HEPARIN SODIUM- heparin sodium injection, solution
from beef lung
Heparin is a heterogenous group of straight-chain anionic mucopolysaccharides, called glycosaminoglycans having anticoagulant properties. Although others may be present, the main sugars occurring in heparin are: (1) ?-L-iduronic acid 2-sulfate, (2) 2-deoxy-2-sulfamino-?-D-glucose 6-sulfate, (3) ?-D-glucuronic acid, (4) 2-acetamido-2-deoxy-?-D-glucose, and (5) ?-L-iduronic acid. These sugars are present in decreasing amounts, usually in the order (2) > (1) > (4) > (3) > (5), and are joined by glycosidic linkages, forming polymers of varying sizes. Heparin is strongly acidic because of its content of covalently linked sulfate and carboxylic acid groups. In heparin sodium, the acidic protons of the sulfate units are partially replaced by sodium ions.
Heparin Sodium Injection, USP is a sterile solution of heparin sodium derived from bovine lung tissue, standardized for anticoagulant activity. It is to be administered by intravenous or deep subcutaneous routes. The potency is determined by a biological assay using a USP reference standard based on units of heparin activity per milligram. Heparin is pyrogen-free.
Each mL of the 1,000 and 5,000 USP Units per mL preparations contains: heparin sodium 1,000 or 5,000 USP Units; 9 mg sodium chloride; 9.45 mg benzyl alcohol added as preservative. Each mL of the 10,000 USP Units per mL preparations contains: heparin sodium 10,000 USP Units; 9.45 mg benzyl alcohol added as preservative.
When necessary, the pH of Heparin Sodium Injection, USP was adjusted with hydrochloric acid and/or sodium hydroxide. The pH range is 5.0–7.5.
Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Heparin acts at multiple sites in the normal coagulation system. Small amounts of heparin in combination with antithrombin III (heparin cofactor) can inhibit thrombosis by inactivating activated Factor X and inhibiting the conversion of prothrombin to 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.
Bleeding time is usually unaffected by heparin. Clotting time is prolonged by full therapeutic doses of heparin; in most cases, it is not measurably affected by low doses of heparin.
Heparin Sodium Indications and Usage
Heparin Sodium Injection is indicated for:
Anticoagulant therapy in prophylaxis and treatment of venous thrombosis and its extension;
(In a low-dose regimen) for prevention of postoperative deep venous thrombosis and pulmonary embolism in patients undergoing major abdomino-thoracic surgery or who for other reasons are at risk of developing thromboembolic disease (see DOSAGE AND ADMINISTRATION);
Prophylaxis and treatment of pulmonary embolism;
Atrial fibrillation with embolization;
Diagnosis and treatment of acute and chronic consumption coagulopathies (disseminated intravascular coagulation);
Prevention of clotting in arterial and heart surgery;
Prophylaxis and treatment of peripheral arterial embolism;
As an anticoagulant in blood transfusions, extracorporeal circulation, and dialysis procedures and in blood samples for laboratory purposes.
DOSAGE AND ADMINISTRATION
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Slight discoloration does not alter potency.
When heparin is added to an infusion solution for continuous intravenous administration, the container should be inverted at least six times to ensure adequate mixing and prevent pooling of the heparin in the solution.