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RXDRUG-BR-1309-10

HEPRIN Heparin Sodium 1000IU / mL Solution for IV/SC Injection 10's

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Description

Indications/Uses

Heparin is anticoagulant used principally in the treatment and prophylaxis of thromboembolic disorders. It is also a prophylaxis in surgical patients and in those pregnant women at particular risk. It is also used in the management of arterial thromboembolism including that associated with unstable angina pectoris, myocardial infarction, acute peripheral arterial occlusion, and stroke. It is often used as a precursor to oral anticoagulant and is withdrawn once the oral anticoagulant is exerting its full effect. It is also used to prevent coagulant during haemodialysis and other extracorporeal circulatory procedures such as cardiopulmonary bypass.

Dosage/Direction for Use

Heparin is administered intravenously preferably by continuous infusion, or by subcutaneous injection. It may be given as the calcium or sodium salt and it is generally accepted that there is a little difference in their effects. Doses of heparin for treatment and in some cases prophylaxis, of thromboembolism should be monitored and determined as under Control of Heparin Therapy. The subcutaneous doses of heparin commonly used for prophylaxis and often-termed "low dose" SC heparin do not require routine monitoring. A test has been recommended for patients with a history of allergy.
For treatment of venous thromboembolism, an IV loading dose of 5000 to 10000 units is followed by continuous IV infusion of 1000 to 2000 units per hour or SC injection of 15000 units every 12 hours. Alternatively, intermittent IV injection of 5000 to 10000 units every 4 to 6 hours is suggested products. Children and small adult are given a lower intravenous loading dose followed by maintenance with continuous intravenous infusion of 15 to 25 units per kg body-weight per hour or SC injection of 250 units per kg every hour.
For prophylaxis of postoperative venous thromboembolism, subcutaneous doses used are 5000 units 2 hours before surgery than every 8 to 12 hours for 7 days or until the patient is ambulant. Similar doses are used to prevent thromboembolism during pregnancy in women with a history of deep-vein thrombosis or pulmonary embolism; the dosage may need to be increased to 10000 units every 12 hours during the third trimester.
In the management of unstable angina or acute peripheral arterial embolism, heparin be given continuous intravenous infusion in the same doses as those recommended for the treatment of venous thromboembolism. Doses for the prevention of re-occlusion of the coronary arteries following thrombolytic therapy in myocardial infarction include either 2000 units of heparin IV followed by 12500 units SC every 12 hours after streptokinase, or 5000 units IV followed by 1000 units per hour intravenously after alteplase; a dose of 12500 units subcutaneously every 12 hours for at least 10 days be used to prevent mural thrombosis.
Control of Heparin Therapy: Treatment with full-dose must be monitored to ensure that the dose is providing the required effect on antithrombin III. The most commonly used test to monitor the action of heparin is the activated partial thromboplastin time (APTT). The APTT of patients on full-dose heparin should generally be maintained at 1.5 to 2.0 times the control value although the optimum therapeutic range varies between individual laboratories depending on the PTT reagent used. Regular monitoring is essential preferably on a daily basis. Prophylaxis with low-dose subcutaneous heparin is not routinely monitored; the APTT is not significantly prolonged in these patients. A dose adjusted regimen to maintain minimal prolongation of the APTT may be required in patients with malignancies or undergoing orthopedic surgery to ensure adequate protection against thromboembolism.
Or as prescribed by the physician.

Overdosage

Treatment of Overdosage: Slight hemorrhage due to overdosage can usually be treated by slopping heparin. Severe bleeding may be reduced by the slow intravenous administration of protamine sulfate. The dose is dependent on the amount of heparin to be neutralized and ideally should be titrated against assessments of the coagulability of the patient's blood. As heparin is continuously excreted the dose of protamine should be reduced if it is more than 15 minutes since the last dose of heparin. Not more than 50 mg of protamine sulfate should be injected for any one dose; patients should be carefully monitored as further doses may be required. The Ph. Eur. 5.5 specifies that 1 mg of protamine sulfate precipitates not less than 100 IU of heparin but adds that this potency is based on a specific reference batch of heparin sodium.

Contraindications

Heparin Sodium should not be used in patients with severe thrombocytopenia; in whom suitable blood coagulation tests e.g. the whole-clotting time; with an uncontrollable active bleeding.

Warnings

Heparin is not intended for intramuscular use. The product contains benzyl alcohol and should not be administered to newborn babies and infants.

Special Precautions

Heparin should not be given to patients who are hemorrhaging. In general it should not be given to patients at serious risk of hemorrhage, although it has been used with every careful control; patients at risk include those with hemorrhagic blood disorders, thrombocytopenia, peptic ulcer disease, cerebrovascular disorders, bacterial endocarditis, severe hypertension, esophageal varices, or patients who have recently undergone surgery at sites where hemorrhage would be an especial risk. Severe renal and hepatic impairment are considered by some to be contra-indications. Heparin should not be given by intramuscular injection. Since heparin has caused thromboembolic complications, platelet counts should be monitored in patients receiving for more than a few days. Heparin should be discontinued if thrombocytopenia develops. A test dose has been recommended for patients with a history of allergy.

Adverse Reactions

Heparin can give rise to hemorrhage as a consequence of its action. It can also cause thrombocytopenia, either through a direct effect or through an immune effect producing a platelet aggregating antibody. Consequent platelet aggregation and thrombosis may therefore exacerbate the condition being treated. The incidence of thrombocytopenia is reported to be greater with bovine than porcine heparin.
Hypersensitivity reactions may occur, as may local irritants effects, and skin necrosis. Alopecia and osteoporosis resulting in spontaneous fractures have occurred after prolonged use of heparin.

Drug Interactions

Heparin should be used with care in conjunction with oral anticoagulants or drugs, such as aspirin and dipyridamole, which affect platelet function. NSAIDs may also increase the risk of hemorrhage. [Other drugs which affect the coagulation process may increase the risk of hemorrhage. This includes dextrans, thrombolytic enzymes such as streptokinase, high doses of penicillins and some cephalosporin, some contrast media, asparaginase, and epoprostenol]. Estimations of oral anticoagulant control may be modified by heparin's action on prothrombin.

Storage

Store at temperatures not exceeding 25°C. Protect from light.

Action

Pharmacology: Heparin inhibits clotting of blood in vitro through its action on antithrombin III. Antithrombin III, which is present in plasma, inhibits the activity of activated clotting factors including thrombin and activated factor X; heparin increases the rate of this inhibition, but in a manner that is dependent on its dose. With normal therapeutic doses heparin has an inhibitory effect on both thrombin and factor Xa. Thus the conversion of fibrinogen is blocked through the thrombin inhibition, while the conversion of prothrombin to thrombin is blocked by the inhibition of factor Xa. The low doses that are given subcutaneously for the prophylaxis of thromboembolism have a selective effect on antithrombin III's inhibition of factor Xa. Very high doses are reported to reduce the activity of antithrombin III. Heparin also has some effect on platelet function inhibits the formation of a stable fibrin clot, and has an antilipidaemic effect.
Pharmacokinetics: Heparin is not absorbed from the gastrointestinal tract. Following intravenous or subcutaneous injection heparin is extensively bound to plasma proteins. It does not cross the placenta and it is not distributed into breast milk. The half-life of heparin depends on the dose and route of administration as well as the method of calculation and is subject to wide inter- and intra-individual variation; a range of 1 to 6 hours with an average of 1.5 hours has been cited. It may be slightly prolonged in renal impairment, decreased in patients with pulmonary embolism and either increased or decreased in patients with liver disorders. Heparin is taken up by the reticoendothelial system. It is excreted in the urine, mainly as metabolites, although, following administration of large doses, up to 50% may be excreted unchanged.

MedsGo Class

Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)

Features

Brand
Heprin
Full Details
Dosage Strength
1000 IU / ml
Drug Ingredients
  • Heparin
Drug Packaging
Solution for Injection (I.V./S.C.) 10's
Generic Name
Heparin Sodium
Dosage Form
Solution for Injection (IV/SC)
Registration Number
BR-1309
Drug Classification
Prescription Drug (RX)
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