Pharmacological properties of sodium heparin is enoxaparin with a low molecular weight with a high anti-Xa activity (100 IU / mg) and low or anti-IIa activity of antithrombin (28 IU / mg). At doses required for a variety of indications, enoxaparin sodium does not increase bleeding time. In prophylactic doses of enoxaparin sodium does not cause a noticeable change in activated partial thromboplastin time (APTT). It has no effect on platelet aggregation or the binding of fibrinogen to platelets.
The pharmacokinetic parameters have been studied using a time of action of the plasma anti-Xa activity and anti-IIa activity in the dose recommended ranges.The absolute bioavailability of enoxaparin sodium after subcutaneous injection of close to 100%. Average maximum anti? A plasma activity was observed in a equipoise dosage period of from 3 to 5 hours after subcutaneous injection. The pharmacokinetics of enoxaparin sodium is likely to have a linear character in the recommended dose range. Even if you reported the difference of pharmacokinetic parameters in equilibrium between single and repeated administration, this difference is expected and within the therapeutic range. The mean maximum plasma anti-IIa activity was observed in the period from 3 to 4 hours after subcutaneous administration.Enoxaparin sodium is primarily metabolized in the liver. The half-life for the anti-Xa activity is between about 4 hours after a single administration, and up to 7 watches – after repeated administration. Renal clearance of the active metabolite is about 10% of the administered dose and total renal excretion of 40% of the dose. In the elderly, since kidney function declines with age, excretion can be reduced. In patients with severe renal failure (creatinine clearance <30 mL / min) AUC increased significantly after repeated subcutaneous injection of 4000 anti-Xa IU 1 time per day.
Indications Solution for injection containing 2000 IU anti-Xa / 0.2 ml and 4,000 IU anti-Xa / 0.4 ml is indicated for the following cases:
- Prevention of venous thrombosis and thromboembolism (particularly orthopedic and surgical operations);
- Prevention of venous thrombosis and thromboembolism in patients undergoing bedrest (CHF class III or IV NYHA, acute respiratory failure, acute infection or acute rheumatic diseases in combination with one of venous thrombosis risk factors: age over 75 years, cancer, thrombosis and thromboembolism history, obesity, hormone therapy, heart failure, chronic respiratory failure).
Solution for injection containing 6000 IU anti-Xa / 0.6 ml is indicated for:
- Treatment of deep vein thrombosis, embolism with or without pulmonary embolism;
- Treatment of unstable angina and myocardial infarction without Q wave on the ECG, if administered with acetylsalicylic acid;
- Prevention giperkoagulyatsii in extracorporeal equipoise dosage circulation during hemodialysis.
The drug should not be used:
- a known hypersensitivity (allergy) to enoxaparin sodium, heparin or other heparins of low molecular weight;
- cerebral aneurysm or vascular dissecting aortic aneurysm (except the surgery);
- in hemorrhagic stroke (established or suspected) and at high risk of uncontrolled bleeding;
- with severe uncontrolled hypertension;
- in severe or enoksaparin- geparinindutsirovannoy thrombocytopenia (in recent months);
- in children (due to lack of data on safety and efficacy of the drug in these patients).
Holding spinal or epidural anesthesia (potential of hematoma); conditions associated with the risk of bleeding – blood coagulation system disorders (including hemophilia, thrombocytopenia, anticoagulation, von Willebrand’s disease, and others.); recent childbirth, severe diabetes, bacterial endocarditis (acute or subacute), peptic equipoise dosage ulcer of the stomach or duodenum 12 or OE erosive and ulcerative lesions of the gastrointestinal tract, intrauterine contraception, neurological or ophthalmological surgery (recently transferred or perceived), pericarditis or pericardial effusion , radiation therapy (recently transferred), renal and / or hepatic failure, diabetic or hemorrhagic retinopathy, a lumbar puncture (recently transferred), severe injury (especially the central nervous system), active tuberculosis, respiratory diseases or urinary tract (acute stage), heavy vasculitis, open wounds on large surfaces, hypertension.
Pregnancy and lactation
There is no evidence that enoxaparin sodium crosses the placental barrier. However, it should be used during pregnancy only if absolutely necessary. Enoxaparin sodium is not recommended for use in pregnant women with prosthetic heart valves (see. “Special Instructions” section). As a precaution, lactating mothers receiving enoxaparin sodium should be advised to avoid breast-feeding.