Heparin Sodium Injection 2ml/12500 IU 5ml/25000 IU Anticoagulant

Heparin Sodium Injection 2ml/12500 IU 5ml/25000 IU Anticoagulant

Product : Heparin Sodium Injection

Specification : 2ml:12500 IU, 5ml:25000 IU

Standard : In - house

Packing : 10vials/box

Description 

Unfractionated heparin (UH) is a heterogenous preparation of anionic, sulfated glycosaminoglycan polymers with weights ranging from 3000 to 30,000 Da. It is a naturally occurring anticoagulant released from mast cells. It binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin (factor IIa) and factor Xa. UH is different from low molecular weight heparin (LMWH) in the following ways: the average molecular weight of LMWH is about 4.5 kDa whereas it is 15 kDa for UH; UH requires continuous infusions; activated partial prothrombin time (aPTT) monitoring is required when using UH; and UH has a higher risk of bleeding and higher risk of osteoporosis in long term use. Unfractionated heparin is more specific than LMWH for thrombin. Furthermore, the effects of UH can typically be reversed by using protamine sulfate.

Indications and Dosages

➤➤To prevent and treat deep vein thrombosis and pulmonary embolism, to treat peripheral arterial embolism, and to prevent thromboembolism before and after cardioversion of chronic atrial fibrillation

i.v. infusion or injection

Adults. Loading: 35 to 70 units/kg or 5,000 units by injection. Then 20,000 to 40,000 units infused over 24 hr.

Children. Loading: 50 units/kg by injection. Then 100 units/kg infused every 4 hr or 20,000 units/m2 infused over 24 hr.

i.v. injection

Adults. Initial: 10,000 units. Maintenance: 5,000 to 10,000 units every 4 to 6 hr.

Children. Initial: 50 units/kg. Maintenance: 100 units/kg/dose every 4 hr.

i.v. or subcutaneous injection

Adults. Loading: 5,000 units I.V. Then 10,000 to 20,000 units subcutaneously.

Maintenance: 8,000 to 10,000 units subcutaneously every 8 hr or 15,000 to 20,000 units subcutaneously every 12 hr.

➤➤To diagnose and treat disseminated intravascular coagulation (DIC)

i.v. infusion or injection

Adults. 50 to 100 units/kg every 4 hr. Drug may be discontinued if no improvement occurs in 4 to 8 hr.

Children. 25 to 50 units/kg every 4 hr. Drug may be discontinued if no improvement occurs in 4 to 8 hr.

➤➤To prevent postoperative thromboembolism

subcutaneous injection

Adults. 5,000 units 2 hr before surgery an then 5,000 units every 8 to 12 hr for 7 day or until patient is fully ambulatory.

➤➤To prevent clots in patients undergoing open-heart and vascular surgery

i.v. infusion or injection

Adults. 300 units/kg for procedures that last less than 60 min; 400 units/kg for procedures that last longer than 60 min Minimum: 150 units/kg.

Children. 300 units/kg for procedures that last less than 60 min. Then dosage based on coagulation test results. Minimum: 150 units/kg.

➤➤To maintain heparin lock patency

i.v. injection

Adults. 10 to 100 units/ml heparin flush solution (enough to fill device) after each

use of device.

Route          Onset           Peak          Duration

I.V.              Immediate      Minutes        Unknown

SubQ          20–60 min     Unknown      Unknown

Pharmacodynamics

Unfractionated heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from 3000 to 30,000 daltons. Heparin is obtained from liver, lung, mast cells, and other cells of vertebrates. Heparin is a well-known and commonly used anticoagulant which has antithrombotic properties. Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Small amounts of heparin in combination with antithrombin III, a heparin cofactor,) can inhibit thrombosis by inactivating Factor Xa and thrombin. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot by inhibiting the activation of the fibrin stabilizing factor. Heparin prolongs several coagulation tests. Of all the coagulation tests, activated partial prothrombin time (aPTT) is the most clinically important value.

Mechanism of action

Under normal circumstances, antithrombin III (ATIII) inactivates thrombin (factor IIa) and factor Xa. This process occurs at a slow rate. Administered heparin binds reversibly to ATIII and leads to almost instantaneous inactivation of factors IIa and Xa The heparin-ATIII complex can also inactivate factors IX, XI, XII and plasmin. The mechanism of action of heparin is ATIII-dependent. It acts mainly by accelerating the rate of the neutralization of certain activated coagulation factors by antithrombin, but other mechanisms may also be involved. The antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Heparin is not a thrombolytic or fibrinolytic. It prevents progression of existing clots by inhibiting further clotting. The lysis of existing clots relies on endogenous thrombolytics.