Improvement of blood properties - Heparin. Heparin sodium (Heparin sodium)

Formula, chemical name: mucopolysaccharide of polysulfuric acid ester.
Pharmacological group: hematotropic agents / anticoagulants
Pharmachologic effect: anticoagulant.

Pharmacological properties

Heparin, binding with antithrombin III, causes conformational changes in its molecule and accelerates its complexation with serine proteases of the coagulation system; this leads to blocking of thrombin, enzymatic activity of activated factors IX, X, XI, XII, kallikrein and plasmin. Heparin binds thrombin; this process has an electrostatic origin and depends, to a greater extent, on the length of the heparin molecule; only a small part of the heparin molecule has similarities with antithrombin III, which mainly provides the anticoagulant activity of heparin. Inhibition of thrombin by antithrombin is a slow process; the formation of the heparin-antithrombin III complex is greatly accelerated due to the direct binding of heparin by gamma-aminolysyl components of antithrombin III and due to the interaction through serine between thrombin and through arginine by the heparin-antithrombin III complex; upon completion of the thrombin inhibition reaction, heparin leaves the heparin-antithrombin III complex and can be used again by the body, and the complexes that remain are removed by the endothelial system.
Heparin reduces blood viscosity, reduces vascular permeability, which is stimulated by histamine, bradykinin and others endogenous factors, and thus prevents the development of stasis. For endogenous analogues of heparin, special receptors have been identified on the surface of endothelial cells. Heparin is capable of surface shaped elements blood and endothelial membranes to be sorbed, increasing their negative charge, this prevents the aggregation and adhesion of platelets, leukocytes, erythrocytes.
Heparin molecules, which have low affinity for antithrombin III, inhibit hyperplasia smooth muscle, including by slowing down the adhesion of platelets with inhibition of the liberation of the growth factor of these cells, inhibit the activation of lipoprotein lipase, thereby preventing the development of atherosclerosis.
Heparin also binds part of the components of the complement system, reducing its activity, prevents the formation of immunoglobulins and the association of lymphocytes, binds serotonin, histamine - due to all this, an antiallergic effect is possible.
Heparin reacts with surfactant, reducing its activity in the lungs.
Heparin affects endocrine system- binds adrenaline, suppresses excessive production of aldosterone in the adrenal cortex, enhances the activity of parathyroid hormone, modulates the ovarian response to hormonal stimuli.
Heparin, as a result of reaction with enzymes, can increase the activity of pepsinogen, brain tyrosine hydroxylase, DNA polymerase and reduce the activity of pyruvate kinase, myosin ATPase, pepsin, RNA polymerase.
Heparin in patients with ischemic disease hearts (together with acetylsalicylic acid) reduces the risk of developing sudden death, myocardial infarction and acute thrombosis coronary arteries. Heparin reduces mortality among patients who have had myocardial infarction and the frequency of recurrent heart attacks.
In high doses, heparin is effective in venous thrombosis and pulmonary embolism, in small doses for the prevention of venous thromboembolism, including after surgical operations.
Heparin, when administered intravenously, slows down blood clotting almost immediately, when administered intramuscularly - after 15-30 minutes, when administered subcutaneously - after 40-60 minutes, after inhalation, the maximum effect is after a day; respectively, the duration of the anticoagulant effect is 4–5 hours, 6 hours, 8 hours, 1–2 weeks, prevention of thrombosis ( therapeutic effect) - lasts much longer. The antithrombotic effect of heparin may limit the deficiency of antithrombin III at the site of thrombosis or plasma. The highest bioavailability of heparin is observed after intravenous administration; when administered subcutaneously, bioavailability is low. The maximum plasma concentration is reached after 2 to 4 hours. The half-life of heparin from blood serum is 1-2 hours. In plasma, heparin is found mainly in a protein-bound state. Heparin is intensively captured by cells of the mononuclear-macrophage system and endothelial cells, accumulates in the spleen and liver. When inhaled, heparin is absorbed by the endothelium of capillaries, large lymphatic and blood vessels, alveolar macrophages: these cells are the main site of accumulation of heparin, from which it is gradually released, maintaining a certain concentration in serum. Heparin undergoes desulfurization under the action of heparinase and platelet N-desulfamidase, which at later stages are included in the metabolism of heparin. Desulfated heparin molecules under the influence of renal endoglycosidase are converted into low molecular weight fragments. The excretion of heparin occurs in the form of metabolites through the kidneys; unchanged excretion is possible only with the introduction of high doses of heparin. Heparin is not released from breast milk does not cross the placental barrier. When applied externally a small amount of heparin is absorbed into the systemic circulation from the surface of the skin. The maximum concentration in the blood after application is noted after 8 hours.

Indications

Parenterally: acute infarction myocardium, unstable angina; thromboembolic complications during surgery blood vessels and heart, myocardial infarction, thrombosis cerebral vessels and coronary arteries, thromboembolism pulmonary artery(including in the pathology of peripheral veins), thrombophlebitis (therapy and prevention); syndrome of disseminated intravascular coagulation, treatment and prevention of microcirculation disorders and microthrombosis; thrombosis of the renal veins; deep vein thrombosis; hemolytic-uremic syndrome; mitral heart disease (prevention of thrombus formation), atrial fibrillation(including accompanied by embolization); bacterial endocarditis; lupus nephritis; glomerulonephritis; prevention of blood coagulation during forced diuresis, extracorporeal methods (hemodialysis, hemosorption, extracorporeal circulation during heart surgery, cytapheresis, peritoneal dialysis); flushing of venous catheters.
Externally: thrombophlebitis of superficial veins, migratory phlebitis (including those with varicose ulcers and chronic varicose disease), aseptic infiltration and local edema, subcutaneous hematoma(including during phlebectomy), complications during surgical operations on the veins, injuries, bruises of tendons, joints, muscle tissue.

Dosing and Administration of Heparin Sodium

Heparin is administered intravenously, subcutaneously, and is used externally. The dosage regimen is individual and depends on the indications used dosage form, clinical situation and age of the patient.
Cancellation of heparin should be carried out gradually. When using heparin, it is necessary to constantly monitor the clotting time. For dilution of heparin, use only saline. In severe thrombocytopenia (a decrease in the number of platelets by 2 times from the initial number or less than 100,000 / µl), the use of heparin should be urgently discontinued. When used externally, do not apply to mucous membranes, open wounds. Gel together with tetracyclines, non-steroidal anti-inflammatory drugs, antihistamines are not assigned.

Contraindications for use

Hypersensitivity; for parenteral use: hemophilia, hemorrhagic diathesis, vasculitis, bleeding, thrombocytopenia (including those caused by a history of heparin), leukemia, polyps, increased vascular permeability, ulcerative lesions and malignant neoplasms gastrointestinal tract, severe uncontrollable arterial hypertension, varicose veins esophageal veins, acute bacterial endocarditis, recent surgery on the eyes, spine, brain, trauma (especially craniocerebral), severe violations functional state kidneys and/or liver;
for outdoor use: traumatic injury skin, purulent, ulcerative-necrotic processes on the skin.

Application restrictions

Thrombocytopenia, increased tendency to bleeding, polyvalent allergy (including bronchial asthma), arterial hypertension, dental procedures, diabetes, endocarditis, pericarditis, the presence intrauterine contraceptive, active tuberculosis, radiation therapy, liver failure, chronic kidney failure, over 60 years of age.

Use during pregnancy and lactation

The use of heparin sodium during pregnancy and breastfeeding possible only under strict conditions.

Side effects of heparin sodium

System effects: nervous system: headache, dizziness;
circulatory and blood system: thrombocytopenia - early (2-4 days of therapy) and late (autoimmune), in rare cases fatal, hemorrhagic complications - bleeding from urinary tract or gastrointestinal tract, retroperitoneal hemorrhages in the adrenal glands (with the development of acute adrenal insufficiency), ovaries;
digestive system: nausea, loss of appetite, vomiting, increased levels of transaminases in the blood, diarrhea;
allergic reactions: drug fever, skin hyperemia, urticaria, pruritus, rash, bronchospasm, anaphylactic shock, anaphylactoid reactions; others: with prolonged use - alopecia, soft tissue calcification, osteoporosis, inhibition of aldosterone production;
injection reactions- hematoma, irritation, pain upon injection.
For outdoor use: allergic reactions, skin hyperemia.

Interaction of sodium heparin with other substances

The effectiveness of sodium heparin is enhanced by dextran, acetylsalicylic acid, phenylbutazone, indomethacin, ibuprofen, dipyridamole, warfarin, hydroxychloroquine, dicumarol - the risk of bleeding increases (with simultaneous use, care must be taken), weakened by tetracyclines, antihistamines, cardiac glycosides, nicotine, changes - nicotinic acid. The simultaneous use of heparin sodium (including in the form of a gel) with indirect anticoagulants may increase the prothrombin time. Clopidogrel increases the risk of bleeding with simultaneous use. The risk of bleeding increases with the simultaneous use of heparin with ketorolac and diclofenac with parenteral administration(avoid this combination including low-dose heparin).

Overdose

Heparin overdose causes bleeding varying degrees gravity. At slight bleeding it is necessary to reduce the dose or stop the use of heparin, if heavy bleeding 1% solution of protamine sulfate is slowly injected intravenously.

Trade names of drugs with the active substance heparin sodium

Combined drugs:
Heparin sodium + Benzocaine: Nigepan®;
Heparin sodium + Benzocaine + Benzyl nicotinate: Heparin ointment;
Allantoin + Heparin sodium + Dexpanthenol: Gepalpan, Gepatrombin;
Heparin sodium + Dexpanthenol + Troxerutin: Venolife®, Troxevasin® Neo;
Escin + Essential phospholipids + Heparin sodium: Venabos®, Essaven®;
Heparin sodium + Escin: Venitan® forte, Ellon gel;
Allantoin + Heparin sodium + Onion bulb extract: Contractubex;
Heparin sodium + Lidocaine + Prednisolone: ​​Hepasolone;
Heparin sodium + Dexpanthenol + Dimethyl sulfoxide: Hepatrombin C, Dolobene;
Mometasone + [Heparin Sodium]: Skinlight®;
Heparin sodium + Prednisolone + Lauromacrogol 600: Hepatrombin G.

Dosage form:  solution for intravenous and subcutaneous injection Compound:

active substance: heparin sodium - 5000 ME

Excipients: gasoline alcohol - 9.0 mg; sodium chloride - 3.4 mg; water for injection - up to 1 ml.

Description: Clear colorless or light yellow solution. Pharmacotherapeutic group:Anticoagulant direct action ATX:  

B.01.A.B.01 Heparin

Pharmacodynamics:

Direct acting anticoagulant; heparin belongs to the group of medium molecular weight heparins, slows down the formation of fibrin. The anticoagulant effect is found in vitro and in vivo, occurs immediately after intravenous administration.

The mechanism of action of heparin is based primarily on its binding to antithrombin III, an inhibitor of activated blood coagulation factors: Pa (thrombin), 1Xa, Xa, X1a, XNa (the ability to inhibit and activated factor X is especially important). binds to antithrombin III and causes conformational changes in its molecule. As a result, the binding of antithrombin III to blood coagulation factors IIa (thrombin), IXa, Xa, XIa and XIIa is accelerated and blocked. enzymatic activity. The binding of sodium heparin to antithrombin III is electrostatic in nature and largely depends on the length and composition of the molecule (for the binding of sodium heparin to antithrombin III, a pentasaccharide sequence containing 3-O-sulfated is required).

Highest value has the ability of heparin in combination with antithrombin III to inhibit coagulation factors IIa () and Xa. The ratio of sodium heparin activity against factor Xa to its activity against factor IIa is 0.9-1.1.

Heparin reduces blood viscosity, reduces vascular permeability stimulated by bradykinin, histamine and other endogenous factors, and thus prevents the development of stasis. is able to be sorbed on the surface of endothelial membranes and blood cells, increasing their negative charge, which prevents adhesion and aggregation of platelets. slows down smooth muscle hyperplasia, activates lipoprotein lipase and thus has a lipid-lowering effect and prevents the development of atherosclerosis.

Heparin sodium binds some components of the complement system, lowering its activity, prevents the cooperation of lymphocytes and the formation of immunoglobulins, binds histamine (i.e., has an anti-allergic effect). increases renal blood flow, increases cerebral vascular resistance, reduces cerebral hyaluronidase activity, reduces surfactant activity in the lungs, suppresses excessive aldosterone synthesis in the adrenal cortex, binds adrenaline, modulates the ovarian response to hormonal stimuli, enhances parathyroid hormone activity. As a result of interaction with enzymes, it can increase the activity of brain tyrosine hydroxylase, pepsinogen, DNA polymerase and reduce the activity of myosin ATPase, pyruvate kinase, RNA polymerase, pepsin. Clinical Significance of these effects of heparin remains uncertain and insufficiently studied.

With acute coronary syndrome without persistent ST segment elevation on the ECG (unstable angina, myocardial infarction without ST segment elevation) in combination with acetylsalicylic acid reduces the risk of myocardial infarction and reduces mortality. In myocardial infarction with ST elevation on the ECG, it is effective in primary percutaneous coronary revascularization in combination with inhibitors of glycoprotein IIb / IIIa receptors and in thrombolytic therapy with streptokinase (increase in the frequency of revascularization).

In high doses, it is effective in pulmonary embolism and venous thrombosis. In small doses, it is effective for the prevention of venous thromboembolism, incl. after surgical operations.

After intravenous administration, the effect of the drug occurs almost immediately, no later than 10-15 minutes and does not last long - 3-6 hours. After subcutaneous administration, the effect of sodium heparin begins slowly - after 40-60 minutes, but lasts 8 hours.

Deficiency of antithrombin III in plasma or at the site of thrombosis may reduce the antithrombotic effect of sodium heparin.

Pharmacokinetics:

After intravenous administration, the maximum concentration (Cmax) is reached almost immediately, after subcutaneous administration - after 2-4 hours.

Communication with plasma proteins - up to 95%, the volume of distribution is very small - 0.06 l / kg (does not leave the vascular bed due to strong binding to blood plasma proteins).

Does not penetrate the placental barrier and into breast milk.

Intensively captured by endothelial cells and cells of the mononuclear-macrophage system (cells of the reticuloendothelial system), concentrated in the liver and spleen. It is metabolized in the liver with the participation of N-desulfamidase and platelet heparinase, which is included in the metabolism of heparin at later stages. Participation in the metabolism of platelet factor IV (antiheparin factor), as well as the binding of sodium heparin to the macrophage system, explain the rapid biological inactivation and short duration of action. Desulfated molecules under the influence of kidney endoglycosidase are converted into low molecular weight fragments. The half-life of the drug (T 1/2) is 1-6 hours (average 1.5 hours). The half-life of heparin sodium is increased in obesity, renal and liver failure, decreases with pulmonary embolism, infectious diseases, malignant neoplasms.

Heparin sodium is excreted by the kidneys as inactive metabolites. With the introduction of high doses, excretion (up to 50%) is possible unchanged. Not excreted by hemodialysis.

Indications:

Prevention and treatment venous thrombosis(including thrombosis of superficial and deep veins lower extremities; renal vein thrombosis) and pulmonary embolism;

Prevention and treatment of thromboembolic complications associated with atrial fibrillation;

Prevention and treatment of peripheral arterial embolism (including those associated with mitral heart disease);

Treatment of acute and chronic consumption coagulopathy (including stage I DIC);

Acute coronary syndrome without persistent ST segment elevation on the ECG (unstable angina, myocardial infarction without ST segment elevation on the ECG);

ST-segment elevation myocardial infarction: with thrombolytic therapy, with primary percutaneous coronary revascularization (balloon angioplasty with or without stenting), and with high risk arterial or venous thrombosis and thromboembolism;

Prevention and therapy of microthrombosis and microcirculation disorders, incl. with hemolytic-uremic syndrome; glomerulonephritis (including lupus nephritis) and with forced diuresis;

Prevention of blood coagulation during blood transfusion, in extracorporeal circulation systems (extracorporeal circulation during heart surgery, hemosorption, cytopheresis) and hemodialysis;

Treatment of peripheral venous catheters.

Contraindications:

Hypersensitivity to heparin sodium and other components of the drug.

Heparin - induced thrombocytopenia (with or without thrombosis) in history or at present.

Bleeding (unless the benefit of sodium heparin outweighs the potential risk).

Heparin sodium in therapeutic dose should not be given unless regular laboratory monitoring of blood coagulation can be provided. Newborns, especially premature or low birth weight infants (if the preparation contains benzyl alcohol).

Pregnancy and the period of breastfeeding.

Carefully:

Patients with polyvalent allergies (including bronchial asthma);

In pathological conditions associated with increased risk bleeding such as:

diseases of cardio-vascular system: acute and subacute infective endocarditis, severe uncontrolled arterial hypertension, aortic dissection, cerebral aneurysm;

erosive and ulcerative lesions of the gastrointestinal tract (GIT) (including stress-induced), esophageal varicose veins in liver cirrhosis and other diseases, long-term use of gastric and small intestine drains, ulcerative colitis, haemorrhoids;

diseases of the hematopoietic organs and lymphatic system: leukemia, hemophilia, thrombocytopenia, hemorrhagic diathesis;

diseases of the central nervous system: hemorrhagic stroke, traumatic brain injury;

malignant neoplasms;

congenital deficiency of antithrombin III and replacement therapy antithrombin III drugs (lower doses of heparin should be used to reduce the risk of bleeding).

Other physiological and pathological conditions: period of menstruation, threatened abortion, early postpartum period, serious illnesses liver with impaired protein-synthetic function, chronic renal failure, recent surgery on the eyes, head or spinal cord, recent spinal (lumbar) puncture or epidural anesthesia, proliferative diabetic retinopathy, vasculitis, childhood up to 3 years (part of benzyl alcohol can cause toxic and anaphylactoid reactions), elderly age(over 60, especially women). The use of heparin sodium is possible in cases where the expected benefit of therapy outweighs the potential risk.

Pregnancy and lactation:

Heparin sodium does not cross the placental barrier. To date, there are no data indicating the possibility of fetal malformations due to the use of sodium heparin during pregnancy, and there are also no results of animal experiments that would indicate an embryo- or fetotoxic effect of sodium heparin. However, there is evidence of an increased risk premature birth and spontaneous abortions associated with bleeding. It is necessary to take into account the possibility of complications when using heparin sodium in pregnant women with comorbidities, as well as in pregnant women receiving additional treatment.

Daily use of high doses of sodium heparin for more than 3 months may increase the risk of osteoporosis in lactating women.

If it is necessary to use during the indicated periods, it is necessary to use other sodium heparin preparations that do not contain benzyl alcohol as an excipient (see "Composition", "Contraindications").

Dosage and administration:

Heparin is administered subcutaneously, intravenously, by bolus or drip.

Heparin is administered as a continuous intravenous infusion or in the form of regular intravenous injections, as well as subcutaneously (in the abdomen).

Heparin sodium should not be administered intramuscularly due to the risk of developing intramuscular hematomas.

Subcutaneous injections are preferably performed in the area of ​​the anterolateral abdominal wall (in exceptional cases enter into upper region shoulder or thigh), while using a thin needle, which should be inserted deeply, perpendicularly, into a fold of skin held between the large and index fingers until the end of the injection. It is necessary to alternate injection sites each time (to avoid the formation of a hematoma). The first injection should be given 1-2 hours before the start of the operation. postoperative period- to enter within 7-10 days, and in case of need - longer time.

The initial dose of heparin sodium administered into medicinal purposes, is usually 5000 IU and is administered intravenously, after which the treatment is continued using subcutaneous injections or intravenous infusion.

Maintenance doses are determined depending on the method of application:

With continuous intravenous infusion, 1000 - 2000 IU / h (24000-48000 IU / day) are prescribed, diluting heparin with 0.9% sodium chloride solution;

With regular intravenous injections prescribe 5000-10000 IU of heparin every 4-6 hours;

When administered subcutaneously, 15000-20000 IU is administered every 12 hours or 8000-10000 IU every 8 hours.

Laboratory monitoring of the efficacy and safety of sodium heparin therapy.

The dose of sodium heparin should be adjusted based on laboratory indicators blood clotting. When using heparin sodium, it is necessary to control the activated partial thromboplastin time (APTT) or blood clotting time (CWT). The administered dose of sodium heparin is considered adequate if the APTT is 1.5-2.5 times the control values ​​or if the patient's ROS is 2.5-3.0 times the control values.

With continuous intravenous infusion of sodium heparin, it is recommended to determine the initial APTT, then determine the APTT every 4 hours, followed by an increase or decrease in the rate of sodium heparin infusion until the target level of APTT is reached (1.5-2.5 times higher than normal), then determine the APTT every b hours.

When bolus intravenous sodium heparin is administered, it is recommended to determine the initial APTT, then determine the APTT before each bolus administration, followed by an increase or decrease in the dose of sodium heparin administered.

With subcutaneous administration of low doses of heparin sodium (5000 IU 2-3 times a day) for the prevention of thrombosis, it is not necessary to regularly monitor the APTT, because it increases slightly.

Continuous intravenous infusion is the most effective way use of sodium heparin, better than regular (periodic) injections, because. provides more stable hypocoagulation and less likely to cause bleeding.

The use of heparin sodium in special clinical situations.

Primary percutaneous coronary angioplasty for non-ST elevation acute coronary syndrome and ST elevation myocardial infarction: is administered intravenously as a bolus at a dose of 70-100 IU / kg (if it is not planned to use inhibitors of glycoprotein IIb / IIIa receptors) or at a dose of 50-60 IU / kg (if joint application with inhibitors of glycoprotein IIb/IIIa receptors).

Thrombolytic therapy for ST elevation myocardial infarction: is administered intravenously as a bolus at a dose of 60 IU/kg ( maximum dose 4000 IU), followed by intravenous infusion at a dose of 12 IU/kg (no more than 1000 IU/hour) for 24-48 hours. The target level of APTT is 50-70 seconds or 1.5-2.0 times higher than the norm; APTT control after 3, 6, 12 and 24 hours after the start of therapy.

Prevention of thromboembolic complications after surgical interventions using low dose heparin infusion: Heparin sodium is injected subcutaneously, deep into the fold of the skin of the abdomen. Initial dose of 5000 IU 2 hours before surgery. In the postoperative period: 5000 IU every 8-12 hours for 7 days or until full recovery patient mobility (whichever comes first). When using heparin sodium in low doses for the prevention of thromboembolic complications, it is not necessary to control APTT.

Application in cardiovascular surgery during operations using extracorporeal circulation systems: The initial dose of sodium heparin is at least 150 IU / kg of body weight. Then it is administered by continuous intravenous infusion at a rate of 15-25 drops / min, 30,000 IU per 1 liter of infusion solution. The total dose of heparin sodium is usually 300 IU/kg of body weight (if the expected duration of the operation is less than 60 minutes) or 400 IU/kg of body weight (if the expected duration of the operation is 60 minutes or more).

Use in hemodialysis. Initial dose of sodium heparin: 25-30 IU/kg (or 10,000 IU) IV bolus followed by continuous infusion of sodium heparin 20,000 IU/100 ml of 0.9% sodium chloride solution at a rate of 1500-2000 IU/h (unless otherwise indicated in guidelines for the use of systems for hemodialysis).

The use of sodium heparin in pediatrics. Adequate controlled studies of the use of sodium heparin in children have not been conducted. The recommendations presented are based on clinical experience.

Initial dose: 75-100 IU/kg IV bolus over 10 minutes.

Maintenance dose: children aged 1-3 months - 25-30 IU / kg / h (800 IU / kg / day), children aged 4-12 months - 25-30 IU / kg / h (700 IU / kg / day). day), children older than 1 year - 18-20 IU / kg / hour (500 IU / kg / day) intravenously.

The dose of heparin sodium should be selected taking into account the indicators of blood coagulation (target level of APTT 60-85 sec).

The duration of therapy depends on the indications and method of application. At intravenous use the optimal duration of treatment is 7-10 days, after which therapy is continued with oral anticoagulants (it is recommended to prescribe oral anticoagulants starting from the 1st day of treatment with sodium heparin or from 5 to 7 days, and stop using sodium heparin on days 4-5 combination therapy). With extensive thrombosis of the iliac-femoral veins, it is advisable to conduct longer courses of treatment with sodium heparin.

Side effects:

World Health Organization (WHO) classification of unwanted drug reactions by frequency of development: very often (> 1/10 appointments); often (>1/100 and<1/10 назначений); нечасто (>1/1000 and<1/100 назначений); редко (>1/10000 and<1/1000 назначений); очень редко (<1/10000), включая отдельные сообщения.

Hemorrhagic complications: develop very frequently. The most typical are bleeding from the gastrointestinal tract, urinary tract, from the injection sites of sodium heparin, from postoperative wounds, as well as hemorrhages in areas subjected to pressure. Hemorrhages in other internal organs may also develop, incl. in the adrenal glands (with the development of acute adrenal insufficiency), retroperitoneal space, ovaries. More frequent occurrence of bleeding is observed in patients older than 60 years (especially in women).

Allergic reactions: infrequently - skin flushing, rash, itching and burning sensation in the soles, pain in the extremities, hyperthermia, urticaria, rhinitis, conjunctivitis, shortness of breath, bronchospasm, angioedema; very rarely - anaphylactic shock.

Reactions at the injection site: often - irritation, soreness, tissue hyperemia, slight hematoma and ulceration at the injection site, infrequently - histamine-like reactions (including skin necrosis at the injection site), very rarely - soft tissue calcification at the injection site (mainly in patients with severe chronic renal failure).

Heparin-induced thrombocytopenia (HIT): severe immune reaction due to the formation of antibodies and leading to irreversible platelet aggregation. It can develop both during heparin therapy (rarely) and within a few weeks after its termination (very rarely). Clinical manifestations: venous and arterial thrombosis (including deep vein thrombosis, pulmonary embolism, cerebral vein thrombosis, stroke, myocardial infarction, thrombosis of the mesenteric and renal arteries, arterial thrombosis of the extremities with the development of gangrene). Laboratory diagnosis: The platelet count should be determined before the appointment of sodium heparin, on the first day of treatment, and then every 2-3 days during the entire period of treatment (especially from 6 to 14 days of therapy).

At the beginning of treatment with Heparin, transient thrombocytopenia can sometimes be noted with platelet counts ranging from 80x10 9 /l to 150x10 9 /l. Usually this situation does not lead to the development of complications and treatment with sodium heparin can be continued. In rare cases, severe thrombocytopenia (white blood clot formation syndrome) can occur, sometimes with a fatal outcome. This complication should be considered in case of a decrease in platelets below 80x10 9 /l or more than 50% of the initial level, in such cases it should be immediately canceled. If necessary, alternative antithrombotic therapy should be prescribed. Patients with severe thrombocytopenia may develop consumption coagulopathy (fibrinogen depletion).

Against the background of heparin-induced thrombocytopenia: skin necrosis, arterial thrombosis, accompanied by the development of gangrene, myocardial infarction, stroke.

If HIT occurs, it should be canceled immediately. The patient should be warned that in the future he should not be prescribed unfractionated heparin and low molecular weight heparins. If the patient requires antithrombotic therapy, other drugs should be used.

With prolonged use: osteoporosis, spontaneous bone fractures, soft tissue calcification, hypoaldosteronism, transient alopecia, priapism.

During therapy with sodium heparin, changes in blood biochemical parameters may be observed (increased activity of hepatic transaminases, free fatty acids and thyroxine in blood plasma; hyperkalemia, reversible hyperlipidemia against the background of discontinuation of sodium heparin, a false increase in blood glucose concentration and a false-positive result of the bromsulfalein test).

Other adverse events:

From the side of the central nervous system and sensory organs: infrequently - dizziness, headache.

From the side of the cardiovascular system: infrequently - a decrease in blood pressure. On the part of the digestive system: infrequently - loss of appetite, nausea, vomiting, diarrhea, often - an increase in the content of "liver" transaminases (ACT and ALT) in the blood plasma.

From the side of the hematopoietic organs: often - moderate thrombocytopenia (platelet count (150-100) x109 / l), not associated with the production of antibodies and not accompanied by thrombosis (may occur in 6-30% of patients receiving heparin); rarely, reversible eosiiophilia.

From the musculoskeletal system: rarely - osteoporosis (with prolonged use of sodium heparin), spontaneous bone fractures.

From the endocrine system: rarely - hypoaldostronism (due to inhibition of aldosterone synthesis).

From the side of water-electrolyte metabolism: rarely - reversible potassium retention, metabolic acidosis.

Others: infrequently - transient alopecia, very rarely - priapism.

Laboratory indicators: often - a reversible increase in the content of "liver" transaminases (ACT and ALT); infrequently - an increase in the content of free fatty acids after discontinuation of heparin, an increase in the content of thyroxine in the blood plasma, a false decrease in cholesterol, a false increase in glucose, and incorrect results of the bromsulfalein test.

If any side effects indicated in the instructions for use are aggravated, or if other undesirable effects occur that are not indicated in the instructions, you should immediately inform your doctor.

Overdose:

Symptoms: signs of bleeding.

Treatment: in case of minor bleeding caused by an overdose of heparin sodium, it is enough to stop its use.

With extensive bleeding, excess sodium heparin is neutralized with protamine sulfate (1 mg of protamine sulfate per 100 IU of sodium heparin). 1% (10 mg / ml) solution of protamine sulfate is administered intravenously very slowly. Every 10 minutes, you can not enter more than 50 mg (5 ml) of protamine sulfate. Given the rapid metabolism of sodium heparin, the required dose of protamine sulfate decreases over time. To calculate the required dose of protamine sulfate, we can assume that the half-life (T 1/2) of sodium heparin is 30 minutes. When using protamine sulfate, severe anaphylactic reactions with a fatal outcome were noted, and therefore the drug should be administered only in a department equipped to provide emergency medical care for anaphylactic shock.

Hemodialysis is ineffective.

Interaction:

Due to the potential for precipitation of the active ingredients, it must not be mixed with other medicinal products.

Pharmaceutical interaction: sodium heparin solution is only compatible with 0.9% sodium chloride solution.

Sodium heparin solution is incompatible with the following drug solutions: alteplase, amikacin, amiodarone, sodium ampicillin, sodium benzylpsicillin, ciprofloxacin, cytarabine, dacarbazine, danorubicin, diazepam, dobutamine, doxorubicin hydrochloride, droperidol, erythromycin, gentamicin sulfate, haloperidol lactate, haloperidol lactate, sodium succinate, glucose, idarubicin, kanamycin sulfate, sodium methicillin, nstylmicin sulfate, opioids, oxytetracycline hydrochloride, polymyxin B sulfate, promazine hydrochloride, promethazine hydrochloride, streptomycin sulfate, sulfafurazole diethanolamine, tetracycline hydrochloride, tobramycin sulfate, cephalothin chloride, sodium comycephaloridine , vinblastine sulfate, labetalol hydrochloride, nicardipine hydrochloride.

Pharmacokinetic interaction: Sodium heparin displaces , and benzodiazepine derivatives from their binding sites with blood plasma proteins, which can lead to an increase in the pharmacological action of these drugs. binds and is inactivated by sodium protamine, alkaline polypeptides, and tricyclic antidepressants.

Pharmacodynamic interaction: The anticoagulant effect of heparin sodium is enhanced with simultaneous use with other drugs that affect hemostasis, incl. with antiplatelet drugs (,, etc.), glucocorticoids and dextran, resulting in an increased risk of bleeding. In addition, the anticoagulant effect of sodium heparin can be enhanced when used together with hydroxychloroquine, sulfinpyrazone, probenecid, ethacrynic acid, cytostatics, cefamandol, cefotetan, valproic acid, propylthiouracil.

Before any surgical intervention with the use of heparin, oral anticoagulants and antiplatelet agents should be canceled at least 5 days in advance, because. they can increase bleeding during operations or in the postoperative period. The anticoagulant effect of sodium heparin decreases with simultaneous use with ACTH, antihistamines, ascorbic acid, ergot alkaloids, nicotine, nitroglycerin, cardiac glycosides, thyroxine, tetracycline and quinine.

Heparin sodium can reduce the pharmacological action of ACTH, glucocorticoids and insulin.

Special instructions:

Switching to warfarin therapy: To ensure a sustained anticoagulant effect, full-dose sodium heparin therapy should be continued until a stable target INR level is reached. After this, the introduction must be stopped.

Switching to dabigatran therapy: continuous intravenous heparin sodium should be discontinued immediately after the first dose of dabigatran. For split intravenous administration, the patient should take the first dose of dabigatran orally 1-2 hours before the scheduled administration of the next dose of sodium heparin.

Before elective surgical interventions, in order to reduce blood loss during surgery and in the postoperative period, it is usually recommended to stop oral anticoagulants () and antiplatelet drugs ( , ) 7 days before surgery. As an antithrombotic therapy, it is possible to prescribe sodium heparin in therapeutic doses. The introduction of heparin sodium is stopped 6 hours before the operation and resumes 6 hours after the end of the operation.

Intramuscular administration of heparin sodium should be avoided (due to the possible occurrence of hematomas).

The use of drugs containing benzyl alcohol as a preservative in neonates (especially premature and underweight infants) can lead to serious adverse events (central nervous system depression, metabolic acidosis, gasping breathing) and death. Therefore, in newborns and children under 1 year of age, sodium heparin preparations that do not contain preservatives should be used.

Resistance to heparin sodium is often observed in fever, thrombosis, thrombophlebitis, infectious diseases, myocardial infarction, malignant neoplasms, as well as after surgical interventions and in antithrombia III deficiency. In such situations, more careful laboratory monitoring (APTT control) is required.

In persons over 60 years of age (especially women), the risk of bleeding is increased, and therefore the dose of heparin sodium in this category of patients should be reduced.

Influence on the ability to drive transport. cf. and fur.:Signs of the effect of heparin on intellectual and psychomotor functions, the ability to drive vehicles and mechanisms, were not identified. Release form / dosage:Solution for intravenous and subcutaneous administration 5000 IU/ml. Package:

In ampoules of 1 ml and 5 ml.

5 ampoules in a blister pack made of PVC film.

1 or 2 blister packs together with instructions for use and an ampoule scarifier in a cardboard box.

5 or 10 ampoules, together with instructions for use and an ampoule scarifier, in a cardboard box with a corrugated liner.

When packing ampoules with a break point or ring, the ampoule scarifier is not included.

Packaging for hospitals. 50, 100 blister packs with ampoules of the drug, together with instructions for use, the number of which is equal to the number of blister packs, are placed in a corrugated cardboard box.

Storage conditions:

In a place protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Best before date:

3 years. Do not use after the expiry date stated on the packaging.

Instructions

When ingested, it is destroyed in the digestive tract, so heparin is used only parenterally. Does not bind to plasma proteins. Refers to anticoagulants of direct action; when administered parenterally, it inhibits blood clotting due to the inactivation of thrombin, V, VII, IX factors and the Hageman factor. Activates the process of fibrinolysis. Inhibits the activity of certain enzymes: hyaluronidase, phosphatase, trypsin. Reduces the inhibitory effect of prostacyclin on platelet aggregation due to the action of adenosine diphosphate. By activating lipoprotein lipase, it slightly reduces the level of cholesterol and lipoproteins in the blood.

The half-life is 1.321.72 hours. The anticoagulant effect of heparin appears immediately after administration and lasts for 23 hours. Does not penetrate into breast milk.

Indications

Systemic use treatment of thrombophlebitis, phlebitis and thromboembolism; early therapy for myocardial infarction; prevention of vein thrombosis and thromboembolism of the branches of the pulmonary artery in the postoperative period and with prolonged immobilization; catheterization of the cavities of the heart; DIC syndrome (first phase); heparinization of blood during renal dialysis and other interventions using extracorporeal circulation, preparation of non-clotting blood samples for laboratory studies;

topical application varicose veins, phlebothrombosis, thrombophlebitis (mainly superficial), superficial periphlebitis, phlebitis after intravenous injections, thrombosis of hemorrhoidal veins, varicose ulcers of the extremities, postoperative varicose phlebitis, complications after removal of the saphenous veins of the lower extremities, bruises, infiltrates, local limited swelling, subcutaneous hematomas, injuries of muscles, tendons and joints.

Application

The dose is set taking into account the indicators of the coagulogram, the nature of the disease, the age, body weight and sensitivity of the patient. For the prevention of thromboembolism during surgical treatment, 50007500 IU of heparin is administered s / c 2 hours before surgery. After the operation, heparin in the same dose is administered every 6-8 hours until the patient is transferred to the active mode. For the prevention of thromboembolic complications in patients with prolonged immobilization, diseases with an increased risk of developing thrombosis, 50007500 IU is administered every 812 hours. 500 IU 2 times a day. In case of venous and arterial thrombosis and thromboembolism, it is administered intravenously. Adults are initially prescribed intravenously 500010,000 IU, then through a perfusor 25,00040,000 IU per day; children are first injected with 50 IU / kg intravenously, then through a perfusor 20 IU / kg at 1 hour. If prolonged intravenous administration is not possible, intermittent intravenous administration or s / c administration can be used. With DIC (first phase), the drug is administered in a daily dose of 25004000 IU, depending on the parameters of laboratory blood tests.

The gel or ointment is applied in a thin layer, gently rubbing into the affected areas of the skin 2-3 times a day. With thrombosis of hemorrhoidal veins, it is used either under a bandage (in the case of extraanal nodes), or injected into the rectum on a swab. Depending on the nature of the disease, the course of treatment is 13 weeks. Do not apply to open wounds, mucous membranes, the area of ​​the purulent process.

Contraindications

Hypersensitivity to heparin, diseases accompanied by a decrease in blood clotting (hemorrhagic diathesis, deficiency of blood clotting factors, thrombocytopenia), peptic ulcer of the stomach, duodenum or gastrojejunal anastomosis, ulcerative colitis, malignant neoplasms, uncorrectable hypertension, hemorrhagic stroke, recent surgery ( especially neurosurgical or ophthalmic), the presence of a stationary probe in the stomach or intestines, CNS trauma, retinopathy, vitreous hemorrhage, bacterial endocarditis, lumbar puncture, spinal anesthesia, epidural anesthesia, the threat of miscarriage, the presence of extensive wound surfaces and skin lesions, destructive pulmonary tuberculosis .

Side effects

Allergic reactions (erythema, urticaria, itching of the skin and mucous membranes, lacrimation, fever, bronchospasm), hemorrhages under the skin and mucous membranes, bleeding from wounds, urinary tract, genital organs, gastrointestinal bleeding, thrombocytopenia, increased serum transaminase activity blood, extremely rarely - transient alopecia, hypoaldosteronism.

special instructions

It is prescribed with caution if a malignant neoplasm is suspected, in patients with a tendency to bleeding, in the elderly, with urolithiasis, and chronic alcoholism.

When using heparin, control of the number of platelets in the peripheral blood should be carried out before administration, the next day after administration, every 3-4 days during the first 3 weeks of treatment, at the end of treatment. With the development of severe thrombocytopenia with a decrease in the number of platelets by 50% of the initial level, heparin is canceled. The number of platelets usually begins to decrease on the 6-14th day of therapy, however, in patients with hypersensitivity, this may occur several hours after the start of treatment.

When using heparin, it is possible to change some indicators of laboratory blood tests: ESR, complement fixation tests, prothrombin time, T3 and T4 levels.

Careful medical supervision is required when using heparin in pregnant women. Women who were treated with heparin during pregnancy are absolutely contraindicated for epidural anesthesia during the birth period.

Interactions

With simultaneous use with acetysalicylic acid, coumarin derivatives, fibrinolytics, dipyridamole, dextran, penicillins in a high dose, the risk of bleeding increases. Co-administration with NSAIDs potentiates the action of heparin. Parenteral administration of nitroglycerin weakens the effect of heparin. Solution of heparin sodium should not be mixed in the same syringe or dropper with solutions of any other medicines.

Overdose

With the development of life-threatening bleeding, protamine sulfate is used as an antidote for heparin (1 mg of protamine sulfate neutralizes the effect of 100 IU of heparin). Within 90 minutes after the on / in the use of heparin, 50% of the calculated dose of protamine should be administered; 25% of the dose in the next 3 hours.

When ingested, it is destroyed in the digestive tract, so heparin is used only parenterally. Does not bind to plasma proteins. Refers to anticoagulants of direct action; when administered parenterally, it inhibits blood clotting due to the inactivation of thrombin, V, VII, IX factors and the Hageman factor. Activates the process of fibrinolysis. Inhibits the activity of certain enzymes: hyaluronidase, phosphatase, trypsin. Reduces the inhibitory effect of prostacyclin on platelet aggregation due to the action of adenosine diphosphate. By activating lipoprotein lipase, it slightly reduces the level of cholesterol and lipoproteins in the blood.
The half-life is 1.32-1.72 hours. The anticoagulant effect of heparin appears immediately after administration and lasts for 2-3 hours. It does not penetrate into breast milk.

Indications for use of the drug Heparin sodium

Systemic use - treatment of thrombophlebitis, phlebitis and thromboembolism; early therapy for myocardial infarction; prevention of vein thrombosis and thromboembolism of the branches of the pulmonary artery in the postoperative period and with prolonged immobilization; catheterization of the cavities of the heart; DIC syndrome (first phase); heparinization of blood during renal dialysis and other interventions using extracorporeal circulation, preparation of non-clotting blood samples for laboratory studies;
topical application - varicose veins, phlebothrombosis, thrombophlebitis (mainly superficial), superficial periphlebitis, phlebitis after intravenous injections, thrombosis of hemorrhoidal veins, varicose ulcers of the extremities, postoperative varicose phlebitis, complications after removal of the saphenous veins of the lower extremities, bruises, infiltrates, local limited swelling, subcutaneous hematomas, injuries of muscles, tendons and joints.

The use of the drug Heparin sodium

The dose is set taking into account the indicators of the coagulogram, the nature of the disease, the age, body weight and sensitivity of the patient. For the prevention of thromboembolism during surgical treatment, 5000-7500 IU of heparin is administered s / c 2 hours before surgery. After surgery, heparin at the same dose is administered every 6-8 hours until the patient is transferred to the active mode. For the prevention of thromboembolic complications in patients with prolonged immobilization, diseases with an increased risk of thrombosis, 5000-7500 IU is administered every 8-12 hours. 500 IU 2 times a day. In case of venous and arterial thrombosis and thromboembolism, it is administered intravenously. Adults are first prescribed intravenously 5000-10,000 IU, then through a perfusor 25,000-40,000 IU per day; children are first injected with 50 IU / kg intravenously, then through a perfusor 20 IU / kg at 1 hour. If prolonged intravenous administration is not possible, intermittent intravenous administration or s / c administration can be used. With DIC (first phase), the drug is administered in a daily dose of 2500-4000 IU, depending on the parameters of laboratory blood tests.
The gel or ointment is applied in a thin layer, gently rubbing into the affected areas of the skin 2-3 times a day. With thrombosis of hemorrhoidal veins, it is used either under a bandage (in the case of extraanal nodes), or injected into the rectum on a swab. Depending on the nature of the disease, the course of treatment is 1-3 weeks. Do not apply to open wounds, mucous membranes, the area of ​​the purulent process.

Contraindications to the use of the drug Heparin sodium

Hypersensitivity to heparin, diseases accompanied by a decrease in blood clotting (hemorrhagic diathesis, deficiency of blood clotting factors, thrombocytopenia), peptic ulcer of the stomach, duodenum or gastrojejunal anastomosis, ulcerative colitis, malignant neoplasms, uncorrectable hypertension (arterial hypertension), recent surgery (especially neurosurgical or ophthalmic), the presence of a stationary probe in the stomach or intestines, CNS trauma, retinopathy, vitreous hemorrhage, bacterial endocarditis, lumbar puncture, spinal anesthesia, epidural anesthesia, the threat of miscarriage, the presence of extensive wound surfaces and skin lesions, destructive tuberculosis lungs.

Side effects of the drug Heparin sodium

Allergic reactions (erythema, urticaria, itching of the skin and mucous membranes, lacrimation, fever, bronchospasm), hemorrhages under the skin and mucous membranes, bleeding from wounds, urinary tract, genital organs, gastrointestinal bleeding, thrombocytopenia, increased serum transaminase activity blood, extremely rarely - transient alopecia, hypoaldosteronism.

Special instructions for the use of the drug Heparin sodium

It is prescribed with caution if a malignant neoplasm is suspected, in patients with a tendency to bleeding, in the elderly, in urolithiasis, and in chronic alcoholism.
When using heparin, control of the number of platelets in the peripheral blood should be carried out before administration, the next day after administration, every 3-4 days during the first 3 weeks of treatment, at the end of treatment. With the development of severe thrombocytopenia with a decrease in the number of platelets by 50% of the initial level, heparin is canceled. The platelet count usually begins to decrease on the 6-14th day of therapy, however, in patients with hypersensitivity, this may occur several hours after the start of treatment.
When using heparin, it is possible to change some indicators of laboratory blood tests: ESR, complement fixation tests, prothrombin time, T3 and T4 levels.
Careful medical supervision is required when using heparin in pregnant women. Women who were treated with heparin during pregnancy are absolutely contraindicated for epidural anesthesia during the birth period.

Drug interactions Heparin sodium

With simultaneous use with acetysalicylic acid, coumarin derivatives, fibrinolytics, dipyridamole, dextran, penicillins in a high dose, the risk of bleeding increases. Co-administration with NSAIDs potentiates the action of heparin. Parenteral administration of nitroglycerin weakens the effect of heparin. Solution of heparin sodium should not be mixed in the same syringe or dropper with solutions of any other medicines.

Overdose of the drug Heparin sodium, symptoms and treatment

With the development of life-threatening bleeding, protamine sulfate is used as an antidote for heparin (1 mg of protamine sulfate neutralizes the effect of 100 IU of heparin). Within 90 minutes after the on / in the use of heparin, 50% of the calculated dose of protamine should be administered; 25% of the dose - in the next 3 hours.

List of pharmacies where you can buy Heparin sodium:

  • St. Petersburg

Heparin sodium (in Latin - Heparin sodium) is a substance that is characterized by anticoagulant properties. This means that thanks to it, the intensity of blood clots is reduced, because. blood viscosity decreases. It is used as the main active ingredient in various types of drugs.

There is a drug of the same name.

Its distinguishing features:

  • one-component composition;
  • a large number of release forms (solid, liquid structure);
  • high efficiency.

The product has many trade names: Heparin-sodium Brown, Heparin-Richter, Heparin sodium salt, etc.

Composition and action

The main active ingredient is heparin. Its concentration varies depending on the form of release: 1000 IU (gel) to 5000 IU (solution).

Auxiliary components of the drug, characterized by a liquid structure:

  • sodium chloride;
  • benzyl alcohol;
  • water d / i.

Other components in the composition of the gel-like substance:

  • ethanol;
  • carbomer;
  • dimethyl sulfoxide;
  • propylene glycol;
  • diethanolamine;
  • methyl and propylparaben;
  • lavender oil and purified water.

The mechanism of action of drugs that affect erythropoiesis and blood coagulation

Release form

On sale you can find the drug in the form of a solution intended for injection. Other forms: gel, ointment.

The solution is available in a package containing 50 ampoules (5 ml each) and in 5 ml vials. This tool is intended for subcutaneous administration; can be used intravenously and intramuscularly.

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The ointment is offered in tubes of 25 g. The gel-like substance can be purchased in tubes of 30 and 50 g.

There are also vacuum tubes with heparin designed for blood sampling.


Mechanism of action of heparin sodium

The agent is characterized by anticoagulant action. Its distinguishing feature is the direct effect on the composition of the blood. This means that the substance reduces the intensity of blood clots. The principle of operation is based on the ability to influence the process of blood clotting. Means of direct action reduce the intensity of thrombin formation, which distinguishes them favorably from analogues of indirect action, tk. the latter are not as fast.

Other pharmacological properties:

  • increased intensity of blood flow in the kidneys;
  • increase in the resistance of cerebral vessels;
  • hypolipidemic action;
  • inhibition of aldosterone synthesis in the adrenal cortex;
  • increased activity of parathyroid hormone;
  • formation of ovarian response to hormonal stimuli;
  • heparin increases the activity of brain tyrosine hydroxylase, pepsinogen, DNA polymerase;
  • there is a decrease in myosin ATPase, pyruvate kinase, RNA polymerase, pepsin.

Blood clotting with heparin | Starsil Hemostat | Auroramed

Anticoagulants: drugs, mechanism of action and main indications

Pharmacodynamics

The anticoagulant effect is due to the binding of heparin to antithrombin III. As a result, a number of changes occur in the structure of its molecule, which leads to an acceleration of antithrombin III complexing. As a result of these changes, thrombin is blocked. In addition, under the influence of heparin, there is a decrease in the permeability of the walls of blood vessels, due to which microcirculation is restored, because. the likelihood of development of stagnant effects decreases.

Another function of the active substance is to reduce adhesion, and at the same time the aggregation of platelets, leukocytes, erythrocytes. With heparin therapy, the likelihood of atherosclerosis is reduced, because. there is a general improvement in the condition of the vessels. In addition, an antihistamine effect is provided, which is due to the binding of histamine, inhibition of the formation of immunoglobulin.

The agent under consideration affects the respiratory function: it reduces the activity of the surfactant in the lungs. It also prevents the development of thrombosis, myocardial infarction. The tool reduces the likelihood of complications and sudden death in patients who have recently had a heart attack. The drug in question is effective in the treatment of diseases and vascular pathologies: thromboembolism, embolism, thrombosis.


Pharmacokinetics

The substance is characterized by a high rate of action. With intravenous administration, the antithrombotic effect is visible instantly. If the solution is administered intramuscularly, the desired result is achieved in less than half an hour. With the subcutaneous method of delivery after the administration of the drug, a positive effect can be seen no earlier than 40-60 minutes later. The duration of the period during which the anticoagulant effect is exerted depends on the intensity of its distribution.

If the composition of the blood is changed (antithrombin III deficiency is noted), the effectiveness of the agent in question may decrease. The solution is distinguished by high bioavailability when administered intravenously, and when administered subcutaneously, on the contrary, it is low. The peak activity of the drug is reached after 2-4 hours. The half-life does not exceed 120 minutes.


Indications for use

  • pulmonary embolism;
  • thrombosis of blood vessels;
  • heart surgery, which is accompanied by a high likelihood of complications;
  • thrombophlebitis;
  • myocardial infarction (in the acute phase);
  • angina;
  • arrhythmia;
  • glomerulonephritis;
  • lupus;
  • prevention of venous thromboembolism.

Heparin sodium for hemorrhoids

Given that the agent in question is effective in various pathologies of the veins, including venous insufficiency, thrombosis, etc., it is recommended to use it when nodes and bumps appear on the sphincter and rectal mucosa. The drug has a moderate analgesic effect, helps to reduce swelling. By reducing blood viscosity and inhibiting the process of thrombosis, the likelihood of congestive effects is eliminated, which is often the cause of the formation of nodes and bumps in the perianal region.

With more often use and. However, these drugs are effective in nodes of 2-3 degrees. In more severe cases (), heparin can only be used as an auxiliary measure. Often with intense symptoms, this drug does not provide the desired result.


Chronic

In this case, the signs of the disease are less pronounced. For this reason, the dosage may be reduced.

With an exacerbation

The frequency of use of the product, as well as the amount of active substance, increases.

The use of heparin sodium

The highest dosages for myocardial infarction: the initial amount of the drug varies from 15,000 to 20,000 IU. After that, treatment continues for another 5-6 days; the daily dosage is up to 40 IU (it should be divided into several doses with a break of at least 4 hours).

If pulmonary thrombosis is diagnosed, 40,000-60,000 IU are prescribed (administration method - drip). This amount should be delivered to the circulatory system within 4-6 hours. After that, a daily dose of at least 40,000 IU is prescribed.

In order to prevent thromboembolism, 5000 IU is used subcutaneously 1-2 times a day. Heparin therapy requires monitoring of blood clotting. This is done 1 time every 2 days; after elimination of acute symptoms - 1 time every 3 days.

Topical preparations are used externally. The gel and ointment are applied to the skin in a thin layer. The frequency of use is determined on an individual basis.

Contraindications

The drug is not prescribed in some cases:

  • negative individual reaction to the components;
  • diathesis with the patient's tendency to hemorrhage;
  • susceptibility to bleeding;
  • thrombocytopenia;
  • high degree of vascular permeability;
  • ulcerative formations in the gastrointestinal tract (intestines, stomach);
  • polyps;
  • malignant neoplasms;
  • varicose veins of the esophagus;
  • hypertension that is difficult to control;
  • recent operations on the organs of vision, heart, spine;
  • injuries, especially craniocerebral;
  • dysfunction of the liver and kidneys.

Side effects

During therapy with the agent in question, the likelihood of the following negative effects is high;

  • dizziness and headaches;
  • bleeding in the digestive tract, from the urinary tract, hemorrhage in the ovaries;
  • loss of appetite;
  • change in the structure of the stool (diarrhea);
  • nausea, against which vomiting may occur;
  • anaphylactic reactions; as a manifestation of allergies, there is also a rash, redness.

With prolonged use of the drug, pain occurs at the injection site, hematoma. Sometimes alopecia, soft tissue calcification develops.

Overdose

If the drug is used in excess, the risk of bleeding increases. Therapeutic measures are selected taking into account its intensity. For example, with mild bleeding, you only need to interrupt the course of therapy. As a result, the symptoms will disappear. With more significant blood loss, the introduction of protamine sulfate is required. Its task is to neutralize the action of heparin. The dose of this compound is determined taking into account the rate of heparin excretion. The later this substance is applied (since the introduction of heparin), the less its amount should be.

special instructions

Caution should be exercised in patients who are diagnosed with an allergy to several types of allergens at the same time. It is also necessary to undergo heparin treatment under the supervision of a physician in patients with diabetes mellitus, hypertension, tuberculosis in the active phase, hepatic and renal dysfunction and when using extrauterine contraceptives.


Do not administer other drugs intramuscularly if heparin is used concomitantly.

An agent characterized by a liquid structure must be diluted with saline.

If severe thrombocytopenia develops while taking heparin, the course of treatment is stopped.

During pregnancy and lactation

It is permissible to use the agent in question, however, a course of therapy should be taken under the supervision of a specialist. Heparin is prescribed for vital indications.

Application in childhood

The drug is used to treat children from 3 years, but care should be taken when doing so. It should be borne in mind that there is no data on how heparin acts on the children's body. The appointment is made only on strict indications.


Medicines containing

The substance in question is used in the manufacture of such drugs:

  • Heparin-Richter;
  • Heparibene sodium;
  • Nigepan (details);
  • Heparin gel 1000 IU;
  • Thrombophobic;
  • Hepatrombin;
  • Heparin ointment.

These drugs have a different structure: candles, gel, ointment.


drug interaction

Under the influence of acetylsalicylic acid, the level of effectiveness of the agent in question increases significantly. A similar result is provided by the drugs Dextran, Ibuprofen, Dipyridamole, Indomethacin. As a result, the likelihood of bleeding increases.

The action of heparin is weakened under the influence of antihistamines, tetracyclines, nicotine, cardiac glycosides.

If you use the agent in question together with anticoagulants of a different principle of action (indirect), the half-life of metabolites will increase.

Heparin is often used simultaneously with allantoin, benzocaine, dexpanthenol.


Analogues

As analogues, the above-mentioned agents containing heparin are used. In this case, sometimes it is necessary to recalculate the dosage if the concentration of the active substance is higher or lower. However, it is permissible to use tools that differ in composition, but have a similar principle of action:

  • Troxerutin;
  • Dexpanthenol.

Terms and conditions of storage

It is forbidden to use the drug after 2 years from the date of production. Recommended storage conditions: temperature within +25°С.

Terms of dispensing from pharmacies

The solution can be purchased with a prescription. Gel - without a prescription.

Price

The cost varies significantly. Pricing is affected by the form of release. You can buy the tool at a price of 60-520 rubles.


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