Fibrinolytic drugs. Fibrinolytic agents Side effects of fibrinolithics

it medicinal productsused to dissolve the formed thrombus.

The fibrinolytic agents catalyze the formation of plasmin (fibrinolysin) - a proteolytic enzyme that destructifies (lyseing) fibrin yarns forming the base of the blood clots, which can lead to the dissolution of the available intravascular thrombus.

Plasmin circulating in the blood is quickly inactivated by α 2 -antiplasmine and other inhibitors and therefore does not normally cause systemic fibrinolysis.

However, the risk of bleeding still exists, since the specificity of the plasmin is not high and it can cause destruction of fibrinogen and some other factors of the coagulation system of blood.

As fibrinolytic agents, streptokinase, urogase, drugs of the human fabric activator plasminogen are used.

Fibrinolytic.

Streptokinase (Strertokinase, Sin. Avelysin)

Fibrinolytic.

Product of vital activity of β-hemolytic streptococcus.

Squirrel with molecular weight of 47000d. It has the ability to bind to plasminogen, which causes a conformational restructuring of its structure and the appearance of proteolytic activity, as a result of which the streptocinase and plasminogen complex acquires the ability to convert plasminogen to plasmin. The latter breaks fibrin, which leads to lysis of the formed thrombus.

Used for fibrinolytic therapy when acute infarction Myocardium (for the first 6 hours), thromboembolism pulmonary artery and its branches, thrombosis and thromboembolis of vessels of the limbs, brain, retina of the eye and other states occurring with sharp embolims and thrombosis in order to cause the reservation of blood vessels and restoring blood flow in them.

Intravenously injected, starting with a dose of 250,000 meters in 50 ml of isotonic sodium chloride solution for 30 minutes. With good tolerance, further administration continues at 100,000 meters per hour before reaching the desired effect, usually within 16 to 18 hours.

If necessary, streptokinase can be introduced intraarterially.

In all cases, the introduction of streptocinase should be started as early as possible because best Effect Observed with fresh blood clots.

Unwanted effects: bleeding, allergic reactions, including anaphylactic shock, fever, hypotension.

FV: Lyophilized powder for preparing a solution for injection in bottles of 100,000, 250,000, 750,000 and 1,500,000 meters.

AISTEPLASE, SIN. Eminase)

The fibrinolytic agent containing a streptocinase complex with an acylated lesine plasminogen.

The presence of an acyl group prevents spontaneous activation of the complex in the blood.

It was believed that the cleavage of the acyl group and the activation of the complex would occur only after the latter contacted the fibrin inside the blood clots. Thus, it was calculated to limit the fibrinolytic effects of ansertrlase only against thrombus and avoid systemic effects.

Unfortunately, even when administered directly to coronary vessels in the recommended doses (30 units), systemic fibrinolysis is observed.

UROKINASE, SIN. ABBOKINASE)

It is obtained from the culture of human embryonic cells.

A protein consisting of two polypeptide chains containing 411 amino acid residues with proteolytic activity, and is, in contrast to streptocinase, a direct activator of plasminogen that turns it into plasmin.

Apply to dissolve fresh thromboms.

Prescribed intravenously, starting with the introduction of a load dose of 1000-4500 U / kg and subsequent infusion at a speed of 4400 units / kg per hour.

Less often compared with streptocinase causes allergic disorders. However, specificity is insufficient in order to activate only fibrin-bound plasminogen as part of the thrombus, in connection with which, similar to streptocynase, causes systemic fibrinolysis and can lead to bleeding.

FV: Lyophilized powder for the preparation of solutions for injection in bottles of 100,000, 500,000 and 1000,000 IU.

Prurokinase, Sin. Saruplase)

Single-stranded urocinase obtained by recombinant.

It has, according to, more high, compared with the two-stranded urchinase, the selectivity of plasminogen associated with fibrin in the composition of the thrombus.

Altepleza (Alteplase, Sin. Actilyse)

Drug recombinant human fabric activator plasminogen (T-PA).

Protein formed in endothelium cells. Contains 527 amino acid residues and has proteolytic activity. Catalyzes plasminogen conversion to plasmin.

Acts mainly on plasminogen associated with fibrin, which takes place in the resulting thrombe.

Blood is binding to specific inhibitors and therefore has a smaller impact on plasminogen circulating in the blood, and also does not have a noticeable effect on other factors of the coagulation system and therefore, to a lesser extent compared with streptocinase and urchinase affect the system coagulation of blood.

Apply for coronary thrombolysis in acute myocardial infarction, as well as pulmonary artery thromboembolism.

Prescribed intravenously, initially 15 mg bolus, then, during the next 30 minutes, drip based on the dose of 0.75 mg / kg and further 0.5 mg / kg for the next hour to the total dose of 35 mg / kg.

Unwanted effects: hemorrhagic complications, hypotension, fever.

FV: Lyophilized powder 50 mg in bottles.

Alteplase (Alteplase)

Synonyms: Actilization.

Pharmachologic effect. Recombinant human plasminogen activator (blood protein, participating in the blood coagulation regulation), which is part of the drug, is a glycoprotein (complex protein), which, after systemic administration, is in plasma in inactive form until the fibrin binding (insoluble protein, generated in blood coagulation process). After activation, the drug activates the transition from plasminogen to plasmin and leads to the dissolution of the fibrin clot, which way increasing fibrinolysis (dissolving blood clot) only in tomb tissue.

Indications for use. Acute arterial and venous thrombosis (blood clot formation in vessel).

Method of use and dose. Administered intravenously for 1-2 minutes at a dose of 10 mg, then drip for 3 hours at a dose of 90 mg (at the same time, 50 mg is administered for 60 minutes, and the remaining 40 mg is introduced within the 2nd and 3rd hours 20 mg / h).

If, due to the overdose of the drug, bleeding occurred, the transfusion of freshly frozen plasma or fresh blood is shown; In addition, inhibitors of fibrinolysis can be used (means forbing the dissolution of blood clot).

Side effect. Nausea, vomiting, temperature rise, allergic reactions in the form of urticaria, headaches, rarely bleeding, reperfusion arrhythmias (violation of heart rhythm due to restoration of blood flow through the arteries of the heart).

Contraindications. Hemorrhagic diathesis (elevated bleeding), bleeding, transferred operation or injury with a prescription less than a week, arterial hypertension malignant character (resistant rise arterial pressure, poorly treatable), bacterial endocarditis (disease inner cavities due to the presence of bacteria in the blood), acute pancreatitis (inflammation of the pancreas), complicated diabetes, sickle-cell anemia ( healthy diseasecharacterized by an increased collapse of erythrocytes having a sickle form and the presence of functionally defective hemoglobin / oxygen carriers /) children's age, pregnancy, breastfeeding, increased sensitivity to the drug. With caution, the drug is prescribed to patients with accompanying pulmonary diseases, as well as patients over the age of 75.

Release form. Dry substance for infusions of 0.02 g and 0.05 g in vials per pack 1 piece bundled with solvent.

Storage conditions. List B. in a cool place.

Streptodecasum Pro INJECTIONIBUS)

It refers to the group of "immobilized" (fixed on the polymer carrier) of enzymes and is an activator of the fibrinolytic (solvent blood clot) of a human system modified by a water-soluble polymeric matrix of polysaccharide nature.

Pharmachologic effect. It has thrombolytic activity (dissolves blood clot), converts plasminogen blood into plasmin and inactivates its inhibitors, has a prolonged (long) fibrinolytic effect.

Indications for use. Acute peripheral arterial thrombosis (formation of blood clot in artery) or thromboembolism (blockage of blood clot vessel), with the exception of "cases when emergency surgery is shown; peripheral phlebotrombosis (blockage of veins of blood clot), acute thromboembolism in the pulmonary artery system or in cases of recurrent The thrombosis of its small branches (periodically repeated blockage of the blood vessel with a blood clot; thrombosis of the central vein and the artery of the retina; acute myocardial infarction in the 1st day of the disease or recurring its course (re-appearance of symptoms of the disease), during retromism after thrombotomy (repeated blockage of blood clot vessel after removing it).

Method of use and dose. Intravenously. Intravenously introduced streptodecase intravenously in the initial dose of 300,000 pm (test dose), then an hour later, in the absence of side effects, an additional 2,700,000 feces are introduced (for 1-2 minutes) (total dose of 3,000,000 pm) at the rate of 300 000-600 000 FE per minute.

In these doses, the drug causes a significant and long-term increase in the fibrinolytic activity of blood, an increase in the content of the activator of the storage unit and plasmin, has a pronounced therapeutic effect.

Sgratodekaza in therapeutic doses little affects blood coagulation indicators.

To prevent retrose (re-blocking a blood clot vessel), combined therapy with streptowecase and heparin. Since the end of the 1st day after the introduction of the therapeutic dose of streptodecadis (3,000,000 feet), heparin is administered at the rate of 40,000 units per day (10,000 meals every 6 hours) within 7-10 days.

Repeated introduction of streptodecadis is permissible not earlier than 3 months. After treatment under the specified scheme and only after the study of the streptococcal antibody titer. If necessary, re-administration is usually produced after 6 months.

To treat thrombosis veins of the retina, the eyes proposed to introduce streptodecase retrobulbarno (for eyeball) 30 000 - 50,000 pm at 0.2-0.3 ml of isotonic sodium solution chloride at intervals of 5 days. In the intervals between injections, retrobulbarly heparin and dexamethasone (see p. 448, 583).

Side effect. Allergic reactions (chills, temperature rise, headache, hyperemia / redness /, urticaria, back pain, etc.), and when combined with heparin - hemorrhagic complications: (bleeding, hematoma formation: limited blood cluster in tissues / bruise /), hematuria (blood in urine) and t. d.

Contraindications. Hemorrhagic diathesis (elevated bleeding), bleeding, ulcerative ulcer of the stomach and duodenal gut, within 4 days. after surgery and childbirth, acute streptococcal infection, sepsis (blood infection by microbes from the hearth purulent inflammation), endocarditis (disease inner cavities of the heart), sharp inflammatory diseases organs abdominal cavity (Pancreatitis, cholecystitis, appendicitis, etc.), pregnancy up to 18 weeks, high arterial hypertension (lifting blood pressure), active tuberculous process, malignant neoplasms, allergies for fibrinolytic drugs in the past; Sugar diabetes, bronchiectatic disease with a pronounced destructive process (bronchial disease associated with the expansion of their lumen, accompanied by the destruction of bronchi), liver cirrhosis, renal disease in the aggravation stage, expressed atherosclerosis.

Release form. Lyophilized (dehydrated by freezing in vacuo) powder 1,500,000 pm (fibrinolytic units) in 10 ml bottles in the package of 2 bottles.

Storage conditions. List B. at a temperature not higher than +10 ° C.

Streptokinase (Streptokinase)

Synonyms: Avelizin, Streptaz, Kabikinase.

Pharmachologic effect. Activates the fibrinolytic (dissolving blood clot) the enzyme system, cleaves fibrin contained in blood clots, resulting in thrombolesis (dissolving blood clot).

Indications for use. Embolia (blockage) of the pulmonary artery and its branches; thrombosis (blood clot formation in vessel) arteries and embolism of peripheral arteries in conservative (non-surgical) treatment; thrombosis of superficial and deep veins of limbs; acute myocardial infarction during the first 12 hours; Plugging vessels of the mesh eye shell.

Method of use and dose. Streptokinase is injected intravenously drip, and in the necessary cases intraarterially.

It is usually administered intravenously in the initial dose of 250,000 me (IE) in 50 ml of isotonic sodium chloride solution for 30 minutes (30 drops per minute). This dose usually causes the beginning of lysis (dissolution) thrombus. The introduction of streptokinase in a dose of 100,000 me per hour continues. The total duration of administration is, as a rule, 16-18 hours. Subsequent treatment is carried out by heparin and anticoagulants of indirect action.

With extensive arterial and venous thrombosis, it is sometimes necessary for a long introduction of streptocinase.

Intiarian administration of streptocinases are used in the acute period of myocardial infarction (the initial dose of 20,000 me; supporting - 2000-4000 me per minute for 30-90 minutes).

In all cases, the introduction of streptinate should begin as early as possible, since the best effect is observed with fresh blood clots.

The treatment of streptokinase is carried out under the control of thrombinime (blood coagulation indicator) and fibrinogen content (one of the factors of blood coagulation).

Side effect. Non-specific reactions to the protein are possible; Headache, nausea, light chills; allergic reactions; hematomas (limited blood cluster in tissue / bruise /) intramuscular injections; bleeding after puncture (piercing needle). To prevent allergic reactions, it is recommended to introduce intravenously 50 mg of prednisolone simultaneously with streptocinase. "

Contraindications. Hemorrhagic diathesis (increased bleeding), recent bleeding, pronounced hypertension (resistant blood pressure), streptococcal sepsis (blood infection by microbes / streptococci / focus of purulent inflammation), ulcer of the stomach, septic endocarditis (disease inland heart cavities due to the presence of microbes in the blood) , severe form sugar diabetespregnancy. The drug should be used with caution in severe liver and kidney diseases, with the active form of tuberculosis.

Release form. In bottles of 100,000, 250,000, 750,000 and 1,500,000 IE streptocinase.

Storage conditions. In a cool place.

UROKINASE

Synonyms: Ukidan.

Pharmachologic effect. Fibrinolytic (dissolving blood clot) agent. Splitting blood clots Due to the activation of plasminogen, which is an inactive predecessor of the plasmin (protein, which destroys the bunch of curved blood).

Indications for use. Thromboembolic occlusal diseases of the vessels (vessel thrombophlebitis / blood wall inflammation with their blockage /, embolism / blockage / pulmonary artery), the formation of local blood clots (blood clots) in arterio-venous hemodialysis shunts (special devices wearable for patients, for periodic connection to the machine " Aksto-venea kidney ") or intravenous cannulas (devices for intravenous infusions), some forms of chronic meningitis (myeliewingocele / spinal hernia /), coronaistrombosis (the formation of blood clot in the artery heart), bleeding in the front chamber of the eye and the vitreous body.

Method of use and dose. The average dose of 1000-2000 IU / kg / h; When applied for 24 hours, generalized proteolysis does not occur (enzymatic splitting of proteins), but fibrinolysis is provided (dissolving blood clot) at the level of blood clot; The treatment continues until the thromba desoblituration ( full recovery Bloodystands in the vessel previously clogged blood cloud) in combination with heparinotherapy. In the case of pulmonary embolism, arterial ischemia (arteries thrombosis), the myocardial myocardial infarction can be introduced in situ (affected by the artery) in a dose of 1000-2000 IU / kg / h; With severe pulmonary embolism - 15000. IU / kg / hour in the form of a single injection with a duration of 10 minutes. In some cases, during thrombosis of shunts (the formation of a blood clot in special devices wearable, for a periodic connection to the artificial kidney device), bleeding in the front chamber of the eye - local installations (instillation) are used for 5000-30,000 ME.

During pregnancy, the concentration of anti-poinase bodies is gradually increasing towards childbirth, making treatment

ineffective. Special observation is required if there is a diabetes in a patient, accompanied by severe retinopathy (non-reliable lesions of the retina of the eye). If it is necessary to combine this preparation with heparin, it should be administered sequentially at a certain time interval. If it is necessary to simultaneously administering the Hodium heparinase in the solution, the pH should create a pH (an acid-alkali state indicator) of more than 5.0, and with calcium heparin - 5.0-7.0.

Side effect. Development of shock, changes in liver samples, nausea, vomiting, loss of appetite, temperature rise, chills, headache, lethargy, with overdose of the drug - bleeding.

Contraindications. Hemorrhagic stroke (acute violation of cerebral circulation as a result of a brain vessel break), bleeding or their risk, recent intracranial surgical intervention, hemostasis deficiency (violation of the blood coagulation function), recent. Biopsy (fabric fence for morphological studies) of any organ, severe Arterial hypertension (resistant blood pressure), severe lack of liver or kidney function. Relative contraindications: recent surgical intervention, recent arterial puncture (piercing), inaccessible for local compression (local squeezing), pregnancy.

Release form. Flakeons containing 5000, 25,000, 100,000, 250,000, 500,000, 1,000,000 meroxinase complete with solvent bottles.

Storage conditions. In a dry, cool place.

Fibrinolysin (Fibrinolysinum)

Dry protein preparation of a natural enzyme isolated from plasma of donor blood.

Pharmachologic effect. The physiological component of the natural antighulating system of the body, the basis of which is the ability to dissolve fibrin threads.

Indications for use. Thromboembolia (blockage of blood clot vessels) of pulmonary and peripheral arteries, brain vessel thromboembolism, fresh myocardial infarction, acute thrombophlebitis (inflammation of the walls of the veins with their blockage), exacerbation of chronic thrombophlebitis.

Method of use and dose. Intravenously (drip) in a sodium chloride isotonic solution (100-160 drugs in 1 ml of solution) with the addition of heparin (up to 20,000 - 40,000 units).

Side effect. Non-specific reactions to protein (hyperemia / redness / face, pain along the veins, pains for the sternum and in the abdomen, chills, an increase in temperature, urticaria, etc.).

Contraindications. Hemorrhagic diathesis (increased bleeding), bleeding, open wounds, ulcerative disease of the stomach and duodenal intestine, nephritis (kidney inflammation), fibrinogenesis (low content in the blood of fibrinogen - one of blood coagulation factors), tuberculosis ( acute form), radiation sickness.

Release form. In bottles of 20,000 units.

Storage conditions. At temperatures from +2 to +10 ° C.

Celyasa (Celyasa)

Pharmachologic effect. The celiacis activates the fibrinolytic proferred contained in the blood (protein involved in the dissolution of the blood clot) - plasminogen, which turns into plasmin. Penetrated inside the blood cloth (blood clot) and causes it to dissolve.

Indications for use. Systemic and local arterial and venous thrombosis (blood clot formation in vessel). The drug is most effective when applied in the first 7 days of the disease.

Method of use and dose. Intravenously drip or intraarterially. The contents of the ampoule are dissolved in 1-2 ml of solvent (total dissolution occurs within 1-2 minutes, the presence of weighing, muta, the precipitate is not allowed). The solvent is used as glucine rolling, sodium chloride isotonic solution, 5% glucose solution. After a complete dissolution, the contents of the ampoule with a syringe are transferred to the bottle with one of the solvents listed above. The solution retains specific activity within 24 hours.

Treatment of celibe is carried out according to a special scheme only in stationary conditions (in the hospital).

Side effect. Resorbent fever (a sharp increase in body temperature associated with the flow of blood-cut production in blood flow). Reactions are possible in the form of hyperthermia (increasing temperature), chills, headaches, pain in the lower back, nausea,

conditioned by the presence in the preparation of heterogeneous (alien) protein.

Contraindications. Diseases and conditions predisposing to bleeding: hemorrhagic diathesis (increased bleeding), ulcerative lesions of the gastrointestinal tract, severe forms of sepsis (blood infection by microbes from the focus of purulent inflammation), hemorrhagic stroke (acute violation of the brain circle circulation as a result of a brain vessel break), tuberculosis lungs with a cavernous process, an active rheumatic process and other infections caused by streptococci; acute alcoholic intoxication (Alcohol poisoning), early (up to 3 days) postoperative, postpartum period, pregnancy. Persistent arterial hypertension (resistant blood pressure). With severe diabetes forms, the use of celibes is possible only on life indications.

Release form. In ampoules in lyophilized form (powder, dehydrated due to freezing in vacuo), 250,000 me, in a package of 10 pieces.

Storage conditions. List B. At temperatures from +2 ° C to + 10 ° C.

Fibrinolytic means I. Fibrinolytic means (+ Greek. Lytikos capable of dissolving; synonym for thrombolytic agents)

drugs contributing to the dissolution of intravascular thrombosis and used in arterial and venous thrombosis, as well as with pulmonary arteries thromboembolism.

Among F. s. distinguish: preparations with direct fibrinolytic effects (, oraza, tricholysine, etc.); Preparations dissolving due to the activation of plasminogen (streptocinase, urocinase, tissue plasminogen, transocinase, an acylated complex of plasminogen-dereocinase - plasminogen activator, streptodecadis); Preparations stimulating the formation of proteins of the fibrinolytic system (anabolic, a nicotinic acid and etc.).

From F. s. Direct action in domestic medical practice is noted mainly fibrinolysin derived from human blood plasma. However, on the effectiveness of fibrinolysin inferior to F. p., Activating, in connection with which modern conditions The most wide use of streptocinase and urchinase preparations.

Preparations that stimulate the formation of proteins of the fibrinolytic system (anabolic steroids, etc.) are usually not able to dissolve the already formed, therefore apply only to prevent thrombosis in individuals with a tendency to their formation.

Streptokinase and urocks are introduced intravenously drip or stroke (slow) for 15 min., Elimase - intravenously for 2-4 min., fibrinolysin - drip intravenously for 3-4 c. at a speed of 100-160 in 1 min.. Dose F. s. Various depending on the localization of blood clots. Thus, in the thrombosis of deep veins, the initial rapid introduction of 250,000 units of streptocinase or 300,000 units of urchinase is recommended, followed by the appointment of drugs for 2-3 days. Daily streptocinase 2,400,000 units, urchinase - 7,200,000 units. With the thromboembolism of pulmonary arteries, 250,000 pieces of streptokinase or 300,000 units of urchinase are initially introduced, then through every hour of 100,000 ug streptocinase or 250,000 unicinders for 12-24 c.. In case of occlusion of peripheral arteries, they resort to local intraarterial or systemic (intravenous) administration. Initial dose with intravenous administration of 250,000 units of streptocinase or 300,000 urkinase. For the next 2-3 days F. with. Apply in the same doses as for thromboembolism of pulmonary arteries. Locally prescribed streptokinase in a daily dose of 240,000 units, and the Urockase is 1,000,000. Introductions continue within 3 days. With myocardial infarction for intravenous administration The following doses are recommended: streptocinases - 1,500,000 units. Urocking - 2,500,000 units (within 60 min.), plasminogen fabric activator - 80 mg. within 180. min., Eminases - 30 units for 2-4 min.. Intorbornly, the urchinase is introduced in a dose of 500,000 units for 60 min Fabric plasminogen activator - 20 mg. For 60. min., Eminazy - 10 units for 15 min.. When using streptocinase, a rapid introduction of 20,000 units is recommended, and then 150,000 units for 60 min.. Simultaneously with plasminogen activators it is not recommended to apply acetylsalicylic acid. It is usually prescribed after 2 c. After the introduction of fibrinolithics.

In the process of therapy F. p. Hemorrhagic complications are most often arising. In addition, allergic reactions in the form of itching, urticaria, hyperemia of the face can be observed, as well as octvinations, an increase in body temperature. These complications rarely require cancellation. However, with the appearance of allergic and pyrogenic reactions, it is necessary to stop the introduction of F. p. and the purpose of glucocorticoids, antihistamine or antipirentic agents. In cases of small bleeding, especially from injection and superficial wounds, they usually do not stop, but are prescribed local. The introduction of F. p. only during bleeding, threatening life, as well as in cases of urgent operational intervention. It is normalized by introducing fibrinogen, factor VIII, whole blood or cryoprecipitate. For rapid neutralization of F. S. Sometimes they are resorted to the appointment of aminocaproic acid or other fibrinolysis inhibitors (see Antifibrinolytic agents) .

Contraindicated F. p. with hemorrhagic diathesis, peptic disease Stomach and duodenal in the stage of exacerbation, cavernous pulmonary tuberculosis under exacerbation, bleeding, open wounds, acute radiation disease in the stage of deployed clinical picture, increase systolic above 200 mm RT. Art. and diastolic blood pressure above 110 mm RT. Art., As well as in the first days after operations and childbirth.

II. Fibrinolithic (Fibrinolytica; + Greek. Lytikos capable of dissolving)

drugs contributing to the dissolution of fibrin bunch and used for the treatment of diseases accompanied by thrombosis (for example, fibrinolysin, streptase).

1. Small medical encyclopedia. - M.: Medical encyclopedia. 1991-96 2. First medical care. - M.: Large Russian Encyclopedia. 1994 3. encyclopedic Dictionary medical terms. - M.: Soviet Encyclopedia. - 1982-1984.

Watch what is "fibrinolytic means" in other dictionaries:

    - (Fibrinolytica; Fibrin + Greek. Lytikos capable of dissolving) drugs contributing to the dissolution of fibrin clot and used to treat diseases accompanied by thrombosis (eg, fibrinolysin, streptase) ... Big Medical Dictionary - I Pleurrites (Pleuritis; Pleurra + ITIS) Inflammation of the pleura, accompanied by the formation of exudate various character in pleural cavity. As a rule, P. is not an independent nosological form, but complicates the course of pathological ... ... Medical encyclopedia

    - (Greek anti counter + fibrinolysis; synonyms of fibrinolysis inhibitors) drugs that reduce the fibrinolytic activity of blood. Distinguish synthetic A. s. (aminocapronic, aminonetylbenzoic and transcamic acids) and A. s. ... ... Medical encyclopedia

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    One of the forms of necrosis of the muscles of the heart caused by acute insufficiency Bloodystands in the corona arteries that feed the fabric of the heart. The insufficiency of coronary (corn-free) blood flow (coronary failure) may be related to either ... ...

    - (r. 10.6.1929, Gorky), Soviet therapist, academician (1971) and member of the Presidium (since 1972) of the USSR AMN, Honored Worker of Science of the RSFSR (1974). Member of the CPSU since 1962. After graduating from the Kiev Medical Institute (1953), he worked in 1 m Moscow ... ... Great Soviet Encyclopedia

    Evgeny Ivanovich (r. 10.6.1929, Gorky), Soviet Therapist, Academician (1971) and member of the Presidium (since 1972) of the USSR AMN, Honored Worker of Science of the RSFSR (1974). Member of the CPSU since 1962. After graduating from the Kiev Medical Institute (1953) ... ... Great Soviet Encyclopedia

The human body is a very complex system in which even one failure can lead to serious consequences.

Fortunately, medicine and science do not stand still, humanity Every year he knows new secrets of anatomy and ways of influence on internal processes.

Drugs are considered one of the most common ways to influence intrasystems in the body.

Now there is a unpelled number of all kinds of drugs, and having heard their name, a person does not always understand their purpose.

These include fibrinolities, the name of which is surprising only.

So let's consider in more detail the drugs of fibrinolics, which is what it is for which they are prescribed.

What is this tools?

Fibrinolytic means is anyone medicalcapable of stimulating the dissolution of the thrombus. They are also called thrombolytic medicinal preparations. The effect of fibrinolithics is directed to the activation of fibrinolysis - the process of dissolving blood clots.

Thus, the fibrinolytic activity of blood is the body's property aimed at the discharge of bunches.

This property distinguishes them from anticoagulants that prevent the formation of blood clots, suppressing the synthesis or the function of various coagulation factors.

The fibrinolytic blood system that exists in the human body is also involved in lysis or dissolving bunches during wound healing. This system suppresses fibrin that inhibits the thrombin enzyme.

The active enzyme involved in the fibrinolytic process is plasmin, which is formed under the influence of an activating factor released from endothelial cells.

Classification of drugs

There are two main class of fibrinolytic agents: direct and indirect action. The first includes fibrinolysis activators, and the second streptocinase and the urchinase. Consider this classification of fibrinolithics in more detail:

  1. Activator fibrinolysis. This family of thrombolytic drugs is used in acute myocardial infarction, cerebrovascular thrombotic stroke and pulmonary embolism. With acute myocardial infarction, fabric activators are usually preferable than streptocinase.
  2. Streptokinaza. Streptocinase and anistoplase are used in acute myocardial infarction, arterial and venous thrombosis and pulmonary embolism. These compounds are antigen, since they are obtained from bacteria streptococci.
  3. Urokinza. The Urockase is sometimes called the urinary plasminogen activator because it is produced by the kidneys and is in the urine. It has limited clinical applicationbecause, like streptokinase, it causes significant fibrinogenolysis; Used for the treatment of pulmonary embolism.

When applied

Fibrinolytic therapy approved for emergency treatment of stroke and heart attack.

The most commonly used preparation for thrombolytic therapy is the fibrinolysis activator, but other drugs of this group can also perform this function.

Ideally, the patient must receive these medicines for the first 30 minutes after arriving at the hospital.. A quick fibrinolytic effect is that, for which these drugs are prescribed in these cases.

Heart attacks

Blood cluster can block arteries in the heart. This can cause a heart attack when part of the heart muscle dies due to lack of oxygen. Thus, thrombolitics quickly dissolve large clots.

It helps to resume blood flow to the heart and prevent damage to the heart muscle. top scores You can achieve if the medicine was introduced within 12 hours after the start of the heart attack.

The drug restores the influx of blood to the heart in most people. Nevertheless, some patients may have blood flow to be not quite normal, and in this connection damage to heart muscles may be observed.

Stroke

Most cases of stroke are caused when blood clots fall into blood vessel In the brain and block the influx of blood to this area.

In such cases also you can use fibrinolities to quickly dissolve the clutch.

The introduction of drugs within 3 hours after the appearance of the first symptoms of the stroke can help avoid brain damage and disability.

These drugs are also used with a decrease in the fibrinolytic blood activity.

In such cases, the body is not capable of preventing the formation of thrombus, so he needs medical care.

Even in case of success of fibrinolization thrombolysis not able to restore fabrics that have already been damaged by blood circulation.

Thus, the patient may require further treatment to eliminate the main reasons for the formation of blood clots and restore damaged tissues and organs.

Contraindications and side effects

Bleeding is the most common risk associated with the use of drugs. It can also threaten the patient's life.

Minor bleeding from gums or nose can be observed about 25% of patients receiving the drug.

Bleeding in the brain occurs about 1% of cases.

This is the same risk for both patients with stroke and heart attack.

Bleeding is often noted on the catheterization site, although gastrointestinal and cerebral hemorrhages are possible.

Therefore, patients who suffered injury or having a history of cerebral hemorrhage usually do not prescribe fibrinolities.

In addition to the serious risk of internal bleeding, others are possible. side effects, eg:

  • bruises on the skin;
  • damage to blood vessels;
  • migration of blood clot into another part of the vascular system;
  • damage to kidneys in patients with diabetes or other kidney disease.

Although fibrinolics can safely and effectively improve blood flow and eliminate symptoms in many patients without the need for invasive surgery, they are not recommended for all.

Such drugs are prohibited for patients who accept funds for blood dilution, as well as for people with increased risk of bleeding. These conditions include:

  • high pressure;
  • bleeding or severe blood loss;
  • hemorrhagic stroke from bleeding in the brain;
  • severe kidney disease;
  • recent operation.

List of drugs

Speaking about the drugs of fibrinolytics, the list can be quite extensive, we will only call some of them.

The most common trademarks of fibrinolithics are as follows:

  • Aktilase;
  • Thrombovazim;
  • Fortelizin;
  • Metalization;
  • Thromboflux and others.

Almost all these drugs are released by a doctor's prescription, as they have a wide range of contraindications and side effectsand therefore can apply potential harm organism.

Conclusion

If you suspect the symptoms of a heart attack or stroke, you need to quickly apply to ambulance, but in no case cannot be engaged in self-medication.

Source: http://varikoznik.com/varikoz/lekarstva/fibrinoliticheskie-sredstva.html

What is fibrinolytic drugs?

drugs contributing to the dissolution of intravascular thrombosis and used in arterial and venous thrombosis, as well as with pulmonary arteries thromboembolism.

Among F. s. They differ: preparations with direct fibrinolytic effect (fibrinolysin, oraza, tricholysine, etc.

); Preparations dissolving the thrombus due to the activation of plasminogen (streptocinase, urocinase, fabric activator plasminogen, transocinase, acylated complex plasminogen-dereocinase - plasminogen activator, streptodecadis); Preparations, stimulating the formation of proteins of the fibrinolytic system (anabolic steroids, nicotinic acid, etc.).

From F. s. Direct action in domestic medical practice is noted mainly fibrinolysin derived from human blood plasma. However, according to the effectiveness of fibrinolysin inferior to F. p., Activating plasminogen, in connection with which, in modern conditions, the most broad use of streptocinase and urchinase preparations were found. Rottenise - an enzyme produced by some strains of β-hemolytic streptockers.

Preparations of streptocinases, close source of obtaining and properties, are produced in various countries under the names of "Tsillias", "Avelizin", "Streptaz", "Kabikinase", etc. Connecting with plasminogen in a stoichiometric ratio (1: 1), streptokinase helps to convert plasminogen molecule in plasmin. In the body of a person, streptocinase is partially associated with antibodies, and therefore only a portion of the administered dose of this drug interacts with plasminogen.

The half-life period of streptocinase associated with antibodies is about 20 minutes, and plasminogen associated with plasminogen - about 80 minutes.

In the body streptocinase, it is metabolized to amino acids and peptides, which are removed by the kidneys, peptocinase has antigenic properties and therefore causes the formation of antibodies to it, the content of which in systematic use of the drug gradually increases, which causes a decrease in streptocinase efficiency, due to its binding to antibodies.

Usually by the 6th day from the beginning of treatment, the level of antibodies becomes so high that the injected drug is almost completely associated with them. For this reason, the further use of streptocinase becomes inappropriate due to the loss of its effectiveness. The height of the antibody titer to streptokinase significantly affects the previous streptococcal infection, which contributes to an increase in their production.

Urocking is a specific proteolytic enzyme derived from human urine and culture of human kidney cells of a human embryo. The urocinase converts plasminogen to plasmin by splitting arginyl-valve ties in its molecule. Like streptokinase, the urchinase reacts both with plasminogen adsorbed on fibrin and with plasminogen circulating in the blood.

The drug acts briefly (half-life during intravenous administration 9-16 min). Urocking reduces the plasminogen content and plasma fibrinogen, as well as the level of α2-antiplasmin, increases the content of fibrin and fibrinogen cleavage products, lengthens the thrombin time. With the introduction of urocinase, allergic reactions are practically no observed, and antibodies to it does not occur.

The fabric activator of plasminogen and transokinase has a more selective fibrinolytic effect and very little affect the content of fibrinogen in the plasma.

The fabric activator plasminogen is produced by the cells of the endothelium of blood vessels. As a serine-protease of a trypsin type, it affects plasminogen only in the presence of fibrin.

The plasmin formed on the fibrin is practically not inhibited by α2-antiplazmine.

The clinical study of the plasminogen tissue activator showed that it is the most active thrombolytic agent, the action of which is not limited to antigenic properties and is practically not accompanied by an increase in the plasmin and fibrinogen content. For medical purposes, the drug is obtained from human melanoma cell culture or with gene technology.

Procurocase on fibrinolytic properties is close to the tissue activator of plasminogen. It differs from the urchinase, it is distinguished by the inhibitors of this enzyme circulating in the blood, as well as the fact that the active form is transformed only during adsorption on fibrin.

The acylated complex of plasminogen-streptokinase - plasminogen activator (AR-SAC; Synonym Elimase) is a drug created on the basis of the principle of enzyme acylation by introducing an acyl group to the active center, which prevents the interaction of this enzyme with streptocinase contained in the complex.

Gradually, freeing from the acyl group, the complex acquires proteolytic activity and dissolves the thrombus. According to efficiency and selectivity, the action is similar to the tissue activator of plasminogen.

With venous thrombosis F. p. There are a pronounced effect in cases where they apply in terms of up to 10 days from the beginning of clinical manifestations of thrombosis. The most high efficiency (lysis of blood clots in 70% of cases) when appointing F. p. In the first 2 days. According to a number of the author, the most optimal is the introduction of F. y: within 12 hours.

This marks the highest percentage of thrombolysis and the smallest frequency of bleeding and pyrogenic reactions. With intracerebral vein thrombosis, F. s. apply only under control computer tomography. When thromboembolism of pulmonary arteries, fibrinolytic agents show the effect in cases of massive occlusion and, subject to the rapid administration of drugs from the start of clinical symptoms.

With arterial thrombosis F. p. There is a pronounced effect in cases where therapy begins for 12 hours from the moment of clinical symptoms. In the presence of chronic stenosis of the arteries, the effectiveness of F. with. significantly decreases. Positive results of applying F. with. Described in thrombosis of renal and mesenteric artery, the thrombosis of the arteries of the retina, and also an intracardular thrombe. With myocardial infarction, the use of streptocinase reduces mortality by 50%.

Preparations that stimulate the formation of proteins of the fibrinolytic system (anabolic steroids, etc.) are usually not able to dissolve the already formed thrombosis, therefore apply only in order to prevent thrombosis in persons with a tendency to their formation. Strectinase and urocinate introduced intravenously drip or stake (slow) in The flow of 15 minutes, the Eminase - intravenously for 2-4 minutes, fibrinolysin - drip intravenously for 3-4 hours with a speed of 100-160 units in 1 min. Dose F. s. Various depending on the localization of blood clots.

Thus, in the thrombosis of deep veins, the initial rapid introduction of 250,000 units of streptocinase or 300,000 units of urchinase is recommended, followed by the appointment of drugs for 2-3 days. Daily dose streptocinase 2,400,000 units, urchinase - 7,200,000 units. In terms of thromboembolism of pulmonary arteries, 250,000 pieces of streptocinase or 300,000 units of urchinase are initially introduced, then through each hour of 100,000 uh streptocinase or 250,000 unicinders for 12-24 hours.

In case of occlusion of peripheral arteries, they resort to local intraarterial or systemic (intravenous) administration. Initial dose with intravenous administration of 250,000 units of streptocinase or 300,000 urkinase. For the next 2-3 days F. with. Apply in the same doses as for thromboembolism of pulmonary arteries. Locally prescribed streptokinase in a daily dose of 240,000 units, and the Urockase is 1,000,000. Introductions continue within 3 days.

With myocardial infarction for intravenous administration, the following doses are recommended: streptocinases - 1,500,000 units. Urokinase - 2,500,000 units (for 60 minutes), plasminogen tissue activator - 80 mg for 180 minutes, Elimases - 30 units for 2-4 minutes. Intorbornly, the Urockase is introduced at a dose of 500,000 units for 60 minutes, plasminogen tissue activator - 20 mg for 60 minutes, Elimase - 10 units for 15 minutes.

When using streptocinase, a rapid introduction of 20,000 units is recommended, and then 150,000 units for 60 minutes. Simultaneously with plasminogen activators, acetylsalicylic acid is not recommended. It is usually prescribed 2 hours after the end of the introduction of fibrinolithics.

In the process of therapy F. p. Hemorrhagic complications are most often arising. In addition, allergic reactions in the form of itching, urticaria, hyperemia of the face, headache, as well as octvinations, body temperature increase can be observed. These complications rarely require cancellation. However, with the appearance of allergic and pyrogenic reactions, it is necessary to stop the introduction of F. p. and the purpose of glucocorticoids, antihistamine or antipirentic agents.

In cases of small bleeding, especially from injection and surface wound places, usually treatment is not stopped, but local hemostatic agents are prescribed. The introduction of F. p. Only with bleeding, threatening life, as well as in cases of necessity of urgent surgery.

It is normalized by hemostasis by administering fibrinogen, factor VIII, whole blood or cryoprecipitate. For rapid neutralization of F. S. Sometimes they are resorted to the appointment of aminocaproic acid or other fibrinolysis inhibitors (see Antifibrinolytic agents).

Contraindicated F. p. In hemorrhagic diattes, ulcerative diseases of the stomach and duodenum in the exacerbation stage, the cavernous tuberculosis of the lungs in the stage of exacerbation, bleeding, open wounds, acute radiation sickness in the stage of a deployed clinical picture, increasing systolic blood pressure above 200 mm RT. Art. and diastolic blood pressure above 110 mm RT. Art., as well as in the first days after operations and childbirth.

drugs contributing to the dissolution of fibrin bunch and used for the treatment of diseases accompanied by thrombosis (for example, fibrinolysin, streptase).

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The mechanism of the action of thrombolytic, indications, side effects

From this article you will learn: how to act thrombolyticsWho and for which they are prescribed. Varieties of drugs. Side effects, interaction with other medicines, contraindications.

Thrombolytics (fibrinolics) are drugs whose action is aimed at the destruction of blood clots.

Unlike antiagregants and anticoagulants, which reduce blood viscosity and prevent thrombosis, thrombolytics are capable of dissolving already formed blood clots.

Therefore, antiagregants and anticoagulants are prevention of blood clots, and thrombolytics are their treatment.

Introduces the drug of this group only an experimental resuscator or a cardiologist in a hospital.

Mechanism of action

For the "viscosity" of blood corresponds to the special protein - fibrin. When it is not enough in the blood - a tendency to bleeding appears and the process of coagulation is slowed down during tissue damage. But when its level is increased - thrombus are formed out of it.

Splits excessive amount of fibrin Special enzyme plasmin. The splitting process is called fibrinolysis. In the blood, this enzyme is present in large quantities in inactive form - in the form of plasminogen. And only if necessary, it turns into plasmin.

Mechanism of physiological fibrinolysis

In healthy people, the amount of fibrin and plasmin in the blood is balanced, but with a tendency to thrombosis, the plasmin level is lowered.

Thrombolytic preparations (another name - fibrinolitics) activate the absorption of blood clots, turning plasminogen into plasmin, which is capable of splitting fibrin - protein forming blood closures.

Indications

Fibrinolitics are prescribed with such pathologies:

  • Myocardial infarction provoked by Tromb.
  • Ischemic stroke.
  • Pulmonary embolism.
  • Thrombosis of any major arteries or veins.
  • Intricultural clomes.

The drug treatment of thrombosis is advisable no later than for 3 days from the moment of the formation of the thrombus. And most effectively it is in the first 6 hours.

Varieties of thrombolytic

For novelty and efficiency, drugs of this group are divided into 3 generations.

Despite the effectiveness of the means, it often causes allergic reactions. The first preparation that has thrombolytic activity has become streptocinase. This enzyme produces bacteria - beta hemolytic streptococci. For the first time, the fibrinolytic effect of this substance was described back in 1940.

Moreover, streptocinase, and the urchinase provoke the splitting of not only hazardous fibrin that has formed a thrombino, but also fibrinogen, promrombin, factor of coagulation 5 and the coagulation factor 8. It is very fraught with bleeding.

These shortcomings of the first thrombolitics and prompted scientists to develop new, more secure fibrinolytic agents.

Thrombolytics2 and 3 generations are more selective. They act to a greater extent purpose on the thrombus and do not so much blood diluted.

This minimizes bleeding, as a side effect of thrombolytic therapy.

However, the risk of bleeding is still preserved, especially if there are predisposing factors (if they are presented, the use of drugs is contraindicated).

In modern medical practice, predominantly thrombolitics 2 generations are used, as they are safer than generation preparations.

Contraindications

Do not conduct thrombolytic therapy in such cases:

  • Abundant internal bleeding in the last six months.
  • Surgical operations on the dorsal or brain in history.
  • Hemorrhagic diathesis.
  • Inflammatory diseases of the vessels.
  • Suspicion of hemorrhagic stroke
  • Severe arterial hypertension, non-drug control (systolic blood pressure above 185 mm Hg. Art. Either diastolic above 110 mm Hg. Art.).
  • Recent brain injury.
  • Transferred 10 days and later severe injury or surgical operation.
  • Birth (10 days ago and later).
  • Conducted less than 10 days ago puncture is connectible or yarem Vienna and other vessels that cannot be fried.
  • Cardiovary resuscitation, which lasted more than 2 minutes, as well as the one that provoked injuries.
  • Hepatic insufficiency, severe liver diseases (cirrhosis, hepatitis, etc.).
  • Varicose extension of the veins of the esophagus.
  • Hemmorrhagic retinopathy (a tendency to the retina hemorrhages is often found in diabetes).
  • The aggravation of ulcerative disease in the last 3 months.
  • Pancreatitis in acute form.
  • Endocarditis of bacterial nature.
  • Aneurysms and other anomalies of large arteries or veins.
  • Tumors with increased risk of bleeding, especially in the gastrointestinal bodies, in the lungs, brain.
  • Hemorrhagic history in history.
  • Intracranted hemorrhage in history.
  • Heavily flowing ischemic stroke, with convulsions among the symptoms.
  • Tuberculosis with hearding.
  • Individual intolerance to the drug.

Hemorrhagic stroke

There are also contraindications regarding blood condition at the moment. Thrombolytics Contraindicated if blood test showed the following deviations:

  • Sugar level above 400 milligrams per deciliter or less than 50 mg / dl.
  • The amount of platelets is less than 100,000 per mm3.

If the drug is used in stroke, that is, age limitations. Fibrinolitics are usually not introduced with insulte patients under 18 and over 80 years old.

Interaction with other medicines

Preparations for thrombolytic therapy are not administered against the background of taking anticoagulant patients (such as warfarin).

With simultaneous use with the means that affect the level of platelets (antibiotics of the group of cephalosporins, non-steroidal anti-inflammatory agents, corticosteroids), increases the risk of bleeding.

In patients who took antiarrhegnants on a permanent basis, the risk of bleeding also increases. The doctor necessarily takes into account this when calculating the dosage of thrombolytic.

If the patient is shortly before the introduction of fibrinolyticism accepted aPF inhibitorsThe risk of an allergic reaction increases.

Side effects

The main side effect of all thrombolytic - bleeding:

    1. External. Of the recent damaged vessels, for example, from which blood was taken for analysis. From gums, nose.
    2. Hemorrhage into the skin. In the form of petechius (points), bruises

Patechian hemorrhage

  1. Internal. From the mucous gastrointestinal tract, organs gOOD SYSTEM. Hemorrhage into the retroperitoneal space. In the brain (manifest neurological symptoms: cramps, speech disorders, intensity). Less often - bleeding from parenchymal organs (liver, adrenal glands, spleen, pancreas, thyroid and other glands, lungs).

Internal bleeding in patients without contraindications are quite rare.

Arrhythmias may also be observed (which will require antiarrhythmic medicines), reduction of blood pressure, nausea, vomiting, increase body temperature.

With an allergic reaction to the drug, the rash, spasm of the bronchi, swelling, pressure reduction appear. Allergies to the medicine can lead to a deadly anaphylactic shock. Therefore, it is important to apply antiallergic tools in time when the first symptoms appear.

The side effects are most pronounced at the ages of 1 generation. When using fibrinolithics 2 and 3 generations, they arise less often and are not so hard.

When using 1 generation thrombolitics, there is so heavy bleeding that it will be necessary blood transfusion.

Further treatment

An increased production of thrombin - substances that increase the thrombosis becomes a response of the organism on a sharp thinning of blood.

This can lead to thrombosis recurrence.

For prophylaxis, a thrombolytic 2 or 3 generation may be reused (but not the 1st due to higher bleeding after their use).

Instead re-administration Fibrinolyticism, for the prevention of re-formation of thromboms, can use anticoagulants (heparin) or antiagregants (acetylsalicylic acid).

Overdose

Since the drug is rapidly excreted from the body, an overdose arises rarely. However, it is very dangerous, as it provokes abundant bleeding, after which blood transfusion is required.

To eliminate overdose, the administration of the drug is stopped.

Antifibrinolitics (fibrinolysis inhibitors) can also be introduced - preparations with reverse action that restore blood coagulation and stop bleeding. The most common medication of this group is an aminocaproic acid.

F and b r and n about l and t and ch e s k and e with r e d with t in

Direct action

Fibrinolysin

Streptokinaza

Streptodekaza

Urokinza

Indirect action (Fabric activators plasminogen)

Alplaza

Aktivaz

Direct Action (thrombolytics)

Fibrinolysin \u003d thrombolycin

Proteolytic enzyme is obtained from plasminogen plasma of donors.

Mechanism of action

Splitting of peptide bonds in a polymerized fibrin molecule

(As a result, fragmentation of the molecule).

In addition, it contributes to the activation of the endogenous plasminogen catalyst (like plasmin)

Application

With thromboembolic complications intravenously, drip

(pulmonary artery thromboembolism, peripheral vessels, acute myocardial infarction, acute thrombophlebitis).

Intravenously drip in 5% R-RE glucose for 2-12 hours

in a dose to 80,000 - 100 000 U / day

Side effects

1. Cover by antigenic properties: allergic reactions, fever

Streptokinase \u003d streptase \u003d celiac disease

The enzyme produced by beta hemolytic streptococcus.

Lyophilized powder.

Mechanism of action.

Activates the conversion of plasminogen to plasmin.

Plazmin has the ability to split fibrin fibrin and fibrinogen, circulating in the blood.

This transformation is catalyzed by a complex, which forms streptocinase with an inactive fraction of plasminogen.

Small doses streptocinase are ineffective (only small portions of the complex are formed).

Application

Intravenously or intraarterially.

Side effects

1. Cover by antigenic properties:

allergic reactions, fever

2. Pain in the joints, nausea. Vomot

3. Possible danger - the possibility of bleeding

(Since rapid formation is happening in the blood of high plasmin concentrations).

Then the fibrinolysis inhibitors are prescribed - epsilon-aminocaproic acid.

Streptokinase cannot be reused for 1 year.

Streptodekaza

This streptocinase immobilized on a water-sized polysaccharide matrix.

Streptocinase is protected from interaction with natural inhibitors,

the toxicity and antigenicity of its protein component decreases (fewer side effects).

The gradual biodegradation of the polysaccharide molecule provides uniform and prolonged release and action of the enzyme.

It is introduced once, intravenously, stove.

Side effects

Hemorrhagic syndrome arises less frequently.

Urokinza

The enzyme that is synthesized in the kidneys and is contained in the urine.

Mechanism of action

Activates plasminogen.

In contrast, streptocinase does not have pronounced antigenic properties.

Action short (15 min.)

High cost, getting difficulty.

Application

1. Eastern widespread thrombosis of deep veins pelvis and lower extremities.

2. Acute massive lung artery thromboembolism.

3. Less pronounced thromboembolism against the background of violations of the functions of the respiratory system and the SCC.

4. Arterial thrombosis when impossible surgical intervention.

5. Chronic stenosis of large arterial vessels.

Indirect action

High affinity for fibrin, minor increase in total fibrinolytic activity.

Indirect fibrinolities (thrombolytics)

(Plasminogen fabric activators, tap)

Preparations: Elimase, activase, alteplelase, retев: High affinity for fibrin and with a slight increase in total fibrinolytic blood activity. Corn half-life

(Metabolized mainly in the liver)

Indications for use:

Myocardial infarction, pulmonary artery thrombosis, peripheral vessels

In the first 12 hours after myocardial infarction, Aldeptalaz is introduced according to the scheme:

10 mg in / in bolus in 1-2 minutes; then 50 mg for the first hour, then 10 mg 30 minutes to a total dose of 100 mg

If no more than 6 hours passed after myocardial infarction, they are injected according to an accelerated scheme - 90 minutes before the total dose of 0.75 mg / kg (52.5 mg / 70 kg

Fabric Activator Plasminogen (TAP)

Recommended by recombinant by controlling the synthesis of DNA RNA of a certain strain of the intestinal stick.

In the absence of fibrin, TAP does not interact with plasminogen.

During thrombosis, the process of fibrin cleavage occurs on a thrombus and inside it without systemic fibrinolysis, which determines a smaller amount of hemorrhagic complications.

The drug with antithrombotic, fibrinolytic and angioprotective action

Sulodekside

A mixture of heparin-sulfate (80%) and dermatantium sulfate (20%).

Mucous membrane extract thin gut animals.

Refers to heparinoids.

Heparinoids are related to heparin by chemical structure.

Antithrotic mechanism

Associated with the suppression of activated factor X,

reducing platelet aggregation

decrease in the synthesis and secretion of prostacyclin,

reducing the concentration of fibrinogen in blood plasma.

An angioprotective mechanism

Associated with the restoration of the structural and functional integrity of the endothelium of blood vessels,

restoration of the normal density of the negative electrical charge of pores of the basal membrane of vessels.

Anticoagulant action in high doses.

Due to the inhibition of the HEPARIN COFACTOR II.

Indications: angiopathy with increased risk of thrombosis or stimulate their education. Ficitis of proseagulantov

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