Нeparin (or Unfractionated heparin ) is an anticoagulant indicated for both the prevention and treatment of thrombotic events such as deep vein thrombosis (DVT) and pulmonary embolism (PE) as well as atrial fibrillation (AF). Heparin can also be used to prevent excess coagulation during procedures such as cardiac surgery, extracorporeal circulation or dialysis, including continuous renal replacement therapy. Heparin administration can be by intravenous (or subcutaneous route. Intravenous heparin is continuously administered for therapeutic anticoagulation, while intermittent subcutaneous administration is used to prevent thromboembolism. Once administered, heparin binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin (factor IIa) and factor Xa. The heparin-ATIII complex can also inactivate factors IX, XI, XII, and plasmin, but the antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Typical adverse effects from heparin use include bleeding, thrombocytopenia, injection site reactions, and other adverse effects only seen with chronic heparin administration. Bleeding is a major complication associated with heparin use. Patients should undergo monitoring for new bleeding that may present in the urine or stool. Bleeding may also present as bruising, petechial rash and nosebleeds.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7281557
Curator's Comment: The possibility of heparin penetration into brain cells was shown. The penetration occurred apparently in the form of heparin complexes with thromboplastin.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1950 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3949807 |
281.0 nM [Kd] | ||
Target ID: CHEMBL3161 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17629851 |
607.0 nM [Kd] | ||
Target ID: CHEMBL5378 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17629851 |
106.0 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | HEPARIN SODIUM Approved UseProphylaxis and treatment of venous thrombosis and pulmonary embolism; Prevention of postoperative deep venous thrombosis and pulmonary embolism in patients undergoing major abdominothoracic surgery or who, for other reasons, are at risk of developing thromboembolic disease; Atrial fibrillation with embolization; Treatment of acute and chronic consumptive coagulopathies (disseminated intravascular coagulation); Prevention of clotting in arterial and cardiac surgery; Prophylaxis and treatment of peripheral arterial embolism.
Anticoagulant use in blood transfusions, extracorporeal circulation, and dialysis procedures. Launch Date1972 |
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Primary | HEPARIN SODIUM Approved UseProphylaxis and treatment of venous thrombosis and pulmonary embolism; Prevention of postoperative deep venous thrombosis and pulmonary embolism in patients undergoing major abdominothoracic surgery or who, for other reasons, are at risk of developing thromboembolic disease; Atrial fibrillation with embolization; Treatment of acute and chronic consumptive coagulopathies (disseminated intravascular coagulation); Prevention of clotting in arterial and cardiac surgery; Prophylaxis and treatment of peripheral arterial embolism.
Anticoagulant use in blood transfusions, extracorporeal circulation, and dialysis procedures. Launch Date1972 |
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Primary | HEPARIN SODIUM Approved UseProphylaxis and treatment of venous thrombosis and pulmonary embolism; Prevention of postoperative deep venous thrombosis and pulmonary embolism in patients undergoing major abdominothoracic surgery or who, for other reasons, are at risk of developing thromboembolic disease; Atrial fibrillation with embolization; Treatment of acute and chronic consumptive coagulopathies (disseminated intravascular coagulation); Prevention of clotting in arterial and cardiac surgery; Prophylaxis and treatment of peripheral arterial embolism.
Anticoagulant use in blood transfusions, extracorporeal circulation, and dialysis procedures. Launch Date1972 |
Sample Use Guides
Deep Subcutaneous (Intrafat) Injection:
Initial -- 5,000 units by intravenous injection, followed by 10,000 units to 20,000 units of a concentrated solution
Every 8 hours: 8,000 units to 10,000 units of a concentrated solution
Intermittent Intravenous Injection:
Initial: 10,000 units, either undiluted or in 50 mL to 100 mL of 0.9% Sodium Chloride Injection, USP by intravenous injection
Every 4 to 6 hours: 5,000 units to 10,000 units, either undiluted or in 50 mL to 100 mL of 0.9% Sodium Chloride Injection, USP
Route of Administration:
Other
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C263
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Code System | Code | Type | Description | ||
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HEPARIN CALCIUM
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PRIMARY | Description: A white or almost white powder. Solubility: Freely soluble in water.Category: Anticoagulant. Storage: Heparin calcium should be kept in a tightly closed container. Labelling: The designation Heparin calcium for parenteral use indicates that the substance complies with the additional requirements and may be used for parenteral administration. The label should also state the name and quantity of any added substances, and the source of the material (lung or mucosal). Expiry date. Additional information: Heparin calcium is moderately hygroscopic.Definition: Heparin calcium is a preparation containing the calcium salt of a sulfated glucosaminoglycan present in mammalian tissues. It has the characteristic property of delaying the clotting of fresh blood.Heparin calcium intended for the manufacture of a parenteral dosage form contains not less than 150 IU per mg, and Heparin calcium not intended for use in the manufacture of a parenteral dosage form contains not less than 120 IU per mg, both calculated with reference to the dried substance. | ||
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100000092067
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37270-89-6
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CHEMBL1201513
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M4F288ZCTR
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SUB02476MIG
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C1034
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20044
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DBSALT001434
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m5958
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PRIMARY | Merck Index |
ACTIVE MOIETY
SUBSTANCE RECORD