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Identification Pharmacology 1/11/2019 Bemiparin - DrugBank Drugs Bemiparin Targets (3) Enzymes (1) Biointeractions (3) IDENTIFICATION Name Bemiparin Accession Number DB09258 Type Small Molecule Groups Approved, Investigational Description 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 [1]. 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 [12, 1]. Synonyms Not Available Product Ingredients INGREDIENT UNII CAS INCHI KEY Bemiparin sodium P59JKU02CE Not Available Not applicable International/Other Badyket / Heporax / Hibor / Zibor Brands Categories Agents causing hyperkalemia Carbohydrates Heparin and similars Anticoagulants Glycosaminoglycans Polysaccharides Blood and Blood Forming Heparin (Low Molecular Weight) Organs UNII PUE0TO3XDR CAS number 91449-79-5 Weight Not Available Chemical Formula Not Available InChI Key Not Available InChI Not Available IUPAC Name Not Available SMILES Not Available PHARMACOLOGY https://www.drugbank.ca/drugs/DB09258 1/7 1/11/2019 Bemiparin - DrugBank Indication Bemiparin is indicated in the following cases: To prevent blood clots in the veins aer 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 inDrugs the veins aer 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) [8]. Pharmacodynamics Bemiparin is an anticoagulant classified under the broad category of low molecular weight heparins. In humans, bemiparin has been proven to possess antithrombotic activity and, at therapeutic doses, does not significantly prolong global clotting laboratory tests [9]. Mechanism of This drug is a second-generation low molecular weight heparin (LMWH). It has a very low mean action molecular weight (3600 Dalton), a long half-life (5.3 hrs) and a large anti-Xa: anti-IIa ratio (8:1)[8]. 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 [11]. 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 [11]. 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 [14]. 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 [1, 2]. TARGET ACTIONS ORGANISM A Coagulation factor X antagonist Humans U Antithrombin-III antagonist Humans U Heparin cofactor 2 antagonist Humans Absorption Hemiparin sodium is rapidly absorbed following its subcutaneous dose of injection, and the bioavailability is estimated to be 96% [7]. Volume of 5.1 L [4]. distribution Protein binding There are currently no data available with regards to plasma protein binding, metabolism and excretion of bemiparin in humans [9]. 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 aer subcutaneous injection [6]. Route of This drug is eliminated by the renal and hepatic routes. Elimination is prolonged in those with elimination renal or hepatic impairment [10]. 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 [7]. Clearance Elimination occurs in a linear fashion, with a mean clearance time of over 7 h and total clearance of 0.9 L/h [4]. Toxicity Bemiparin, like other drugs in its class, may suppress adrenal secretion of aldosterone, leading to elevated potassium (hyperkalemia) This may occur more frequently in patients with conditions https://www.drugbank.ca/drugs/DB09258 2/7 1/11/2019 Bemiparin - DrugBank elevated potassium (hyperkalemia). This may occur more frequently in patients with conditions such as diabetes mellitus, chronic renal failure, metabolic acidosis, an increased plasma potassium, and those ingesting potassium sparing drugs. There is a linear relationship between duration of therapy and adverse effects, but this is usually reversible with cessation of treatment. Drugs Serum electrolytes should be measured in at-risk patients before starting bemiparin, and these patients should be monitored regularly thereaer particularly if treatment is prolonged beyond 1 week. In rare cases, mild transient thrombocytopenia (HIT type I) at the beginning of therapy with heparin with platelet counts between 100,000/mm3 and 150,000/mm3 due to temporary platelet activation has been noted in clinical studies. On rare occasions, antibody-mediated severe thrombocytopenia (HIT type II) with platelet counts clearly below 100,000/mm3 has been observed (see section 4.8). This effect usually occurs within 5-21 days aer the initiation of treatment, although in patients with a history of heparin-induced thrombocytopenia this may occur more rapidly. Platelet count studies are recommended before the administration of bemiparin, on the first day of therapy and then every 3-4 days, in addition to repeating platelet studies at the end of therapy. Treatment must be discontinued immediately and an alternate therapy initiated if significant reductions in platelet counts are observed ( 30% decrease and above) [7]. As with other heparin products, cases of cutaneous necrosis, oen preceded by purpura or painful erythematous, ecchymose-like lesions have been reported with bemiparin. In these cases, treatment should cease immediately [7]. Overdosage aer subcutaneous or other routes of administration of bemiparin may lead to hemorrhagic complications. Neutralization can be obtained by slow intravenous of a suitable dose of the antidote protamine sulphate [8]. Affected organisms Humans Pathways Not Available Pharmacogenomic Not Available Effects/ADRs INTERACTIONS Drug Interactions ALL DRUGS APPROVED VET APPROVED NUTRACEUTICAL ILLICIT WITHDRAWN INVESTIGATIONAL EXPERIMENTAL Show 10 entries Search DRUG ↑↓ INTERACTION ↑↓ (1,2,6,7-3H)Testosterone The therapeutic efficacy of Bemiparin can be increased when used in combination with (1,2,6,7-3H)Testosterone. (R)-warfarin The risk or severity of bleeding can be increased when Bemiparin is combined with (R)- warfarin. (S)-Warfarin The risk or severity of bleeding can be increased when Bemiparin is combined with (S)- Warfarin. 1-Testosterone The therapeutic efficacy of Bemiparin can be increased when used in combination with 1- Testosterone. 18-methyl-19- The therapeutic efficacy of Bemiparin can be increased when used in combination with nortestosterone 18-methyl-19-nortestosterone. 4-hydroxycoumarin The risk or severity of bleeding can be increased when Bemiparin is combined with 4- hydroxycoumarin. https://www.drugbank.ca/drugs/DB09258 3/7 1/11/2019 Bemiparin - DrugBank DRUG ↑↓ INTERACTION ↑↓ 4-Hydroxytestosterone The therapeutic efficacy of Bemiparin can be increased when used in combination with 4- Hydroxytestosterone. Drugs 5beta- The therapeutic efficacy of Bemiparin can be increased when used in combination with dihydrotestosterone 5beta-dihydrotestosterone. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Bemiparin. Acebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Bemiparin. Showing 1 to 10 of 830 entries ‹ 1 2 3 4 5 … 83 › Food Interactions Not Available REFERENCES General References 1. Chapman TM, Goa KL: Bemiparin: a review of its use in the prevention of venous thromboembolism and treatment of deep vein thrombosis. Drugs. 2003;63(21):2357-77. [PubMed:14524738] 2. Planes A: Review of bemiparin sodium--a new second-generation low molecular weight heparin and its applications in venous thromboembolism. Expert Opin Pharmacother. 2003 Sep;4(9):1551-61. [PubMed:12943485] 3. Jeske WP, Hoppensteadt D, Gray A, Walenga JM, Cunanan J, Myers L, Fareed J, Bayol A, Rigal H, Viskov C: A common standard is inappropriate for determining the potency of ultra low molecular weight heparins such as semuloparin
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