2010/06/09

Dalteparin sodium

International name:
Dalteparin sodium (Dalteparin sodium)

Group Affiliation:
Direct anticoagulant

Description of the active substance (INN):
Dalteparin sodium

Dosage form:
injection

Mode of action:
Direct-acting anticoagulant, is associated with plasma antithrombin III, inhibits certain coagulation factors, especially factor Xa and thrombin, but suppresses the formation of thrombin is somewhat less conventional heparin. Virtually no effect on clotting time. Little effect on the adhesion of platelets (compared with heparin) and, thus has less effect on primary hemostasis. also has fibrinolytic, koronarodilatiruyuschee, hypolipidemic and immunosuppressive effects, suppresses trombokinazu. Effect develops rapidly and lasts 4-6 hours

Indications:
Acute deep vein thrombosis, pulmonary embolism, unstable angina, acute myocardial infarction (without Q wave on ECG). Prevention of clotting in the extracorporeal circulation during long-term hemodialysis, prevention of thrombosis during surgical operations.

Contraindications:
Hypersensitivity, hypocoagulation (various origins), hemophilia, erosive and ulcerative lesions GIT (exacerbation) with a tendency to bleeding, pulmonary tuberculosis, liver cirrhosis, nefrourolitiaz, renal and hepatic failure, bacterial endocarditis, trauma central nervous system, organs of vision, surgical intervention these organs, spinal and epidural punktsii.C caution. Thrombocytopenia, BPD.

Side effects:
Bleeding (when used in high doses), thrombocytopenia, allergic reactions (rash, itching, rare - anaphylactic shock), osteoporosis, spontaneous fractures, increased activity of "liver" transaminases, alopecia, skin necrosis, hematoma in the field vvedeniya.Peredozirovka. Symptoms: Hemorrhagic syndrome. Treatment: Introduction protamine (1 mg protamine inhibits dalteparina 100 IU).

Dosage and administration:
Prevention of clotting in the extracorporeal circulation during hemodialysis or hemofiltration in patients with chronic renal failure with or without the risk of bleeding - in / jet at a dose of 30-40 IU / kg followed by infusion at a rate of 10-15 IU / kg / h (duration hemodialysis at least 4 h is also possible once in / jet introduction to the doses of 5 thousand m). The activity of factor Xa in plasma should be 0.5-1 IU / ml. In acute renal failure in patients at high risk of bleeding - in / on 5-10 IU / kg in the jet, then drip at a rate of 4-5 IU / kg / h, the activity of factor Xa in plasma should be 0.2-0.4 IU / ml. In acute deep vein thrombosis and / or pulmonary embolism (usually with indirect anticoagulants - vitamin K antagonists) - n / a dose of 200 IU / kg once , or 100 IU / kg every 12 hours (at an increased risk of bleeding). The maximum single dose - 18 tys.ME. The activity of factor Xa in plasma should not exceed 0.5-1 IU / ml. Duration of treatment - 5 days (up to normalization of prothrombin index). Prevention of thrombosis in surgical interventions (factor Xa activity should be 0.1-0.4 IU / ml). Patients at risk for thromboembolic complications - n / a 2.5 thousand m for 2 h before surgery and then every morning with the same dose throughout the period of bed rest, usually - 5-7 days. If there are additional risk factors for thromboembolism (in m . h. malignant tumors) and during orthopedic surgery (including the endoprosthetics) in the case of initiation of therapy up to 1 day before surgery - S / by 5 thousand m night before the operation, then - to 5 thousand m night after the operation, with the start of therapy on the day of operation - n / a 2,500 IU for 2 h before operation and after 8-12 h (but not earlier than 4 h) after surgery at the same dose, then daily in the morning five thousand m . After 4-8 hours (no earlier than 4 h) after orthopedic surgery sc injected 2.5 thousand m, then - to 5 thousand m daily. The course of treatment in the presence of additional risk factors for thromboembolism - the duration of bed rest (usually 5-7 days), and orthopedic operations - for 5 weeks. At a myocardial infarction (without Q-wave on ECG) and unstable angina (usually in combination with ASA in doses of 75-325 mg / d) - n / a, 120 IU / kg every 12 hours for women weighing less than 80 kg and men weighing less than 70 kg - 5 thousand m s / c every 12 h, women with body weight over 80 kg or more and men with a body weight of 70 kg or more - by 7.5 thousand m every 12 h. The maximum dose - 10 thousand m every 12 hours therapy is carried out to stabilize the clinical condition (usually not less than 6 days but not more than 45 days). Factor Xa activity should be within 0.5-1 IU / ml. In elderly patients the dose is reduced.

Cautions:
The application is only possible under the supervision of active suppression of factor Xa by anti-Xa analysis using the chromogenic protein substrate. Clotting time varies slightly. At the level of activity suppression factor Xa more than 1.5 IU / ml dramatically increased risk of bleeding. Health and Safety during pregnancy and lactation not established.

Interaction:
ASA, indomethacin and other NSAIDs, indirect anticoagulants, inhibitors of platelet aggregation (including ticlopidine), thrombolytics (alteplase, streptokinase, urokinase) vitamin K antagonists, dipyridamole, dextran, fenilbutazon, sulfinpirazon, blockers tubular secretion, ethacrynic acid , cytostatics (with in / in the introduction) increase anticoagulant effect (risk of bleeding), antihistamine drugs, cardiac glycosides, tetracyclines, ascorbic acid - decrease.