Hemostatic drugs - ATC classification of drugs. Drugs that help stop bleeding (hemostatic drugs) ATX B02 Hemostatic drugs

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).

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. 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.

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 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.

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).

The use of hemostatic agents is important when it is difficult to stop bleeding. Hemostatic drugs can be local or general; the methods of their use (externally, intravenously, intramuscularly, etc.) and the recommended dosage depend on the degree of damage, the rate of blood loss, the patient’s age and his general well-being.

Hemostatic agents of local and general action are divided into three groups:

  • Coagulants (direct and indirect action)- thrombin, vikasol, fibrinogen;
  • Fibrinolysis inhibitors (substances that increase the formation of fibrin clots)- aminocaproic acid amben, para-acid (PAMCGCA), trasylol, contrical;
  • Stimulators of platelet aggregation (or adhesion)- calcium, adrenomimetic substances, serotonin.

For HFN, hemostatic agents are used; for ICT, diuretics and, if necessary, anticonvulsants are used along with hemostatic therapy.

Effective hemostatic drugs

Adroxon- a synthetic hemostatic drug used for capillary bleeding. Apply topically in the form of a 0.025% solution, which is used to soak napkins or tampons. Administered intramuscularly or subcutaneously in a dose of 0.5-1 ml; tablet form is used orally - 2.5 mg 3-6 times a day.

Aminocaproic acid inhibits fibrinolysis, used for bleeding associated with increased fibrinolysis. Preparations of this hemostatic agent are prescribed intravenously and orally at 0.1-0.2 g/(kg day) - no more than 4 g. Available in powder and in the form of a 5% solution in 100 ml bottles.

Ascorbic acid for bleeding, it is used intravenously, intramuscularly in the form of a 5% solution of 1-2 ml and orally - 0.05-0.1 g 2-3 times a day.

Vikasol- a synthetic analogue of vitamin K. Used for bleeding caused by low levels of prothrombin in the blood. Apply orally or intramuscularly.

Method of administration for newborns in the presence of hemorrhages: a 1% solution of Vikasol is administered intramuscularly at 0.2-0.5 ml (2-5 mg), for children of other age groups - 2-15 mg/day in 1 or 2 doses.

Hemostatic sponge prepared from native human blood plasma and thromboplastin. It is a dry compact mass of light yellow color. Used topically to stop capillary and parenchymal bleeding, bleeding from muscles and small vessels.

Doxium The mechanism of action is similar to etamsylate. Prescribed orally during or after meals at 10-15 mg/(kg day). Release form: tablets of 0.25 g.

Calcium directly participates in the aggregation and adhesion of platelets, and also activates the formation of thrombin and fibrin and, thus, stimulates the formation of platelet and fibrin blood clots.

It is of primary importance for bleeding caused by a decrease in calcium levels in the blood plasma. Use calcium gluconate in the form of a 10% solution - intravenously at 0.5-1 ml/year of life, but not more than 10 ml.

Rutin prescribed for impaired vascular permeability, hemorrhagic syndrome - 0.01-0.03 g orally 3 times a day. Available in tablets of 0.02 g.

Thrombin- a natural component of the blood coagulation system, obtained from donor blood plasma. It is a white amorphous powder. This local hemostatic drug is used topically to stop bleeding from small vessels. For melena, newborns are given orally in combination with aminocaproic acid and adroxon.

The contents of one ampoule (0.01 g of dry thrombin) are dissolved in 50 ml of a 5% solution of aminocaproic acid and 1 ml of a 0.025% solution of vdroxon is added. The recommended dosage is one teaspoon 3-4 times a day.

Fibrinogen- a protein that, when interacting with thrombin, turns into fibrin; constantly circulates in the blood. For bleeding, it is prescribed locally in the form of fibrin films. For hypo- and afibrinogenemia, hemophilia A, DIC syndrome, it is administered intravenously in a stream or drip in a daily dose of 0.5-2 g, depending on the level of fibrinogen in the blood.

The contents of the ampoule with this local hemostatic agent are diluted in 250 ml of water for injection before use.

Ethamsylate (dicinone) normalizes the permeability of the vascular wall, improves microcirculation, and has a hemostatic effect. Used to stop capillary bleeding intravenously, intramuscularly, orally at 10-15 mg/(kg day) in 3 doses. Available in the form of a 12.5% ​​solution in ampoules of 2 ml, in tablets of 0.25 g.

Hemostatic agents of animal and plant origin

Medical gelatin- a product of partial hydrolysis of collagen contained in animal cartilage and bones. Produced in the form of a 10% solution of 0.5% sodium chloride solution in 10 ml ampoules. A gelatinous mass turns into liquid when heated. Administered subcutaneously, intravenously, orally 5-10 ml every 1-2 hours.

Lagochilus intoxicating used for nosebleeds and other bleeding in the form of infusion and tincture of flowers and leaves, as well as tablets containing Lagochilus extract. An infusion (1:10 or 1:20) of this hemostatic drug of plant origin is prescribed 1-2 teaspoons 3-6 times a day, a tincture - 5-10 drops 2-3 times a day.

nettle leaf contains vitamin C, carotene, vitamin K and other substances. Used as an infusion. Briquettes of crushed nettle leaf are produced. One slice of briquette is poured with a glass of boiling water, left for 10 minutes, filtered, cooled and given to the child 1-2 teaspoons 3 times a day.

Yarrow herb contains vitamin C, carotene. Use an infusion of this hemostatic agent 1-2 teaspoons 3 times a day.

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Index of drug descriptions

Aminocaproic acid
Aminomethylbenzoic acid
Menadione sodium bisulfite
Thrombin
Etamzilat

Drugs of this group, by increasing blood clotting, stop bleeding and protect the body from blood loss when the integrity of the vascular bed is violated. This property of this group of drugs is used in dental practice to stop bleeding and protect the body from blood loss during traumatic interventions in the highly vascularized maxillofacial area.

Hemostatics are divided into:

  • coagulants:
- indirect action - menadione sodium bisulfite (Vicasol);
- direct action - thrombin, fibrinogen;
  • fibrinolysis inhibitors (aminocaproic and aminomethylbenzoic acids (Amben) and heparin antagonists (protamine sulfate and protamine chloride);
  • hemostatic agents of different groups (medical gelatin, etamsylate (dicinone), hypertonic solutions).
From the last group, etamsylate (dicinone) is used in dental practice, which affects capillary permeability and the platelet component of hemostasis. Medical gelatin, which increases blood viscosity, and hypertonic solutions, which increase its osmotic pressure, are rarely used in outpatient dental practice.

Mechanism of action and pharmacological effects

To stop bleeding, a large number of drugs have been created that have different mechanisms of action, which allows them to be used locally or for resorptive action.

Of the hemostatic agents used for resorptive action (fibrinogen, fibrinolysis inhibitors, menadione sodium bisulfite, heparin antagonists, medical gelatin, etamsylate (dicinone), hypertonic solutions), menadione sodium bisulfite is most widely used in outpatient dental practice.

Menadione sodium bisulfite (Vicasol) is a synthetic water-soluble preparation of vitamin K, an antagonist of indirect anticoagulants. Vitamin K affects the energy processes of cells, stimulates protein synthesis in the liver, incl. a number of hemocoagulation factors (prothrombin, proconvertin, IX and X blood coagulation factors), ATP, creatine phosphate, a number of enzymes. Menadione sodium bisulfite substrate stimulates vitamin K reductase, activating vitamin K, which is involved in the synthesis of plasma coagulation factors. Vitamin K is necessary for the transition of prothrombin to thrombin, under the influence of which fibrinogen turns into fibrin.

Thrombin, fibrinogen (isogenic fibrin film), and caprofer are used locally to stop bleeding.

Thrombin and fibrinogen are natural components of the hemostatic system. Thrombin catalyzes the entire process of blood coagulation, starting with the formation of thromboplastin and ending with the conversion of fibrinogen into fibrin monomer, activates the fibrin-stabilizing factor and platelet aggregation. Thrombin is used only locally, since if it enters the vascular bed it can cause widespread thrombosis. Fibrinogen is a substrate for the formation of fibrin, necessary for the organization of a blood clot, and can be used not only topically, but also by injection (during surgical operations against the background of a low fibrinogen content in the blood).

Fibrinolysis inhibitors aminocaproic and aminomethylbenzoic acids (Amben) block the transition of profibrinolysin (plasminogen) to fibrinolysin (plasmin) and have a direct inhibitory effect on fibrinolysin, which prevents the dissolution of the resulting blood clot.

Aminocaproic acid, which when applied topically promotes the organization of a blood clot and stimulates regeneration, is included in the composition of caprofer along with iron chloride. It is produced in the form of a solution, which allows it to be applied not only to wound surfaces, but also to be injected into the canals of the teeth to stop bleeding from the pulp. When used systemically, it has a hemostatic effect, inhibits the fibrinolytic effect of urokinase, streptokinase and tissue kinases, reduces the activity of kallikrein, trypsin and hyaluronidase, reduces capillary permeability, and has a slight anti-inflammatory and antiallergic effect.

Etamsylate reduces the activity of hyaluronidase, prevents the breakdown of mucopolysaccharides, stabilizes ascorbic acid, increases resistance and reduces capillary permeability, has an angioprotective effect, moderately accelerates the formation of tissue thromboplastin and increases the number of platelets, accelerates the formation of a blood clot in a damaged vessel.

Pharmacokinetics

Menadione sodium bisulfite after oral administration is absorbed in the upper parts of the small intestine. After intramuscular administration, it is easily and quickly absorbed. In the blood it binds to plasma proteins. Metabolized in the liver, excreted mainly in the form of metabolites (monophosphate, phosphate, diglucuronide) in urine and bile. The hemostatic effect when taking the drug orally develops after 12-24 hours, when administered intramuscularly - after 2-3 hours.

Aminocaproic acid, when taken orally, is quickly absorbed from the gastrointestinal tract (by 60% or more). Cmax in blood plasma is created after 1-3 hours. It practically does not bind to blood plasma proteins. It is excreted by the kidneys 40-60% unchanged. T1/2 is 2-4 hours. With intravenous administration, Cmax in the blood plasma is created in 10-15 minutes, T1/2 is 1 hour. It penetrates the placental barrier well. When applied topically (implantation of a medicinal napkin containing aminocaproic acid), the drug is completely utilized within 23-28 days.

Aminomethylbenzoic acid, when taken orally, is well absorbed from the gastrointestinal tract, creating Cmax in the blood plasma after 3 hours. After IM administration, Cmax in the blood plasma is created in 30-60 minutes, after IV - by the end of administration, the therapeutic concentration remains for 3 hours. It is released kidneys mainly (50-80%) unchanged. T1/2 is 2-4 hours. With intravenous administration, Cmax in the blood plasma is created in 10-15 minutes, T1/2 is 1 hour. It penetrates the placental barrier well.

Etamsylate is well absorbed when taken orally and when administered intramuscularly, and is evenly distributed in tissues depending on their vascularization. It binds weakly to proteins and blood cells and is quickly excreted from the body, mainly unchanged. With intravenous administration, the effect begins after 15 minutes, the maximum effect is achieved after 1-2 hours, the duration of action is up to 4-5 hours.

Place in therapy

Menadione sodium bisulfite (Vicasol) is used for stomatitis, gingivitis, hemorrhages of various etiologies, as well as for the prevention of bleeding before traumatic surgical interventions.

In dental practice, thrombin, fibrinogen, hemostatic sponge and caprofer, which promote the formation of a blood clot when applied topically, are used to stop bleeding after traumatic operations in the maxillofacial area, during curettage of periodontal pockets, after removal of dental pulp, etc.

Fibrinolysis inhibitors aminocaproic and aminomethylbenzoic acids (Ambene) can be used topically, orally and by injection to stop bleeding during traumatic interventions in the maxillofacial area.

Etamsylate is used for the prevention and treatment of bleeding during surgical interventions in the maxillofacial area.

Tolerability and side effects

Aminocaproic and aminomethylbenzoic acids cause side effects mainly when administered intravenously: nausea, vomiting, diarrhea, increased or decreased blood pressure, rarely - orthostatic hypotension; arrhythmia, tachycardia; headache, dizziness, tinnitus; renal colic; catarrhal symptoms from the upper respiratory tract, nasal congestion; allergic reactions when applied topically; local phenomena - thrombophlebitis at the injection site.

When using menadione sodium bisulfite, allergic reactions (skin rash, itching, urticaria, bronchospasm), hemolytic anemia, hemolysis in newborns with congenital deficiency of glucose-6-phosphate dehydrogenase, hyperbilirubinemia, jaundice (especially in premature infants) may occur.

Side effects of etamzilate include heartburn, a feeling of heaviness in the epigastric region, paresthesia in the lower extremities, facial flushing, slight dizziness, headache, and a decrease in systolic blood pressure.

Contraindications

Hypersensitivity, hypercoagulation, tendency to thrombosis and thromboembolism, hemolytic disease of newborns.

Aminocaproic and aminomethylbenzoic acids are contraindicated in cases of cerebrovascular accident, severe angina and renal failure, the hypercoagulable phase of DIC syndrome, gross hematuria, and pregnancy.

Interaction

Aminocaproic and aminomethylbenzoic acids can be used topically in combination with fibrin films, thrombin and other hemostatics.

Aminocaproic and aminomethylbenzoic acids are compatible with hydrolysates, dextrose solution, and anti-shock liquids; reduce the effect of antiplatelet agents, direct and indirect anticoagulants. In case of acute fibrinolysis, fibrinogen is additionally administered.

Combination with proteases can lead to massive thrombus formation.

Menadione sodium bisulfite reduces the effect of indirect anticoagulants.

Etamsylate is not pharmaceutically compatible in the same syringe with other drugs. Combination with aminocaproic acid, menadione sodium bisulfite, anticoagulants, calcium chloride is acceptable. Reduces the severity of hemorrhagic syndrome caused by acetylsalicylic acid and indirect anticoagulants. Preliminary administration of ethamsylate removes the effect of rheopolyglucin, and vice versa.

For bleeding, hemostatic agents are used. They are divided into the following groups.

  • 1. Aggregants – agents that stimulate platelet adhesion and aggregation.
  • 2. Coagulants (hemostatics) – agents that stimulate thrombus formation:
    • a) direct action – thrombin;
    • b) indirect action – Menadione sodium bisulfite"Vikasol" (vitamin K).
  • 3. Antifibrinolytics (fibrinolysis inhibitors) – agents that reduce the activity of the fibrinolytic system.

Let's consider representatives of these groups.

Aggregates. Calcium is a vital mineral necessary to maintain the balance of electrolytes in the body, the adequate functioning of numerous regulatory mechanisms, is directly involved in platelet aggregation and adhesion, but in addition, it activates thrombin and fibrin. Thus, it stimulates the formation of both platelet and fibrin blood clots. Calcium preparations are mainly used for bleeding associated with a decrease in its level in the blood plasma. Used as drugs calcium chloride(intravenously or orally) and calcium gluconate(intravenously, intramuscularly or orally). Rapid intravenous administration of calcium chloride can cause cardiac arrest and low blood pressure.

Etamzilat(“Dicynon”) inhibits the synthesis of prostacyclin and thereby reduces its effect on platelet aggregation. It promotes compaction of the basement membrane of capillaries, increasing the polymerization of hyaluronic acid in it and normalizing cerebral blood flow. When administered intravenously, the hemostatic effect develops within 5–15 minutes.

Serotonin isolated in 1947, found in various tissues, including blood (platelet). Serotonin is released from platelets when they are destroyed and takes part in the process of blood clotting. In diseases accompanied by thrombocytopenia, the amount of serotonin in the blood drops sharply (Werlhof's disease, purpura, leukemia, etc.). The hemostatic effect of serotonin is also associated with a peripheral vasoconstrictor effect. If bleeding is severe, they begin with intravenous administration; when bleeding decreases, they switch to intramuscular injections.

Coagulants. Direct-acting coagulants are preparations from blood plasma of donors, preparations for topical use ( thrombin, "Hemostatic sponge").

Thrombin – a natural component of the hemocoagulation system, formed in the body from prothrombin during its enzymatic activation by thromboplastin. Thrombin solution is used only locally to stop bleeding from small vessels and parenchymal organs (for example, during operations on the liver, brain, kidneys). Gauze swabs are soaked in thrombin solution and applied to the bleeding surface. Parenteral administration of thrombin solutions is not allowed because they cause the formation of blood clots in the vessels. "Hemostatic sponge" contains boric acid, nitrofural and collagen, has a hemostatic and antiseptic effect, stimulates tissue regeneration. It is contraindicated in case of bleeding of large vessels, hypersensitivity to furatsilin and other nitrofurans.

Indirect coagulant menadione sodium bisulfite(“Vikasol”) is a synthetic analogue of vitamin K. Only two vitamins of the K group are isolated from natural substances: vitamin K from alfalfa, and K2 from rotting fishmeal. In addition to natural vitamins K, a number of naphthoquinone derivatives with an antihemorrhagic effect, which are obtained synthetically, are currently known. In 1943, K. Dam and E. A. Doisy received the Nobel Prize for the discovery and establishment of the chemical structure of vitamin K. Vitamins K (phyloquinones ) enter the body with plant foods (spinach leaves, cauliflower, rose hips, pine needles, green tomatoes), are found in products of animal origin and are synthesized by intestinal flora. Indications for use: "Vikasol" is used for all diseases accompanied by a decrease in the content of prothrombin in the blood (hypoprothrombinemia) and bleeding. These are primarily jaundice and acute hepatitis, peptic ulcer of the stomach and duodenum, radiation sickness, septic diseases with hemorrhagic manifestations. "Vikasol" is also effective for parenchymal bleeding, bleeding after injury or surgery, hemorrhoidal, prolonged nosebleeds, etc. It is also used prophylactically before surgery, during long-term treatment with sulfonamide drugs and antibiotics that inhibit the intestinal flora, which synthesizes vitamin K. Also it is used for bleeding caused by an overdose of indirect anticoagulants. The effect develops slowly - 12–18 hours after administration.

"Vikasol" can accumulate, so the daily dose should not exceed 1-2 tablets or 2 ml of a 1% solution intramuscularly for no more than 3-4 days. If necessary, repeated administration of the drug is possible after a 4-day break and testing the blood clotting rate. Vikasol is contraindicated in case of increased hemocoagulation and thromboembolism.

Herbal preparations used as a source of vitamin K also contain other vitamins, bioflavonoids, and various substances that can promote blood clotting and reduce the permeability of the vascular wall. This is first of all stinging nettle leaves, viburnum fruits, water pepper herb, arnica. From the listed plants, infusions, tinctures, and extracts are prepared, which are used internally. Some of these drugs are used topically, moistened with gauze pads and applied to the bleeding surface for 2-5 minutes.

Fibrinolysis inhibitors. Aminocaproic acid – lysine derivative. Fibrinogen and fibrin molecules contain lysine; it is with this that the active centers of plasminogen plasmin interact, subsequently subjecting these proteins to hydrolysis. Aminocaproic acid interacts with these areas of plasminogen and plasmin, eliminates their activity, preserving the fibrin molecule and the thrombus consisting of it.

Aprotinin(“Contrical”) is an anti-enzyme drug obtained from the lungs of cattle. It forms inactive complexes with plasminogen.

Aminocaproic acid and aprotinin are prescribed for bleeding associated with increased activity of the fibrinolytic system and fibrinogen deficiency, for example, with cirrhosis of the liver, portal hypertension, with bleeding after operations on organs rich in tissue plasminogen activator, with the use of heart-lung machines, with an overdose of fibrinolytic agents, with massive transfusions of canned blood (possibility of developing secondary hypofibrinogenemia), etc.

In addition, these drugs, by inhibiting proteolytic enzymes, directly (aprotinin) or indirectly, through the fibrinolysis system (aminocaproic acid), inhibit the activity of kinins. Therefore, they are used for traumatic shock, pancreatitis, burns, concussion, meningitis, i.e. in pathological conditions characterized by increased kinin activity.

Aminocaproic acid is administered orally, intramuscularly and intravenously; aprotinin - only intravenously.

Antihemostatics. Antihemostatics reduce the level of blood clotting. The slow process of blood clotting and the dissolution of formed clots constantly occurs in the bloodstream. A diagram of the sequential activation of blood coagulation factors is shown in Fig. 5.10.

Normally, this does not lead to disruption of blood flow. Fibrinous clots in the bloodstream occur when the function of the blood anticoagulation system is impaired. The formation of fibrinous clots causes the occurrence of blood clots and embolisms.

Rice. 5.10.

In the process of treating thrombosis and embolism, the ability to melt a clot formed in the bloodstream by timely use of the enzyme fibrinolysin, but always in combination with heparin, becomes of great importance.

To suppress blood clotting in a vessel, anti-clotting agents are used: antiplatelet agents, anticoagulants, fibrinolytics.

Antiplatelet agents. They are classified as follows:

  • cyclooxygenase inhibitors: acetylsalicylic acid(“Aspirin Cardio”, “Buferin”, “Novandol”, “Thrombo ACC”);
  • modulators of the adenylate cyclase-CAMP system: dipyridamole;
  • glycoprotein GP receptor blockers: abciximab("Reopro");
  • eptifibatide(“Integrilin”);
  • purine receptor blockers: ticlopidine, clopidogrel.

Antiplatelet agent acetylsalicylic acid at a dose of 150–300 mg (according to European recommendations) is indicated in case of acute coronary syndrome (myocardial infarction or primary unstable angina). The enteric form is not suitable for these purposes, since its onset of action is slow. Further, acetylsalicylic acid is used for life at a dose of 75–162 mg/day. If there are contraindications to acetylsalicylic acid, use clopidogrel in the first loading dose of 300 mg and subsequently 75 mg/day. The combination of clopidogrel with aspirin is more effective than aspirin monotherapy. Eptifibatide(“Integrilin”) is a synthetic heptapeptide, an inhibitor of platelet aggregation, belonging to the class of arginine-glycine-aspartate mimetics. Indications for use are early prevention of myocardial infarction.

Anticoagulants(drugs that interfere with the formation of blood clots). Direct anticoagulants - heparin and its drugs, hirudin, sodium hydrogen citrate, concentrate antithrombin III.

Indirect anticoagulants – oxycoumarin derivatives: warfarin, acenocoumarol("Sinkumar"); indanedione derivatives – phenylin. New anticoagulants Xabans and Gatrans - dabigatran etexilate("Pradaxa"), rivaroxaban("Xarelto"). Direct-acting anticoagulants are injectable drugs used in the initial stages of treatment and prevention of thrombosis in a short course. Indirect anticoagulants (inhibit the synthesis of coagulation factors in the liver) act slowly and are used orally.

Direct acting anticoagulants. Heparin belongs to the group of medium molecular heparins, the ability to inhibit thrombin and factor X is especially important. Activated factor X combines with factor V and phospholipids of platelets and tissues, forming a complex called prothrombin activator. This complex, in turn, within a few seconds initiates the breakdown of prothrombin to form thrombin, setting in motion the final phase of the coagulation process. Heparin is used for thrombosis, thromboembolism, and to inhibit blood clotting during extracorporeal circulation. Heparin ointment and other heparin preparations for topical use prevent the formation of blood clots in thrombophlebitis of the superficial veins, and are used for tendon and joint injuries, soft tissue bruises. Rectal suppositories are prescribed for hemorrhoids. A side effect of heparin is thrombocytopenia. The antagonist of heparin is protamine sulfate. 1 mg of protamine sulfate neutralizes 80–120 units of heparin in the blood. Complex formation is due to the binding of cationic groups (due to arginine) with the anionic centers of heparin. The action of protamine occurs immediately after intravenous administration and lasts 2 hours.

Enoxaparin sodium(“Clexane”) is a low-molecular-weight heparin that rarely causes side effects—thrombocytopenia.

Fondaparinux sodium(Arixtra), unlike heparin, causes thrombocytopenia in more rare cases.

Anticoagulants of indirect action. Warfarin– one of the most commonly used anticoagulants. But it has a number of disadvantages:

  • risk of developing severe hemorrhagic complications;
  • the need for regular laboratory monitoring;
  • drug and food interactions;
  • narrow therapeutic range.

New drugs are free of these side effects. Dabigatran etexilate– a strong competitive reversible direct inhibitor of thrombin. Rsharoxaban– a selective direct factor Xa inhibitor that blocks the formation of thrombin. Used to prevent stroke and systemic thromboembolism in patients with atrial fibrillation.

Fibrinolytics. Fibrinolytic drugs (fibrinolytics), as well as anticoagulants, are used for the prevention and treatment of thrombosis. Streptokinase, urokinase, alteplase(“Actilyse”) dissolves a blood clot (thrombolysis). This restores blood flow, limits the size of the infarction, and reduces mortality. Thrombolysis is carried out as early as possible and within 12 hours from the onset of the disease.

Contraindications for all drugs that reduce blood clotting are bleeding, erosions and ulcers of the gastrointestinal tract, recent multiple injuries, arterial hypertension and other conditions that threaten bleeding.

In case of heavy bleeding due to tissue damage or pathological processes occurring in internal organs, it is necessary to use hemostatic drugs to prevent significant blood loss. Medicines that help stop the flow of blood can be local or systemic. Each individual case requires the use of a specific medication that can eliminate the problem in the shortest possible time.

What are hemostatic drugs

The process of blood coagulation in the human body is represented by a complex system of interactions between a group of substances (blood coagulation factors). Most of these substances are proteins. To date, the presence of 35 coagulation factors has been established: 13 plasma and 22 platelet. A deficiency of one of these components leads to bleeding of various types.

Hemostatic drugs (from the Greek - stopping blood) are designed to eliminate the causes of disorders in the body and block blood loss. The principle of action of hemostatic agents is based on replenishing the deficiency of its own enzymes, stimulating thrombus formation on the surface of damaged vessels and suppressing fibrinolytic activity (dissolution of blood clots).

How to stop bleeding during menstruation

Heavy blood loss in women during menstruation (more than the daily norm of 80 ml) can be caused by various reasons. Before buying a hemostatic medicine at a pharmacy on the advice of a pharmacist, you should consult a gynecologist about this problem. Only a professional doctor will be able to determine the factor that caused the deviation from the norm and recommend a targeted hemostatic agent.

Hemostatic medications used during treatment are not a panacea for diseases that cause bleeding. They temporarily prevent the rapid outflow of blood to allow the body to make up for the resulting deficiency. The course of treatment is prescribed by a doctor and includes medications that act directly on the cause of the pathology.

Pills

Hemostatic tablets are an effective remedy for heavy bleeding during menstruation. Properly selected drugs based on the identified genesis of bleeding can restore the deficiency of coagulation factors. Before you start taking hemostatic drugs, you should know that some of them may have side effects and contraindications. A description of the most common hemostatic tablets is presented in the table:

Drug name

Description

Contraindications

Side effects

Synthetic analogue of vitamin K. Designed to stimulate the synthesis of prothrombin

Pathologically high blood clotting, inflammatory thrombosis

Skin reactions in the form of itchy rashes

Erythrostat

Vasoconstrictor drug based on medicinal herbs with an astringent effect

High blood pressure, pregnancy, lactation period

Manifestation of allergic symptoms

Askorutin

Vascular strengthening effect along with a decrease in capillary permeability

Urological diseases, thrombosis

Rash, hives

Stimulates the production of thromboplastin, which promotes accelerated formation of the primary thrombus

Thromboembolism, thrombosis

Headache, attacks of nausea, loss of sensation in the limbs

Tranexam

Suppresses the formation of the protein plasmin, which is responsible for the resorption of blood clots

Cerebral hemorrhage, myocardial infarction

Vomiting, color vision problems, dizziness

Erythrostat for menstruation

Drug treatment of blood loss with Erythrostat involves taking two or three hemostatic tablets every 5 hours before meals. The course should not last longer than 10 days, after which it is necessary to take a break of at least 3 months. If a relapse occurs during this period, you should consult a doctor for advice. In such a situation, treatment with another hemostatic drug may be prescribed.

Ascorutin for uterine bleeding

Ascorbic acid, which is part of Ascorutin, is considered an important component for the formation of collagen fibers. Thanks to this quality, a hemostatic effect is achieved. Periodic use of the drug Ascorutin for prevention helps strengthen the walls of blood vessels and reduce their fragility. You should take 1 tablet four times a day. The effect of the medicine is cumulative, so the positive effect will be more noticeable with each use. The course lasts 3 weeks.

Dicynone and Tranexam at the same time

Some anti-bleeding pills work more effectively when taken orally at the same time. The drugs Dicynon and Tranexam are prescribed by specialists in cases requiring emergency care. The task of Tranexam is to quickly stop blood loss, and Dicinon is to protect the body from the possibility of thrombosis. These hemostatic agents should be taken according to the following scheme: the first dose is 2 tablets of each, then one tablet every 6 hours.

Injections

An emergency measure for very rapid blood loss is hemostatic injections. Intravenous administration of the drug promotes the fastest formation of clots (thrombi), which block bleeding. The effect of injection therapy is achieved in 10-15 minutes. after introduction. The most effective hemostatic solutions for infusion when prescribing urgent treatment are considered:

  • Etamsylate;
  • Calcium chloride;
  • Aminocaproic acid;
  • Contrikal;
  • Oxytocin;
  • Methylergometrine;
  • Vikasol.

Oxytocin for uterine bleeding

The effect of the hemostatic drug Oxytocin is to enhance the contractile activity of the smooth muscles of the uterus. As a consequence of this process, the calcium concentration inside the cells increases and the bleeding process stops. It is recommended to administer the drug solution intramuscularly to achieve the best effect. The dose is calculated individually for each patient based on available data on sensitivity to the drug. A single administration cannot exceed 3 IU.

Aminocaproic acid during menstruation

The strong hemostatic effect of aminocaproic acid is based on the suppression of the transition of profibrinolysin (inactive form of plasmin) to fibrinolysin (active form). The use of this drug for heavy periods involves intravenous administration of a five percent solution every hour until the amount of bleeding decreases.

Hemostatic agents for cuts

To prevent blood loss due to mechanical damage to soft tissues, local medicinal hemostatic agents are used. Minor cuts and wounds on the skin can simply be treated with hydrogen peroxide to disinfect. The foaming effect of peroxide can stop mild capillary bleeding. A more severe case requires the use of drugs with enhanced hemostatic effect.

Convenient to use hemostatic powder with anesthetics. The main active ingredient adrenaline has a vasoconstrictor effect, which achieves the effect of stopping minor bleeding in case of superficial damage. Preparations for external treatment of wounds are made from specially treated human or animal blood.

Hemostatic drugs for nosebleeds

To stop nosebleeds of various etiologies, packing should be done. For these purposes, a gauze, foam rubber or pneumatic base can be used. Hemostatic medications previously applied to the tampon will help enhance the effect. Such drugs are:

  • Etamsylate;
  • Dicynone;
  • Epsilon-aminocaproic acid;
  • Calcium chloride;
  • Vikasol.

The most common cause of nosebleeds is arterial hypertension, so it is important to ensure a rapid hypotensive effect. It involves lowering blood pressure through medication. Drugs that are designed for long-term use are not suitable for emergency treatment of nosebleeds.

For hemorrhoids

Sudden bleeding caused by a rupture of the hemorrhoid can be stopped with the help of hemostatic agents used for other types of blood loss (Ditsinon, Vikasol, Etamzilat, etc.). In addition, an effective drug is Relief, which is available in the form of suppositories and ointments. Oils, glycerin and vitamin complex, which are the basis of suppositories, have wound healing and hemostatic properties. Using suppositories to block blood flow on an ongoing basis is contraindicated.

For local anesthesia and stopping local bleeding from anal fissures, you can use a hemostatic self-absorbing sponge soaked in a solution of targeted drugs. The introduction of suppositories and sponges helps to quickly eliminate bleeding, but you should not count on a long-term effect.

Contraindications

The active substances contained in hemostatic drugs can provoke allergic reactions. To avoid negative consequences, it is necessary to warn the doctor about the presence of existing allergies. Hypersensitivity to one of the components of the drug is a direct contraindication to its use, so you should carefully study the instructions and composition. Ignoring the recommendations contained in the instructions for the drugs, regarding violation of the dosage and frequency of administration, can lead to the development of thrombohemorrhagic syndrome.

Price

After receiving a doctor’s recommendations regarding the use of a hemostatic drug, you can turn to the services of an electronic catalog of medicines to familiarize yourself with the selection of available drugs. In order to buy the item you are interested in at an affordable price in an online store, you should familiarize yourself with the average cost of medicines in your region of residence. You can order the selected product based on the approximate data presented in the table:

Name of the drug

Manufacturer

Price, rubles

Vikasol, 20 tablets.

Russia, JSC Biosintez

Ascorutin, 50 tablets.

Russia, Pharmstandard

Dicynone, 100 tab.

Slovenia, Lek D.D.

Tranexam, 30 tablets.

Russia, Nizhpharm JSC

Tranexam, 10 ampoules

Russia, Nizhpharm JSC

Oxytocin, 5 ampoules

Hungary, Gedeon Richter

Relief, candles 12 pcs.

Germany, Bayer

Aminocaproic acid, 100 ml bottle

Russia, Dalkhimfarm

Etamsylate, 100 tablets.

China, Alvils LLC

Methylergometrine, 50 ampoules

Serbia, Hemofarm

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Attention! The information presented in the article is for informational purposes only. The materials in the article do not encourage self-treatment. Only a qualified doctor can make a diagnosis and make recommendations for treatment based on the individual characteristics of a particular patient.

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