Heparin solution and / I / / n / k 5000me / ml 5ml vial 5 pcs

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Heparin solution and / I / / n / k 5000me / ml 5ml vial 5 pcs

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Description

Composition
Description:
Solution for intravenous or subcutaneous administration.
Product form:
Solution for intravenous and subcutaneous administration of 5000 IU / ml in ampoules of 1 ml and 5 ml.
Dosage
5000 IU / ml
Indications
– prevention and treatment of venous thromboses (including thrombosis of the superficial and deep veins of the lower extremities, venous thrombosis, renal) 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 coagulopathies (including stage I DIC); – acute coronary syndrome without segment ST resistant rise to ECG (unstable angina, myocardial infarction without ST segment lifting the ECG); – elevation myocardial infarction segment ST: in thrombolytic therapy, primary percutaneous coronary revascularization (balloon angioplasty with or without stenting), and at high risk of arterial or venous thrombosis and thromboembolism; – prevention and microthrombogenesis therapy and microcirculation disorders, including when hemolytic-uremic syndrome; glomerulonephritis (including lupus nephritis) and diuresis; – prevention of blood coagulation during blood transfusion, in extracorporeal circulation systems (extracorporeal circulation during cardiac surgery, hemosorbtion, cytapheresis) and in hemodialysis; – treatment of peripheral venous catheters.
pharmachologic effect
Pharmacological group:
Anticoagulant means of direct action.
Pharmacodynamics:
Anticoagulant direct action; Heparin belongs to the group of middle-weight heparins, inhibits the formation of fibrin. The anticoagulant effect is detected 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: IIa (thrombin), IXa, Xa, XIa, XIIa (especially important is the ability to inhibit thrombin and activated Factor X). Sodium Heparin binds antithrombin III and causes conformational changes in the molecule. As a result, accelerating the binding of antithrombin III with blood clotting factor IIa (thrombin), IXa, Xa, XIa and XIIa and blocked their enzymatic activity. Binding of sodium heparin to antithrombin III is electrostatic in nature and is largely dependent on the length and composition of the molecule (sodium heparin for binding with antithrombin III required pentasaccharide sequence comprising 3-O-sulfated glucosamine).
Most importantly, the ability of heparin to complex with antithrombin III inhibiting coagulation factors IIa (thrombin) and Xa. The ratio of sodium heparin activity against Factor Xa to its activity against factor IIa is 0.9-1.1.
Heparin lowers blood viscosity, reduces vascular permeability stimulated by bradykinin, histamine and other endogenous factors, and thus prevents the development of stasis. Heparin sodium capable adsorbed on the surface of endothelial membranes and blood cells, increasing their negative charge which prevents platelet adhesion and aggregation. Heparin sodium slows hyperplasia of smooth muscle activates lipoprotein lipase and thus has hypolipidemic effect and prevents the development of atherosclerosis.
Sodium Heparin binds some components of the complement system and decreasing its activity, inhibits lymphocyte cooperation and education immunoglobulin binds histamine, serotonin (i.e., has anti-allergic effect). Sodium Heparin increases renal blood flow, cerebral blood vessels increases resistance, reduces cerebral hyaluronidase activity, reduces the activity of the surfactant in the lungs, suppresses excessive synthesis of aldosterone in the adrenal cortex, binds epinephrine to modulate ovarian response to hormonal stimuli, enhances the activity of PTH. As a result of interaction with enzymes sodium heparin may increase tyrosine hydroxylase activity of the brain, pepsinogen, DNA polymerase and reduce the activity of myosin ATPase, pyruvate kinase, RNA polymerase, pepsin. The clinical significance of these effects of heparin remains uncertain and poorly understood.
In acute coronary syndromes without persistent ST-segment elevation on the electrocardiogram (unstable angina, myocardial infarction without ST segment lift) of sodium heparin in combination with acetylsalicylic acid reduces the risk of myocardial infarction and reduce mortality. In myocardial infarction with ST segment elevation on the ECG, heparin sodium is effective in primary percutaneous coronary revascularization in combination with inhibitors of glycoprotein IIb / IIIa receptor and streptokinase in thrombolytic therapy (increased frequency revascularization).
At high doses of heparin sodium is effective in pulmonary embolism, and venous thrombosis. In low doses of heparin sodium is effective for the prevention of venous thromboembolism, including after surgery.
After intravenous administration of drug action occurs almost immediately, no later than 10-15 minutes and lasts long – 3-6 hours after subcutaneous administration of heparin sodium action begins slowly -. Over 40-60 min, but lasts 8 hours.
Antithrombin III deficiency in a plasma or at the site of thrombosis could reduce the antithrombotic effect of heparin sodium.
Pharmacokinetics:
After intravenous administration, the maximum concentration (Cmax) is achieved almost immediately after the subcutaneous administration – after 2-4 hours.
Communication with plasma proteins – up to 95% volume distribution is very small – 0.06 L / kg (not leave the bloodstream because strong binding to plasma proteins).
It does not cross the placental barrier and into breast milk.
Intensively captured endothelial cells and cells of the mononuclear macrophage system (the reticuloendothelial system cells) is concentrated in the liver and spleen. It is metabolized in the liver with N-desulfamidazy and heparinase platelet metabolism include heparin at later stages. Involved in the metabolism of platelet factor IV (antigeparinovogo factor), and binding of heparin sodium to macrophage system explain rapid biological inactivation and the short duration of action. Desulfated molecules under the influence of endoglycosidases kidney transformed into low molecular weight fragments.
The half-life (T1 / 2) was 1-6 hours (mean 1.5 hours). The half-life of heparin sodium increases in obesity, hepatic and renal failure, while decreasing pulmonary embolism, infectious diseases, malignancies.
Heparin sodium excreted by the kidneys in the form of inactive metabolites. At high doses may excretion (50%) unaltered. Not output by hemodialysis.
Dosing and Administration
Heparin is administered subcutaneously, intravenously or by bolus infusion.
Heparin was administered as a continuous intravenous infusion or in the form of regular intravenous injection and subcutaneous injection (in the abdomen).
Heparin sodium should not be administered intramuscularly because of the risk of hematoma intramuskulyarnyh.
Subcutaneous injection is preferably carried out in the antero-lateral wall of the abdomen (exceptionally introduced into the upper shoulder area or thigh) while using a thin needle to be administered deep, perpendicular, in a fold of skin, held between thumb and forefinger to closure administration solution. It should be alternated each time the injection site (to avoid the formation of hematomas). The first injection is necessary to carry out for 1-2 hours prior to surgery, postoperative – administered for 7-10 days, and if necessary – longer.
The initial dose of heparin sodium introduced for therapeutic purposes, usually 5000 IU and administered intravenously, after which the treatment is continued using subcutaneous injection or intravenous infusion.
Maintenance dose is determined depending on the application: – when continuous intravenous infusion administered of 1000 – 2000 IU / h (24000-48000 IU / day) 0.9% heparin spreading sodium chloride solution; – at regular prescribed intravenous injections of 5000-10000 IU heparin every 4-6 hours; – when administered subcutaneously administered every 12 hours at 15,000-20,000 IU or every 8 h at 8000-10000 IU.
Laboratory monitoring of the efficacy and safety of sodium heparin therapy.
The dose of heparin sodium must be adjusted on the basis of laboratory values ​​of blood clotting. In the application of sodium heparin necessary to control the activated partial thromboplastin time (APTT) or coagulation time (FAC). The administered dose of heparin sodium is considered adequate if APTT 1.5-2.5 times greater than control value, or if the patient’s HSC 2.5-3.0 times higher than control values.
In continuous intravenous infusion of sodium heparin to determine the recommended initial aPTT, then determine APTT every 4 h, followed by increasing or decreasing the rate of infusion of heparin sodium to reach the target level of APTT (1.5-2.5 times higher than normal) further define every APTT 6 o’clock.
When a bolus intravenous injection of sodium heparin to determine the recommended initial aPTT, then determine APTT before each bolus followed by an increase or decrease in the dose administered sodium heparin.
In subcutaneous administration of heparin sodium recommended control APTT 4-6 hours after injection, with a consequent increase or decrease in the dose administered sodium heparin.
In subcutaneous administration of low doses of heparin sodium (5000 IU 2-3 times a day) for preventing thrombogenesis regularly monitor APTT not necessarily, since it increases slightly.
Continuous intravenous infusion is the most effective use of sodium heparin better than regular (periodic) injection, since It provides a more stable and less likely to cause hypocoagulation bleeding.
The use of sodium heparin in specific clinical situations
Primary percutaneous coronary angioplasty during acute coronary syndromes without ST-segment elevation and myocardial infarction segment elevation ST: Sodium Heparin is administered intravenously in a bolus dose of 70-100 IU / kg (if not planned use of inhibitors of glycoprotein IIb / IIIa receptor antagonist) or a dose of 50 -60 IU / kg (or combined with inhibitors of glycoprotein IIb / IIIa receptor).
Thrombolytic therapy in myocardial infarction segment elevation ST: Sodium Heparin administered i.v. bolus dose of 60 IU / kg (maximum dose of 4000 IU), followed by intravenous infusion at a dose of 12 IU / kg (1000 IU / h) over 24 48 hours. Target aPTT level of 50-70 seconds or 1.5-2.0 times higher than normal; control aPTT after 3, 6, 12 and 24 h after initiation of therapy.
Prevention of thromboembolic complications following surgical interventions using low doses of sodium heparin Sodium heparin is administered subcutaneously, deeply pleated abdominal skin. Starting dose 5000 IU for 2 hours before the operation. Postoperatively: 5000 IU every 8-12 h for 7 days or until the full recovery of the patient mobility (whichever comes first). In the application of sodium heparin at low doses for the prevention of thromboembolic complications not necessarily control the aPTT.
Application in cardiovascular surgery in operations using extracorporeal circulation systems The initial dose of heparin sodium – at least 150 IU / kg body weight. Further, heparin sodium is administered by continuous intravenous infusion at a rate of 15-25 drops / min at 30,000 IU per 1 liter of infusion solution. The total dose of sodium heparin is usually 300 IU / kg body weight (if the estimated duration of surgery less than 60 minutes) or 400 IU / kg body weight (if the intended duration of operation of 60 minutes or more).
Use in hemodialysis. The initial dose of sodium heparin: 25-30 IU / kg (or 10,000 IU) i.v. bolus, followed by continuous infusion of sodium heparin 20000 IU / 100 ml 0.9% sodium chloride solution at a rate of 1500-2000 IU / h (unless otherwise indicated in manual application systems for hemodialysis).
Heparin sodium in pediatrics. Adequate controlled studies the use of sodium heparin were not conducted in children. The recommendations 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), children older than 1 year – 18-20 IU / kg / h (500 IU / kg / day) intravenously.
The dose of heparin sodium to be selected based on indicators of blood coagulation (APTT target level of 60-85 sec).
The duration of therapy depends on indications and method of application. For intravenous use, the optimal treatment duration is 7-10 days, followed by continued treatment with oral anticoagulants (oral anticoagulants recommended to appoint, starting from 1 day of treatment with heparin sodium or 5 to 7 days, and the use of sodium heparin terminate at 4-5 day combined therapy). With extensive thrombosis of the iliac-femoral veins advisable to conduct a longer course of treatment with heparin sodium.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

Russia

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