Bemiparin
Drug group: Cardiovascular agents
Bemiparin is an antithrombotic and belongs to the group of drugs known as the low molecular weight heparins (LMWH). Like semuloparin, bemiparin is classified as an ultra-LMH because of its low mean molecular mass of 3600 daltons, which is a unique property of this class.
These heparins have lower anti-thrombin activity than the traditional low molecular weight heparins and act mainly on factor-Xa, reducing the risk of bleeding due to selectivity for this specific clotting factor. Interestingly, current research is underway for the potential benefit of bemiparin in the treatment of tumors and diabetic foot ulcers
These heparins have lower anti-thrombin activity than the traditional low molecular weight heparins and act mainly on factor-Xa, reducing the risk of bleeding due to selectivity for this specific clotting factor. Interestingly, current research is underway for the potential benefit of bemiparin in the treatment of tumors and diabetic foot ulcers
Mechanism of effect
This drug is a second-generation low molecular weight heparin (LMWH). It has a very low mean molecular weight (3600 Dalton), a long half-life (5.3 hrs) and a large anti-Xa: anti-IIa ratio (8:1). The mechanism of action of bemiparin is inhibition of factor Xa, which is a necessary step in the clotting cascade. Factor-Xa is necessary for the propagation of a thrombus. Combined with various co-factors that bind to activated platelets, Factor-Xa increases coagulation by converting prothrombin to thrombin. Activated Factor-X, bound as part of the prothrombinase complex on the external surface of activated platelets, converts significant amounts of prothrombin to thrombin, promoting the so-called ‘thrombin burst’, referring to a burst of thrombin release.
A secondary but less potent mechanism of action of this drug is binding to antithrombin III and activated factor II (Factor IIa), which further prevents the propagation of thrombi.
Due to its excellent pharmacological profile-the second-generation LMWH with the lowest molecular weight, the longest half-life and the highest anti-Factor Xa/anti-Factor IIa activity ratio-it can be safely used in special categories of patients (children, elderly, patients with renal impairment and congestive heart failure). Several studies demonstrated its safety and efficacy, while cost analyses show the economic benefits of bemiparin treatment as compared to other heparins.
A secondary but less potent mechanism of action of this drug is binding to antithrombin III and activated factor II (Factor IIa), which further prevents the propagation of thrombi.
Due to its excellent pharmacological profile-the second-generation LMWH with the lowest molecular weight, the longest half-life and the highest anti-Factor Xa/anti-Factor IIa activity ratio-it can be safely used in special categories of patients (children, elderly, patients with renal impairment and congestive heart failure). Several studies demonstrated its safety and efficacy, while cost analyses show the economic benefits of bemiparin treatment as compared to other heparins.
Pharmacodynamic
Absorption
Hemiparin sodium is rapidly absorbed following its subcutaneous dose of injection, and the bioavailability is estimated to be 96%
Metabolism
In a study of healthy volunteers, bemiparin 3500 IU achieved more anti-Xa activity than enoxaparin 4000 IU, measured by the area under the curve. The peak of anti-Xa activity was reached at 3h post-administration, and there were anti-Xa measurable levels up to 16 h after subcutaneous injection
Half life
Bemiparin, when administered in the dose range of 2,500 IU to 12,500 (therapeutic dosing), it has an approximate half-life of 5-6 hours
Excretion
This drug is eliminated by the renal and hepatic routes. Elimination is prolonged in those with renal or hepatic impairment
Hemiparin sodium is rapidly absorbed following its subcutaneous dose of injection, and the bioavailability is estimated to be 96%
Metabolism
In a study of healthy volunteers, bemiparin 3500 IU achieved more anti-Xa activity than enoxaparin 4000 IU, measured by the area under the curve. The peak of anti-Xa activity was reached at 3h post-administration, and there were anti-Xa measurable levels up to 16 h after subcutaneous injection
Half life
Bemiparin, when administered in the dose range of 2,500 IU to 12,500 (therapeutic dosing), it has an approximate half-life of 5-6 hours
Excretion
This drug is eliminated by the renal and hepatic routes. Elimination is prolonged in those with renal or hepatic impairment
Drug indications
Bemiparin is indicated in the following cases: To prevent blood clots in the veins after general abdominal surgery in patients with a moderate risk of venous thromboembolism; in the prevention of the thromboembolic disease in non-surgical patients; prevention of clotting in the extracorporeal circuit during hemodialysis; to prevent blood clots in the veins after a major orthopedic surgery in patients with high risk of venous thromboembolism; secondary prevention of venous thromboembolism; recurrence in patients with deep vein thrombosis; transient prevention and treatment of deep vein thrombosis (DVT).
Interactions
Tanacetum parthenium , Feverfew , Citalopram , Naproxen , Quinine , Ginkgo biloba , fenoprofen , Diflunisal , Butabarbital , Cordyceps , Netonal , Triphasic , Benorilate , bazedoxifene/conjugated estrogensUser's questions
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