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Description

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

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
281.0 nM [Kd]
607.0 nM [Kd]
106.0 nM [Kd]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
HEPARIN SODIUM
Primary
HEPARIN SODIUM
Primary
HEPARIN SODIUM

PubMed

Sample Use Guides

In Vivo Use Guide
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
Substance Class Polymer
Record UNII
T2410KM04A
Record Status Validated (UNII)
Record Version