the body and cause serious consequences.

The high mortality rate due to cardiovascular diseases is explained by the formation of blood clots: thrombosis was detected in almost half of those who died from cardiac pathology.

Venous thrombosis and pulmonary embolism are the most common causes of disability and mortality. Therefore, cardiologists recommend starting to use anticoagulants immediately after detection of vascular and heart diseases.

Their early use helps prevent the formation and enlargement of a blood clot and clogging of blood vessels.

Most anticoagulants do not act on the blood clot itself, but on the blood coagulation system.

After a series of transformations, plasma clotting factors are suppressed and thrombin is produced, an enzyme required to create fibrin threads that form a thrombotic clot. As a result, thrombus formation slows down.

Use of anticoagulants

Anticoagulants are indicated for:

Contraindications and side effects of anticoagulants

Anticoagulants are contraindicated for people suffering from the following diseases:

Bleeding hemorrhoids;
Peptic ulcer of the duodenum and stomach;
Kidney and liver failure;
Liver fibrosis and chronic hepatitis;
Thrombocytopenic purpura;
Urolithiasis disease;
Deficiency of vitamins C and K;
Cavernous pulmonary tuberculosis;
Pericarditis and endocarditis;
Malignant neoplasms;
Hemorrhagic pancreatitis;
Intracerebral aneurysm;
Myocardial infarction with hypertension;
Leukemia;
Crohn's disease;
Alcoholism;
Hemorrhagic retinopathy.

Anticoagulants should not be taken during menstruation, pregnancy, lactation, in the early postpartum period, or in the elderly.

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

Complications of therapy - bleeding from internal organs:

Nasopharynx;
Intestines;
Stomach;
Hemorrhages in joints and muscles;
The appearance of blood in the urine.

To prevent the development of dangerous consequences, it is necessary to monitor the patient’s condition and monitor blood counts.

Natural anticoagulants

They can be pathological and physiological. In some diseases, pathological ones appear in the blood. Physiological ones are normally found in plasma.

Physiological anticoagulants are divided into primary and secondary. The former are independently synthesized by the body and are constantly present in the blood. Secondary ones appear when coagulation factors are broken down during the formation and dissolution of fibrin.

Primary natural anticoagulants

Classification:

Antithrombins;
Antithromboplastins;
Inhibitors of fibrin self-assembly.

When the level of primary physiological anticoagulants in the blood decreases, the risk of thrombosis appears.

This group of substances includes the following list:

Secondary physiological anticoagulants

Formed during the process of blood clotting. They also appear when clotting factors are broken down and fibrin clots dissolve.

Secondary anticoagulants - what are they:

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

Pathological anticoagulants

With the development of a number of diseases, strong immune coagulation inhibitors, which are specific antibodies, like the lupus anticoagulant, can accumulate in the plasma.

These antibodies indicate a certain factor; they can be produced to combat the manifestations of blood clotting, however, according to statistics, these are inhibitors of factors VII, IX.

Sometimes, during a number of autoimmune processes, pathological proteins that have an antithrombin or inhibitory effect can accumulate in the blood and paraproteinemia.

Mechanism of action of anticoagulants

These are drugs that affect blood clotting and are used to reduce the risk of blood clot formation.

Due to the formation of blockages in organs or blood vessels, the following may develop:

Gangrene of the limbs;
Ischemic stroke;
Thrombophlebitis;
Cardiac ischemia;
Inflammation of blood vessels;
Atherosclerosis.

According to the mechanism of action, anticoagulants are divided into drugs with direct/indirect action:

"Direct"

They act directly on thrombin, reducing its activity. These drugs are prothrombin deactivators, thrombin inhibitors and inhibit thrombus formation. To prevent internal bleeding, it is necessary to monitor the parameters of the coagulation system.

Direct anticoagulants quickly enter the body, are absorbed into the gastrointestinal tract and reach the liver, have a therapeutic effect and are excreted in the urine.

They are divided into the following groups:

Heparins;
Low molecular weight heparin;
Hirudin;
Sodium hydrogen citrate;
Lepirudin, danaparoid.

Heparin

The most common anti-clotting agent is Heparin. This is a direct acting anticoagulant drug.

It is administered intravenously, intramuscularly and subcutaneously, and is also used as an ointment as a local remedy.

Heparins include:

Adreparin;
Nadroparin sodium;
Parnaparin;
Dalteparin;
Tinzaparin;
Enoxaparin;
Reviparin.

Local antithrombotic drugs are not very effective and have low tissue permeability. Used to treat hemorrhoids, varicose veins, and bruises.

The following drugs are most often used with heparin:

Heparins for subcutaneous and intravenous administration are anti-clotting drugs that are individually selected and are not replaced by one another during the treatment process, since they are not equivalent in action.

The activity of these drugs reaches a maximum after about 3 hours, and the duration of action is a day. These heparins block thrombin, reduce the activity of plasma and tissue factors, prevent the formation of fibrin threads and prevent platelet aggregation.

For the treatment of angina pectoris, heart attack, pulmonary embolism and deep vein thrombosis, Deltaparin, Enoxaparin, Nadroparin are usually prescribed.

To prevent thrombosis and thromboembolism, Reviparin and Heparin are prescribed.

Sodium hydrogen citrate

This anticoagulant is used in laboratory practice. It is added to test tubes to prevent blood clotting. It is used for the preservation of blood and its components.

"Indirect"

They influence the biosynthesis of side enzymes of the coagulation system. They do not suppress the activity of thrombin, but completely destroy it.

In addition to the anticoagulant effect, drugs in this group have a relaxing effect on smooth muscles, stimulate blood supply to the myocardium, remove urates from the body and have a hypocholesterolemic effect.

“Indirect” anticoagulants are prescribed for the treatment and prevention of thrombosis. They are used exclusively internally. The tablet form is used for a long time in an outpatient setting. Abrupt withdrawal leads to increased prothrombin and thrombosis.

These include:

Substances	Description
Coumarin	Coumarin is naturally found in plants (clover, bison) in the form of sugars. Dicoumarin, a derivative isolated from clover in the 1920s, was first used in the treatment of thrombosis.
Indane-1,3-dione derivatives	Representative - Fenilin. This oral drug is available in tablets. The action begins 8 hours after administration, and maximum effectiveness occurs a day later. When taking it, it is necessary to check the urine for the presence of blood, and also monitor the prothrombin index.

“Indirect” drugs include:

Neodicoumarin;
Warfarin;
Acenocoumarol.

Warfarin (thrombin inhibitors) should not be taken in case of certain diseases of the liver and kidneys, thrombocytopenia, with a tendency to bleeding and acute bleeding, during pregnancy, with disseminated intravascular coagulation syndrome, congenital deficiency of proteins S and C, lactase deficiency, if the absorption of glucose and galactose is impaired.

Side effects include nausea, vomiting, abdominal pain, diarrhea, bleeding, nephritis, alopecia, urolithiasis, allergies. Itching, skin rash, vasculitis, eczema may occur.

The main disadvantage of Warfarin is the increased risk of bleeding (nasal, gastrointestinal and others).

New generation oral anticoagulants (NOACs)

Anticoagulants are essential drugs used in the treatment of many pathologies, such as thrombosis, arrhythmias, heart attacks, ischemia and others.

However, medications that have proven to be effective have many side effects.. Development continues, and new anticoagulants occasionally appear on the market.

Scientists are striving to develop universal remedies that are effective for various diseases. Products are being developed for children and patients for whom they are contraindicated.

New generation blood thinners have the following advantages:

The effect of the drug comes and goes quickly;
When taken, the risk of bleeding is reduced;
The drugs are indicated for patients who cannot take Warfarin;
Inhibition of thrombin-binding factor and thrombin is reversible;
The influence of food consumed, as well as other medications, is reduced.

However, new drugs also have disadvantages:

Must be taken regularly, whereas older medications can be skipped due to their long-lasting effects;
Lots of tests;
Intolerance by some patients who could take old pills without side effects;
Risk of bleeding in the gastrointestinal tract.

The list of new generation drugs is small.

New drugs Rivaroxaban, Apixaban and Dabigatran may be an alternative in case of atrial fibrillation. Their advantage is that there is no need to constantly donate blood during use, and they do not interact with other drugs.

However, NOACs are equally effective with no greater risk of bleeding.

Antiplatelet agents

They also help thin the blood, but they have a different mechanism of action: antiplatelet agents prevent platelets from sticking together. They are prescribed to enhance the effect of anticoagulants. In addition, they have a vasodilator and antispasmodic effect.

The most famous antiplatelet agents:

Aspirin is the most common antiplatelet agent. An effective blood thinner, dilates blood vessels and prevents blood clots;
Tirofiban – interferes with platelet adhesion;
Eptifibatitis – inhibits platelet aggregation;
Dipyridamole is a vasodilator;
Ticlopidine - used for heart attacks, cardiac ischemia and for the prevention of thrombosis.

The new generation includes Brilint with the substance ticagrelor. It is a reversible antagonist of the P2Y receptor.

Conclusion

Anticoagulants are indispensable drugs in the treatment of pathologies of the heart and blood vessels. They cannot be taken on their own.

Anticoagulants have many side effects and contraindications, and uncontrolled use can cause bleeding, including hidden bleeding. The prescription and calculation of dosage are carried out by the attending physician, who can take into account all possible risks and features of the course of the disease.

During treatment, regular laboratory monitoring is required.

It is very important not to confuse anticoagulants and antiplatelet agents with thrombolytic agents. The difference is that anticoagulants do not destroy the blood clot, but only slow down or prevent its development.

The blood system (coagulation and anticoagulation) in the human body is in constant dynamic equilibrium. This is why the outflow of blood is not hampered and the veins are not thrombosed.

But as soon as this balance begins to be disturbed, a favorable environment is created for vascular thrombosis, and in severe cases (shock, trauma, sepsis), disseminated intravascular coagulation syndrome can occur, which can cause death.

Cases in which blood clotting is increased

In the human body, blood clotting increases due to disseminated intravascular coagulation syndrome, as well as in the presence of venous and arterial acute thrombosis.

DIC syndrome:

Various injuries
Sepsis (as a result of large release of blood clotting factors from tissues)

Acute arterial thrombosis:

Myocardial infarction
PE (blockage of the pulmonary artery by numerous blood clots)
Ischemic stroke
Injuries of the arteries that occurred against the background or inflammatory process and are acute in nature

Acute venous thrombosis:

Against the background of varicose veins of the lower extremities, phlebitis
Thrombosis of hemorrhoidal veins
Thrombosis in the inferior vena cava system

Therefore, at an early stage of pathology, it is necessary to undergo a course of examination and treatment.

In case of cardiovascular diseases, despite the prescribed treatment, it is necessary to take proactive measures. Therefore, anticoagulant drugs are used as a prophylaxis for unstable angina, atrial fibrillation, and heart valve defects. In addition, a course of prophylaxis will be prescribed for patients who are directly on hemodialysis, or after various heart surgeries.

Anticoagulant drugs are often prescribed as treatment for various diseases. However, first you need to know what an anticoagulant is. These are drugs that help reduce blood clotting and restore its rheological properties. In addition, the medicine prevents the re-formation of thrombosis.

The classification distinguishes two types of anticoagulants, which have different actions. The first group includes direct-acting drugs, the so-called direct anticoagulants. The second group includes already indirect ones, they are also called indirect anticoagulants.

How to choose the right anticoagulants - heparins?

I often use medications to prevent blood clots and thromboembolism. Klivarin and Troparin.

To treat thromboembolic complications, such as heart attack, pulmonary embolism or unstable angina, broad-spectrum drugs are used. These include anticoagulant drugs from the following list:

Fragmin
Clexane
Fraxiparine

If the patient is on hemodialysis, then drugs are used to prevent thrombosis Fragmin, Fpaxiparin.

Side effects of the drug:

bleeding;
nausea to the point of vomiting;
diarrhea;
severe pain in the abdominal area;
hives;
eczema;
vasculitis;
urolithiasis disease;
necrosis;
hair loss;
itching of the skin.

Medicines that enhance the effect of Warfarin: Allopurinol, Digoxin, Amiodarone, Sulindac, Sulfapyrazone, Testosterone, Danazol, Tamoxifen, Glibenclamide, Ifosfamide, Methotrexate, Etoposide, Metolazone, Piroxicam, Omeprazole, Simvastatin, Bezafibrate, Clofibrate, Fenofibrate, Vitamins A and E, Glucagon, Cimetidine.

What is INR and why should it be determined?

INR is the International Normalized Ratio. In fact, this is the time during which blood begins to clot in the human body. Therefore, it is worth noting that the higher the INR, the worse a person’s blood begins to clot. Normal values are considered to be a number in the range of 0.85–1.25, obtained as the ratio of the patient’s prothrombin time to the standard prothrombin time.

INR is an indicator of blood clotting that influences the patient's prescription of Warfarin or any other anticoagulant. Also, with the help of INR, the following is carried out:

monitoring the effectiveness of therapeutic treatment;
dosage adjustment;
assessment of the risks of complications.

The normal value for treatment with Warfarin should reach 2–3 units.

In order to select the correct dosage of the drug and stabilize the INR to 3 units, at least 10 days must pass. After which it is necessary to monitor the dose of the drug, which is carried out once every 2-4 weeks.

INR values

INR is less than 2 units - this means the dose of Warfarin is insufficient. Therefore, it is necessary to increase the dose to 2.5 milligrams and conduct weekly monitoring.
If more than 3 units, then it is necessary to reduce the dose of the drug. Therefore, take 1 tablet once a week. After the dose of the drug is reduced, it is necessary to monitor the INR.
If the INR is within 3.51–4.5. It is necessary to reduce the drug intake by one tablet, and it is also recommended to carry out monitoring after three days.
If the indicator is from 4 to 6, you also need to reduce the dose of the drug. But at the same time, check the INR every other day. Note that if the indicator exceeds 6 units, then stop taking the drug.

1. Coagulants (drugs that stimulate the formation of fibrin blood clots):

a) direct action (thrombin, fibrinogen);

b) indirect action (vicasol, phytomenadione).

2. Fibrinolysis inhibitors:

a) synthetic origin (aminocaproic and tranexamic acids, Ambien);

b) animal origin (aprotinin, contrical, pantripin, gordox "Gedeon"

Richter", Hungary);

3. Stimulators of platelet aggregation (serotonin adipate, calcium chloride).

4. Agents that reduce vascular permeability:

a) synthetic (adroxon, etamsylate, iprazochrome) b) vitamin preparations (ascorbic acid, rutin, quercetin).

c) preparations of plant origin (nettle, yarrow, viburnum, water pepper, arnica, etc.)

II. Anticoagulants or antithrombotics:

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, actilise).

3. Antiplatelet agents:

a) platelet drugs (acetylsalicylic acid, dipyridamole, pentoxifylline, ticlopidine, indobufen);

b) erythrocyte (pentoxifylline, reopolyglucin, reogluman, rondex).

Drugs that increase blood clotting (hemostatics) coagulants

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

1) for local use (thrombin, hemostatic sponge, fibrin film, etc.)

2) for systemic use (fibrinogen, Vicasol).

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

Apply only locally. Prescribed to patients with bleeding from small vessels and parenchymal organs (surgeries on the liver, kidneys, lungs, brain), bleeding from the gums. Use locally in the form of a hemostatic sponge soaked in thrombin solution, a hemastatic collagen sponge, or simply by applying a tampon soaked in thrombin solution.

It is usually prescribed into 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 warmed water for injection. It is administered intravenously by drip or slow stream.

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 vitamin K deficiency caused by:

1) bleeding from parenchymal organs;

2) the procedure of exchange blood transfusion, if canned blood was transfused (to the child);

and also when:

3) long-term use of vitamin K antagonists - aspirin and NSAIDs (impairing platelet aggregation);

4) long-term use of broad-spectrum antibiotics (chloramphenicol, ampicillin, tetracycline, aminoglycosides, fluoroquinolones);

5) use of sulfonamides;

6) prevention of hemorrhagic disease of newborns;

7) prolonged diarrhea in children;

8) cystic fibrosis;

9) in pregnant women, especially those suffering from tuberculosis and epilepsy and receiving appropriate treatment;

10) overdose of indirect anticoagulants;

11) jaundice, hepatitis, as well as after injuries, bleeding (hemorrhoids, ulcers, radiation sickness);

12) preparation for surgery and in the postoperative period.

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

Side effects: hemolysis of red blood cells when administered intravenously.

Side effects: hypercoagulation phenomena if the dosage regimen is not followed.

Among the drugs related to direct-acting coagulants, the clinic also uses the following drugs:

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

2) antihemophilic globulin (factor VIII).